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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。
The establishment of a rat liver homogenate as a metabolic method in vitro, combined with HPLC-DAD-MS analysis as a metabolic fingerprint platform, on this basis, the single Chinese herbal medicine Salvia in vitro metabolism, using HPLC-DAD-MS The differences and similarities of fingerprints before and after metabolites were compared by MALDI-TOF-MS, and the activities of three main components of Salvia miltiorrhiza extracts and their metabolites were determined by antibacterial and hemagglutination pharmacological experiments in vitro. Inhibition of E. coli activity and hemagglutination activity Pharmacological experimental results show that Salvia metabolites were higher than its activity. The antibacterial activity and hemagglutination activity of cryptotanshinone, tanshinone Ⅰ and tanshinone Ⅱ_A were studied, and the in vitro hepatic homogenate metabolism experiments were explained to explain the reason: the increased activity of Danshen inhibited Escherichia coli is due to the high inhibition rate of cryptotanshinone metabolism into Of tanshinone Ⅱ_A caused; blood coagulation activity of Salvia extract increased after the metabolism is due to the conversion of cryptotanshinone into hemostatic activity higher tanshinone Ⅱ_A caused.