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Search results for: antimalarial activity
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6243</div> </div> </div> </div> <h1 class="mt-3 mb-3 text-center" style="font-size:1.6rem;">Search results for: antimalarial activity</h1> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6243</span> HPTLC Metabolite Fingerprinting of Artocarpus champeden Stembark from Several Different Locations in Indonesia and Correlation with Antimalarial Activity</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Imam%20Taufik">Imam Taufik</a>, <a href="https://publications.waset.org/abstracts/search?q=Hilkatul%20Ilmi"> Hilkatul Ilmi</a>, <a href="https://publications.waset.org/abstracts/search?q=Puryani"> Puryani</a>, <a href="https://publications.waset.org/abstracts/search?q=Mochammad%20Yuwono"> Mochammad Yuwono</a>, <a href="https://publications.waset.org/abstracts/search?q=Aty%20Widyawaruyanti"> Aty Widyawaruyanti</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Artocarpus champeden Spreng stembark (Moraceae) in Indonesia well known as ‘cempedak’ had been traditionally used for malarial remedies. The difference of growth locations could cause the difference of metabolite profiling. As a consequence, there were difference antimalarial activities in spite of the same plants. The aim of this research was to obtain the profile of metabolites that contained in A. champeden stembark from different locations in Indonesia for authentication and quality control purpose of this extract. The profiling had been performed by HPTLC-Densitometry technique and antimalarial activity had been also determined by HRP2-ELISA technique. The correlation between metabolite fingerprinting and antimalarial activity had been analyzed by Principle Component Analysis, Hierarchical Clustering Analysis and Partial Least Square. As a result, there is correlation between the difference metabolite fingerprinting and antimalarial activity from several different growth locations. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=antimalarial" title="antimalarial">antimalarial</a>, <a href="https://publications.waset.org/abstracts/search?q=artocarpus%20champeden%20spreng" title=" artocarpus champeden spreng"> artocarpus champeden spreng</a>, <a href="https://publications.waset.org/abstracts/search?q=metabolite%20fingerprinting" title=" metabolite fingerprinting"> metabolite fingerprinting</a>, <a href="https://publications.waset.org/abstracts/search?q=multivariate%20analysis" title=" multivariate analysis"> multivariate analysis</a> </p> <a href="https://publications.waset.org/abstracts/58321/hptlc-metabolite-fingerprinting-of-artocarpus-champeden-stembark-from-several-different-locations-in-indonesia-and-correlation-with-antimalarial-activity" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/58321.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">311</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6242</span> Quantitative Structure-Activity Relationship Study of Some Quinoline Derivatives as Antimalarial Agents</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=M.%20Ouassaf">M. Ouassaf</a>, <a href="https://publications.waset.org/abstracts/search?q=S.%20Belaid"> S. Belaid</a> </p> <p class="card-text"><strong>Abstract:</strong></p> A series of quinoline derivatives with antimalarial activity were subjected to two-dimensional quantitative structure-activity relationship (2D-QSAR) studies. Three models were implemented using multiple regression linear MLR, a regression partial least squares (PLS), nonlinear regression (MNLR), to see which descriptors are closely related to the activity biologic. We relied on a principal component analysis (PCA). Based on our results, a comparison of the quality of, MLR, PLS, and MNLR models shows that the MNLR (R = 0.914 and R² = 0.835, RCV= 0.853) models have substantially better predictive capability because the MNLR approach gives better results than MLR (R = 0.835 and R² = 0,752, RCV=0.601)), PLS (R = 0.742 and R² = 0.552, RCV=0.550) The model of MNLR gave statistically significant results and showed good stability to data variation in leave-one-out cross-validation. The obtained results suggested that our proposed model MNLR may be useful to predict the biological activity of derivatives of quinoline. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=antimalarial" title="antimalarial">antimalarial</a>, <a href="https://publications.waset.org/abstracts/search?q=quinoline" title=" quinoline"> quinoline</a>, <a href="https://publications.waset.org/abstracts/search?q=QSAR" title=" QSAR"> QSAR</a>, <a href="https://publications.waset.org/abstracts/search?q=PCA" title=" PCA"> PCA</a>, <a href="https://publications.waset.org/abstracts/search?q=MLR" title=" MLR "> MLR </a>, <a href="https://publications.waset.org/abstracts/search?q=MNLR" title="MNLR">MNLR</a>, <a href="https://publications.waset.org/abstracts/search?q=MLR" title=" MLR"> MLR</a> </p> <a href="https://publications.waset.org/abstracts/100879/quantitative-structure-activity-relationship-study-of-some-quinoline-derivatives-as-antimalarial-agents" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/100879.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">156</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6241</span> Synthesis, Biological Evaluation and Molecular Modeling Studies on Chiral Chloroquine Analogues as Antimalarial Agents</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Srinivasarao%20Kondaparla">Srinivasarao Kondaparla</a>, <a href="https://publications.waset.org/abstracts/search?q=Utsab%20Debnath"> Utsab Debnath</a>, <a href="https://publications.waset.org/abstracts/search?q=Awakash%20Soni"> Awakash Soni</a>, <a href="https://publications.waset.org/abstracts/search?q=Vasantha%20%20Rao%20Dola"> Vasantha Rao Dola</a>, <a href="https://publications.waset.org/abstracts/search?q=Manish%20Sinha"> Manish Sinha</a>, <a href="https://publications.waset.org/abstracts/search?q=Kumkum%20Kumkum%20Srivastava"> Kumkum Kumkum Srivastava</a>, <a href="https://publications.waset.org/abstracts/search?q=Sunil%20K.%20%20Puri"> Sunil K. Puri</a>, <a href="https://publications.waset.org/abstracts/search?q=Seturam%20B.%20Katti"> Seturam B. Katti</a> </p> <p class="card-text"><strong>Abstract:</strong></p> In a focused exploration, we have designed synthesized and biologically evaluated chiral conjugated new chloroquine (CQ) analogs with substituted piperazines as antimalarial agents. In vitro as well as in vivo studies revealed that compound 7c showed potent activity [for in vitro IC₅₀= 56.98nM (3D7), 97.76nM (K1); for in vivo (up to at the dose of 12.5 mg/kg); SI = 3510] as a new lead of antimalarial agent. Other compounds 6b, 6d, 7d, 7h, 8c, 8d, 9a, and 9c are also showing moderate activity against CQ-sensitive (3D7) strain and superior activity against resistant (K1) strain of P. falciparum. Furthermore, we have carried out docking and 3D-QSAR studies of all in-house data sets (168 molecules) of chiral CQ analogs to explain the structure activity relationships (SAR). Our new findings specified the significance of H-bond interaction with the side chain of heme for biological activity. In addition, the 3D-QSAR study against 3D7 strain indicated the favorable and unfavorable sites of CQ analogs for incorporating steric, hydrophobic and electropositive groups to improve the antimalarial activity. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=piperazines" title="piperazines">piperazines</a>, <a href="https://publications.waset.org/abstracts/search?q=CQ-sensitive%20strain-3D7" title=" CQ-sensitive strain-3D7"> CQ-sensitive strain-3D7</a>, <a href="https://publications.waset.org/abstracts/search?q=in-vitro%20and%20in-vivo%20assay" title=" in-vitro and in-vivo assay"> in-vitro and in-vivo assay</a>, <a href="https://publications.waset.org/abstracts/search?q=docking" title=" docking"> docking</a>, <a href="https://publications.waset.org/abstracts/search?q=3D-QSAR" title=" 3D-QSAR"> 3D-QSAR</a> </p> <a href="https://publications.waset.org/abstracts/95175/synthesis-biological-evaluation-and-molecular-modeling-studies-on-chiral-chloroquine-analogues-as-antimalarial-agents" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/95175.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">171</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6240</span> 4(3H)-Quinazolinone Derivatives' Synthesis and Evaluation as Antimalarial and Anti-Leishmanial Agents</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Alemu%20Tadesse%20Feroche">Alemu Tadesse Feroche</a> </p> <p class="card-text"><strong>Abstract:</strong></p> In this study, some 2, 3 distributed quinazoline -4 (3H) - one derivative were synthesized using a three-step synthetic route. They were obtained in a good yield (59.5-85%) by applying different chemical reactions like cyclization and condensation reactions. The chemical structure of the final compounds was also verified by spectroscopic methods (IR, ¹HNMR) and elemental microanalysis. The in vivo antimalarial activity of these compounds on P. berghei infected mice was found to be moderate to high at an oral dose of 0.04846 mmol/kg /day. This is equal to 25 mg/kg of chloroquine phosphate, which causes 100% inhibition of the parasite. It is worth mentioning that most active compounds (E) -3 Phenyl -2- [2- (pyridine -4- yl) vinyl] -4 (3H) -quinazolinone IVa (64.02%, (E)-2-[2-(4 - Hydroxy-3 - methoxystyryl) - vinyl) -3 - phenyl -4 (3H ) - quinazolinone IVc (77.25%) and (E)-2 –[2 –(Pyridin -4-yl) –vinyl] -3 phenenylamine -4(3H) quinazolinone IVe (73.54%) showed a dose-dependent increase in present suppression in antimalarial activities. Furthermore, the synthesized compounds were screened for their in vitro antileishmanial activity against L. aethiopica isolate (CL/039/09). All tested compounds (IVa (0.03766 ug/ml), IVb (0.00538 ug/ml, IVc (0.00412 ug/ml, IVd (0.00110 ug/ml), IVe (0.03017 ug/ml) and IVf (0.03894 ug/ml)) showed excellent potency that is much better than amphotericin B (IC50 = 0,04359 ug/ml). The results of acute toxicity indicated that all test compounds (IVa –IVf) proved to be nontoxic and well tolerated by the experimental animals up to 300 mg/kg in oral and 140 mg/kg in parental studies. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=4%283H%29-quinazolinone" title="4(3H)-quinazolinone">4(3H)-quinazolinone</a>, <a href="https://publications.waset.org/abstracts/search?q=in%20vivo%20antimalarial%20activity" title=" in vivo antimalarial activity"> in vivo antimalarial activity</a>, <a href="https://publications.waset.org/abstracts/search?q=in%20vitro%20antileishmanial%20activity" title=" in vitro antileishmanial activity"> in vitro antileishmanial activity</a>, <a href="https://publications.waset.org/abstracts/search?q=acute%20toxicity" title=" acute toxicity"> acute toxicity</a> </p> <a href="https://publications.waset.org/abstracts/153719/43h-quinazolinone-derivatives-synthesis-and-evaluation-as-antimalarial-and-anti-leishmanial-agents" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/153719.