In vitro proguanil activation to cycloguanil by human liver microsomes is mediated by CYP3A isoforms as well as by S-mephenytoin hydroxylase.
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چکیده
منابع مشابه
Anticancer drugs as inhibitors of two polymorphic cytochrome P450 enzymes, debrisoquin and mephenytoin hydroxylase, in human liver microsomes.
To identify potential substrates for the debrisoquin and mephenytoin hydroxylation polymorphisms, we performed in vitro inhibition studies with human liver microsomes and the respective prototype substrates in the absence and presence of several anticancer drugs. (+)-Bufuralol 1'-hydroxylation (as the prototype reaction for the debrisoquin polymorphism) was tested at 5 microM substrate concentr...
متن کاملAssay of mephenytoin metabolism in human liver microsomes by high-performance liquid chromatography.
The metabolism of mephenytoin to its two major metabolites, 4-OH-mephenytoin (4-OH-M) and 5-phenyl-5-ethylhydantoin (nirvanol) was studied in human liver microsomes by a reversed phase HPLC assay. Because of preferential hydroxylation of S-mephenytoin in vivo, microsomes (5-300 micrograms protein) were incubated separately with S- and R-mephenytoin. After addition of phenobarbital as internal s...
متن کاملIn vitro activation of rat liver phenylalanine hydroxylase by phosphorylation.
Essentially pure phenylalanine hydroxylase from rat liver can be activated between 2.5- and 3.0-fold by treatment with Mg2+, ATP, protein kinase, and cyclic AMP. The activation is seen when the hydroxylase is assayed in the presence of tetrahydrobiopterin, but not in the presence of 2-amino-4-hydroxy-6,7-dimethyltetrahydropteridine. In the presence of [gamma-32P]ATP, activation is accompanied b...
متن کاملIn vitro metabolism of isoliquiritigenin by human liver microsomes.
Isoliquiritigenin (2',4',4-trihydroxychalcone), a chalcone found in licorice root and other plants, has shown potent antitumor, antioxidant, and phytoestrogenic activity in vitro. In preparation for in vivo studies, the metabolism of isoliquiritigenin by human liver microsomes was investigated, and seven phase 1 metabolites were identified. In addition to aromatic hydroxylation that occurred on...
متن کاملrisk taking in english to persian translation process by novice iranian translators
این پژوهش به بررسی ریسک پذیری مترجمان تازه کار در طی فرآیند ترجمه از زبان انگلیسی به فارسی می پردازد. پژوهش درباره مترجمان به عنوان اولین خواننده متن مبدا از اهمیت به سزایی برخوردار است. مترجمان تازه کار (و حرفه ای) در طی فرآیند ترجمه با مشکلات متعددی روبرو می شوند که باعث عدم اطمینان آنها از متن ترجمه شده می شود. با توجه به اینکه عدم اطمینان به انجام ریسک منتهی می شود، هدف این پژوهش بررسی کیفی...
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ژورنال
عنوان ژورنال: British Journal of Clinical Pharmacology
سال: 1994
ISSN: 0306-5251
DOI: 10.1111/j.1365-2125.1994.tb05707.x