6种藏族药提取物体外抗HIV-1活性的初步探讨

In Vitro Anti-HIV-1 Activity of Extracts from 6 Traditional Tibetan Medicines

摘要:

目的：对斑花黄堇、木藤蓼、野棉花、黄花铁线莲、黑心虎耳草和短尾铁线莲6种藏药提取物的体外抗艾滋病病毒Ⅰ型（HIV-1）病毒活性的评价及其作用机制的初步研究。方法：采用细胞计数试剂盒（CCK-8）法细胞毒性实验和HIV-1假病毒单周期感染实验检测提取物的体外抗病毒活性和细胞毒性；利用表面等离子共振（surface plasmon resonance，SPR）技术、蛋白酶、整合酶和逆转录酶体外活性抑制实验初步探讨药物的作用靶点。结果：在这6种藏药提取物中，木藤蓼、野棉花、黑心虎耳草提取物具有较好的体外抗HIV-1病毒活性，半数抑制浓度（half maximal inhibitory concentration，IC₅₀）分别为（6.47±0.78），（11.97±1.09），（11.7±0.79）mg·L^-1，且细胞毒性较小，三者均具有较好的体外抑制整合酶活性。结论：木藤蓼、野棉花、黑心虎耳草提取物具有较好的抗HIV-1病毒的作用，其作用机制与整合酶的抑制作用有关。

Abstract:

Objective: To evaluate the in vitro anti-HIV-1 activities and mechanism of extracts from 6 traditional Tibetan medicines:Corydalis conspersa, Fallopia aubertii, Anemone vitifolia, Clematis urophylla, Saxifraga melanocentra and C. hexapetala. Method: Cell counting kit(CCK-8) cell cytotoxicity test and HIV-1 single cycle infection experiments were used to detect the in vitro anti-HIV-1 effect and cytotoxicity of extracts. The surface plasma resonance(SPR) technology, protease, integrase and reverse transcriptase inhibition assay were used to identify the potential targets of these extracts. Result: The extracts from F. aubertii, A. vitifolia and S. melanocentra showed dose-dependent anti-HIV-1 effect with little cytotoxicity. Their half maximal inhibitory concentrations (IC₅₀) were (6.47±0.78), (11.97±1.09), (11.7±0.79) mg·L^-1, respectively. All the above three extracts inhibited integrase activity. Conclusion: F. aubertii, A. vitifolia and S. melanocentra extracts potently inhibited HIV-1 virus in vitro, possibly through down-regulating integrase activity.