一种磷脂酶A_2抑制剂体外筛选方法的建立  

A method for screening Phospolipase A_2 inhibitors in vitro

作　　者：刘彬[1] 齐云[1] 王敏[1] 蔡润兰[1] 宋杨[1] 

机构地区：[1]中国医学科学院中国协和医科大学药用植物研究所,北京100094

出　　处：《中国药理学通报》2006年第7期890-892,共3页Chinese Pharmacological Bulletin

基　　金：北京市自然科学基金资助课题(No7042039);国家中医药管理局资助课题(No04-05ZL04)

摘　　要：目的建立磷脂酶A2(PLA2)抑制剂体外筛选的方法。方法以大豆磷脂酰胆碱为底物,通过分光光度法测定PLA2水解底物产生游离脂肪酸的量,间接反映待测物对PLA2活性的影响,并考查酶浓度、底物浓度及反应时间与游离脂肪酸生成量的线性关系。结果在一定范围内,酶浓度、底物浓度及反应时间与游离脂肪酸生成量呈良好的线性关系,氯丙嗪对PLA2的IC50为501μmol.L-1,甘草甜素对PLA2的IC50为461μmol.L-1。结论建立的磷脂酶A2抑制剂体外筛选方法,具有灵敏度高、快捷、准确、可操作性强的特点。Aim To establish a photometric method in vitro for screening Phospholipase A2 （ PLA2 ） inhibitors. Methods With soy-bean phosphatidylcholine as a substrate, PLA2 activity was quantified indirectly by detecting the amount of long-chain free fatty acids liberated from phosphatidylcholine. Result Good linear relationship was observed between PLA2 concentration, substrate concentration or incubation time and the liberation of free fatty acids related to PLA2 activity. Chlorpromazine and Glycyrrhizin could inhibit PLA2 activity in a dose -dependent manner （IC50 of 501 μmol ·L^-1 and 461 μmol·L^-1 ）. Conclusion The method is sensitive, rapid, accurate and valid for screening the PLAz inhibitors in vitro.

关 键 词：磷脂酶A2 抑制剂 体外 分光光度法 

分 类 号：R345.61[医药卫生—基础医学] R965.1