Activation of P-glycoprotein and CYP 3A by Coptidis Rhizoma in vivo: Using cyclosporine as a probe substrate in rats.
作者： Chung-Ping Yu , Ching-Ya Huang , Shiuan-Pey Lin , Yu-Chi Hou
DOI: 10.1016/J.JFDA.2017.11.005
关键词:
摘要: Coptidis Rhizoma (CR), the rhizome of Coptis chinensis FRANCH, is a popular Chinese herb. CR contains plenty isoquinoline alkaloids such as berberine, coptisine and palmatine. Cyclosporine (CSP), an important immunosuppressant with narrow therapeutic window, employed probe substrate P-glycoprotein (P-gp) CYP3A4 in order to investigate in vivo modulation effect on P-gp CYP3A4. Three groups rats were orally administered CSP without single dose or repeated dosing parallel design. Blood samples collected at specific time points blood concentration was determined by monoclonal fluorescence polarization immunoassay. The results showed that (1.0 g/kg) 7th significantly decreased Cmax 56.9% 70.4%, reduced AUC0-540 56.4% 68.7%, respectively. Cell study indicated decoction, coptisine, palmatine all activated efflux transport P-gp. Ex-vivo serum metabolites CYP 3A4. In conclusion, through using substrate, we have verified oral intake functions CYP3A based in vitro studies.
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