Abstract
Five compounds( tenuifoliside C,tenuifoliside D,telephiose A,telephiose C and polygalaxanthone Ⅲ) from polygala tenuifolia willd 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-mephenytoin( CYP2C19),dextromethorphan( CYP2D6),chlorzoxazone( CYP2E1),midazolam( CYP3A) were selected as the isoform specific substrate. And the formation of paracetamol,7-hydroxycoumarin,6α-hydroxy paclitaxel,4'-hydroxydiclofenac,dextrorphan,6-hydro xychlorzoxazone,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,CYP3 A. And IC50 value was 38. 73,54. 14,61. 77,62. 22,50. 56 μmol·L-1,respectively.
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