角蒿咖啡酸酯对小鼠耳肿胀的抑制作用  

Effect of Incarvillea caffeate on mouse ear edema

作　　者：黎丽[1,2] 李玉珍[2] 丁利平[1] 黄钟[1] Li Li Li Yuzhen Ding Liping and Huang Zhong(School of Medicine, Shenzhen University, Shenzhen 518060, Guangdong Province, P. R. China Department of Pharmacy, The Eighth Affiliated Hospital, Sun Yat-sen University, Shenzhen 518033, Guangdong Province, P. R. China)

机构地区：[1]深圳大学医学部,广东深圳518060 [2]中山大学第八附属医院药学部,广东深圳518033

出　　处：《深圳大学学报（理工版）》2017年第1期46-50,共5页Journal of Shenzhen University(Science and Engineering)

基　　金：中国博士后科学基金资助项目(2015M572370)~~

摘　　要：研究了角蒿咖啡酸酯((+)-2-(1-hydroxyl-4-oxocyclohexyl)ethyl caffeate,JH2)对花生四烯酸(arachidonic acid,AA)致小鼠耳肿胀的抑制作用,探讨其作用机制,采用花生四烯酸诱导的小鼠急性耳肿胀模型评价JH2的体内药效,通过酶联免疫吸附测定实验检测JH2对AA通路中5-脂氧合酶(5-lipoxygenase,5-LOX)活性的影响.实验结果显示,在AA诱导的小鼠耳肿胀模型中,JH2能显著抑制AA所致的小鼠耳肿胀程度和组织蛋白渗出量,并降低小鼠发炎耳组织中白三烯B4(leukotrienes B4,LTB4)的生成量.体外活性研究显示,JH2对5-LOX有较强的抑制活性,半抑制浓度IC50值为12.16μmol/L.说明JH2对AA诱导的小鼠耳肿胀急性炎症具有抑制作用,其作用机制可能与JH2抑制AA通路中5-LOX的活性从而降低炎症介质LTB4的产生有关.We investigated the effect of Incarvillea caffeate （ （ ＋ ） -2-（1-hydroxyl-4-oxocyclohexyl） ethyl caffeate, JH2） on arachidonic acid （AA） and its possible mechanism. We used AA-induced mouse acute ear edema model to determine the effect of JH2 on in vivo. We also studied the effect of JH2 on the enzyme activities of 5-1ipoxygenase （5-LOX） by ELISA. The results showed that topical treatment with JH2 markedly inhibits the extent of oedema and protein permeability. Importantly, leukotrienes B, （LTB4） production in ear mouse is also drastically suppressed by JH2 and reaches a maximum inhibition rate of 87.50%. Activity assay in vitro showed that JH2 inhibits 5-LOX activity with half maximal inhibitory concentration （ICs0） of 12. 16 μmol/L. JH2 presents anti-inflammatory effect on AA-induced mouse acute ear edema model through controlling the excessive production of LTB4 by inhibiting the activity of 5-LOX.

关 键 词：药理学 耳肿胀 角蒿咖啡酸酯 花生四烯酸 5-脂氧酶 白三烯B4 

分 类 号：R392[医药卫生—免疫学]