Anti-HIV-1 activities of compounds isolated from the medicinal plant Rhus chinensis

J Ethnopharmacol. 2008 May 8;117(2):249-56. doi: 10.1016/j.jep.2008.01.037. Epub 2008 Feb 9.

Abstract

Aim of the study: Previously, we reported that the petroleum ether fraction, RC-1, and EtOAc fraction, RC-2, of the medicinal plant Rhus chinensis showed potent anti-HIV-1 activities. To address anti-HIV-1 constituents of RC-1 and RC-2, 17 compounds were isolated. Anti-HIV-1 activities and possible action mechanisms of these compounds were investigated.

Methods: The syncytial formation induced by HIV-1 was determined under the inverted microscope, cellular toxicity and protection assay were assessed by MTT method, reduction of p24 antigen expression level and RT activity were measured by ELISA, and inhibition of recombinant HIV-1 PR was monitored by the fluorescent signal.

Results: The compounds 1 and 13 inhibited HIV-1-induced syncytium formation potently with TI value of 42.31 and 19.07, respectively. Compounds 4, 5, 6, 9 and 10 were less potent with TI value of 8.94, 8.22, 4.14, 5.11 and 5.34, respectively. Compound 1, a benzofuranone-type compound, previously reported as a novel anti-HIV-1 agent, might target late-steps of HIV-1 life cycle. Compound 13 inhibited HIV-1 replication with EC(50) of 7.16mug/ml and might target at/before integration step.

Conclusion: These compounds might contribute to anti-HIV-1 activities extracts of the medicinal plant Rhus chinensis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / isolation & purification
  • Anti-HIV Agents / pharmacology*
  • Cell Line
  • Enzyme-Linked Immunosorbent Assay
  • Giant Cells / drug effects
  • Giant Cells / physiology
  • HIV Core Protein p24 / metabolism
  • HIV Infections / drug therapy
  • HIV Infections / virology
  • HIV-1 / drug effects*
  • Humans
  • Magnetic Resonance Spectroscopy
  • Plant Extracts / chemistry
  • Plant Extracts / pharmacology
  • Plant Stems / chemistry
  • Rhus / chemistry*
  • Tetrazolium Salts
  • Thiazoles

Substances

  • Anti-HIV Agents
  • HIV Core Protein p24
  • Plant Extracts
  • Tetrazolium Salts
  • Thiazoles
  • thiazolyl blue