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目的:探讨卵叶槲寄生化学成分的体外抗人免疫缺陷病毒(HIV)活性。方法:采用四甲基偶氮唑蓝法测定化合物的细胞毒性;细胞病变法检测化合物对HIV急性感染的抑制活性;HIV-1p24抗原ELISA方法检测化合物对慢性感染细胞中HIV复制的影响。计算化合物的抑制率和半数抑制浓度(EC50)。结果:多种卵叶槲寄生的化学成分具有体外抑制HIV复制的作用,特别是3,5,7,4′-四羟基-3′-甲氧基黄烷酮和圣草酚。3,5,7,4′-四羟基-3′-甲氧基黄烷酮在2～3μg·mL-1的浓度范围内对HIV-1和HIV-2复制的抑制率均≥50%,而对C8166细胞的半数细胞毒性浓度(CC50)>200μg·mL-1。圣草酚在低浓度(1.5～2.5μg·mL-1)时,对HIV-1和HIV-2复制的抑制率达50%,其对C8166细胞的CC50为43.40μg·mL-1。结论:卵叶槲寄生化学成分3,5,7,4′-四羟基-3′-甲氧基黄烷酮和圣草酚对HIV-1和HIV-2的体外复制均有不同程度的抑制作用。
Objective: To investigate the in vitro anti-human immunodeficiency virus (HIV) activity of the chemical components of the mistletoe. Methods: The cytotoxicity of the compound was determined by MTT method. The inhibitory activity of the compound against HIV infection was detected by cytopathic method. The HIV-1 p24 antigen ELISA method was used to detect the effect of the compound on HIV replication in chronic infected cells. The compound inhibition rate and half-value inhibitory concentration (EC50) were calculated. RESULTS: The chemical constituents of a variety of egg-leaf mistletoe strains have the effect of inhibiting HIV replication in vitro, especially 3,5,7,4’-tetrahydroxy-3’-methoxyflavanone and eriodictyol. The inhibitory rates of 3,5,7,4’-tetrahydroxy-3’-methoxyflavanone on the replication of HIV-1 and HIV-2 in the range of 2 ~ 3μg · mL-1 were both above 50% While the half-cell cytotoxicity (CC50) of C8166 cells> 200μg · mL-1. The inhibitory rate of eriodictyol to HIV-1 and HIV-2 was 50% at low concentration (1.5 ~ 2.5μg · mL-1), and the CC50 of C8166 cells was 43.40μg · mL-1. Conclusion: The chemical constituents of 3, 5, 7, 4’-tetrahydroxy-3’-methoxyflavanone and eriodictyol in egg-leaf mistletoe inhibit the replication of HIV-1 and HIV-2 in vitro to some extent effect.