Search results for: microsome

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microsome</title> <meta name="description" content="Search results for: microsome"> <meta name="keywords" content="microsome"> <meta name="viewport" content="width=device-width, initial-scale=1, minimum-scale=1, maximum-scale=1, user-scalable=no"> <meta charset="utf-8"> <link href="https://cdn.waset.org/favicon.ico" type="image/x-icon" rel="shortcut icon"> <link href="https://cdn.waset.org/static/plugins/bootstrap-4.2.1/css/bootstrap.min.css" rel="stylesheet"> <link href="https://cdn.waset.org/static/plugins/fontawesome/css/all.min.css" rel="stylesheet"> <link href="https://cdn.waset.org/static/css/site.css?v=150220211555" rel="stylesheet"> </head> <body> <header> <div class="container"> <nav class="navbar navbar-expand-lg navbar-light"> <a class="navbar-brand" href="https://waset.org"> <img src="https://cdn.waset.org/static/images/wasetc.png" alt="Open Science Research Excellence" title="Open Science Research Excellence" /> </a> <button class="d-block d-lg-none navbar-toggler ml-auto" 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id="custom-search-input"> <div class="input-group"> <i class="fas fa-search"></i> <input type="text" class="search-query" name="q" placeholder="Author, Title, Abstract, Keywords" value="microsome"> <input type="submit" class="btn_search" value="Search"> </div> </div> </form> </div> </div> <div class="row mt-3"> <div class="col-sm-3"> <div class="card"> <div class="card-body"><strong>Commenced</strong> in January 2007</div> </div> </div> <div class="col-sm-3"> <div class="card"> <div class="card-body"><strong>Frequency:</strong> Monthly</div> </div> </div> <div class="col-sm-3"> <div class="card"> <div class="card-body"><strong>Edition:</strong> International</div> </div> </div> <div class="col-sm-3"> <div class="card"> <div class="card-body"><strong>Paper Count:</strong> 4</div> </div> </div> </div> <h1 class="mt-3 mb-3 text-center" style="font-size:1.6rem;">Search results for: microsome</h1> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">4</span> Investigation of Mutagenicity and DNA Binding Properties of Metal-Free and Metallophthalocyanines Containing α-Napththolbenzein Groups on the Peripheral Positions</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Meltem%20Bet%C3%BCl%20Sa%C4%9Flam">Meltem Betül Sağlam</a>, <a href="https://publications.waset.org/abstracts/search?q=Halil%20I%CC%87brahim%20G%C3%BCler"> Halil İbrahim Güler</a>, <a href="https://publications.waset.org/abstracts/search?q=Aykut%20Sa%C4%9Flam"> Aykut Sağlam</a> </p> <p class="card-text"><strong>Abstract:</strong></p> In this work, phthalocyanine compounds containing α-naphtholbenzeinunits have been synthesized. Mutagenicity and DNA binding properties of the compounds were investigated by Salmonella/Microsome Assay and spectrophotometer. According to the results of the preliminary range finding tests, the compounds gave no toxic effect to all tester strain S. typhimurium TA98 and TA100 at doses of 500, 1100, 350, 500 and 750 µg/plate in the presence and absence of S9, respectively. This study showed that all compounds exhibited efficient DNA-binding activity. In conclusion, these non-toxic compounds may be used as effective DNA dyes for molecular biology studies. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=dye" title="dye">dye</a>, <a href="https://publications.waset.org/abstracts/search?q=mutagenicity" title=" mutagenicity"> mutagenicity</a>, <a href="https://publications.waset.org/abstracts/search?q=phthalocyanine" title=" phthalocyanine"> phthalocyanine</a>, <a href="https://publications.waset.org/abstracts/search?q=toxicity" title=" toxicity"> toxicity</a> </p> <a href="https://publications.waset.org/abstracts/73822/investigation-of-mutagenicity-and-dna-binding-properties-of-metal-free-and-metallophthalocyanines-containing-a-napththolbenzein-groups-on-the-peripheral-positions" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/73822.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">231</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">3</span> Mutagenic in vitro Activity and Genotoxic Effect of Zygophyllum Cornutun Methanolic Extract </h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Awatif%20Boumaza">Awatif Boumaza</a>, <a href="https://publications.waset.org/abstracts/search?q=Abderraouf%20Hilali"> Abderraouf Hilali</a>, <a href="https://publications.waset.org/abstracts/search?q=Hayat%20Talbi"> Hayat Talbi</a>, <a href="https://publications.waset.org/abstracts/search?q=Houda%20Sbayou"> Houda Sbayou</a> </p> <p class="card-text"><strong>Abstract:</strong></p> The methanolic extract of Zygophyllum cornutun coss, an Algerian medicinal plant, was screened to the presence of mutagenic activity and genotoxic effect using the Ames test (Salmonella/microsome) and the micronucleus assay respectively. Positive results were obtained with both tests. The Ames test showed mutagenic activity in the presence of microsomal activation, while negative result was observed without microsomal activation. In the micronucleus test, two parameters were evaluated: the frequency of the micronucleus that increased in a dose dependent way and the proliferation index that decreased according to the micronucleus frequency. Even that further studies must be carried out, the mutagenic activity and the genotoxic effect of Zygophyllum cornutum should be taken in consideration when used as therapeutic plant. