青蒿素和二氢青蒿素的抗炎作用及机制  

Anti-inflammatory effect and mechanism of artemisinin and dihydroartemisinin

作　　者：喻婉莹[1] 阚伟娟[1] 于鹏霞[1] 李敏敏[1] 宋吉帅 赵烽[1] 

机构地区：[1]烟台大学药学院,山东烟台264005 [2]烟台赛尔斯生物技术有限公司,山东烟台264006

出　　处：《中国中药杂志》2012年第17期2618-2621,共4页China Journal of Chinese Materia Medica

基　　金：国家教育部回国人员科研启动基金

摘　　要：目的:研究并比较青蒿素和二氢青蒿素的抗炎作用及其分子机制。方法:用LPS刺激小鼠单核巨噬细胞RAW 264.7释放TNF-α,IL-6,NO等炎症介质,评价药物对巨噬细胞释放以上炎症介质的抑制作用。以ELISA法检测TNF-α,IL-6的含量,以Griess法检测NO的含量,同时以MTT法评价细胞毒性。Western blot法检测iNOS,COX-2及内参蛋白β-actin水平。比色法检测COX-2酶活性。结果:二氢青蒿素在12.5～100μmol.L-1可明显抑制LPS诱导小鼠巨噬细胞RAW 264.7释放TNF-α,IL-6及NO,并呈现良好的剂量依赖关系。青蒿素仅对IL-6具有一定程度的抑制作用。结论:二氢青蒿素通过下调iNOS蛋白表达,抑制巨噬细胞释放炎症因子TNF-α,IL-6和炎症介质NO发挥抗炎活性,青蒿素可能通过代谢为二氢青蒿素发挥抗炎作用。Objective： To study and compare the anti-inflammatory effect and molecular mechanism of artemisinin and dihydroartemisinin. Method： Mouse mononuclear macrophage RAW264.7 cells were stimulated to release inflammatory mediators such as TNF-α, IL-6 and NO, in order to assess the drugs＇ inhibitory effect on macrophage＇s release of above inflammatory mediators. The levels of TNF-α and IL-6 were determined by ELISA and the cytotoxicity was determined by MTT method. The protein expression of iNOS, COX-2 and β-actin were tested by Western blot. The enzymatic activity of COX-2 was determined by colorimetric method. Result： Dihydroartemisinin significantly inhibited LPS-induced release of TNF-α, IL-6 and NO from RAW264.7 in mice with the concentration range of 12.5-100 μmol·L-1, and showed good dose dependence. Artemisinin only inhibited the IL-6 release to a certain extent. Conclusion： Dihydroartemisinin inhibits macrophages from releasing inflammatory factors TNF-α and IL-6 and inflammatory mediators NO by down-regulating iNOS protein. Artemisinin may help dihydroartemisinin to show its anti-inflammatory effect through metabolism.

关 键 词：青蒿素 二氢青蒿素 TNF-Α IL-6 NO COX-2 

分 类 号：R285[医药卫生—中药学]