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">100</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6239</span> In silico Designing and Insight into Antimalarial Potential of Chalcone-Quinolinylpyrazole Hybrids by Preclinical Study in Mice</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Deepika%20Saini">Deepika Saini</a>, <a href="https://publications.waset.org/abstracts/search?q=Sandeep%20Jain"> Sandeep Jain</a>, <a href="https://publications.waset.org/abstracts/search?q=Ajay%20%20Kumar"> Ajay Kumar</a> </p> <p class="card-text"><strong>Abstract:</strong></p> The quinoline scaffold is one of the most widely studied in the discovery of derivatives with various heterocyclic moieties due to its potential antimalarial activities. In the present study, a chalcone series of quinoline derivatives clubbed with pyrazole were synthesized to evaluate their antimalarial property by in vitro schizont maturation inhibition assay against both chloroquine sensitive, 3D7 and chloroquine resistant, RKL9 strain of Plasmodium falciparum. Further, top five compounds were studied for in vivo preclinical study for antimalarial potential against P. berghei in Swiss albino mice. To understand the mechanism of synthesized analogues, they were screened computationally by molecular docking techniques. Compounds were docked into the active site of a protein receptor, Plasmodium falciparum Cysteine Protease Falcipain-2. The compounds were successfully synthesized, and structural confirmation was performed by FTIR, 1H-NMR, mass spectrometry and elemental analysis. In vitro study suggested that the compounds 5b, 5g, 5l, 5s and 5u possessed best antimalarial activity and further tested for in vivo screening. Compound 5u (CH₃ on both rings) with EC₅₀ 0.313 & 0.801 µg/ml against CQ-S & CQ-R strains of P. falciparum respectively and 78.01% suppression of parasitemia. The molecular docking studies of the compounds helped in understanding the mechanism of action against falcipain-2. The present study reveals the binding signatures of the synthesized ligands within the active site of the protein, and it explains the results from in vitro study in their EC₅₀ values and percentage parasitemia. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=antimalarial%20activity" title="antimalarial activity">antimalarial activity</a>, <a href="https://publications.waset.org/abstracts/search?q=chalcone" title=" chalcone"> chalcone</a>, <a href="https://publications.waset.org/abstracts/search?q=docking" title=" docking"> docking</a>, <a href="https://publications.waset.org/abstracts/search?q=quinoline" title=" quinoline"> quinoline</a> </p> <a href="https://publications.waset.org/abstracts/63591/in-silico-designing-and-insight-into-antimalarial-potential-of-chalcone-quinolinylpyrazole-hybrids-by-preclinical-study-in-mice" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/63591.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">409</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6238</span> Pyrazolylpyrazolines: Design, Synthesis and Biological Evaluation as Dual Acting Antimalarial-Antileishmanial Agents</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Adnan%20Bekhit">Adnan Bekhit</a>, <a href="https://publications.waset.org/abstracts/search?q=Eskedar%20Lodebo"> Eskedar Lodebo</a>, <a href="https://publications.waset.org/abstracts/search?q=Ariaya%20Hymete"> Ariaya Hymete</a>, <a href="https://publications.waset.org/abstracts/search?q=Hanan%20Ragab"> Hanan Ragab</a>, <a href="https://publications.waset.org/abstracts/search?q=Alaa%20El-Din%20Bekhit"> Alaa El-Din Bekhit</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Malaria and leishmaniasis have emerged as serious universal health problems throughout history of mankind. According to the WHO 2008 malarial report, half of the world population is at risk of malarial infection with an estimate of 1 million deaths occurring annually mainly in the African region. Furthermore, 12-15 million people are infected with Leishmaniasis worldwide. Despite the continuous introduction of a large number of agents for the treatment of malaria, there is still unmet medical needs due to the emergence of resistance. Resistance has occurred for almost all therapeutic agents approved for the treatment of malaria. Accordingly, it was the aim of this work to design and synthesis a group of antimalarial-antileshmanial agents that would show inhibitory activity against chloroquine-resistant strain of Plasmodium falciparum. The synthesized compounds were designed to contain a pyrazolylpyrazoline moiety having an aromatic group (p-tolyl or p-chlorophenyl) at N1-position of one pyrazoline ring due to the reports of promising activities of such compounds. A formyl or acyl substituent was introduced at the N1-position of the other pyrazoline ring, to investigate the effect of bulkiness of acyl substituents at this position. The synthesized compounds were evaluated for their in-vivo antimalarial activity against Plasmodium berghei infected mice at dose levels of 20 and 30 mg/Kg. the two most active compounds were evaluated for their antimalarial activity against chloroquin-resistant strain (RKL9) of Plasmodium falciparum. In addition, the synthesized compounds were tested for their in-vitro antileshmanial activity against Leishmania aethiopica promastigotes and amastigotes. For both antimalarial and antileishmanial activities, compounds having an N1-p-tolyl group at the first pyrazoline ring did not require bulkiness at the second pyrazoline ring nitrogen where the compound bearing an acetyl group proved to be the most active of the whole series. On the other hand, bulkiness at the N1-position of the second pyazoline ring was necessary in case of compounds carrying the p-chlorophenyl group, where the two derivatives having an N1-butanoyl and an N1-benzoyl moieties at the second pyrazoline showed the best activity. Furthermore, the toxicity of the active compounds were tested and were proved to be non-toxic at 125, 250 and 500 mg/Kg. In addition, docking of the most active compound (having a p-tolyl group at the first pyrazoline-N and an acetyl moiety on the other pyrazoline-N) was performed against dihydrofolate reductase enzyme. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=pyrazoline%20derivatives" title="pyrazoline derivatives">pyrazoline derivatives</a>, <a href="https://publications.waset.org/abstracts/search?q=in-vivo%20antimalarial%20activity" title=" in-vivo antimalarial activity"> in-vivo antimalarial activity</a>, <a href="https://publications.waset.org/abstracts/search?q=docking" title=" docking"> docking</a>, <a href="https://publications.waset.org/abstracts/search?q=dihydrofolate%20reductase" title=" dihydrofolate reductase"> dihydrofolate reductase</a> </p> <a href="https://publications.waset.org/abstracts/62770/pyrazolylpyrazolines-design-synthesis-and-biological-evaluation-as-dual-acting-antimalarial-antileishmanial-agents" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/62770.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">341</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6237</span> Assessment of Antiplasmodial and Some Other Biological Activities, Essential Oil Constituents, and Phytochemical Screening of Azadirachta indica Grown in Ethiopia</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Dawit%20Chankaye">Dawit Chankaye</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Background: Azadirachta indica is the most versatile medicinal plant known as “the village pharmacy”. The plant is known for its broad spectrum of biological activity in India and various countries throughout history by many different human cultures. The present study was undertaken to determine the antimalarial and antidiabetic properties of the leaf extracts of A. indica grown in Ethiopia when treated in vivo. This work has also been concerned with determining essential oil composition and the antimicrobial activity of the plant in vitro. Methods: Leaf extracts were prepared using three different selected solvents. Standard and clinical isolates were treated with extracts of the leaves of A. indica using the agar well diffusion method. The antimalarial and antidiabetic tests were conducted in vivo in mice. Phytochemical screening was done using various chemical tests, and the volatile oil constituents were determined using gas chromatography-mass spectrometry (GC/MS). Results: In vivo antimalarial activity studies showed 85.23%, 69.01%, and 81.54% suppression of parasitemia for 70% ethanol, acetone, and water extracts, respectively. The extracts collected from the leaves also showed reduced blood sugar levels in alloxan-induced diabetic mice. In addition, the solvent extracts were shown to have an inhibitory effect on the growth of microorganisms under the study. The minimum inhibitory concentration (MIC) ranged from 850 to 1050 µg/ml. Notably, the phytochemical investigation of the ethanol extracts showed the presence of secondary metabolites. Seventeen compounds (mainly sesquiterpenes) that represent 75.45% of the essential oil were characterized by GC/MS analysis. Conclusion: Extracts examined in this study indicated that the leaf of A. indica grown in Ethiopia retained the biological activities demonstrating the extent equivalent to when it was grown in its natural habitat. In addition, phytochemical investigation and GC/MS analysis of volatile oil constituents showed comparable results to those presented in India and elsewhere. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=Azadirachta%20indica" title="Azadirachta indica">Azadirachta indica</a>, <a href="https://publications.waset.org/abstracts/search?q=vivo" title=" vivo"> vivo</a>, <a href="https://publications.waset.org/abstracts/search?q=antimalarial%20activity" title=" antimalarial activity"> antimalarial activity</a>, <a href="https://publications.waset.org/abstracts/search?q=antidiabetic%20activity" title=" antidiabetic activity"> antidiabetic activity</a>, <a href="https://publications.waset.org/abstracts/search?q=alloxan" title=" alloxan"> alloxan</a>, <a href="https://publications.waset.org/abstracts/search?q=mice" title=" mice"> mice</a>, <a href="https://publications.waset.org/abstracts/search?q=phytochemical" title=" phytochemical"> phytochemical</a> </p> <a href="https://publications.waset.org/abstracts/171066/assessment-of-antiplasmodial-and-some-other-biological-activities-essential-oil-constituents-and-phytochemical-screening-of-azadirachta-indica-grown-in-ethiopia" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/171066.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">79</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6236</span> Formulation and Evaluation of Curcumin-Zn (II) Microparticulate Drug Delivery System for Antimalarial Activity</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=M.%20R.%20Aher">M. R. Aher</a>, <a href="https://publications.waset.org/abstracts/search?q=R.%20B.%20Laware"> R. B. Laware</a>, <a href="https://publications.waset.org/abstracts/search?q=G.%20S.%20%20Asane"> G. S. Asane</a>, <a href="https://publications.waset.org/abstracts/search?q=B.%20S.