乌药茎中鞣质类成分及其抗HIV-1整合酶活性研究

Inhibitory activities of tannins extracted from stem of Lindera aggregata against HIV-1 integrase

目的 研究樟科药用植物乌药 [Linderaaggregata (Sims)Kosterm .]的抗HIV 1整合酶的活性成分。 方法 采用 6 0 %丙酮冷浸提取 ,通过反复SephadexLH 2 0和MCI gelCHP 2 0P柱色谱从乌药茎中分离缩合鞣质类化合物 ,通过波谱解析和理化常数进行结构鉴定 ,采用MIA法进行抗HIV 1整合酶活性筛选。结果 分离得到 3个寡聚缩合鞣质类化合物 :二倍体 pro cyanidinB1(LA 1) ,三倍体cinnamtaninB1(LA 2 )和四倍体cinnamtanninB2 (LA 3)。活性筛选结果表明 ,寡聚缩合鞣质具有抗HIV 1整合酶的活性。结论 寡聚缩合鞣质是乌药茎抗HIV 1整合酶的主要活性成分 ,四倍体cinnamtanninB2 (3)

OBJECTIVE: To obtain compounds with inhibitory activities against HIV-1 integrase from the stem of Lindera aggregata (Sims) Kosterm. METHODS: The compounds were extracted with 60% acetone, isolated via column chromatography on Sephadex LH-20 and MCI-gel CHP-20P. The inhibitory activities were studied by the method of MIA(multiplate integration assay). RESULTS: Three oligomeric procyanidins were isolated from the stem of Lindera aggregata. On the basis of the properties and spectral analysis, their structures were identified as: procyanidin B1 (LA-1), cinnamtanin B1 (LA-2) and cinnamtannin B2 (LA-3). MIA test showed the three compounds had inhibitory activities against HIV-1 integrase. CONCLUSION: Oligomeric procyanidins may be the main active components of the stem of Lindera aggregata against HIV-1 integrase. Cinnamtannin B2 (LA-3) was isolated from this plant for the first time.