1,2,6-tri-O-galloyl-beta-D-glucopyranose inhibits gp41-mediated HIV envelope fusion with target cell membrane.
- Author:
Wei SUN
1
;
Hong-tao WANG
;
Cheng-lai XIA
;
Shu-guang WU
;
Shi-bo JIANG
;
Zhi-hong JIANG
;
Shu-wen LIU
Author Information
- Publication Type:Journal Article
- MeSH: Anti-HIV Agents; pharmacology; Cell Membrane; drug effects; metabolism; HIV Envelope Protein gp41; metabolism; HIV Fusion Inhibitors; pharmacology; HIV-1; drug effects; growth & development; metabolism; Humans; Hydrolyzable Tannins; pharmacology; Membrane Fusion; drug effects
- From: Journal of Southern Medical University 2008;28(7):1127-1131
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVETo observe the inhibitory effect of 1,2,6-Tri-O-galloyl-beta-D-glucopyranose (TGGP) from Balanophora japonica Makino on human immunodeficiency virus (HIV) entry into the host cells and explore the mechanisms.
METHODSTGGP was purified from Balanophora japonica Makino by n-hexane and ethyl acetate extraction and column chromatography. The inhibitory activity of TGGP on HIV gp41 six-helix bundle formation was measured with ELISA, N-PAGE and SE-HPLC, and the inhibitory effect of TGGP on HIV envelope grlycoprotein-induced cell-cell fusion was detected using a non-infectious cell-based assay.
RESULTSTGGP inhibited HIV gp41 six-helix bundle formation, with an IC50 of 1.37-/+0.19 microg/ml as determined by ELISA, and this activity was further confirmed by N-PAGE and SE-HPLC. TGGP at 25 microg/ml significantly inhibited syncytium formation between the effector (CHO-WT) and the target (MT-2) cells.
CONCLUSIONThe HIV transmembrane subunit gp41 mediates the entry of HIV into the target cells. TGGP can inhibit HIV fusion and entry into the target cells by inhibiting the formation of gp41 six-helix bundles, suggesting the potential of TGGP as a microbicide to prevent sexual transmission of HIV.
