卵叶槲寄生化学成分体外抗HIV活性的初步研究

Anti-HIV activities of chemical constituents from V. album L.var. meridianum Danser

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 activities of anti-HIV of chemical constituents from V.album L.var. meridianum Danser and provid the references for the further studies and development.Methods：MTT assay was used to determine the cytotoxicity of compounds. The anti-HIV activities on acute infection of chemical constituents were evaluated by cytopathic effect（CPE） assay. The inhibition of HIV-1 replication in chronically infected cells was evaluated by p24 antigen expression（ELISA method）. Results：Several compounds from V. album var. meridianum showed potent inhibition HIV replication. 3,5,7,4＇-tetrahydroxy-3＇-methoxyflavanone and eriodictyol had the potent anti-HIV-1 and HIV-2 activities with EC50 of 2-3 μg·mL^-1 and 1.5-2.5 μg·mL^-1,respectively. Meantime,no significant cytotoxicy was obtained on T lymphocytes cell lines C8166. Conclusion：Compounds 3,5,7,4＇-tetrahydroxy-3＇-methoxyflavanone and eriodictyol extracted from V. album L.var. meridianum have anti-HIV-1 and HIV-2 activities.