番石榴叶总皂苷对HIV-1包膜蛋白介导的细胞融合的影响  

Inhibition of HIV-1 Mediated Cell-cell Fusion by Saponin Fraction from Psidium guajava Leaf

作　　者：毛芹超[1] 周迎春[2] 李润明[1] 胡义平[1] 刘叔文[1] 李晓娟[1] 

机构地区：[1]南方医科大学药学院 [2]南方医科大学中医药学院,广东广州510515

出　　处：《中药材》2010年第11期1751-1754,共4页Journal of Chinese Medicinal Materials

基　　金：国家自然科学基金(30729001;30801413)

摘　　要：目的:研究番石榴叶总皂苷对HIV-1病毒进入靶细胞的影响,为寻找新的HIV-1进入抑制剂提供实验依据。方法:SA-1型大孔树脂纯化获得番石榴叶总皂苷(TSGL),观察其对HIV-1包膜蛋白介导的MT-2和CHO-WT细胞融合的作用,采用MTT法检测其细胞毒性,通过ELISA、N-PAGE等方法分析TSGL对HIV-1 gp41六螺旋束形成的影响。结果:TSGL能显著抑制HIV介导的细胞融合,IC50为(7.33±0.40)μg/mL,在此剂量下对MT-2和CHO-WT两种细胞均无生长抑制作用。ELISA实验表明,TSGL能显著抑制HIVgp41六螺旋束(6-HB)的形成,25μg/mL时抑制率达到95.93%,而N-PAGE结果进一步确证了药物对6-HB的抑制作用。结论:番石榴叶中总皂苷能抑制HIV进入靶细胞,其作用机制可能与阻止HIV-1包膜蛋白gp41亚基六螺旋束的形成有关。Objective：To investigate the effects of the total saponin of Psidium guajava leaf（TSGL） on HIV-1 envelop proteins（env） mediated virus entry into target cells.Methods：The TSGL was purified and concentrated using SA-1 macropore resin.The effect of TSGL on HIV-1 entry into target cells was tested using a cell-cell fusion assay by mixing CHO-WT and MT-2 cells.The cytotoxicity of TSGL was measured by MTT assay.The activity of TSGL on blocking the HIV-1 gp41 six helical bundle（6-HB） formation was analyzed by ELISA and Native-PAGE（N-PAGE）.Results：The TSGL could inhibit HIV env mediated cell-cell fusion with an IC50 of（7.33±0.40） μg/mL,and displayed little cytotoxicity at that concentration.ELISA assay showed that the TSGL could prevent gp41 6-HB formation with inhibitory activity of 95.93% at 25 μg/mL.N-PAGE study confirmed the inhibitory effect of TSGL on gp41 6-HB formation.Conclusions：The TSGL can inhibit HIV entry target cells by interfering the envelop subunit gp41 form the critical 6-HB structure.

关 键 词：番石榴叶总皂苷 细胞融合 HIV-1gp41 六螺旋束 

分 类 号：R285.5[医药卫生—中药学]