title: In vitro metabolism of glycyrrhetic acid by human cytochrome P450.
abstract: 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%.
authors.affiliation: Hubei Province Key Laboratory of Biotechnology of Chinese Traditional Medicine, Hubei University, Wuhan 430062, China.
authors.forename: Li
authors.initials: L
authors.lastname: Liu
authors.forename: Juan
authors.initials: J
authors.lastname: Xiao
authors.forename: Zhi-Hong
authors.initials: ZH
authors.lastname: Peng
authors.forename: Yong
authors.initials: Y
authors.lastname: Chen
mesh_terms: D001189:Aryl Hydrocarbon Hydroxylases / Q000037:antagonists & inhibitors / Q000378:metabolism; D065731:Cytochrome P-450 CYP2C19; D065729:Cytochrome P-450 CYP2C9; D051544:Cytochrome P-450 CYP3A / Q000378:metabolism*; D065692:Cytochrome P-450 CYP3A Inhibitors; D004791:Enzyme Inhibitors / Q000494:pharmacology; D006034:Glycyrrhetinic Acid / Q000302:isolation & purification / Q000493:pharmacokinetics* / Q000494:pharmacology; D006035:Glycyrrhiza / Q000737:chemistry; D006801:Humans; D007527:Isoenzymes / Q000378:metabolism; D008862:Microsomes, Liver / Q000201:enzymology / Q000378:metabolism; D018517:Plant Roots / Q000737:chemistry; D010946:Plants, Medicinal / Q000737:chemistry
chemical_list: D065692:Cytochrome P-450 CYP3A Inhibitors; D004791:Enzyme Inhibitors; D007527:Isoenzymes; C450260:CYP2C9 protein, human; D065729:Cytochrome P-450 CYP2C9; D001189:Aryl Hydrocarbon Hydroxylases; C045793:CYP2C19 protein, human; D065731:Cytochrome P-450 CYP2C19; D051544:Cytochrome P-450 CYP3A; C510163:CYP3A4 protein, human; D006034:Glycyrrhetinic Acid