Study of the mechanism of caffeoyl glucopyranoses in inhibiting HIV-1 entry using pseudotyped virus system / 南方医科大学学报
Journal of Southern Medical University
;
(12): 720-723, 2010.
Article
in Chinese
| WPRIM
| ID: wpr-355035
ABSTRACT
<p><b>OBJECTIVE</b>To investigate the inhibitory activities of caffeoyl glucopyranoses purified from Balanophora japonica Makino on HIV entry and their mechanism.</p><p><b>METHODS</b>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.</p><p><b>RESULTS</b>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.</p><p><b>CONCLUSION</b>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.</p>
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
Plant Extracts
/
Cell Line
/
Chemistry
/
HIV-1
/
Anti-HIV Agents
/
Balanophoraceae
/
Hydrolyzable Tannins
/
Gallic Acid
/
Glucose
Limits:
Humans
Language:
Chinese
Journal:
Journal of Southern Medical University
Year:
2010
Type:
Article
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