%20Kuchekar"> B. S. Kuchekar</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Objective: Studies have shown that a new combination therapy with Artemisinin derivatives and curcumin is unique, with potential advantages over known ACTs. In present study an attempt was made to prepare microparticulate drug delivery system of Curcumin-Zn complex and evaluate it in combination with artemether for antimalarial activity. Material and method: Curcumin Zn complex was prepared and encapsulated using sodium alginate. Microparticles thus obtained are further coated with various enteric polymers at different coating thickness to control the release. Microparticles are evaluated for encapsulation efficiency, drug loading and in vitro drug release. Roentgenographic Studies was conducted in rabbits with BaSO 4 tagged formulation. Optimized formulation was screened for antimalarial activity using P. berghei-infected mice survival test and % paracetemia inhibition, alone (three oral dose of 5mg/day) and in combination with arthemether (i.p. 500, 1000 and 1500µg). Curcumin-Zn(II) was estimated in serum after oral administration to rats by using spectroflurometry. Result: Microparticles coated with Cellulose acetate phthalate showed most satisfactory and controlled release with 479 min time for 60% drug release. X-ray images taken at different time intervals confirmed the retention of formulation in GI tract. Estimation of curcumin in serum by spectroflurometry showed that drug concentration is maintained in the blood for longer time with tmax of 6 hours. The survival time (40 days post treatment) of mice infected with P. berghei was compared to survival after treatment with either Curcumin-Zn(II) microparticles artemether combination, curcumin-Zn complex and artemether. Oral administration of Curcumin-Zn(II)-artemether prolonged the survival of P.berghei-infected mice. All the mice treated with Curcumin-Zn(II) microparticles (5mg/day) artemether (1000µg) survived for more than 40 days and recovered with no detectable parasitemia. Administration of Curcumin-Zn(II) artemether combination reduced the parasitemia in mice by more than 90% compared to that in control mice for the first 3 days after treatment. Conclusion: Antimalarial activity of the curcumin Zn-artemether combination was more pronounced than mono therapy. A single dose of 1000µg of artemether in curcumin-Zn combination gives complete protection in P. berghei-infected mice. This may reduce the chances of drug resistance in malaria management. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=formulation" title="formulation">formulation</a>, <a href="https://publications.waset.org/abstracts/search?q=microparticulate%20drug%20delivery" title=" microparticulate drug delivery"> microparticulate drug delivery</a>, <a href="https://publications.waset.org/abstracts/search?q=antimalarial" title=" antimalarial"> antimalarial</a>, <a href="https://publications.waset.org/abstracts/search?q=pharmaceutics" title=" pharmaceutics"> pharmaceutics</a> </p> <a href="https://publications.waset.org/abstracts/26467/formulation-and-evaluation-of-curcumin-zn-ii-microparticulate-drug-delivery-system-for-antimalarial-activity" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/26467.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">394</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6235</span> Antiplasmodial Activity of Drimane Sesquiterpene Isolated from Warburgia salutaris</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Mthokozisi%20Simelane">Mthokozisi Simelane</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Background: Malaria remains a life-threatening disease in tropical regions despite the advances in the treatment of this disease, it still remains a significant burden as some parasites have become resistant to the currently available drugs. This has created a necessity for the development of alternative, more efficient antimalarial drugs. Warburgia salutaris is a traditional medicinal plant used in malaria treatment by Zulu traditional healers. Materials and methods: The W. salutaris stem-bark was extracted with dichloromethane and the compound was isolated through column chromatography. The compound was identified and characterized by spectroscopic analysis (1H NMR, 13C NMR, IR and MS) and the structure was also confirmed by x-ray crystallography. The anti-plasmodial activity (in vitro) was studied on NF54 Plasmodium falciparum strain (CQS). Cytotoxicity was measured using the MTT assay on HEK239 and HEPG2 cell lines. Docking of Mukaadial acetate was conducted in AutoDock Vina. Structural modifications were conducted in UCSF Chimera and molecular interactions examined in LigPlot. Results: The compound, Mukaadial Acetate showed appreciable inhibition (IC50 0.44±0.10 µg/ml) of the parasite growth and cytotoxicity activity of 0.124±0.109 and 0.199±0.083 (µg/ml) on HEK293 and HEPG2 cells respectively. Molecular docking revealed that Mukaadial Acetate binds to the purine, pyrophosphate and ribose binding sites of the PfHGXPRT with an optimum binding conformation and forms hydrogen bond, steric and hydrophobic interactions with the residues inhabiting the respective binding sites. Conclusion: It is apparent that W. salutaris contains components (including Mukaadial Acetate) that exhibit antimalarial activity. This study scientifically validates the use of this plant in folk medicine. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=plasmodium%20falciparum" title="plasmodium falciparum">plasmodium falciparum</a>, <a href="https://publications.waset.org/abstracts/search?q=molecular%20docking" title=" molecular docking"> molecular docking</a>, <a href="https://publications.waset.org/abstracts/search?q=antimalarial%20activity" title=" antimalarial activity"> antimalarial activity</a>, <a href="https://publications.waset.org/abstracts/search?q=PfHGXPRT" title=" PfHGXPRT"> PfHGXPRT</a>, <a href="https://publications.waset.org/abstracts/search?q=Warburgia%20salutaris" title=" Warburgia salutaris"> Warburgia salutaris</a>, <a href="https://publications.waset.org/abstracts/search?q=mukaadial%20acetate" title=" mukaadial acetate"> mukaadial acetate</a> </p> <a href="https://publications.waset.org/abstracts/70831/antiplasmodial-activity-of-drimane-sesquiterpene-isolated-from-warburgia-salutaris" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/70831.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">197</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6234</span> NMR-Based Metabolomic Study of Antimalarial Plant Species Used Traditionally by Vha-Venda People in Limpopo Province, South Africa</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Johanna%20Bapela">Johanna Bapela</a>, <a href="https://publications.waset.org/abstracts/search?q=Heino%20Heyman"> Heino Heyman</a>, <a href="https://publications.waset.org/abstracts/search?q=Marion%20Meyer"> Marion Meyer</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Regardless of the significant advances accomplished in reducing the burden of malaria and other tropical diseases in recent years, malaria remains a major cause of mortality in endemic countries. This is especially the case in sub-Saharan Africa where 99% of the estimated global malaria deaths occurs on an annual basis. The emergence of resistant Plasmodium species and the lack of diversified chemotherapeutic agents provide the rationale for bioprospecting for antiplasmodial scaffolds. Crude extracts from twenty indigenous antimalarial plant species were screened for antimalarial activity and then subjected to 1H NMR-based metabolomic analysis. Ten plant extracts exhibited significant in vitro antiplasmodial activity (IC50 ≤ 5 µg/ml). The Principal Component Analysis (PCA) of the acquired 1H NMR spectra could not separate the analyzed plant extracts according to the detected antiplasmodial bioactivity. Application of supervised Orthogonal Projections to Latent Structures–Discriminant Analysis (OPLS-DA) to the 1H NMR profiles resulted in a discrimination pattern that could be correlated to bioactivity. A contribution plot generated from the OPLS-DA scoring plot illustrated the classes of compounds responsible for the observed grouping. Given the preliminary in vitro results, Tabernaemontana elegans Stapf. (Apocynaceae) and Vangueria infausta Burch. subsp. infausta (Rubiaceae) were subjected to further phytochemical investigations. Two indole alkaloids, dregamine and tabernaemontanine possessing antiplasmodial activity were isolated from T. elegans. Two compounds were isolated from V. infausta subsp. infausta and identified as friedelin (IC50 = 3.01 µg/ml) and morindolide (IC50 = 18.5 µg/ml). While these compounds have been previously identified, this is the first account of their occurrence in the genus Vangueria and their antiplasmodial activity. Based on the results of the study, metabolomics can be used to globally identify classes of plant secondary metabolites that are responsible for antiplasmodial activity. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=ethnopharmacology" title="ethnopharmacology">ethnopharmacology</a>, <a href="https://publications.waset.org/abstracts/search?q=Malaria" title=" Malaria"> Malaria</a>, <a href="https://publications.waset.org/abstracts/search?q=medicinal%20plants" title=" medicinal plants"> medicinal plants</a>, <a href="https://publications.waset.org/abstracts/search?q=metabolomics" title=" metabolomics"> metabolomics</a> </p> <a href="https://publications.waset.org/abstracts/55170/nmr-based-metabolomic-study-of-antimalarial-plant-species-used-traditionally-by-vha-venda-people-in-limpopo-province-south-africa" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/55170.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">341</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6233</span> Malaria Management among Dispensers in Drug Retail Outlets in Buea Community: An Assessment of Knowledge of Malaria and Antimalarial Drug Prescription and Dispensing Practices</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Marcelus%20U.%20Ajonina">Marcelus U. Ajonina</a>, <a href="https://publications.waset.org/abstracts/search?q=Deodata%20B.%20Ngonga"> Deodata B. Ngonga</a>, <a href="https://publications.waset.org/abstracts/search?q=Kenric%20B.%20Ware"> Kenric B. Ware</a>, <a href="https://publications.waset.org/abstracts/search?q=Carine%20K.%20Nfor"> Carine K. Nfor</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Background: Lack of knowledge of rational use of antimalarial drugs among dispensers is a serious problem, especially in areas of intense transmission, thus increasing the risk of resistance and adverse drug reactions. This study was aimed at assessing the knowledge of malaria as well as perception and dispensing practices of antimalarials among vendors in Buea community. Methods: A community-based cross-sectional survey of a random sample of 140 drug vendors living within the Buea community was conducted between March and June 2017. A questionnaire was designed to obtain information from drug vendors on the general knowledge of malaria as well as dispensing practices. Data were analyzed using SPSS Statistics 20.0 and were considered significant at p ≤ 0.05. Results: Knowledge of malaria symptoms, transmission, and prevention was reasonable among 55.8% (77) of the respondents. Only 33.6% (47) of the respondents could attribute the cause of malaria to protozoan of genus Plasmodium species. Of the 140 vendors, 115 (82.7%) prescribe antimalarial drugs. The knowledge of the national protocol was malaria case management among dispensers was 35.0%. Vendors in hospital/community pharmacies were 2.4 times (OR = 3.14, 95% CI: 4.14 - 8.74, p < 0.001) more knowledgeable about malaria treatment protocol than those of in drugstores. The prevalence of self-prescription of antimalarials was 39.3%. Self-prescription was significantly higher in drugstores than hospital/community pharmacies (p=0.004). In all, 56 (40.6%) of vendors showed good practices regarding antimalarial drug dispensing with the majority (51.7%) from community pharmacies (OR=2.27,95% CI: 1.13-4.56). Conclusion: Findings reveal moderate knowledge of malaria but poor prescription and dispensing practices of antimalarial drugs among vendors, thus indicating a need for routine monitoring and evaluation to prevent the emergence of resistant strains to current efficacious antimalarials. