Isolation, structure determination, and anti-HIV evaluation of tigliane-type diterpenes and biflavonoid from Stellera chamaejasme

J Nat Prod. 2013 May 24;76(5):852-7. doi: 10.1021/np300815t. Epub 2013 Apr 23.

Abstract

Five novel tigliane-type diterpenes, stelleracins A-E (3-7), a novel flavanone dimer, chamaeflavone A (8), and six known compounds were isolated from the roots of Stellera chamaejasme. Their structures were elucidated by extensive spectroscopic analyses. The isolated compounds were evaluated for anti-HIV activity in MT4 cells. New compounds 3-5 showed potent anti-HIV activity (EC90 0.00056-0.0068 μM) and relatively low or no cytotoxicity (IC50 4.4-17.2 μM). These new compounds represent promising new leads for development into anti-AIDS clinical trial candidates.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acquired Immunodeficiency Syndrome / drug therapy
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / isolation & purification*
  • Anti-HIV Agents / pharmacology*
  • Cell Survival / drug effects
  • Diterpenes / chemistry
  • Diterpenes / isolation & purification*
  • Diterpenes / pharmacology*
  • Flavanones / chemistry
  • Flavanones / isolation & purification*
  • Flavanones / pharmacology*
  • Molecular Structure
  • Nepal
  • Nuclear Magnetic Resonance, Biomolecular
  • Plant Roots / chemistry
  • Thymelaeaceae / chemistry*

Substances

  • Anti-HIV Agents
  • Diterpenes
  • Flavanones
  • flavanone