[Effect of comparability of Coptis chinensis and Scutellaria baicalensis on five sub-enzymatic activities of liver microsomes in rats].
To study the mechanism of metabolic interaction between Coptis chinensis and Scutellaria baicalensis. Rats were given C. chinensis and S. baicalensis for 7 days to produce hepatic microsomal enzyme. Cocktail probe substrate and liver microsome in vitro temperature incubation method were adopted. Meanwhile, the metabolic elimination percentages of the five probe substrates were detected with HPLC, in order to evaluate the effect of each administration group on the enzymatic activity of rat liver microsome CYP450. Compared with the blank group, C. chinensis obviously inhibited CYP2D6 and CYP1A2, and S. baicalensis remarkably inhibited CYP1A2, CYP2E1 and CYP2C9. The compatibility of C. chinensis and S. baicalensis with the ratio of 1:1 not only inhibited CYP1A2, but also remarkably activated CYP2D6 and CYP3A4. However, their activation effect disappeared under the ratio of 2: 1, and turned into the inhibitory effect on CYP1A2 and CYP2C9. The results showed that C. chinensis and S. baicalensis had an inhibitory effect on CYP450, but their compatibility with certain ratio resulted in double effects of activation and inhibition, which was related to their compatibility ratio. It is speculated that the inhibitory and inducing effects of C. chinensis and S. baicalensis on metabolic enzymes are among causes for their attenuation and synergistic effects.
School of Chinese Materia Medica, Beiing University of Chinese Medicine, Beijing 100102, China.
Ling-Yu
LY
Wei
Yu-Jie
YJ
Zhang
Bao-Hong
BH
Wei
Jing
J
Ye
Xiao-Yan
XY
Yang
Gui-Xia
GX
Sun
D000818:Animals; D002851:Chromatography, High Pressure Liquid; D039323:Coptis / Q000737:chemistry*; D019388:Cytochrome P-450 CYP1A2 / Q000378:metabolism; D019389:Cytochrome P-450 CYP2D6 / Q000378:metabolism; D004357:Drug Synergism; D004365:Drugs, Chinese Herbal / Q000494:pharmacology; D004789:Enzyme Activation / Q000187:drug effects; D008862:Microsomes, Liver / Q000201:enzymology*; D051381:Rats; D031364:Scutellaria baicalensis / Q000737:chemistry*
D004365:Drugs, Chinese Herbal; D019388:Cytochrome P-450 CYP1A2; D019389:Cytochrome P-450 CYP2D6