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=antimalarials" title="antimalarials">antimalarials</a>, <a href="https://publications.waset.org/abstracts/search?q=drug%20retail%20outlets" title=" drug retail outlets"> drug retail outlets</a>, <a href="https://publications.waset.org/abstracts/search?q=dispensing" title=" dispensing"> dispensing</a>, <a href="https://publications.waset.org/abstracts/search?q=drug%20resistance" title=" drug resistance"> drug resistance</a>, <a href="https://publications.waset.org/abstracts/search?q=prescription" title=" prescription"> prescription</a> </p> <a href="https://publications.waset.org/abstracts/108565/malaria-management-among-dispensers-in-drug-retail-outlets-in-buea-community-an-assessment-of-knowledge-of-malaria-and-antimalarial-drug-prescription-and-dispensing-practices" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/108565.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">136</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6232</span> A Greener Approach towards the Synthesis of an Antimalarial Drug Lumefantrine</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Luphumlo%20Ncanywa">Luphumlo Ncanywa</a>, <a href="https://publications.waset.org/abstracts/search?q=Paul%20Watts"> Paul Watts</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Malaria is a disease that kills approximately one million people annually. Children and pregnant women in sub-Saharan Africa lost their lives due to malaria. Malaria continues to be one of the major causes of death, especially in poor countries in Africa. Decrease the burden of malaria and save lives is very essential. There is a major concern about malaria parasites being able to develop resistance towards antimalarial drugs. People are still dying due to lack of medicine affordability in less well-off countries in the world. If more people could receive treatment by reducing the cost of drugs, the number of deaths in Africa could be massively reduced. There is a shortage of pharmaceutical manufacturing capability within many of the countries in Africa. However one has to question how Africa would actually manufacture drugs, active pharmaceutical ingredients or medicines developed within these research programs. It is quite likely that such manufacturing would be outsourced overseas, hence increasing the cost of production and potentially limiting the full benefit of the original research. As a result the last few years has seen major interest in developing more effective and cheaper technology for manufacturing generic pharmaceutical products. Micro-reactor technology (MRT) is an emerging technique that enables those working in research and development to rapidly screen reactions utilizing continuous flow, leading to the identification of reaction conditions that are suitable for usage at a production level. This emerging technique will be used to develop antimalarial drugs. It is this system flexibility that has the potential to reduce both the time was taken and risk associated with transferring reaction methodology from research to production. Using an approach referred to as scale-out or numbering up, a reaction is first optimized within the laboratory using a single micro-reactor, and in order to increase production volume, the number of reactors employed is simply increased. The overall aim of this research project is to develop and optimize synthetic process of antimalarial drugs in the continuous processing. This will provide a step change in pharmaceutical manufacturing technology that will increase the availability and affordability of antimalarial drugs on a worldwide scale, with a particular emphasis on Africa in the first instance. The research will determine the best chemistry and technology to define the lowest cost manufacturing route to pharmaceutical products. We are currently developing a method to synthesize Lumefantrine in continuous flow using batch process as bench mark. Lumefantrine is a dichlorobenzylidine derivative effective for the treatment of various types of malaria. Lumefantrine is an antimalarial drug used with artemether for the treatment of uncomplicated malaria. The results obtained when synthesizing Lumefantrine in a batch process are transferred into a continuous flow process in order to develop an even better and reproducible process. Therefore, development of an appropriate synthetic route for Lumefantrine is significant in pharmaceutical industry. Consequently, if better (and cheaper) manufacturing routes to antimalarial drugs could be developed and implemented where needed, it is far more likely to enable antimalarial drugs to be available to those in need. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=antimalarial" title="antimalarial">antimalarial</a>, <a href="https://publications.waset.org/abstracts/search?q=flow" title=" flow"> flow</a>, <a href="https://publications.waset.org/abstracts/search?q=lumefantrine" title=" lumefantrine"> lumefantrine</a>, <a href="https://publications.waset.org/abstracts/search?q=synthesis" title=" synthesis"> synthesis</a> </p> <a href="https://publications.waset.org/abstracts/78893/a-greener-approach-towards-the-synthesis-of-an-antimalarial-drug-lumefantrine" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/78893.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">202</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6231</span> New Strategy for Breeding of Artemisia annua L. for a Sustainable Production of the Antimalarial Drug Artemisinin</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Nadali%20Babaeian%20Jelodar">Nadali Babaeian Jelodar</a>, <a href="https://publications.waset.org/abstracts/search?q=Chan%20Lai%20Keng"> Chan Lai Keng</a>, <a href="https://publications.waset.org/abstracts/search?q=Arvind%20Bhatt"> Arvind Bhatt</a>, <a href="https://publications.waset.org/abstracts/search?q=Laleh%20Bordbar"> Laleh Bordbar</a>, <a href="https://publications.waset.org/abstracts/search?q=Leow%20E%20Shuen"> Leow E Shuen</a>, <a href="https://publications.waset.org/abstracts/search?q=Kamaruzaman%20Mohamed"> Kamaruzaman Mohamed</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Recently artemisinin (the endoperoxide sesquiterpene lactone) has received considerable attention because of its antimalarial activity. It is isolated from the aerial part of the Artemisia annua L. Artemisinin is very difficult to synthesise also its production by mean of cell, tissue or organ cultures is very low. Presently, only its extraction from A. annua L. plants remains the only source of the drug. The reported yield of artemisinin from leaves of A. annua L. is very low and unstable, with yields typically less than 1% of leaf dry weight. To increase the percentage of artemisinin, researchers have been engaged in developing new varieties. A review concerning the breeding of A. annua L. is presented. The aim of this review is to bring together most of the available scientific research papers about the breeding conducted on the genus A. annua L., which is currently scattered across various publications. Through this review the authors hope to attract the attention of breeders throughout the world to focus on the unexplored potential of A. annua L. species. Also the future scope of this plant has been emphasized with a view of the importance of breeding of A. annua L. for increasing of artemisinin content. By releasing of new cultivar of A. annua L. and cultivation of this plant offers the opportunity to optimize yield and achieve a uniform, high quality product. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=Artemisia%20annua%20L." title="Artemisia annua L.">Artemisia annua L.</a>, <a href="https://publications.waset.org/abstracts/search?q=breeding" title=" breeding"> breeding</a>, <a href="https://publications.waset.org/abstracts/search?q=artemisinin" title=" artemisinin"> artemisinin</a>, <a href="https://publications.waset.org/abstracts/search?q=cultivation" title=" cultivation"> cultivation</a>, <a href="https://publications.waset.org/abstracts/search?q=medicinal%20plant" title=" medicinal plant"> medicinal plant</a> </p> <a href="https://publications.waset.org/abstracts/9710/new-strategy-for-breeding-of-artemisia-annua-l-for-a-sustainable-production-of-the-antimalarial-drug-artemisinin" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/9710.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">263</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6230</span> Triazenes: Unearthing Their Hidden Arsenal Against Malaria and Microbial Menace</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Frans%20J.%20Smit">Frans J. Smit</a>, <a href="https://publications.waset.org/abstracts/search?q=Wisdom%20A.%20Munzeiwa"> Wisdom A. Munzeiwa</a>, <a href="https://publications.waset.org/abstracts/search?q=Hermanus%20C.%20M.%20Vosloo"> Hermanus C. M. Vosloo</a>, <a href="https://publications.waset.org/abstracts/search?q=Lyn-Marie%20Birkholtz"> Lyn-Marie Birkholtz</a>, <a href="https://publications.waset.org/abstracts/search?q=Richard%20K.%20Haynes"> Richard K. Haynes</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Malaria and antimicrobial infections remain significant global health concerns, necessitating the continuous search for novel therapeutic approaches. This abstract presents an overview of the potential use of triazenes as effective agents against malaria and various antimicrobial pathogens. Triazenes are a class of compounds characterized by a linear arrangement of three nitrogen atoms, rendering them structurally distinct from their cyclic counterparts. This study investigates the efficacy of triazenes against malaria and explores their antimicrobial activity. Preliminary results revealed significant antimalarial activity of the triazenes, as evidenced by in vitro screening against P. falciparum, the causative agent of malaria. Furthermore, the compounds exhibited broad-spectrum antimicrobial activity, indicating their potential as effective antimicrobial agents. These compounds have shown inhibitory effects on various essential enzymes and processes involved in parasite survival, replication, and transmission. The mechanism of action of triazenes against malaria involves interactions with critical molecular targets, such as enzymes involved in the parasite's metabolic pathways and proteins responsible for host cell invasion. The antimicrobial activity of the triazenes against bacteria and fungi was investigated through disc diffusion screening. The antimicrobial efficacy of triazenes has been observed against both Gram-positive and Gram-negative bacteria, as well as multidrug-resistant strains, making them potential candidates for combating drug-resistant infections. Furthermore, triazenes possess favourable physicochemical properties, such as good stability, solubility, and low toxicity, which are essential for drug development. The structural versatility of triazenes allows for the modification of their chemical composition to enhance their potency, selectivity, and pharmacokinetic properties. These modifications can be tailored to target specific pathogens, increasing the potential for personalized treatment strategies. In conclusion, this study highlights the potential of triazenes as promising candidates for the development of novel antimalarial and antimicrobial therapeutics. Further investigations are necessary to determine the structure-activity relationships and optimize the pharmacological properties of these compounds. The results warrant additional research, including MIC studies, to further explore the antimicrobial activity of the triazenes. Ultimately, these findings contribute to the development of more effective strategies for combating malaria and microbial infections. