抗老年性痴呆复方开心散有效提取物血清药物化学研究

Plasma Pharmacochemistry Study of Effective Extracivet from Kai-xinsan on Alzhemer's Disease

目的:分析开心散60%乙醇提取物(KXS-60%E)体外各成分的归属来源及大鼠灌服KXS-60%E后药物入血成分。方法:应用UPLC-TOF-MS技术建立KXS-60%E体外成分以及大鼠灌服药物后含药血清样品的分析方法,根据各单味药的色谱峰确定全方主要成分的来源归属;对比空白血清、含药血清的成分异同,分析药物的入血成分。结果:通过对比KXS-60%E与各单味药的正负总离子流图,归属了94个主要色谱峰的来源;大鼠口服KXS-60%E后,在血中分析指定了41个入血成分,其中13个为新产生的代谢产物,28个成分为KXS-60%E的原形成分。结论:血中移行成分及其代谢产物是KXS-60%E防治老年性痴呆(AD)的更直接药效物质基础,对其进行深入的研究将有助于阐明开心散防治AD的作用机制。

Objective：To analyse the origin of peaks in Kaixinsan （KXS） extracted by 60％ ethano （KXS-60％ E） Ⅰ and the constituents in rat plasma after oral administration-of KXS-60％ E.Method：A UPLC-TOF-MS method for analyzing the constituents in KXS-60％ E and in rat plasma after oral administration of KXS-60％ E,has been established.The origin of peaks in KXS-60％ E were pointed out compared with each single herb in the formula similarly,the origin of peaks in treated serum after oral KXS-60％ E were identified by contrasting the control rat serum.Result：Ninty-four compounds were detected in KXS-60％ E in vitro,by compare with control rat plasma,41 peaks were pointed out in treated plasma.Concluding 28 original form in KXS-60％ E and 13 metabolites.Conclusion：The constituents absorbed into blood and their metabolites of KXS-60％ E were the direct basis of action of the drug,further study on these constituents may clarify the mechanism of KXS prevention and treatment on Alzhemer＇s disease.