荧光光谱法研究青蒿素及双氢青蒿素与肝微粒体的相互作用  

Spectroscopic study on the interactions between artemisinin or dihydroartemisinin and rat or human liver microsomes

作　　者：孙坤[1] 张爱平[1] 王锐利[1] 李赟[1] 张淑秋[1] 

机构地区：[1]山西医科大学药学院临床药学教研室,太原030001

出　　处：《中国药物与临床》2011年第6期617-620,共4页Chinese Remedies & Clinics

基　　金：国家自然科学基金(30572367;30973589);山西省回国留学人员科研项目(2009-47);山西医科大学青年基金(02200704)

摘　　要：目的研究抗疟药青蒿素(ART)与双氢青蒿素(DHA)和大鼠肝微粒体(RLM)以及人肝微粒体(HLM)之间的相互作用。方法在模拟人体生理条件下,采用荧光光谱法,得出青蒿素、DHA与RLM和HLM的结合参数。结果青蒿素和DHA对RLM和HLM的猝灭机制不同,它们对RLM的猝灭机制均为静态猝灭,而对HLM的猝灭作用为混合猝灭;其相互间作用力均为氢键和范德华力,其结合反应均为自发的热力学反应。结论青蒿素和DHA对大鼠和人肝微粒体均有结合,且结合力存在种属差异,同时青蒿素和DHA与同种肝微粒体的结合能力也存在差异。Objective To investigate the interaction between antimalarial drug artemisinin （ART） or dihy droartemisinin （DHA） and rat liver microsomes （RLM） or human liver microsomes （HLM）.Methods The Binding parameters of ART or DHA with RLM or HLM were studied under simulated physiological conditions by fluorescience spectra.Results For both reactions of ART and DHA to RLM,the quenching mechanisms were static quenchings,but to HLM,they were mixed static and dynamic quenchings.All of the reactions were spontaneous thermodynamics reactions,and the major driving forces were hydrogen bond and van der Waals force.Conclusion There were some species differences in binding capabilities between RLM and HLM to ART or DHA.Meanwhile,there were some bingding capabilities differences between ART and DHA to same kind of microsomes.

关 键 词：光谱法 荧光 青蒿素 微粒体 肝 

分 类 号：R285.5[医药卫生—中药学]