Mao Qin-Chao, Zhou Ying-Chun, Li Run-Ming, Hu Yi-Ping, Liu Shu-Wen, Li Xiao-Juan
School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China.
Zhong Yao Cai. 2010 Nov;33(11):1751-4.
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.
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).
The TSGL could inhibit HIV env mediated cell-cell fusion with an IC50 of (7.33 +/- 0.40) microg/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 microg/mL. N-PAGE study confirmed the inhibitory effect of TSGL on gp41 6-HB formation.
The TSGL can inhibit HIV entry target cells by interfering the envelop subunit gp41 form the critical 6-HB structure.
研究番石榴叶总皂苷（TSGL）对HIV-1包膜蛋白（env）介导的病毒进入靶细胞的影响。
采用SA-1大孔树脂对TSGL进行纯化和浓缩。通过混合CHO-WT细胞和MT-2细胞，利用细胞-细胞融合试验检测TSGL对HIV-1进入靶细胞的影响。采用MTT法测定TSGL的细胞毒性。通过ELISA和非变性聚丙烯酰胺凝胶电泳（N-PAGE）分析TSGL阻断HIV-1 gp41六螺旋束（6-HB）形成的活性。
TSGL能够抑制HIV env介导的细胞-细胞融合，IC50为（7.33±0.40）μg/mL，且在该浓度下细胞毒性很小。ELISA试验表明，TSGL能够阻止gp41 6-HB的形成，在25μg/mL时抑制活性为95.93%。N-PAGE研究证实了TSGL对gp41 6-HB形成的抑制作用。
TSGL可通过干扰包膜亚基gp41形成关键的6-HB结构来抑制HIV进入靶细胞。
