title: [Effects of six kinds of Chinese herb extracts on the activities of rat liver microsomes in vitro].
abstract: Effects of six kinds of Chinese herb extracts, including Folium Crataegi extract, Herba Epimedii extract, Folium Acanthopanacis Senticosi extract, Trifolium pratense L. extract, Folium Ginkgo extract and Radix Puerariae extract, on the activities of CYP450 isozymes (CYP1A2, CYP2C, CYP2E1, CYP2D, CYP3A) in rat hepatic microsomals were studied by using a UPLC-MS/MS (MRM) and cocktail probe substrates method. The results showed that effects of six kinds of Chinese herb extracts on each CYP450 isozyme activity were inhibitory. The IC50 of Folium Crataegi extract for the inhibition of rat microsomal CYP2D activity was only for 4.04 microg x mL(-1), which showed the highest inhibition; Trifolium pratense L. extract had strong inhibitory action to CYP2D, the IC50 value was 5.73 microg x mL(-1); Folium Crataegi extract also had strong inhibitory action on CYP2E1, the IC50 value was 10.91 microg x mL(-1). Furthermore, the IC50 of Folium Ginkgo extract for the inhibition of rat microsomal CYP3A, 2D, 2E1 activities were 45.12, 35.45 and 22.41 microg x mL(-1), respectively, and the IC50 of Folium Acanthopanacis Senticosi extract on the inhibition of rat microsomal CYP2E1 activity was 32.89 microg x mL(-1). In addition, mechanism of inhibition experimental results showed that the inhibiting abilities of Folium Crataegi extract and Radix Puerariae extract on each CYP450 isozyme increased with the increasing of the preincubation time, therefore, the inhibitory effects were a mechanism-based inhibition.
authors.affiliation: College of Food Science and Engineering, Jilin Agricultural University, Changchun 130118, China.
authors.forename: Yun-Feng
authors.initials: YF
authors.lastname: Bi
authors.forename: Hong-Bin
authors.initials: HB
authors.lastname: Zhu
authors.forename: Jun-Peng
authors.initials: JP
authors.lastname: Xing
authors.forename: Zhi-Qiang
authors.initials: ZQ
authors.lastname: Liu
authors.forename: Feng-Rui
authors.initials: FR
authors.lastname: Song
mesh_terms: D000818:Animals; D002851:Chromatography, High Pressure Liquid; D027825:Crataegus / Q000737:chemistry; D019388:Cytochrome P-450 CYP1A2 / Q000378:metabolism; D019392:Cytochrome P-450 CYP2E1 / Q000378:metabolism; D051544:Cytochrome P-450 CYP3A / Q000378:metabolism; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism*; D004365:Drugs, Chinese Herbal / Q000302:isolation & purification / Q000494:pharmacology*; D028001:Eleutherococcus / Q000737:chemistry; D034181:Epimedium / Q000737:chemistry; D020441:Ginkgo biloba / Q000737:chemistry; D020128:Inhibitory Concentration 50; D008297:Male; D008862:Microsomes, Liver / Q000201:enzymology*; D010946:Plants, Medicinal / Q000737:chemistry*; D029908:Pueraria / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D053719:Tandem Mass Spectrometry; D029921:Trifolium / Q000737:chemistry
chemical_list: D004365:Drugs, Chinese Herbal; C400322:cytochrome P-450 CYP2C subfamily; D003577:Cytochrome P-450 Enzyme System; D019392:Cytochrome P-450 CYP2E1; D019388:Cytochrome P-450 CYP1A2; D051544:Cytochrome P-450 CYP3A