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=ames%20test" title="ames test">ames test</a>, <a href="https://publications.waset.org/abstracts/search?q=micronucleus%20test" title=" micronucleus test"> micronucleus test</a>, <a href="https://publications.waset.org/abstracts/search?q=mutagenic%20activity" title=" mutagenic activity"> mutagenic activity</a>, <a href="https://publications.waset.org/abstracts/search?q=genotoxicity" title=" genotoxicity"> genotoxicity</a>, <a href="https://publications.waset.org/abstracts/search?q=Zygophyllum%20cornutum" title=" Zygophyllum cornutum"> Zygophyllum cornutum</a> </p> <a href="https://publications.waset.org/abstracts/17170/mutagenic-in-vitro-activity-and-genotoxic-effect-of-zygophyllum-cornutun-methanolic-extract" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/17170.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">510</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">2</span> The Metabolite Profiling of Fulvestrant-3 Boronic Acid under Biological Oxidation</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Changde%20Zhang">Changde Zhang</a>, <a href="https://publications.waset.org/abstracts/search?q=Qiang%20Zhang"> Qiang Zhang</a>, <a href="https://publications.waset.org/abstracts/search?q=Shilong%20Zheng"> Shilong Zheng</a>, <a href="https://publications.waset.org/abstracts/search?q=Jiawang%20Liu"> Jiawang Liu</a>, <a href="https://publications.waset.org/abstracts/search?q=Shanchun%20Guo"> Shanchun Guo</a>, <a href="https://publications.waset.org/abstracts/search?q=Qiu%20Zhong"> Qiu Zhong</a>, <a href="https://publications.waset.org/abstracts/search?q=Guangdi%20Wang"> Guangdi Wang</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Fulvestrant was approved by FDA to treat breast cancer as a selective estrogen receptor downregulator (SERD) with intramuscular injection administration. ZB716, a fulvestarnt-3 boronic acid, is an SERD with comparable anticancer effect to fulvestrant, but could produce good pharmacokinetic properties under oral administration with mice or rat models. To understand why ZB716 produced much better oral bioavailability, it was proposed that the boronic acid blocked the phase II direct biotransformation with the hydroxyl group on the 3 position of the aromatic ring on fulvestrant. In this study, ZB716 or fulvestrant was incubated with human liver microsome and oxidation cofactor NADPH in vitro. Their metabolites after oxidation were profiled with the Q-Exactive, a high-resolution mass spectrometer. The result showed that ZB716 blocked the forming of hydroxyl groups on its benzene ring except for the oxidation of C-B bond forming fulvestrant in its metabolites, and the concentration of fulvestrant with one more hydroxyl group found in the metabolites from incubation with fulvestrant was about 34 fold high as that formed from incubation with ZB716. Compared to fulvestrant, ZB716 is expected to be much difficult to be further bio-transformed into more hydrophilic compounds, to be difficult excreted out of blood system, and to have longer residence time in blood, which can lead to higher oral bioavailability. This study provided evidence to explain the high bioavailability of ZB716 after oral administration from the perspective of its difficulty of oxidation, a phase I biotransformation, on positions on its aromatic ring. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=biotransformation" title="biotransformation">biotransformation</a>, <a href="https://publications.waset.org/abstracts/search?q=fulvestrant" title=" fulvestrant"> fulvestrant</a>, <a href="https://publications.waset.org/abstracts/search?q=metabolite%20profiling" title=" metabolite profiling"> metabolite profiling</a>, <a href="https://publications.waset.org/abstracts/search?q=ZB716" title=" ZB716"> ZB716</a> </p> <a href="https://publications.waset.org/abstracts/72780/the-metabolite-profiling-of-fulvestrant-3-boronic-acid-under-biological-oxidation" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/72780.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">259</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">1</span> Identification, Synthesis, and Biological Evaluation of the Major Human Metabolite of NLRP3 Inflammasome Inhibitor MCC950</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Manohar%20Salla">Manohar Salla</a>, <a href="https://publications.waset.org/abstracts/search?q=Mark%20S.