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| 同分异构体齐墩果酸和熊果酸对CYP450酶抑制作用的差异 | |
| 引用本文： | 王亚平,董瑞华,刘泽源,胡园,刘皈阳.同分异构体齐墩果酸和熊果酸对CYP450酶抑制作用的差异[J].中国药物应用与监测,2012,9(4):201-203,210. |
| 作者姓名： | 王亚平 董瑞华 刘泽源 胡园 刘皈阳 |
| 作者单位： | 1. 解放军总医院第一附属医院药剂药理科,北京100037;河北北方学院,河北张家口,075000;军事医学科学院附属医院临床药理室,北京100071 2. 军事医学科学院附属医院临床药理室,北京,100071 3. 解放军总医院临床药理室,北京,100853 4. 解放军总医院第一附属医院药剂药理科,北京,100037 |
| 摘 要： | 目的:比较同分异构体齐墩果酸和熊果酸对人肝微粒体CYP450酶的抑制作用。方法:以人肝微粒体孵育体系为模型,加入齐墩果酸或熊果酸与CYP450探针底物共同孵育;以不同浓度的齐墩果酸对不同浓度的CYP3A4探针底物咪达唑仑的抑制,计算抑制率(Ki)。结果:熊果酸对CYP450酶没有明显的抑制作用;齐墩果酸可轻微抑制CYP1A2的活性,明显抑制CYP3A4酶的活性,Ki为39.2μmol.L-1。结论:齐墩果酸对CYP450酶的抑制作用强于熊果酸。 |
| 关 键 词： | 齐墩果酸 熊果酸 同分异构体 细胞色素P450 |
Inhibitory effect of oleanolic acid and ursolic acid isomers on cytochrome P450 |
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| Authors: | WANG Ya-ping DONG Rui-hua LIU Ze-yuan HU Yuan LIU Gui-yang |
| Institution: | 1. Department of Pharmacy, the Affiliated Hospital of Chinese PLA General Hospital, Beijing 100037, China; 2. Hebei North University, Zhangjiakou 075000, China; 3. Department of Clinical Pharmacology, Affliated Hospital of Chinese Academy of Military Medical Sciences, Beijing 100071, China; 4. Department of Clinical Pharmacology and Pharmacy, PLA General Hospital, Beijing 100853, China) |
| Abstract: | Objective： To compare the inhibitory effect of oleanolic acid and ursolic acid isomers on cytochrome P450. Methods： Oleanolic acid or ursolic acid was incubated together with CYP probe substrate in human liver microsomes, the inhibition ratio （K0 was calculated by comparing the inhibition for different concentrations of oleanolic acid with the different concentrations of midazolam （substrate of CYP3A4）. Results： Ursolic acid had no significant inhibitory effect on CYP450, while oleanolic acid had little inhibitory effect on CYP1A2, and could significantly inhibit CYP3A4 activity （Ki = 39.2μmol·L-1）. Conclusion： The inhibitory effect of oleanolic acid on CYP450 was stronger than that ofursolic acid. |
| Keywords: | Oleanolic acid Ursolic acid Isomer Cytochrome P450 |
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