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.

中文翻译：

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远志中低聚糖酯类和聚galaxanthoneⅡ对细胞色素P450的影响

将野生远志的五种化合物（tenuifoliside C，tenuifoliside D，telophose A，telefose C和polygalaxanthone III）与CYP探针底物一起在人肝微粒体中孵育，以研究其对CYP450酶的抑制作用。分别选择咪达唑仑（Pyacetin）（CYP1A2），香豆素（CYP2A6），紫杉醇（CYP2C8），双氯芬酸（CYP2C9），S-外周血素（CYP2C19），右美沙芬（CYP2D6），氯唑沙宗（CYP2E1），异氰菊酯（P）作为底物。高压液相色谱法分别检测扑热息痛，7-羟基香豆素，6α-羟基紫杉醇，4'-羟基双氯芬酸，右美芬，6-羟基氯唑沙宗，1'-羟基咪达唑仑，4'-羟基苯甲酰吗啉的形成，以测定其对CYP450的作用。 （HPLC）。结果表明，远志中的5种化合物将显着抑制CYP2E1催化的氯唑沙宗6-羟基化，而对CYP1A2，CYP2A6，CYP2C8，CYP2C9，CYP2C19，CYP2D6，CYP3A无影响。IC50值分别为38.73、54.14、61.77、62.22、50.56 micromol x L（-1）。