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=malaria" title="malaria">malaria</a>, <a href="https://publications.waset.org/abstracts/search?q=anti-microbials" title=" anti-microbials"> anti-microbials</a>, <a href="https://publications.waset.org/abstracts/search?q=triazene" title=" triazene"> triazene</a>, <a href="https://publications.waset.org/abstracts/search?q=resistance" title=" resistance"> resistance</a> </p> <a href="https://publications.waset.org/abstracts/168948/triazenes-unearthing-their-hidden-arsenal-against-malaria-and-microbial-menace" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/168948.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">102</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6229</span> Assessing the Impact of Antiretroviral Mediated Drug-Drug Interactions on Piperaquine Antimalarial Treatment in Pregnant Women Using Physiologically Based Pharmacokinetic Modelling</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Olusola%20Omolola%20Olafuyi">Olusola Omolola Olafuyi</a>, <a href="https://publications.waset.org/abstracts/search?q=Michael%20Coleman"> Michael Coleman</a>, <a href="https://publications.waset.org/abstracts/search?q=Raj%20Kumar%20Singh%20Badhan"> Raj Kumar Singh Badhan</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Introduction: Malaria in pregnancy has morbidity and mortality implication on both mother and unborn child. Piperaquine (PQ) based antimalarial treatment is emerging as a choice antimalarial for pregnant women in the face of resistance to current antimalarial treatment recommendation in pregnancy. Physiological and biochemical changes in pregnant women may affect the pharmacokinetics of the antimalarial drug in these. In malaria endemic regions other infectious diseases like HIV/AIDs are prevalent. Pregnant women who are co-infected with malaria and HIV/AID are at even more greater risk of death not only due to complications of the diseases but also due to drug-drug interactions (DDIs) between antimalarials (AMT) and antiretroviral (ARVs). In this study, physiologically based pharmacokinetic (PBPK) modelling was used to investigate the effect of physiological and biochemical changes on the impact of ARV mediated DDIs in pregnant women in three countries. Method: A PBPK model for PQ was developed on SimCYP® using published physicochemical and pharmacokinetic data of PQ from literature, this was validated in three customized population groups from Thailand, Sudan and Papua New Guinea with clinical data. Validation of PQ model was also done in presence of interaction with efavirenz (pre-validated on SimCYP®). Different albumin levels and pregnancy stages was simulated in the presence of interaction with standard doses of efavirenz and ritonavir. PQ day 7 concentration of 30ng/ml was used as the efficacy endpoint for PQ treatment.. Results: The median day 7 concentration of PQ remained virtually consistent throughout pregnancy and were satisfactory across the three population groups ranging from 26-34.1ng/ml; this implied the efficacy of PQ throughout pregnancy. DDI interaction with ritonavir and efavirenz resulted in modest effect on the day 7 concentrations of PQ with AUCratio ranging from 0.56-0.8 and 1.64-1.79 for efavirenz and ritonavir respectively over 10-40 gestational weeks, however, a reduction in human serum albumin level reflective of severe malaria resulted in significantly reduced the number of subjects attaining the PQ day 7 concentration in the presence of both DDIs. The model demonstrated that the DDI between PQ and ARV in pregnant women with different malaria severities can alter the pharmacokinetic of PQ. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=antiretroviral" title="antiretroviral">antiretroviral</a>, <a href="https://publications.waset.org/abstracts/search?q=malaria" title=" malaria"> malaria</a>, <a href="https://publications.waset.org/abstracts/search?q=piperaquine" title=" piperaquine"> piperaquine</a>, <a href="https://publications.waset.org/abstracts/search?q=pregnancy" title=" pregnancy"> pregnancy</a>, <a href="https://publications.waset.org/abstracts/search?q=physiologically-based%20pharmacokinetics" title=" physiologically-based pharmacokinetics"> physiologically-based pharmacokinetics</a> </p> <a href="https://publications.waset.org/abstracts/72751/assessing-the-impact-of-antiretroviral-mediated-drug-drug-interactions-on-piperaquine-antimalarial-treatment-in-pregnant-women-using-physiologically-based-pharmacokinetic-modelling" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/72751.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">185</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6228</span> Quantitative Assessment of Different Formulations of Antimalarials in Sentinel Sites of India </h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Taruna%20Katyal%20Arora">Taruna Katyal Arora</a>, <a href="https://publications.waset.org/abstracts/search?q=Geeta%20Kumari"> Geeta Kumari</a>, <a href="https://publications.waset.org/abstracts/search?q=Hari%20Shankar"> Hari Shankar</a>, <a href="https://publications.waset.org/abstracts/search?q=Neelima%20Mishra"> Neelima Mishra</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Substandard and counterfeit antimalarials is a major problem in malaria endemic areas. The availability of counterfeit/ substandard medicines is not only decreasing the efficacy in patients, but it is also one of the contributing factors for developing antimalarial drug resistance. Owing to this, a pilot study was conducted to survey quality of drugs collected from different malaria endemic areas of India. Artesunate+Sulphadoxine-Pyrimethamine (AS+SP), Artemether-Lumefantrine (AL), Chloroquine (CQ) tablets were randomly picked from public health facilities in selected states of India. The quality of antimalarial drugs from these areas was assessed by using Global Pharma Health Fund Minilab test kit. This includes physical/visual inspection and disintegration test. Thin-layer chromatography (TLC) was carried out for semi-quantitative assessment of active pharmaceutical ingredients. A total of 45 brands, out of which 21 were for CQ, 14 for AL and 10 for AS+SP were tested from Uttar Pradesh (U.P.), Mizoram, Meghalaya and Gujrat states. One out of 45 samples showed variable disintegration and retension factor. The variable disintegration and retention factor which would have been due to substandard quality or other factors including storage. However, HPLC analysis confirms standard active pharmaceutical ingredient, but may be due to humid temperature and moisture in storage may account for the observed result. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=antimalarial%20medicines" title="antimalarial medicines">antimalarial medicines</a>, <a href="https://publications.waset.org/abstracts/search?q=counterfeit" title=" counterfeit"> counterfeit</a>, <a href="https://publications.waset.org/abstracts/search?q=substandard" title=" substandard"> substandard</a>, <a href="https://publications.waset.org/abstracts/search?q=TLC" title=" TLC"> TLC</a> </p> <a href="https://publications.waset.org/abstracts/46779/quantitative-assessment-of-different-formulations-of-antimalarials-in-sentinel-sites-of-india" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/46779.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">320</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6227</span> Determination of the Inhibitory Effects of N-Methylpyrrole Derivatives on Glutathione Reductase Enzyme</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Esma%20Kocaoglu">Esma Kocaoglu</a>, <a href="https://publications.waset.org/abstracts/search?q=Oktay%20Talaz"> Oktay Talaz</a>, <a href="https://publications.waset.org/abstracts/search?q=Huseyin%20Cavdar"> Huseyin Cavdar</a>, <a href="https://publications.waset.org/abstracts/search?q=Murat%20Senturk"> Murat Senturk</a>, <a href="https://publications.waset.org/abstracts/search?q=Deniz%20Eki%CC%87nci%CC%87"> Deniz Eki̇nci̇</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Glutathione reductase (GR) is a crucial antioxidant enzyme which is responsible for the maintenance of the antioxidant GSH (glutathione) molecule. Antimalarial effects of some chemical molecules are attributed to their inhibition of GR; thus inhibitors of this enzyme are expected to be promising candidates for the treatment of malaria. In this work, GR inhibitory properties of N-Methylpyrrole derivatives are reported. Firstly, GR was purified by means of affinity chromatography using 2’,5’-ADP-Sepharose 4B as ligand. Enzymatic activity was measured by Beutler’s method. Synthesis of the compounds was approved by thin layer chromatography and column chromatography. Different inhibitor concentrations were used and all compounds were tested in triplicate at each concentration used. It was found that all compounds have better inhibitory activity than the strong GR inhibitor N,N-bis(2-chloroethyl)-N-nitrosourea, especially three molecules, 8m, 8n, and 8q, are the best among them with low micromolar I₅₀ values. Findings of our study indicate that these Schiff base derivatives are strong GR inhibitors which can be used as leads for designation of novel antimalaria candidates. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=glutathione%20reductase" title="glutathione reductase">glutathione reductase</a>, <a href="https://publications.waset.org/abstracts/search?q=antimalaria" title=" antimalaria"> antimalaria</a>, <a href="https://publications.waset.org/abstracts/search?q=inhibitor" title=" inhibitor"> inhibitor</a>, <a href="https://publications.waset.org/abstracts/search?q=enzyme" title=" enzyme"> enzyme</a> </p> <a href="https://publications.waset.org/abstracts/96801/determination-of-the-inhibitory-effects-of-n-methylpyrrole-derivatives-on-glutathione-reductase-enzyme" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/96801.