Inhibitory effect of PNS on drug metabolism enzyme CYP3A in rat livers and its kinetic analysis.
- Author:
Zi-Ming YANG
1
;
Xiu-Fen YANG
Author Information
- Publication Type:Journal Article
- MeSH: Animals; Cytochrome P-450 CYP3A; chemistry; genetics; metabolism; Cytochrome P-450 CYP3A Inhibitors; Enzyme Inhibitors; chemistry; pharmacology; Kinetics; Liver; chemistry; drug effects; enzymology; Male; Panax notoginseng; chemistry; Rats; Rats, Sprague-Dawley; Rhizome; chemistry; Saponins; chemistry; pharmacology
- From: China Journal of Chinese Materia Medica 2012;37(22):3486-3489
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVETo study the inhibitory effect of total saponins of the root and rhizome of Panax notoginseng (PNS) on drug metabolism enzyme CYP3A in rat livers and its kinetic analysis.
METHODMicrosome enzyme was prepared by differential velocity centrifugation. Michaelis constant (Km) and maximum velocity (Vmax) of CYP3A, 50% inhibitory concentration of PNS on CYP3A, and the inhibition type and the inhibition constant of CYP3A (Ki, Kis) of PNS on CYP3A were calculated by Lineweaver-Burk and the low of semi-effect-probit.
RESULTTotal saponins of the root and rhizome of panax notoginseng inhibited CYP3A activity, with IC50 of 689.54 mg x L(-1). Compared with the substrate aminopyrine, CYP3A showed Km of 0.036 mmol x L(-1) and Vmax of 21.01 micromol min(-1) x g(-1). Total saponins of the root and rhizome of panax notoginseng showed a mixed inhibition on CYP3A, with the inhibition constants of 247.79 mg x L(-1) (Ki) and 321.79 mg x L(-1) (Kis).
CONCLUSIONTotal saponins of the root and rhizome of panax notoginseng have a significant effect on CYP3A activity in rat livers.
