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- W2357582904 abstract "Objective: To investigate the metabolism based herb-drug interaction between AVT and lipid-lowering Herb Medicine(Fang-2) and its six individual herbs(Rhizoma Et Radix Polygoni Cuspidati, Rhizoma Alismatis, Rhizoma Atractylodis, Radix Et Rhizoma Glycyrrhizae, Cortex Magnoliae Officinalis, and Spica Prunellae) by using in vitro technologies. Method:(1) The test articles of herbs were prepared by a standard procedure using liquid extraction.(2) CYP3A4 inhibition study: Human and rat liver microsomes were incubated with extract of Fang-2 or its individual herb at 37℃ for 15 minutes, and then with testosterone, probe substrate of CYP3A4 in the presence of β-NADPH. Enzyme activity of CYP3A4, 6β-hydroxylation of testosterone was quantified by using LC-MS/MS.(3) Herb-Drug interaction study: Liver microsomes were preincubated with extract of Fang-2 or its individual herb at 37℃ for 15 minutes, and then with AVT in the presence of β-NADPH. Parent depletion of AVT was quantified by using developed LC-MS/MS methods. Results:(1) CYP3A4 inhibition: Fang-2 showed inhibitive potential on CYP3A4 activity with IC50 of 9.884 mg/mL.(2) AVT was extensively depleted by the 1st pass metabolism with intrinsic clearance rate(Clint) of 41.10 ml/mg/min and T1/2 of 60.43 min in liver microsomal incubation. The parent depletion of AVT was affected by preincubation with Fang-2. The inhibition of CYP3A4 by Fang-2 and its herbs was correlated with their preventing AVT from 1st pass metabolism by Fang-2 and its element positively. Conclusions: The article first studied the metabolism based herb-drug interaction between AVT and lipid-lowering herbs by using in vitro technologies. Furth investigation for metabolism based Herb-Drug interaction between Fang-2 and AVT will have significant clinical benefits in cardiovascular clinical pharmacology." @default.
- W2357582904 created "2016-06-24" @default.
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- W2357582904 date "2014-01-01" @default.
- W2357582904 modified "2023-09-23" @default.
- W2357582904 title "Metabolism based Herb-Drug Interaction-Lipid-lowering Herbs and Atorvastatin in vitro" @default.
- W2357582904 hasPublicationYear "2014" @default.
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