雷公藤红素药理作用分子靶点的研究进展  

Research progress in pharmacologic molecular targets of celastrol

作　　者：丁海鹏[1] 李相鹏[1] 张伟[2] 丁宁[2] 王鹏[1] 李国强[1] 李英霞[2] 

机构地区：[1]中国海洋大学医药学院海洋药物教育部重点实验室山东省海洋药物重点实验室,山东青岛266003 [2]复旦大学药学院药物化学系,上海201203

出　　处：《中国药理学与毒理学杂志》2012年第4期570-576,共7页Chinese Journal of Pharmacology and Toxicology

基　　金："十一五"国家新药创制重大专项(2009ZX09102-014)~~

摘　　要：雷公藤红素是从传统中药雷公藤中提取分离得到的一种醌甲基三萜,具有抗炎、免疫抑制及抗肿瘤等药理活性。雷公藤红素几个特殊的分子靶点大多会抑制IKK-NF-κB信号通路,包括:①抑制IKKα/β激酶;②失活热休克蛋白90的分子伴侣蛋白细胞分裂周期蛋白37及P23;③抑制蛋白酶体的功能;④激活热激因子1诱导热休克蛋白反应;⑤影响肿瘤细胞的增殖;⑥影响细胞凋亡;⑦影响丝裂原活化蛋白激酶;⑧影响Akt/mTOR信号级联;⑨影响血管生成和转移;⑩抗炎作用。本文对其药理作用分子靶点研究进展做一综述。Celastrol, a quinone methide triterpene, is a pharmacologically active compound present in Tripterygium wilfordii（Thunder God Vine） root extracts. As a potential medicine, celastrol shows significant pharmacological activity on many diseases, such as cancer, inflammatory and autoimmune diseases. Its molecular tar- gets are mostly centered on the inhibition of IKK-NF-KB signaling, such as by ① inhibiting the IKKα/β kinases, ② inactivating the cell division cycle protein 37 and P23 proteins which are co-chaperones of heat shock protein 90, ③ inhibiting the function of proteasomes, ④ activating the heat shock transcription factor-1 and subsequently triggering the heat shock response, ⑤ affecting proliferation of tumor cells, ⑥ affecting apoptosis, ⑦ affcting mitogen-activated protein kinases, ⑧ affcting Akt/mTOR and ⑨ exerting anti-inflammatory effect signaling cascade, ⑩affecting angiogenesis and metastasis,

关 键 词：雷公藤红素 药理作用 分子靶点 NF-ΚB 热休克蛋白90 细胞分裂周期蛋白 P23 

分 类 号：R285.5[医药卫生—中药学]