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">270</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6226</span> Sulfonic Acid Functionalized Ionic Liquid in Combinatorial Approach: A Recyclable and Water Tolerant-Acidic Catalyst for Friedlander Quinoline Synthesis</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Jafar%20Akbari">Jafar Akbari</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Quinolines are very important compounds partially because of their pharmacological properties which include wide applications in medicinal chemistry. notable among them are antimalarial drugs, anti-inflammatory agents, antiasthamatic, antibacterial, antihypertensive, and tyrosine kinase inhibiting agents. Despite quinoline usage in pharmaceutical and other industries, comparatively few methods for their preparation have been reported.The Friedlander annulation is one of the simplest and most straightforward methods for the synthesis of poly substituted quinolines. Although, modified methods employing lewis or br¢nsted acids have been reported for the synthesis of quinolines, the development of water stable acidic catalyst for quinoline synthesis is quite desirable. One of the most remarkable features of ionic liquids is that the yields can be optimized by changing the anions or the cations. Recently, sulfonic acid functionalized ionic liquids were used as solvent-catalyst for several organic reactions. We herein report the one pot domino approach for the synthesis of quinoline derivatives in Friedlander manner using TSIL as a catalyst. These ILs are miscible in water, and their homogeneous system is readily separated from the reaction product, combining advantages of both homogeneous and heterogeneous catalysis. In this reaction, the catalyst plays a dual role; it ensures an effective condensation and cyclization of 2-aminoaryl ketone with second carbonyl group and it also promotes the aromatization to the final product. Various types of quinolines from 2-aminoaryl ketones and β-ketoesters/ketones were prepared in 85-98% yields using the catalytic system of SO3-H functionalized ionic liquid/H2O. More importantly, the catalyst could be easily recycled for five times without loss of much activity. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=antimalarial%20drugs" title="antimalarial drugs">antimalarial drugs</a>, <a href="https://publications.waset.org/abstracts/search?q=green%20chemistry" title=" green chemistry"> green chemistry</a>, <a href="https://publications.waset.org/abstracts/search?q=ionic%20liquid" title=" ionic liquid"> ionic liquid</a>, <a href="https://publications.waset.org/abstracts/search?q=quinolines" title=" quinolines"> quinolines</a> </p> <a href="https://publications.waset.org/abstracts/52922/sulfonic-acid-functionalized-ionic-liquid-in-combinatorial-approach-a-recyclable-and-water-tolerant-acidic-catalyst-for-friedlander-quinoline-synthesis" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/52922.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">210</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6225</span> Development and in vitro Evaluation of Polymer-Drug Conjugates Containing Potentiating Agents for Combination Therapy</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Blessing%20A.%20Aderibigbe">Blessing A. Aderibigbe</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Combination therapy is a treatment approach that is used to prevent the emergence of drug resistance. This approach is used for the treatment of many chronic and infectious diseases. Potentiating agents are currently explored in combination therapy, resulting in excellent therapeutic outcomes. Breast cancer and malaria are two chronic conditions responsible globally for high death rates. In this research, a class of polymer-drug conjugates containing potentiating agents with either antimalarial or anticancer drugs were prepared by Michael Addition Polymerization reaction and ring-opening polymerization reaction. Conjugation of potentiating agents with bioactive compounds into the polymers resulted in conjugates with good water solubility, highly selective and non-toxic. In vitro cytotoxicity and in vitro antiplasmodial evaluation on the conjugates revealed that the conjugates were more effective when compared to the free drugs. The drug release studies further showed that the release profile of the drugs from the conjugates was sustained. The findings revealed the potential of polymer-drug conjugates to overcome drug toxicity and drug resistance, which is common with the currently used antimalarial and anticancer drugs. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=anticancer" title="anticancer">anticancer</a>, <a href="https://publications.waset.org/abstracts/search?q=antimalarials" title=" antimalarials"> antimalarials</a>, <a href="https://publications.waset.org/abstracts/search?q=combination%20therapy" title=" combination therapy"> combination therapy</a>, <a href="https://publications.waset.org/abstracts/search?q=polymer-drug%20conjugates" title=" polymer-drug conjugates"> polymer-drug conjugates</a> </p> <a href="https://publications.waset.org/abstracts/111039/development-and-in-vitro-evaluation-of-polymer-drug-conjugates-containing-potentiating-agents-for-combination-therapy" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/111039.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">133</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6224</span> Synthesis and Pharmaco-Potential Evaluation of Quinoline Hybrids</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Paul%20Awolade">Paul Awolade</a>, <a href="https://publications.waset.org/abstracts/search?q=Parvesh%20Singh"> Parvesh Singh</a> </p> <p class="card-text"><strong>Abstract:</strong></p> The global threat of pathogenic resistance to available therapeutic agents has become a menace to clinical practice, public health and man’s existence inconsequential. This has therefore led to an exigency in the development of new molecular scaffolds with profound activity profiles. In this vein, a versatile synthetic tool for accessing new molecules by incorporating two or more pharmacophores into a single entity with the unique ability to be recognized by multiple receptors hence leading to an improved bioactivity, known as molecular hybridization, has been explored with tremendous success. Accordingly, aware of the similarity in pharmacological activity spectrum of quinoline and 1,2,3-triazole pharmacophores such as; anti-Alzheimer, anticancer, anti-HIV, antimalarial and antimicrobial to mention but a few, the present study sets out to synthesize hybrids of quinoline and 1,2,3-triazole. The hybrids were accessed via click chemistry using copper catalysed azide-alkyne 1,3-dipolar cycloaddition reaction. All synthesized compounds were evaluated for their pharmaco-potential in an antimicrobial assay out of which the 3-OH derivative emerged as the most active with MIC value of 4 μg/mL against Cryptococcus neoformans; a value superior to standard Fluconazole and comparable to Amphotericin B. Structures of synthesized hybrids were elucidated using appropriate spectroscopic techniques (1H, 13C and 2D NMR, FT-IR and HRMS). <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=bioisostere" title="bioisostere">bioisostere</a>, <a href="https://publications.waset.org/abstracts/search?q=click%20chemistry" title=" click chemistry"> click chemistry</a>, <a href="https://publications.waset.org/abstracts/search?q=molecular%20hybridization" title=" molecular hybridization"> molecular hybridization</a>, <a href="https://publications.waset.org/abstracts/search?q=quinoline" title=" quinoline"> quinoline</a>, <a href="https://publications.waset.org/abstracts/search?q=1" title=" 1"> 1</a>, <a href="https://publications.waset.org/abstracts/search?q=2" title="2">2</a>, <a href="https://publications.waset.org/abstracts/search?q=3-triazole" title="3-triazole">3-triazole</a> </p> <a href="https://publications.waset.org/abstracts/99723/synthesis-and-pharmaco-potential-evaluation-of-quinoline-hybrids" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/99723.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">129</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6223</span> Immunoliposome-Mediated Drug Delivery to Plasmodium-Infected and Non-Infected Red Blood Cells as a Dual Therapeutic/Prophylactic Antimalarial Strategy</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Ernest%20Moles">Ernest Moles</a>, <a href="https://publications.waset.org/abstracts/search?q=Patricia%20Urb%C3%A1n"> Patricia Urbán</a>, <a href="https://publications.waset.org/abstracts/search?q=Mar%C3%ADa%20Bel%C3%A9n%20Jim%C3%A9nez-D%C3%ADaz"> María Belén Jiménez-Díaz</a>, <a href="https://publications.waset.org/abstracts/search?q=Sara%20Viera-Morilla"> Sara Viera-Morilla</a>, <a href="https://publications.waset.org/abstracts/search?q=I%C3%B1igo%20Angulo-Barturen"> Iñigo Angulo-Barturen</a>, <a href="https://publications.waset.org/abstracts/search?q=Maria%20Ant%C3%B2nia%20Busquets"> Maria Antònia Busquets</a>, <a href="https://publications.waset.org/abstracts/search?q=Xavier%20Fern%C3%A0ndez-Busquets"> Xavier Fernàndez-Busquets</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Bearing in mind the absence of an effective vaccine against malaria and its severe clinical manifestations causing nearly half a million deaths every year, this disease represents nowadays a major threat to life. Besides, the basic rationale followed by currently marketed antimalarial approaches is based on the administration of drugs on their own, promoting the emergence of drug-resistant parasites owing to the limitation in delivering drug payloads into the parasitized erythrocyte high enough to kill the intracellular pathogen while minimizing the risk of causing toxic side effects to the patient. Such dichotomy has been successfully addressed through the specific delivery of immunoliposome (iLP)-encapsulated antimalarials to Plasmodium falciparum-infected red blood cells (pRBCs). Unfortunately, this strategy has not progressed towards clinical applications, whereas in vitro assays rarely reach drug efficacy improvements above 10-fold. Here, we show that encapsulation efficiencies reaching >96% can be achieved for the weakly basic drugs chloroquine (CQ) and primaquine using the pH gradient active loading method in liposomes composed of neutrally charged, saturated phospholipids. Targeting antibodies are best conjugated through their primary amino groups, adjusting chemical crosslinker concentration to retain significant antigen recognition. Antigens from non-parasitized RBCs have also been considered as targets for the intracellular delivery of drugs not affecting the erythrocytic metabolism. Using this strategy, we have obtained unprecedented nanocarrier targeting to early intraerythrocytic stages of the malaria parasite for which there is a lack of specific extracellular molecular tags. Polyethylene glycol-coated liposomes conjugated with monoclonal antibodies specific for the erythrocyte surface protein glycophorin A (anti-GPA iLP) were capable of targeting 100% RBCs and pRBCs at the low concentration of 0.5 μM total lipid in the culture, with >95% of added iLPs retained into the cells. When exposed for only 15 min to P. falciparum in vitro cultures synchronized at early stages, free CQ had no significant effect over parasite viability up to 200 nM drug, whereas iLP-encapsulated 50 nM CQ completely arrested its growth. Furthermore, when assayed in vivo in P. falciparum-infected humanized mice, anti-GPA iLPs cleared the pathogen below detectable levels at a CQ dose of 0.5 mg/kg. In comparison, free CQ administered at 1.75 mg/kg was, at most, 40-fold less efficient. Our data suggest that this significant improvement in drug antimalarial efficacy is in part due to a prophylactic effect of CQ found by the pathogen in its host cell right at the very moment of invasion. