桂枝汤有效成分苯丙烯类化合物干预IL-1β刺激小鼠脑微血管内皮细胞释放PGE_2的构效关系  

Structure-activity relationship of phenylallyl compounds inhibiting PGE_2 release in mouse cerebral microvascular endothelial cells induced by IL-1β

作　　者：马悦颖[1] 尚明英[2] 李沧海[3] 霍海如[1] 蔡少青[2] 姜廷良[1] 

机构地区：[1]中国中医科学院中药研究所唐氏中药研究中心,北京100700 [2]北京大学药学院,北京100083 [3]中国中医科学院医学实验中心,北京100700

出　　处：《药学学报》2007年第7期798-802,共5页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金重大项目(90209006)

摘　　要：To observe the effects of phenylallyl compounds on prostaglandin E2（PGE2）release in mouse cerebral microvascular endothelial cells （bEnd.3） stimulated by IL-1β, and to analyze their structure-activity relationship. Different concentrations of phenylallyl compounds were added separately, and the content of PGE2 induced by IL-1β in the culture media was measured by ELISA assay. The 50% inhibitory concentration （IC 50 ） of PGE2 was calculated. Studies showed that phenylallyl compounds could affect the PGE2 release differently in bEnd.3 cells induced by IL-1β. Close relationships were shown between the inhibitory activities and the location and number of the substituent groups. In conclusion, phenylallyl compounds exhibited inhibitory activities at different extent on PGE2 release in bEnd.3 cells stimulated by IL-1β and presented certain structure-activity relationship.To observe the effects of phenylallyl compounds on prostaglandin E2 （PGE2 ）release in mouse cerebral microvascular endothelial cells （bEnd. 3） stimulated by IL-1β, and to analyze their structure-activity relationship. Different concentrations of phenylallyl compounds were added separately, and the content of PGE2 induced by IL-1β in the culture media was measured by ELISA assay. The 50% inhibitory concentration （IC50） of PGE2 was calculated. Studies showed that phenylallyl compounds could affect the PGE： release differently in bEnd. 3 cells induced by IL-1β. Close relationships were shown between the inhibitory activities and the location and number of the substituent groups. In conclusion, phenylallyl compounds exhibited inhibitory activities at different extent on PGE2 release in bEnd. 3 cells stimulated by IL-1β and presented certain structure-activity relationship.

关 键 词：苯丙烯类化合物 前列腺素E2 构效关系 脑微血管内皮细胞 白介素1 桂枝汤 

分 类 号：R289.12[医药卫生—方剂学]