代谢指纹谱用于丹参活性成分的分析与筛选  

Screen and Analysis of Bioactive Compounds in Radix Salviae Miltiorrhizae by Metabolic Fingerprinting Analysis

作　　者：吴曦[1] 罗碧容[1] 袁文杰[2] 于凤娇[1] 孔亮[1,3] 李伟[1] 李微[1] 雷小元[3] 邹汉法[3] 

机构地区：[1]大连海洋大学,大连116023 [2]大连理工大学,大连116024 [3]中国科学院大连化学物理研究所,大连116023

出　　处：《世界科学技术-中医药现代化》2011年第1期170-179,共10页Modernization of Traditional Chinese Medicine and Materia Medica-World Science and Technology

基　　金：国家自然科学基金(21075012):线粒体能量代谢指纹谱用于中药活性成分筛选与分析的研究,负责人:孔亮;国家自然科学基金(31071612):贝类凝集素对水产品中常见致病菌的抑菌效应及作用机制的研究,负责人:李伟;辽宁省高等学校优秀人才支持计划(2009R13):基于生物指纹谱原理的天然海洋药物活性物质筛选技术平台的研究,负责人:孔亮;辽宁省教育厅实验室专项(2008S066):基于生物指纹谱原理的天然海洋药物活性物质筛选,负责人:孔亮

摘　　要：建立了以SD大鼠肝匀浆作为体外代谢方法,并结合HPLC-DAD-MS分析手段作为代谢指纹谱平台,在此基础上,对单味中药丹参进行体外代谢,采用HPLC-DAD-MS辅以MALDI-TOF-MS对代谢前后的指纹谱差异与相似性进行比较,结合抑菌、血凝体外药理实验测定丹参提取物及其代谢物、3种主要成分的活性。抑制大肠杆菌活性和血凝活性药理实验结果表明,丹参代谢物活性均高于其提取物。通过考察隐丹参酮、丹参酮Ⅰ、丹参酮Ⅱ_A的抑菌活性与血凝活性,并结合体外肝匀浆代谢实验,解释了其中的原因:丹参抑制大肠杆菌活性增高是因为隐丹参酮代谢转化为抑制率高的丹参酮Ⅱ_A引起的;丹参提取物血凝活性在代谢后升高的原因是由于隐丹参酮谢转化为血凝活性更高的丹参酮Ⅱ_A引起的。A new strategy for the screen and analysis of bioactive compounds in Radix Salviae Miltiorrhizae of traditional Chinese medicine has been developed using metabolic fingerprinting analysis. The metabolizing method was established based on the in vitro metabolism of the SD rat liver bomogenate. By means of metabolism methods in vitro, antimicrobial and agglutination activities were determined from the extracts. Metabolites and compounds of Radix Salviae Miltiorrhizae were processed by pharmacological assays in vitro. The changes of activities about the Radix Salvioe Miltiorrhizae extract were observed that the antimicrobial activity against E. coli and agglutination activity of blood cells were increased after metabolism. The results indicated that Tanshinone ⅡA, the metabolite of Cryptoanshinone from Radix Salviae Miltiorrhizae, showed higher activities than Cryptoanshinone.

关 键 词：代谢指纹谱 丹参 肝匀浆 总差异率 抑菌活性 血凝活性 

分 类 号：R284.2[医药卫生—中药学]