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目的:评价两种非核苷类逆转录酶抑制剂(JB25、JB26)与3种已上市药物齐多夫定(AZT)、依非韦仑(EFV)、沙奎那韦(SQV)联合应用的体外抗HIV活性。方法:将10个浓度的JB25、JB26分别与AZT、EFV、SQV的7个浓度组成各种浓度的组合,加入384孔细胞培养板,与HIV-1ⅢB急性感染的MT-2细胞共培养3d,最后利用TZMbl细胞报告基因检测HIV-1的表达,共重复3次。利用MacSynergyⅡ软件对数据进行分析,得到药物相互作用的情况。结果:JB25与AZT、EFV、SQV的平均协同/拮抗容量分别是244.45/-5.05,119.58/-65.93,145.83/-0.32(nmol/L)2%;JB26与AZT、EFV、SQV的平均协同/拮抗容量分别是398.90/0,103.62/-0.49,138.473/-0.27(nmol/L)2%。结论:两种非核苷类逆转录酶抑制剂与3种已上市的药物在体外联合应用,具有协同抗HIV作用,MacSynergyⅡ软件可以全面评价两种药物的联合作用情况。
AIM: To evaluate the efficacy of two non-nucleoside reverse transcriptase inhibitors (JB25, JB26) in combination with three marketed drugs, zidovudine (AZT), efavirenz (EFV) and saquinavir In vitro anti-HIV activity. Methods: The 10 concentrations of JB25 and JB26 were respectively combined with 7 concentrations of AZT, EFV and SQV to make various concentrations. The 384-well cell culture plates were co-cultured with MT-2 cells infected with HIV-1 Ⅲ B for 3 days. Finally, the TZMbl cell reporter gene was used to detect the expression of HIV-1 for a total of 3 times. The use of MacSynergy Ⅱ software to analyze the data obtained drug interactions. Results: The average synergistic / antagonistic capacities of JB25, AZT, EFV and SQV were 244.45 / -5.05, 119.58 / -65.93 and 145.83 / -0.32 (nmol / L) Antagonistic capacity was 398.90 / 0,103.62 / -0.49,138.473 / -0.27 (nmol / L) 2%. Conclusion: Two non-nucleoside reverse transcriptase inhibitors and three marketed drugs are used in vitro and in combination with anti-HIV. MacSynergyⅡ software can comprehensively evaluate the combined effect of the two drugs.