New Rev-export inhibitor from Alpinia galanga and structure-activity relationship

Bioorg Med Chem Lett. 2009 May 1;19(9):2555-7. doi: 10.1016/j.bmcl.2009.03.047. Epub 2009 Mar 17.

Abstract

Bioassay-guided separation by use of the fission yeast expressing NES of Rev, an HIV-1 viral regulatory protein, disclosed 1'-acetoxychavicol acetate (ACA, 1) as a new inhibitor for nuclear export of Rev from the roots of Alpinia galanga. Both analysis for mechanism of action with biotinylated probe (2) and several synthesized analogs established crucial portions in 1 for Rev-export inhibitory activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acquired Immunodeficiency Syndrome / drug therapy
  • Alpinia / genetics*
  • Alpinia / metabolism*
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology*
  • Benzyl Alcohols / chemistry
  • Benzyl Alcohols / pharmacology*
  • Biological Assay
  • Biotinylation
  • Chemistry, Pharmaceutical / methods
  • Drug Design
  • HIV-1 / metabolism
  • HeLa Cells
  • Humans
  • Plant Extracts / chemistry
  • Plant Extracts / pharmacology*
  • Plant Roots
  • Structure-Activity Relationship
  • rev Gene Products, Human Immunodeficiency Virus / antagonists & inhibitors*
  • rev Gene Products, Human Immunodeficiency Virus / chemistry

Substances

  • Anti-HIV Agents
  • Benzyl Alcohols
  • Plant Extracts
  • rev Gene Products, Human Immunodeficiency Virus
  • 1'-acetoxychavicol acetate