人细胞色素P450对甘草次酸的体外代谢
In vitro metabolism of glycyrrhetic acid by human cytochrome P450.
作者信息
Liu Li, Xiao Juan, Peng Zhi-Hong, Chen Yong
机构信息
Hubei Province Key Laboratory of Biotechnology of Chinese Traditional Medicine, Hubei University, Wuhan 430062, China.
出版信息
Yao Xue Xue Bao. 2011 Jan;46(1):81-7.
Licorice root has been frequently used as antitode in traditional Chinese medicine. As the main active component of Licorice root, glycyrrhetic acid (GA) is mainly metabolized in liver. This study was designed to investigate the in vitro metabolism of GA by human liver microsomes (HLM) and human recombinant cytochrome P450 (CYP) isoforms. The results indicated that GA was metabolized mainly by CYP3A4. The K(m), V(max) and CL(int) of GA in HLM were 18.6 micromol x L(-1), 4.4 nmol x mg(-1) (protein) x min(-1) and 0.237 mL x mg(-1) (protein) x min(-1), respectively. At concentration up to 50 micromol x L(-1), GA inhibited CYP2C19, CYP2C9 and CYP3A4 enzyme activities with the inhibitory potencies up to 50%.
甘草根在传统中药中常被用作解毒剂。作为甘草根的主要活性成分，甘草次酸（GA）主要在肝脏中代谢。本研究旨在研究人肝微粒体（HLM）和人重组细胞色素P450（CYP）同工酶对GA的体外代谢。结果表明，GA主要由CYP3A4代谢。GA在HLM中的K(m)、V(max)和CL(int)分别为18.6 μmol·L(-1)、4.4 nmol·mg(-1)（蛋白质）·min(-1)和0.237 mL·mg(-1)（蛋白质）·min(-1)。在浓度高达50 μmol·L(-1)时，GA抑制CYP2C19、CYP2C9和CYP3A4酶活性，抑制效力高达50%。
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