Theaflavin derivatives in black tea and catechin derivatives in green tea inhibit HIV-1 entry by targeting gp41
| Autor: | Jinkui Niu, Shuwen Liu, Hong Lu, Shibo Jiang, Shuguang Wu, Asim Kumar Debnath, Qian Zhao, Yuxian He |
|---|---|
| Rok vydání: | 2005 |
| Předmět: |
Anti-HIV Agents
Stereochemistry Biophysics HIV Envelope Protein gp120 Virus Replication Gp41 Membrane Fusion Biochemistry Catechin chemistry.chemical_compound Gallic Acid Biflavonoids Humans Moiety Gallic acid Theaflavin Molecular Biology Coiled coil food and beverages Lipid bilayer fusion HIV Envelope Protein gp41 chemistry Polyphenol CD4 Antigens HIV-1 |
| Zdroj: | Biochimica et Biophysica Acta (BBA) - General Subjects. 1723:270-281 |
| ISSN: | 0304-4165 |
| DOI: | 10.1016/j.bbagen.2005.02.012 |
| Popis: | Theaflavin derivatives and catechin derivatives are the major polyphenols in black tea and green tea, respectively. Several tea polyphenols, especially those with galloyl moiety, can inhibit HIV-1 replication with multiple mechanisms of action. Here we showed that the theaflavin derivatives had more potent anti-HIV-1 activity than catechin derivatives. These tea polyphenols could inhibit HIV-1 entry into target cells by blocking HIV-1 envelope glycoprotein-mediated membrane fusion. The fusion inhibitory activity of the tea polyphenols was correlated with their ability to block the formation of the gp41 six-helix bundle, a fusion-active core conformation. Computer-aided molecular docking analyses indicate that these tea polyphenols, theaflavin-3,3'-digallate (TF3) as an example, may bind to the highly conserved hydrophobic pocket on the surface of the central trimeric coiled coil formed by the N-terminal heptad repeats of gp41. These results indicate that tea, especially black tea, may be used as a source of anti-HIV agents and theaflavin derivatives may be applied as lead compounds for developing HIV-1 entry inhibitors targeting gp41. |
| Databáze: | OpenAIRE |
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