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=immunoliposomal%20nanoparticles" title="immunoliposomal nanoparticles">immunoliposomal nanoparticles</a>, <a href="https://publications.waset.org/abstracts/search?q=malaria" title=" malaria"> malaria</a>, <a href="https://publications.waset.org/abstracts/search?q=prophylactic-therapeutic%20polyvalent%20activity" title=" prophylactic-therapeutic polyvalent activity"> prophylactic-therapeutic polyvalent activity</a>, <a href="https://publications.waset.org/abstracts/search?q=targeted%20drug%20delivery" title=" targeted drug delivery"> targeted drug delivery</a> </p> <a href="https://publications.waset.org/abstracts/42679/immunoliposome-mediated-drug-delivery-to-plasmodium-infected-and-non-infected-red-blood-cells-as-a-dual-therapeuticprophylactic-antimalarial-strategy" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/42679.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">375</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6222</span> Antioxidant Activity of the Algerian Traditional Kefir Supernatant</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=H.%20Amellal-Chibane">H. Amellal-Chibane</a>, <a href="https://publications.waset.org/abstracts/search?q=N.%20Dehdouh"> N. Dehdouh</a>, <a href="https://publications.waset.org/abstracts/search?q=S.%20Ait-Kaki"> S. Ait-Kaki</a>, <a href="https://publications.waset.org/abstracts/search?q=F.%20%20Halladj"> F. Halladj</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Kefir is fermented milk that is produced by adding Kefir grains, consisting of bacteria and yeasts, to milk. The aim of this study was to investigate the antioxidant activity of the kefir supernatant and the raw milk. The Antioxidant activity assays of kefir supernatant and raw milk were evaluated by assessing the DPPH radical-scavenging activity. Kefir supernatant demonstrated high antioxidant activity (87.75%) compared to the raw milk (70.59 %). These results suggest that the Algerian kefir has interesting antioxidant activity. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=antioxidant%20activity" title="antioxidant activity">antioxidant activity</a>, <a href="https://publications.waset.org/abstracts/search?q=kefir" title=" kefir"> kefir</a>, <a href="https://publications.waset.org/abstracts/search?q=kefir%20supernatant" title=" kefir supernatant"> kefir supernatant</a>, <a href="https://publications.waset.org/abstracts/search?q=raw%20milk" title=" raw milk "> raw milk </a> </p> <a href="https://publications.waset.org/abstracts/24330/antioxidant-activity-of-the-algerian-traditional-kefir-supernatant" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/24330.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">506</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6221</span> Total Synthesis of Natural Cyclic Depsi Peptides by Convergent SPPS and Macrolactonization Strategy for Anti-Tb Activity</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Katharigatta%20N.%20Venugopala">Katharigatta N. Venugopala</a>, <a href="https://publications.waset.org/abstracts/search?q=Fernando%20Albericio"> Fernando Albericio</a>, <a href="https://publications.waset.org/abstracts/search?q=Bander%20E.%20Al-Dhubiab"> Bander E. Al-Dhubiab</a>, <a href="https://publications.waset.org/abstracts/search?q=T.%20Govender"> T. Govender </a> </p> <p class="card-text"><strong>Abstract:</strong></p> Recent years have witnessed a renaissance in the field of peptides that are obtained from various natural sources such as many bacteria, fungi, plants, seaweeds, vertebrates, invertebrates and have been reported for various pharmacological properties such as anti-TB, anticancer, antimalarial, anti-inflammatory, anti-HIV, antibacterial, antifungal, and antidiabetic, activities. In view of the pharmacological significance of natural peptides, serious research efforts of many scientific groups and pharmaceutical companies have consequently focused on them to explore the possibility of developing their potential analogues as therapeutic agents. Solid phase and solution phase peptide synthesis are the two methodologies currently available for the synthesis of natural or synthetic linear or cyclic depsi-peptides. From a synthetic point of view, there is no doubt that the solid-phase methodology gained added advantages over solution phase methodology in terms of simplicity, purity of the compound and the speed with which peptides can be synthesised. In the present study total synthesis, purification and structural elucidation of analogues of natural anti-TB cyclic depsi-peptides such as depsidomycin, massetolides and viscosin has been attempted by solid phase method using standard Fmoc protocols and finally off resin cyclization in solution phase method. In case of depsidomycin, synthesis of linear peptide on solid phase could not be achieved because of two turn inducing amino acids in the peptide sequence, but total synthesis was achieved by convergent solid phase peptide synthesis followed by cyclization in solution phase method. The title compounds obtained were in good yields and characterized by NMR and HRMS. Anti-TB results revealed that the potential title compound exhibited promising activity at 4 µg/mL against H37Rv and 16 µg/mL against MDR strains of tuberculosis. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=total%20synthesis" title="total synthesis">total synthesis</a>, <a href="https://publications.waset.org/abstracts/search?q=cyclic%20depsi-peptides" title=" cyclic depsi-peptides"> cyclic depsi-peptides</a>, <a href="https://publications.waset.org/abstracts/search?q=anti-TB%20activity" title=" anti-TB activity"> anti-TB activity</a>, <a href="https://publications.waset.org/abstracts/search?q=tuberculosis" title=" tuberculosis"> tuberculosis</a> </p> <a href="https://publications.waset.org/abstracts/16893/total-synthesis-of-natural-cyclic-depsi-peptides-by-convergent-spps-and-macrolactonization-strategy-for-anti-tb-activity" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/16893.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">623</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6220</span> Biological Activity of Essential Oils from Salvia nemorosa L.</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Abdol-Hassan%20Doulah">Abdol-Hassan Doulah </a> </p> <p class="card-text"><strong>Abstract:</strong></p> In this study, antimicrobial activity of essential oil and ethyl acetate and ether extracts of S. nemorosa were examined against some species of bacteria and fungi. The essential oil of the aerial part of S. nemorosa was examined by GC and GC-MS. In the essential oil of S. nemorosa 26 Compounds have been identified. 2-Nonanone (44.09 %), 2-Undecanone (33.79 %), E-Caryophyllene (3.74 %) and 2-Decanone (2.89 %) were the main components of the essential oil. The essential oil analysis showed greatest antimicrobial activity against Staphylococcus epidermidis (5.3 μg/ml) and S. cerevisiae (9.3 μg/ml). The ethyl acetate showed greatest antimicrobial activity against Bacillus subtilis (106.7 μg/ml), Candida albicans (5.3 μg/ml) and ether extract showed greatest antimicrobial activity against Klebseilla pneumoniae (10.7 μg/ml) and Saccharomyces cerevisiae (10.7 μg/ml). In conclusion, we suggest that the antimicrobial activity of S. nemorosa may be due to its content of germacrene and linalool. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=antibacterial%20activity" title="antibacterial activity">antibacterial activity</a>, <a href="https://publications.waset.org/abstracts/search?q=antifungal%20activity" title=" antifungal activity"> antifungal activity</a>, <a href="https://publications.waset.org/abstracts/search?q=Salvia%20nemorosa%20L." title=" Salvia nemorosa L."> Salvia nemorosa L.</a>, <a href="https://publications.waset.org/abstracts/search?q=essential%20oils" title=" essential oils"> essential oils</a>, <a href="https://publications.waset.org/abstracts/search?q=biological%20activity" title=" biological activity"> biological activity</a> </p> <a href="https://publications.waset.org/abstracts/31804/biological-activity-of-essential-oils-from-salvia-nemorosa-l" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/31804.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">493</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6219</span> Prevalence of Physical Activity Levels and Perceived Benefits of and Barriers to Physical Activity among Jordanian Patients with Coronary Heart Disease: A Cross-Sectional Study</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Eman%20Ahmed%20Alsaleh">Eman Ahmed Alsaleh</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Background: Many studies published in other countries identified certain perceived benefits and barriers to physical activity among patients with coronary heart disease. Nevertheless, there is no data about the issue relating to Jordanian patients with coronary heart disease. Objective: This study aimed to describe the prevalence of level of physical activity, benefits of and barriers to physical activity as perceived by Jordanian patients with coronary heart disease, and the relationship between physical activity and perceived benefits of and barriers to physical activity. In addition, it focused on examining the influence of selected sociodemographic and health characteristics on physical activity and the perceived benefits of and barriers to physical activity. Methods: A cross-sectional design was performed on a sample of 400 patients with coronary heart disease. They were given a list of perceived benefits and barriers to physical activity and asked to what extent they disagreed or agreed with each. Results: Jordanian patients with coronary heart disease perceived various benefits and barriers to physical activity. Most of these benefits were physiologically related (average mean = 5.7, SD = .7). The most substantial barriers to physical activity as perceived by the patients were: feeling anxiety, not having enough time, lack of interest, bad weather, and feeling of being uncomfortable. Sociodemographic and health characteristics that significantly influenced perceived barriers to physical activity were age, gender, health perception, chest pain frequency, education, job, caring responsibilities, ability to travel alone, smoking, and previous and current physical activity behaviour. Conclusion: This research demonstrates that patients with coronary heart disease have perceived physiological benefits of physical activity, and they have perceived motivational, physical health, and environmental barriers to physical activity, which is significant in developing intervention strategies that aim to maximize patients' participation in physical activity and overcome barriers to physical activity. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=prevalence" title="prevalence">prevalence</a>, <a href="https://publications.waset.org/abstracts/search?q=coronary%20heart%20disease" title=" coronary heart disease"> coronary heart disease</a>, <a href="https://publications.waset.org/abstracts/search?q=physical%20activity" title=" physical activity"> physical activity</a>, <a href="https://publications.waset.org/abstracts/search?q=perceived%20barriers" title=" perceived barriers"> perceived barriers</a> </p> <a href="https://publications.waset.org/abstracts/158570/prevalence-of-physical-activity-levels-and-perceived-benefits-of-and-barriers-to-physical-activity-among-jordanian-patients-with-coronary-heart-disease-a-cross-sectional-study" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/158570.