Preclinical development of the green tea catechin, epigallocatechin gallate, as an HIV-1 therapy

J Allergy Clin Immunol. 2009 Feb;123(2):459-65. doi: 10.1016/j.jaci.2008.12.024.


Background: Previously, we presented evidence that at physiologic concentrations the green tea catechin, epigallocatechin gallate (EGCG), inhibited attachment of HIV-1 glycoprotein 120 to the CD4 molecule on T cells, but the downstream effects of EGCG on HIV-1 infectivity were not determined.

Objective: To evaluate the inhibition of HIV-1 infectivity by EGCG and begin preclinical development of EGCG as a possible therapy.

Methods: PBMCs, CD4(+) T cells, and macrophages were isolated from blood of HIV-1-uninfected donors. HIV-1 infectivity was assessed by an HIV-1 p24 ELISA. Cell survival was assessed by cell viability by Trypan blue exclusion assay, cell growth by thymidine incorporation, and apoptosis by flow-cytometric analysis of annexin-V binding.

Results: Epigallocatechin gallate inhibited HIV-1 infectivity on human CD4(+) T cells and macrophages in a dose-dependent manner. At a physiologic concentration of 6 mumol/L, EGCG significantly inhibited HIV-1 p24 antigen production across a broad spectrum of both HIV-1 clinical isolates and laboratory-adapted subtypes (B [P < .001], C, D, and G [P < .01]). The specificity of the EGCG-induced inhibition was substantiated by the failure of EGCG derivatives lacking galloyl and/or pyrogallol side groups to alter HIV-1 p24 levels. EGCG-induced inhibition of HV-1 infectivity was not a result of cytotoxicity, cell growth inhibition, or apoptosis.

Conclusion: We conclude that by preventing the attachment of HIV-1-glycoprotein 120 to the CD4 molecule, EGCG inhibits HIV-1 infectivity. Because this inhibition can be achieved at physiologic concentrations, the natural anti-HIV agent EGCG is a candidate as an alternative therapy in HIV-1 therapy.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Antioxidants / pharmacology*
  • Antioxidants / therapeutic use
  • Apoptosis / drug effects
  • CD4-Positive T-Lymphocytes / drug effects
  • Camellia sinensis / chemistry*
  • Catechin / analogs & derivatives*
  • Catechin / pharmacology
  • Catechin / therapeutic use
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Cells, Cultured
  • HIV Core Protein p24 / antagonists & inhibitors*
  • HIV Core Protein p24 / biosynthesis
  • HIV Infections / drug therapy*
  • HIV-1 / drug effects*
  • HIV-1 / metabolism
  • Humans
  • Macrophages / drug effects
  • Macrophages / physiology


  • Antioxidants
  • HIV Core Protein p24
  • Catechin
  • epigallocatechin gallate