Epigallocatechin gallate, the main polyphenol in green tea, binds to the T-cell receptor, CD4: Potential for HIV-1 therapy.

摘要: Background The green tea flavonoid, epigallocatechin gallate (EGCG), has been proposed to have an anti–HIV-1 effect by preventing the binding of HIV-1 glycoprotein (gp) 120 CD4 molecule on T cells. Objective To demonstrate that EGCG binds at gp120 attachment site and inhibits physiologically relevant levels, thus establishing as a potential therapeutic treatment for infection. Methods Nuclear magnetic resonance spectroscopy was used examine control, (-)-catechin, CD4-IgG 2 (PRO 542®). Gp120 human + cells analyzed flow cytometry. Results Addition produced linear decrease in nuclear signal intensity from but not (-)-catechin. In saturation transfer difference experiments, addition 5.8 μmol/L 310 strong aromatic rings EGCG, identical concentrations (-)-catechin much smaller effects, implying EGCG/CD4 enough reduce gp120/CD4 substantially. Molecular modeling studies suggested D1 domain CD4, pocket gp120. Physiologically (0.2 μmol/L) inhibited isolated Conclusion We demonstrated clear evidence high-affinity with K d approximately 10 nmol/L inhibition Clinical implications Epigallocatechin use adjunctive therapy