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五味子对CYP450活性的影响及其机制探讨
引用本文:翟健秀,刘志惠,韩娜,殷军.五味子对CYP450活性的影响及其机制探讨[J].世界科学技术-中医药现代化,2015,17(1):52-55.
作者姓名:翟健秀  刘志惠  韩娜  殷军
作者单位:沈阳药科大学中药学院/辽宁省东北道地药材资源研发重点实验室 沈阳 110016,沈阳药科大学中药学院/辽宁省东北道地药材资源研发重点实验室 沈阳 110017,沈阳药科大学中药学院/辽宁省东北道地药材资源研发重点实验室 沈阳 110018,沈阳药科大学中药学院/辽宁省东北道地药材资源研发重点实验室 沈阳 110019
基金项目:辽宁省科技厅重点实验室项目(辽科发[2011]20号):辽宁省东北道地药材资源研发重点实验室,负责人:殷军。
摘    要:五味子为木兰科五味子属植物五味子Schisandra chinensis(Turcz.) Baill.的干燥成熟果实,在临床上主要用于与其他药物的联合治疗,研究其药物-药物相互作用对于今后的临床应用意义重大。本文对相关文献进行归纳,分析了五味子生药及其中主要活性成分木脂素对CYP450酶活性的作用,并对其作用途径进行了初步推测。结果表明,五味子中主要木脂素类成分甲素、乙素、醇乙于3个水平影响CYP450的活性分别为诱导CYP450基因表达、诱导CYP450 mRNA翻译及直接作用于酶蛋白并抑制蛋白活性。这3个水平的作用于宏观表现为五味子对CYP450活性的双重作用。6、9位亲脂取代基或者大基团取代基是抑制CYP450活性的结构基础。

关 键 词:五味子  CYP450  双重作用  机制
收稿时间:2014/8/13 0:00:00
修稿时间:2015/1/19 0:00:00

Study on Effect and Mechanism of Fructus Schisandrae on CYP450 Activity
Zhai Jianxiu,Liu Zhihui,Han Na and Yin Jun.Study on Effect and Mechanism of Fructus Schisandrae on CYP450 Activity[J].World Science and Technology-Modernization of Traditional Chinese Medicine,2015,17(1):52-55.
Authors:Zhai Jianxiu  Liu Zhihui  Han Na and Yin Jun
Institution:School of Traditional Chinese Materia, Shenyang Pharmaceutical University /Liaoning Key Laboratory of Northeast Genuine Medicinal Materials Resource, Shenyang 110016, China,School of Traditional Chinese Materia, Shenyang Pharmaceutical University /Liaoning Key Laboratory of Northeast Genuine Medicinal Materials Resource, Shenyang 110017, China,School of Traditional Chinese Materia, Shenyang Pharmaceutical University /Liaoning Key Laboratory of Northeast Genuine Medicinal Materials Resource, Shenyang 110018, China and School of Traditional Chinese Materia, Shenyang Pharmaceutical University /Liaoning Key Laboratory of Northeast Genuine Medicinal Materials Resource, Shenyang 110019, China
Abstract:Fructus Schisandrae is the dried mature fruits of Schisandra chinensis (Turcz.) Baill., which is mainly combined with other medicine in clinical use. It is of great importance to investigate the possibility of drug-drug interaction between Fructus Schisandrae and other medicine. In order to study the effects of schisandra lignans on CYP450 activity, related literatures were reviewed and summarized. Initial speculation was made its effect pathways. The analysis results showed that the schisandra lignans (deoxyschizandrin, r-schizandrin and schisandrol) influenced CYP450 activity on three levels, which were induction of CYP450 expression, induction of CYP450 mRNA translation, and inhibition of CYP450 protein activity. Influence on these three levels showed the dual effect of Fructus Schisandrae on CYP450 activity. The inhibition was based on lipophilic substituents or large steric hindrance group on carbon 6 or 9.
Keywords:Fructus Schisandrae  CYP450  dual effect  mechanism
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