Metabolism Of The Active Ingredients Of Astragalus And Oridonin By Liver Microsome In Vitro

Cytochrome P450 is widely present in animals, and plays a very important role in the drug metabolism. Taking Astragalosideâ…£, flavonoids and Oridonin as the research object, this research mainly focuses on the inhibitory effects of these components on catalytic activity of cytochrome P450 enzyme in rat liver microsomes and comparative metabolism of Oridonin in liver microsomes from mouse, rat, dog, minipig, monkey, and human. The main contents include the following aspects:1. Inhibitory effects of Astragalosideâ…£on cytochrome P450 enzyme of rat liver microsomes. Tolbutamide, chlorzoxazone, coumarin, nifedipine, and phenacetin were prepared as the probe substrates of rat CYP2C9, CYP2E1, CYP2A6, CYP3A4, and CYP1A2. Probe substrates of cytochrome P450 enzymes were incubated in rat liver microsomes with Astragalosideâ…£. Study the inhibitory effects of Astragaloside IV on cytochrome P450 enzyme.2. Inhibitory effects of flavonoids on cytochrome P450 enzyme of rat liver microsomes. Tolbutamide, chlorzoxazone, testosterone, and phenacetin were prepared as probe substrates of rat CYP2C9, CYP2E1, CYP3A4, and CYP1A2. Probe substrates of cytochrome P450 enzymes were incubated in rat liver microsomes with flavonoids. Study the inhibitory effects of flavonoids on cytochrome P450 enzyme.3. Comparative metabolism of Oridonin in liver microsomes from mouse, rat, dog, minipig, monkey, and human. Firstly, determine the in vitro incubation system.Then, compare the metabolism of Oridonin in liver microsomes from mouse, rat, dog, minipig, monkey, and human.