title: [Effect of oligosaccharide esters and polygalaxanthone Ill from Polygala tenuifolia willd towards cytochrome P450].
abstract: Five compounds (tenuifoliside C, tenuifoliside D, telephiose A, telephiose C and polygalaxanthone III) from polygala tenuifolia wild were incubated together with CYP probe substrate in human liver microsomes to investigate the inhibitory effect towards CYP450 enzyme. Phenacetin (CYP1A2), coumarin (CYP2A6), paclitaxel (CYP2C8), diclofenac (CYP2C9), S-mepheriytoin (CYP2C19), dextromethorphan (CYP2D6), chlorzoxazone (CYP2E1), midazolam (CYP3A) were selected as the isoforfn specific substrate. And the formation of paracetamol, 7-hydroxycoumarin, 6alpha-hydroxy paclitaxel, 4'-hydroxydiclofenac, dextrorphan, 6-hydroxychlorzoxazone, 1'-hydroxymidazolam, 4'-hydroxymephenytoin were detected respectively to measure the effect towards CYP450 by high-pressure liquid chromatography (HPLC). The result shows that five compounds from polygala tenuifolia willd significantly inhibit chlorzoxazone 6-hydroxylation catalyzed by CYP2E1, while showed no effect towards CYP1A2, CYP2A6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP3A. And IC50 value was 38.73, 54.14, 61.77, 62.22, 50.56 micromol x L(-1), respectively.
authors: Zhao-liang
authors: ZL
authors: Li
authors: Xian-zhe
authors: XZ
authors: Dong
authors: Dong-xiao
authors: DX
authors: Wang
authors: Rui-hua
authors: RH
authors: Dong
authors: Ting-ting
authors: TT
authors: Guo
authors: Yan
authors: Y
authors: Sun
authors: Ping
authors: P
authors: Liu
mesh_terms: D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism*; D004952:Esters / Q000494:pharmacology*; D006027:Glycosides / Q000494:pharmacology*; D006801:Humans; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology; D009844:Oligosaccharides / Q000494:pharmacology*; D031801:Polygala / Q000737:chemistry*; D044004:Xanthones / Q000494:pharmacology*
chemical_list: D004952:Esters; D006027:Glycosides; D009844:Oligosaccharides; D044004:Xanthones; C092101:polygalaxanthone III; D003577:Cytochrome P-450 Enzyme System