苦豆碱的体外细胞毒性以及抗HIV-1活性实验研究

Experimental study on cytotoxicity and anti-HIV-1 activity of aloperine in vitro

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-1_(IIIB)系统和MT-2-HIV-1_(IIIB)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-1_(IIIB)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-1_(IIIB)系统中,苦豆碱对TZM-bl细胞的半数细胞毒性浓度(CC_(50))> 215. 183μM,苦豆碱对HIV-1_(IIIB)的半数抑制浓度(IC50)为3. 403μM,治疗指数(TI)> 63. 2。在MT-2-HIV-1_(IIIB)系统中,苦豆碱对MT-2细胞的CC_(50)为802. 000μM,对HIV-1_(IIIB)的IC_(50)为47. 190μM,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。

Objective To 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. Methods The 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. Results In the TZM-bl-HIV-1 IIIB system, the half cytotoxic concentration (CC 50 ) of aloperine on TZM-bl cells was greater than 215.183 μM, the half inhibitory concentration (IC 50 ) was 3.403 μM and the treatment index (TI) was greater than 63.2. In the MT-2-HIV-1 IIIB system, the CC 50 of aloperine on MT-2 cells was 802.000 μM, the IC 50 was 47.190 μM and the TI was greater than 16.9. Conclusion Aloperine shows weak cytotoxicity and obvious anti-HIV-1 activity effect, it will be worthy of further study.