%20Butler"> Mark S. Butler</a>, <a href="https://publications.waset.org/abstracts/search?q=Ruby%20Pelingon"> Ruby Pelingon</a>, <a href="https://publications.waset.org/abstracts/search?q=Geraldine%20Kaeslin"> Geraldine Kaeslin</a>, <a href="https://publications.waset.org/abstracts/search?q=Daniel%20E.%20Croker"> Daniel E. Croker</a>, <a href="https://publications.waset.org/abstracts/search?q=Janet%20C.%20Reid"> Janet C. Reid</a>, <a href="https://publications.waset.org/abstracts/search?q=Jong%20Min%20Baek"> Jong Min Baek</a>, <a href="https://publications.waset.org/abstracts/search?q=Paul%20V.%20Bernhardt"> Paul V. Bernhardt</a>, <a href="https://publications.waset.org/abstracts/search?q=Elizabeth%20M.%20J.%20Gillam"> Elizabeth M. J. Gillam</a>, <a href="https://publications.waset.org/abstracts/search?q=Matthew%20A.%20Cooper"> Matthew A. Cooper</a>, <a href="https://publications.waset.org/abstracts/search?q=Avril%20A.%20B.%20Robertson"> Avril A. B. Robertson</a> </p> <p class="card-text"><strong>Abstract:</strong></p> MCC950 is a potent and selective inhibitor of the NOD-like receptor pyrin domain-containing protein 3 (NLRP3) inflammasome that shows early promise for treatment of inflammatory diseases. The identification of major metabolites of lead molecule is an important step during drug development process. It provides an information about the metabolically labile sites in the molecule and thereby helping medicinal chemists to design metabolically stable molecules. To identify major metabolites of MCC950, the compound was incubated with human liver microsomes and subsequent analysis by (+)- and (−)-QTOF-ESI-MS/MS revealed a major metabolite formed due to hydroxylation on 1,2,3,5,6,7-hexahydro-s-indacene moiety of MCC950. This major metabolite can lose two water molecules and three possible regioisomers were synthesized. Co-elution of major metabolite with each of the synthesized compounds using HPLC-ESI-SRM-MS/MS revealed the structure of the metabolite (±) N-((1-hydroxy-1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4-(2-hydroxypropan-2-yl)furan-2-sulfonamide. Subsequent synthesis of individual enantiomers and coelution in HPLC-ESI-SRM-MS/MS using a chiral column revealed the metabolite was R-(+)- N-((1-hydroxy-1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4-(2-hydroxypropan-2-yl)furan-2-sulfonamide. To study the possible cytochrome P450 enzyme(s) responsible for the formation of major metabolite, MCC950 was incubated with a panel of cytochrome P450 enzymes. The result indicated that CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C18, CYP2C19, CYP2J2 and CYP3A4 are most likely responsible for the formation of the major metabolite. The biological activity of the major metabolite and the other synthesized regioisomers was also investigated by screening for for NLRP3 inflammasome inhibitory activity and cytotoxicity. The major metabolite had 170-fold less inhibitory activity (IC50-1238 nM) than MCC950 (IC50-7.5 nM). Interestingly, one regioisomer had shown nanomolar inhibitory activity (IC50-232 nM). However, no evidence of cytotoxicity was observed with any of these synthesized compounds when tested in human embryonic kidney 293 cells (HEK293) and human liver hepatocellular carcinoma G2 cells (HepG2). These key findings give an insight into the SAR of the hexahydroindacene moiety of MCC950 and reveal a metabolic soft spot which could be blocked by chemical modification. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=Cytochrome%20P450" title="Cytochrome P450">Cytochrome P450</a>, <a href="https://publications.waset.org/abstracts/search?q=inflammasome" title=" inflammasome"> inflammasome</a>, <a href="https://publications.waset.org/abstracts/search?q=MCC950" title=" MCC950"> MCC950</a>, <a href="https://publications.waset.org/abstracts/search?q=metabolite" title=" metabolite"> metabolite</a>, <a href="https://publications.waset.org/abstracts/search?q=microsome" title=" microsome"> microsome</a>, <a href="https://publications.waset.org/abstracts/search?q=NLRP3" title=" NLRP3 "> NLRP3 </a> </p> <a href="https://publications.waset.org/abstracts/60838/identification-synthesis-and-biological-evaluation-of-the-major-human-metabolite-of-nlrp3-inflammasome-inhibitor-mcc950" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/60838.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">252</span> </span> </div> </div> </div> </main> <footer> <div id="infolinks" class="pt-3 pb-2"> <div class="container"> <div style="background-color:#f5f5f5;" class="p-3"> <div class="row"> <div class="col-md-2"> <ul class="list-unstyled"> About <li><a href="https://waset.org/page/support">About Us</a></li> <li><a href="https://waset.org/page/support#legal-information">Legal</a></li> <li><a target="_blank" rel="nofollow" href="https://publications.waset.org/static/files/WASET-16th-foundational-anniversary.pdf">WASET celebrates its 16th foundational 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Search results for: microsome