title: [1,2,6-tri-O-galloyl-beta-D-glucopyranose inhibits gp41-mediated HIV envelope fusion with target cell membrane].
abstract: OBJECTIVE
  To 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.
  
  
  METHODS
  TGGP 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.
  
  
  RESULTS
  TGGP 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.
  
  
  CONCLUSIONS
  The 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.
authors.affiliation: School of Pharmaceutical Science, Southern Medical University, Guangzhou 510515, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Sun
authors.forename: Hong-tao
authors.initials: HT
authors.lastname: Wang
authors.forename: Cheng-lai
authors.initials: CL
authors.lastname: Xia
authors.forename: Shu-guang
authors.initials: SG
authors.lastname: Wu
authors.forename: Shi-bo
authors.initials: SB
authors.lastname: Jiang
authors.forename: Zhi-hong
authors.initials: ZH
authors.lastname: Jiang
authors.forename: Shu-wen
authors.initials: SW
authors.lastname: Liu
mesh_terms: D019380:Anti-HIV Agents / Q000494:pharmacology*; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D015700:HIV Envelope Protein gp41 / Q000378:metabolism*; D023581:HIV Fusion Inhibitors / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects / Q000254:growth & development / Q000378:metabolism; D006801:Humans; D047348:Hydrolyzable Tannins / Q000494:pharmacology*; D008561:Membrane Fusion / Q000187:drug effects
chemical_list: C106217:1,3,6-tri-O-galloylglucopyranose; D019380:Anti-HIV Agents; D015700:HIV Envelope Protein gp41; D023581:HIV Fusion Inhibitors; D047348:Hydrolyzable Tannins