目的研究白附子提取物抗HIV-1的作用,寻找新型高效的抗HIV-1中药先导化合物。方法采用植物化学技术对禹白附进行提取分离,再通过细胞生物学方法[细胞病变观察法(CPE)法和MTT法]检验提取物的抗HIV-1作用,并结合作用靶点的研究对提取物的作用机制进行探讨。结果发现禹白附提取物具有很好的抗HIV-1作用,筛选出3个抗HIV-1作用显著的有效部位,其中两个有效部位的作用靶点分别为HIV-1的gP-41跨膜蛋白和Vif表达蛋白。结论禹白附提取物具有很强的抗HIV--1作用,为进一步寻找高效低毒的抗HIV-1先导化合物奠定了基础,值得进行深入研究。

Objective To study the effect of anti-HIV-1 virus with extracts from the tuber of Typhonium giganteum,so as to discover new and high efficient anti-HIV-1 leading compounds from natural products and Chinese materia medica.Methods Extract from the tuber of T.giganteum was isolated and purified by the way of phytochemistry,such as column chromatography.Then anti-HIV-1 activities of the extracts were assessed by in vitro method,MT4 cells and HIVⅢB virus were used for the experiment.The results were judged by cytopathic effect(CPE) method and p24 antigen assay method.Mechanism studies were carried out by BIA techniques(BIACORE~(?) 3000 molecule coupled equipment).Results The extracts of T.giganteum showed potential anti-HIV-1 activities.Two of them showed gp-41 transmembrance protein and Vif protein expression inhibition,respectively.Conclusion These extracts in the tuber of T.giganteum might rewardingly contribute to anti-HIV-1 activities,which could be developed to be more efficient and less toxic leading compounds in the further.

北京市自然科学基金资助项目(7092007)