内科

目的探讨单体化合物苦豆碱的体外细胞毒性以及抗HIV-1活性作用，为寻找新的艾滋病治疗药物提供依据。方法以TZM-bl-HIV-1IIIB系统和MT-2-HIV-1IIIB系统为实验模型，用不同稀释度的苦豆碱溶液分别与TZM-bl细胞、MT-2细胞共同培养。采用ATP细胞活力检测试剂检测细胞的相对活力，观察苦豆碱对TZM-bl细胞、MT-2细胞的毒性作用；用HIV-1IIIB感染TZM-bl细胞和MT-2细胞，利用基于TZM-bl细胞的荧光素酶检测试剂，检测HIV病毒相对水平，观察苦豆碱抑制HIV-1活性的作用。结果在TZM-bl-HIV-1IIIB系统中，苦豆碱对TZM-bl细胞的半数细胞毒性浓度（CC50）＞215.183 μM，苦豆碱对HIV-1IIIB的半数抑制浓度（IC50）为3.403 μM，治疗指数（TI）＞63.2。在MT-2-HIV-1IIIB系统中，苦豆碱对MT-2细胞的CC50为802.000 μM，对HIV-1IIIB的IC50为47.190 μM， TI为＞16.9。结论苦豆碱毒性小，抗HIV-1活性明显，具有潜在的开发利用价值。

ObjectiveTo observe the cytotoxicity and anti-HIV-1 activity effect of the monomeric compound aloperine and provide a basis for finding new drugs for AIDS treatment. MethodsThe TZM-bl-HIV-1IIIB system and the MT-2-HIV-1IIIB system were used as experimental models, the different concentrations of aloperine solution were used to co-culture with TZM-bl cells and MT-2 cells, respectively. The relative viability of cells was detected by ATP cell viability assay, and the toxicity of aloperine to TZM-bl cells and MT-2 cells was observed. HIV-1IIIB was used to infect TZM-bl cells and MT-2 cells, and the relative level of HIV-1 virus was detected by using the luciferase detection reagent based on TZM-bl cells, so as to observe the effect of aloperine on inhibiting the HIV-1 activity. ResultsIn the TZM-bl-HIV-1 IIIB system, the half cytotoxic concentration (CC50) of aloperine on TZM-bl cells was greater than 215.183 μM, the half inhibitory concentration (IC50) was 3.403 μM and the treatment index (TI) was greater than 63.2. In the MT-2-HIV-1 IIIB system, the CC50 of aloperine on MT-2 cells was 802.000 μM, the IC50 was 47.190 μM and the TI was greater than 16.9. ConclusionAloperine shows weak cytotoxicity and obvious anti-HIV-1 activity effect, it will be worthy of further study.