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目的:研究从药用植物金佛山雪胆分离的雪胆素A和雪胆素B两个三萜类化合物的体外抗HIV活性。方法:应用合胞体抑制实验、p24抗原产生的抑制实验、慢性感染细胞和正常细胞间的细胞融合抑制实验等技术检测化合物的体外抗HIV-1活性;利用HIV-1逆转录酶、蛋白酶抑制实验,NCp7锌离子逐出实验探讨化合物的作用机制。结果:雪胆素A和雪胆素B在体外有较好的抑制HIV-1活性,其活性主要表现为:(1)抑制HIV-1诱导合胞体形成,EC50值分别为3.09μg.mL-1和2.53μg.mL-1;(2)抑制HIV-1急性感染的C8166细胞p24抗原产生,EC50值分别为3.97μg.mL-1和18.90μg.mL-1; (3)抑制HIV-1慢性感染H9与正常C8166细胞间融合, EC50分别为1.76μg.mL-1和11.95μg.mL-1。雪胆素A和雪胆素B对HIV-1逆转录酶、蛋白酶、NCp7锌离子逐出均没有抑制作用。雪胆素A对HIV-1整合酶有微弱的结合活性,而雪胆素B对HIV-1整合酶没有结合活性。在共培养实验中,雪胆素A和雪胆素B预处理C8166细胞组比未经预处理细胞组能够更有效的抑制HIV-1活性。结论:化合物雪胆素A和雪胆素B体外有较好的抗HIV-1活性,可能主要作用于HIV-1病毒进入细胞阶段。
Objective: To study the in vitro anti-HIV activity of the two triterpenoids, sebastrin A and sertin B, isolated from Xuefeng Xuedan, a medicinal plant. METHODS: In vitro anti-HIV-1 activity of compounds was tested using techniques such as syncytia inhibition assays, inhibition experiments of p24 antigen production, cell fusion inhibition between chronically infected cells and normal cells, and HIV-1 reverse transcriptase and protease inhibition assays. , NCp7 zinc ion expulsion experiments explore the mechanism of action of the compound. RESULTS: The activity of HIV-1 was significantly inhibited in vitro by argentin A and cytokinin B. The main activities were as follows: (1) Inhibition of HIV-1-induced syncytium formation with EC50 values of 3.09 μg.mL- 1 and 2.53 μg.mL-1; (2) Inhibition of p24 antigen production in acutely infected HIV-1 C8166 cells with EC50 values of 3.97 μg.mL-1 and 18.90 μg.mL-1, respectively; (3) Inhibition of HIV-1 Chronic fusion between H9 and normal C8166 cells showed an EC50 of 1.76 μg.mL-1 and 11.95 μg.mL-1, respectively. Xuelin A and Xuebaosu B had no inhibitory effect on HIV-1 reverse transcriptase, protease, and NCp7 zinc expulsion. Snow caprine A has a weak binding activity to HIV-1 integrase, and sertin B has no binding activity to HIV-1 integrase. In the co-culture experiments, the pretreatment of C8166 cells with Xuebiruin A and Xuebao B was more effective in inhibiting HIV-1 activity than the untreated cells. CONCLUSIONS: The compounds, Xuelin A and Xuebao B, have good anti-HIV-1 activity in vitro and may play a major role in the entry of the HIV-1 virus into the cell stage.