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">113</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6218</span> The Investigation of Correlation between Body Composition and Physical Activity in University Students</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Ferruh%20Taspinar">Ferruh Taspinar</a>, <a href="https://publications.waset.org/abstracts/search?q=Gulce%20K.%20Seyyar"> Gulce K. Seyyar</a>, <a href="https://publications.waset.org/abstracts/search?q=Gamze%20Kurt"> Gamze Kurt</a>, <a href="https://publications.waset.org/abstracts/search?q=Eda%20O.%20Okur"> Eda O. Okur</a>, <a href="https://publications.waset.org/abstracts/search?q=Emrah%20Afsar"> Emrah Afsar</a>, <a href="https://publications.waset.org/abstracts/search?q=Ismail%20Saracoglu"> Ismail Saracoglu</a>, <a href="https://publications.waset.org/abstracts/search?q=Betul%20Taspinar"> Betul Taspinar</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Alterations of physical activity can effect body composition (especially body fat ratio); however body mass index may not sufficient to indicate these minimal differences. The aim of this study was to evaluate the relationship between body composition and physical activity in university students. In this study, 132 university students (mean age; 21.21±1.51) were included. Tanita BC-418 and International Physical Activity Questionnaire (IPAQ) were used to evaluate participants. The correlation between the parameters was analysed via Spearman correlation analysis. Significance level in statistical analyses was accepted is 0.05. The results showed that there was no correlation between body mass index and physical activity (p>0.05). There was a positive correlation between body muscle ratio and physical activity, whereas a negative correlation between body fat ratio and physical activity (p<0.05). This study showed that body fat and muscle ratio affects the level of physical activity in healthy university students. Therefore, we thought that physical activity might reduce effects of the diseases caused by disturbed body composition. Further studies are required to support this idea. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=body%20composition" title="body composition">body composition</a>, <a href="https://publications.waset.org/abstracts/search?q=body%20mass%20index" title=" body mass index"> body mass index</a>, <a href="https://publications.waset.org/abstracts/search?q=physical%20activity" title=" physical activity"> physical activity</a>, <a href="https://publications.waset.org/abstracts/search?q=university%20student" title=" university student"> university student</a> </p> <a href="https://publications.waset.org/abstracts/60659/the-investigation-of-correlation-between-body-composition-and-physical-activity-in-university-students" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/60659.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">355</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6217</span> Chemical Composition and Antioxidant Activity of Methanolic Extract of Spilanthes acmella Murr.</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Wanthani%20Paengsri">Wanthani Paengsri</a>, <a href="https://publications.waset.org/abstracts/search?q=Thanyarat%20Chuesaard"> Thanyarat Chuesaard</a>, <a href="https://publications.waset.org/abstracts/search?q=Napapha%20Promsawan"> Napapha Promsawan</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Spilanthes acmella Murr. was extracted with methanol, yielding methanol crude extract 5.86 %w/w. This study aimed to examine the chemical composition and antioxidant activity of methanolic crude extract. The chemical composition of methanolic crude extract was analyzed by gas chromatography-mass spectrometry (GC-MS). The predominant components were found to be palmitic acid (40.08%), 2-hexadecanoyl glycerol (6.96%) and octadecanoic acid (4.06%). Antioxidant activity was determined using 2,2-diphenyl-1-picryl hydrazyl (DPPH) free radical, for evaluating free radicle scavenging activity. The methanolic extract at 150 µg/mL showed an antioxidant activity with high of radical scavenging activity (75.23%). <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=antioxidant%20activity" title="antioxidant activity">antioxidant activity</a>, <a href="https://publications.waset.org/abstracts/search?q=GC-MS%20analysis" title=" GC-MS analysis"> GC-MS analysis</a>, <a href="https://publications.waset.org/abstracts/search?q=Spilanthes" title=" Spilanthes"> Spilanthes</a>, <a href="https://publications.waset.org/abstracts/search?q=Phak-Kratt%20Hauwaen" title=" Phak-Kratt Hauwaen"> Phak-Kratt Hauwaen</a> </p> <a href="https://publications.waset.org/abstracts/80642/chemical-composition-and-antioxidant-activity-of-methanolic-extract-of-spilanthes-acmella-murr" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/80642.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">531</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6216</span> Polyphenols Content and Antioxidant Activity of Extracts from Peganum harmala Seeds</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Rachid%20Kacem">Rachid Kacem</a>, <a href="https://publications.waset.org/abstracts/search?q=Sara%20Talbi"> Sara Talbi</a>, <a href="https://publications.waset.org/abstracts/search?q=Yasmina%20Hemissi"> Yasmina Hemissi</a>, <a href="https://publications.waset.org/abstracts/search?q=Sofia%20%20Bouguattoucha"> Sofia Bouguattoucha</a> </p> <p class="card-text"><strong>Abstract:</strong></p> The aim of the present work is the evaluation of the antioxidant activity of the Peganum harmala (P. harmala) seeds extracts. The antioxidant activity was evaluated by applying two methods, the method of ß-carotene bleaching and DPPH (2, 2-Diphenyl-1-Picryl-Hydrazyl). Using Folin-Ciocalteu assay, these results revealed that the concentration of polyphenols in EthOH E. (122.28 ± 2.24 µg GAE/mg extract) is the highest. The antiradical activity of the P. harmala seeds extracts on DPPH was found to be dose dependent with polyphenols concentration. The E. EthOH extract showed the highest antioxidant activity (IC = 252.10 ± 11.18 μg /ml). The test of β-carotene bleaching indicates that the E. EthOH of P. harmala showed the highest percentage of the antioxidant activity (49.88 %). <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=antioxidant%20activity" title="antioxidant activity">antioxidant activity</a>, <a href="https://publications.waset.org/abstracts/search?q=Peganum%20harmala" title=" Peganum harmala"> Peganum harmala</a>, <a href="https://publications.waset.org/abstracts/search?q=polyphenols" title=" polyphenols"> polyphenols</a>, <a href="https://publications.waset.org/abstracts/search?q=flavonoids" title=" flavonoids "> flavonoids </a> </p> <a href="https://publications.waset.org/abstracts/32852/polyphenols-content-and-antioxidant-activity-of-extracts-from-peganum-harmala-seeds" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/32852.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">506</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6215</span> Polyphenol and Antimicrobial Activity in Olive Oil from Algeria</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Kamel%20Zemour">Kamel Zemour</a>, <a href="https://publications.waset.org/abstracts/search?q=Kada%20Mohamed%20Amine%20Chouhim"> Kada Mohamed Amine Chouhim</a>, <a href="https://publications.waset.org/abstracts/search?q=Mohamed%20Mairif"> Mohamed Mairif</a>, <a href="https://publications.waset.org/abstracts/search?q=Tadj%20Eddine%20Adda%20Ardjan"> Tadj Eddine Adda Ardjan</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Many recent studies show the positive effect of phenolic compounds in olive oil on health. They are known for their biological properties, where they have shown potential activity as an antioxidant, anti-inflammatory, and antimicrobial agents. However, this characteristic is rarely studied in olive oil from different regions of Algeria. Different samples collected from the western region of Algeria were evaluated for their polyphenol content, antioxidant activity, and antimicrobial effect. The obtained results demonstrated that this oil is rich in polyphenols and revealed high antimicrobial activity against Staphylococcus aureus and Escherichia coli. Finally, this study has highlighted the nutritional and pharmaceutical importance of olive oil grown in Algeria. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=olive%20oil" title="olive oil">olive oil</a>, <a href="https://publications.waset.org/abstracts/search?q=polyphenols" title=" polyphenols"> polyphenols</a>, <a href="https://publications.waset.org/abstracts/search?q=antioxidant%20activity" title=" antioxidant activity"> antioxidant activity</a>, <a href="https://publications.waset.org/abstracts/search?q=antimicrobial%20activity" title=" antimicrobial activity"> antimicrobial activity</a> </p> <a href="https://publications.waset.org/abstracts/159649/polyphenol-and-antimicrobial-activity-in-olive-oil-from-algeria" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/159649.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">152</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6214</span> The Effect of Solution pH of Chitosan on Antimicrobial Properties of Nylon 6,6 Fabrics</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Nil%C3%BCfer%20Y%C4%B1ld%C4%B1z%20Varan">Nilüfer Yıldız Varan</a> </p> <p class="card-text"><strong>Abstract:</strong></p> The antimicrobial activities of chitosan against various bacteria and fungi are well known, and the antimicrobial activity of chitosan depends on pH. This study investigates the antimicrobial activity at different pH levels. Nylon 6,6 fabrics were treated with different chitosan solutions. Additionally, samples were treated also in basic conditions to see the antimicrobial activities. AATCC Test Method 100 was followed to evaluate the antimicrobial activity using Staphylococcus aureus ATCC 6538 test inoculum. The pH of the chitosan solutions was controlled below 6.5 since chitosan shows its antimicrobial activity only in acidic conditions because of its poor solubility above 6.5. In basic conditions, the samples did not show any antimicrobial activity. It appears from SEM images that the bonded chitosan in the structures exists. In acidic media (ph < 6.5), all samples showed antimicrobial activity. No correlation was found between pH levels and antimicrobial activity in acidic media. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=chitosan" title="chitosan">chitosan</a>, <a href="https://publications.waset.org/abstracts/search?q=nylon%206" title=" nylon 6"> nylon 6</a>, <a href="https://publications.waset.org/abstracts/search?q=6" title="6">6</a>, <a href="https://publications.waset.org/abstracts/search?q=crosslinking" title=" crosslinking"> crosslinking</a>, <a href="https://publications.waset.org/abstracts/search?q=pH%20stability" title=" pH stability"> pH stability</a>, <a href="https://publications.waset.org/abstracts/search?q=antimicrobial" title=" antimicrobial"> antimicrobial</a> </p> <a href="https://publications.waset.org/abstracts/74096/the-effect-of-solution-ph-of-chitosan-on-antimicrobial-properties-of-nylon-66-fabrics" class="btn btn-primary btn-sm">Procedia</a> <a 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