Unprecedented NES non-antagonistic inhibitor for nuclear export of Rev from Sida cordifolia

  • Bioorg Med Chem Lett. 2010 Mar 15;20(6):1837-9. doi: 10.1016/j.bmcl.2010.01.165.
Satoru Tamura  1 ,  Masafumi Kaneko ,  Atsushi Shiomi ,  Guang-Ming Yang ,  Toshiaki Yamaura ,  Nobutoshi Murakami
Affiliations
  • 1. Graduate School of Pharmaceutical Sciences, Osaka University, Suita, Osaka, Japan.
PMID: 20176483 DOI: 10.1016/j.bmcl.2010.01.165
Abstract

Bioassay-guided separation from the MeOH extract of the South American medicinal plant Sida cordifolia resulted in isolation of (10E,12Z)-9-hydroxyoctadeca-10,12-dienoic acid (1) as an unprecedented NES non-antagonistic inhibitor for nuclear export of Rev. This mechanism of action was established by competitive experiment by the biotinylated probe derived from leptomycin B, the known NES antagonistic inhibitor. Additionally, structure-activity relationship analysis by use of the synthesized analogs clarified cooperation of several functionalities in the Rev-export inhibitory activity of 1.