Results 121 to 130 of about 23,100 (164)

In Vitro Metabolism of Isoliquiritigenin by Human Liver Microsomes

Drug Metabolism and Disposition, 2008
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
Jian, Guo, Dongting, Liu, Dejan, Nikolic, Dongwei, Zhu, John M, Pezzuto, Richard B, van Breemen   +5 more
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Inactivation of CYP3A4 by Benzbromarone in Human Liver Microsomes

Drug Metabolism Letters, 2016
Benzbromarone is a uricosuric drug in current clinical use that can cause serious hepatotoxicity. Chemically reactive and/or cytotoxic metabolites of benzbromarone have been identified; however there is a lack of available information on their role in benzbromarone hepatotoxicity.
Yasuhiro, Masubuchi, Shinji, Kondo
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Phenobarbital N-glucosylation by human liver microsomes

European Journal of Drug Metabolism and Pharmacokinetics, 2004
Glucosylation of xenobiotics in mammals has been observed for a limited number of drugs. Generally, these glucoside conjugates are detected as urinary excretion products with limited information on their formation. An in vitro assay is described for measuring the formation of the phenobarbital N-glucoside diasteriomers ((5R)-PBG, (5S)-PBG) using human ...
Sheela G, Paibir, William H, Soine, Diana F, Thomas, Robert A, Fisher   +3 more
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Biotransformation of 1,8-Cineole by Human Liver Microsomes

Natural Product Letters, 2001
The biotransformation of 1,8-cineole has been investigated by using human liver microsomes. A single oxidized metabolite, 2-exo-hydroxy-1,8-cineole, was isolated. Its formation was investigated under various conditions by changing incubation time, P450 level in liver microsomes, and substrate concentration.
M, Miyazawa, M, Shindo
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Bioactivation of Flutamide Metabolites by Human Liver Microsomes

Drug Metabolism and Disposition, 2008
Flutamide, a widely used nonsteroidal antiandrogen drug for the treatment of prostate cancer, has been associated with rare incidences of hepatotoxicity in patients. It is believed that bioactivation of flutamide and subsequent covalent binding to cellular proteins is responsible for its toxicity. A novel N-S glutathione adduct has been identified in a
Ping, Kang, Deepak, Dalvie, Evan, Smith, Sue, Zhou, Alan, Deese, James A, Nieman   +5 more
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Metabolism of benz[a]anthracene by human liver microsomes

Cancer Letters, 1994
The metabolism of benz[a]anthracene (BA) by human hepatic microsomes was investigated. Only dihydrodiols were observed when BA was the substrate. No tetrahydrotetrols were detected, indicating lack of diol epoxide formation. The BA-dihydrodiols identified by GCMS analysis and comparison to authentic standards were BA-8,9-dihydrodiol (42.4% of total ...
Y, Sahali, L R, Kidd, P L, Skipper, S R, Tannenbaum   +3 more
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Raloxifene Glucuronidation in Human Intestine, Kidney, and Liver Microsomes and in Human Liver Microsomes Genotyped for the UGT1A1*28 Polymorphism

Drug Metabolism and Disposition, 2011
Raloxifene, a selective estrogen receptor modulator, exhibits quite large interindividual variability in pharmacokinetics and pharmacodynamics. In women, raloxifene is metabolized extensively by different isoforms of UDP-glucuronosyltransferase (UGT) to its glucuronides.
Tina, Trdan Lusin, Jurij, Trontelj, Ales, Mrhar   +2 more
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Characterization of fimasartan metabolites in human liver microsomes and human plasma

Xenobiotica, 2015
1. The metabolites of fimasartan (FMS), a new angiotensin II receptor antagonist, were characterized in human liver microsomes (HLM) and human subjects. 2. We developed a method for a simultaneous quantitative and qualitative analysis using predictive multiple reaction monitoring information-dependent acquisition-enhanced product ion scanning.
Ji-Yoon, Lee, Young Jae, Choi, Soo Jin, Oh, Yong Ha, Chi, Soo Heui, Paik, Ki Ho, Lee, Jae-Kyung, Jung, Chang Seon, Ryu, Kwon-Bok, Kim, Dong-Hyun, Kim, Young-Ran, Yoon, Sang Kyum, Kim   +11 more
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Anthracyclines and their metabolism in human liver microsomes and the participation of the new microsomal carbonyl reductase

Chemico-Biological Interactions, 2011
Anthracyclines (ANTs) are widely used in the treatment of various forms of cancer. Although their usage contributes to an improvement in life expectancy, it is limited by severe adverse effects-acute and chronic cardiotoxicity. Several enzymes from both AKR and SDR superfamilies have been reported as participants in the reduction of ANTs.
Adam, Skarka, Lucie, Skarydová, Hana, Stambergová, Vladimír, Wsól   +3 more
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Metabolism of coumarin by rat, gerbil and human liver microsomes

Xenobiotica, 1992
1. o-Hydroxyphenylacetaldehyde was the major metabolite of coumarin (1 mM) in rat, gerbil and human liver microsomes. 2. Treatment of rats with phenobarbitone (PB) or beta-naphthoflavone increased the o-hydroxyphenylacetaldehyde formed. 3-Hydroxycoumarin was the other main metabolite produced by rat liver microsomes. 3.
J H, Fentem, J R, Fry
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