Ellagic acid inhibits HIV-1 infection in vitro: Potential role as a novel microbicide

Oral Dis. 2018 Mar;24(1-2):249-252. doi: 10.1111/odi.12835.

Abstract

Objective: To investigate the in vitro effects of ellagic acid on HIV-1 replication.

Methods: Anti-HIV-1 activity of ellagic acid was determined in vitro using X4-tropic HIV-1NPO3 and R5-tropic pBaL Env-recombinant virus. Anti-HIV-1NPO3 activity of ellagic acid was investigated at a multiplicity of infection (MOI) of 0.01. Anti-HIV-1 integrase and protease activities of ellagic acid were tested using in vitro integration and proteolytic cleavage assays.

Results: Ellagic acid, added either before or after HIV-1NPO3 exposure, suppressed replication of the virus in C8166 cells up to 34%. Ellagic acid showed an anti-integrase IC50 of 8.7 μM. No cytotoxicity of ellagic acid at concentrations ranging from 12.5 to 100 μM was observed.

Conclusion: We conclude that ellagic acid can inhibit HIV-1 infection without cytotoxicity. Thus, it may be a new effective agent that has potential to be developed as a novel microbicide against HIV-1.

Keywords: HIV-1; ellagic acid; infection; integrase; microbicide; protease.

MeSH terms

  • CD4-Positive T-Lymphocytes / physiology
  • Cell Line
  • Cell Survival / drug effects
  • Ellagic Acid / pharmacology*
  • HIV Infections / prevention & control*
  • HIV Integrase / drug effects
  • HIV Protease / drug effects
  • HIV-1 / drug effects*
  • HIV-1 / enzymology
  • Humans
  • Virus Replication / drug effects*

Substances

  • Ellagic Acid
  • HIV Integrase
  • HIV Protease