Antileishmanial activity of natural diterpenes from Cistus sp. and semisynthetic derivatives thereof

Biol Pharm Bull. 2006 Aug;29(8):1775-8. doi: 10.1248/bpb.29.1775.

Abstract

Eleven cis-clerodane diterpenes, seven labdane type diterpenes and one triterpene isolated from Cistus monspeliensis and the resin "Ladano" of Cistus creticus subsp. creticus were evaluated against Leishmania donovani promastigotes, the causative agent for visceral leishmaniasis. In addition, eleven semisynthetic manoyl oxide, seventeen labdane type derivatives and a triterpene were also evaluated for their antileishmanial activity. 18-Acetoxy-cis-clerod-3-en-15-ol, 15,18-diacetoxy-cis-clerod-3-ene and 13-(E)-8a-hydroxylabd-13-en-15-ol 2-chloroethylcarbamate exhibited the most potent and selective leishmanicidal activity with IC50 values of 3.3 microg/ml, 3.4 microg/ml and 3.5 microg/ml, respectively.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Antiprotozoal Agents / chemistry
  • Antiprotozoal Agents / isolation & purification
  • Antiprotozoal Agents / pharmacology*
  • Chlorocebus aethiops
  • Cistus / chemistry*
  • Diterpenes / chemistry
  • Diterpenes / isolation & purification
  • Diterpenes / pharmacology*
  • Leishmania donovani / drug effects*
  • Molecular Structure
  • Species Specificity
  • Vero Cells

Substances

  • Antiprotozoal Agents
  • Diterpenes