日本蛇菰中咖啡酰基葡萄糖类化合物抑制HIV-1进入的机制

Translated title of the contribution: Study of the mechanism of caffeoyl glucopyranoses in inhibiting HIV-1 entry using pseudotyped virus system

夏承来*, 毛芹超, 李润明, 陈之朋, 姜世勃, 姜志宏, 刘叔文

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

1 Citation (Scopus)

Abstract

To investigate the inhibitory activities of caffeoyl glucopyranoses purified from Balanophora japonica Makino on HIV entry and their mechanism. HIV-1 Env pseudovirus was used to evaluate the anti-HIV-1 activity of those compounds. ELISA and molecular docking were used to study the mechanism of the actions of the active compounds. We used the HIV-1 Env pseudovirus to test the anti-HIV-1 activity of the six phenolic compounds (final concentration 25 microg/ml), and found that only 1,2,6-Tri-O-caffeoyl-beta-D-glucopyranose (TCGP) and 1,3-Di-O-caffeoyl-4-O-galloyl-beta-D- glucopyranose (DCGGP) could effectively inhibit the entry of HIV-1 Env pseudovirus into the target cells in a dose-dependent manner, with IC(50) values of 5.5-/+0.2 and 5.3-/+0.1 microg/ml, respectively. These two compounds could also blocked the gp41 six-helix bundle formation. Molecular docking analysis suggested that they might bind to the hydrophobic cavity of the gp41 N-trimeric coiled-coil. TCGP and DCGGP are potent HIV-1 entry inhibitors targeting gp41 and can serve as lead compounds for developing novel anti-HIV-1 microbicides for prevention of sexual HIV-1 transmission.

Translated title of the contributionStudy of the mechanism of caffeoyl glucopyranoses in inhibiting HIV-1 entry using pseudotyped virus system
Original languageChinese (Simplified)
Pages (from-to)720-723
Number of pages4
Journal​南方医科大学学报
Volume30
Issue number4
Publication statusPublished - Apr 2010

Scopus Subject Areas

  • Medicine(all)

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