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
em Zh
| WPRIM
| ID: wpr-355035
Biblioteca responsável:
WPRO
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>
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Índice:
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Assunto principal:
Farmacologia
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Extratos Vegetais
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Linhagem Celular
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Química
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HIV-1
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Fármacos Anti-HIV
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Balanophoraceae
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Taninos Hidrolisáveis
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Ácido Gálico
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Glucose
Limite:
Humans
Idioma:
Zh
Revista:
Journal of Southern Medical University
Ano de publicação:
2010
Tipo de documento:
Article