In vitro antitrypanosomal activity of plant terpenes against Trypanosoma brucei

Phytochemistry. 2011 Nov;72(16):2024-30. doi: 10.1016/j.phytochem.2011.07.015. Epub 2011 Aug 16.

Abstract

During the course of screening to discover antitrypanosomal compounds, 24 known plant terpenes (6 sesquiterpenes, 14 sesquiterpene lactones and 4 diterpenes) were evaluated for in vitro antitrypanosomal activity against Trypanosoma brucei brucei. Among them, 22 terpenes exhibited antitrypanosomal activity. In particular, α-eudesmol, hinesol, nardosinone and 4-peroxy-1,2,4,5-tetrahydro-α-santonin all exhibited selective and potent antitrypanosomal activities in vitro. Detailed here in an in vitro antitrypanosomal properties and cytotoxicities of the 24 terpenes compared with two therapeutic antitrypanosomal drugs (eflornithine and suramin). This finding represents the first report of promising trypanocidal activity of these terpenes. Present results also provide some valuable insight with regard to structure-activity relationships and the possible mode of action of the compounds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Diterpenes / chemistry
  • Diterpenes / isolation & purification
  • Diterpenes / pharmacology
  • Eflornithine / pharmacology
  • Plants / chemistry
  • Structure-Activity Relationship
  • Suramin / pharmacology
  • Terpenes / chemistry
  • Terpenes / isolation & purification
  • Terpenes / pharmacology*
  • Trypanocidal Agents / chemistry
  • Trypanocidal Agents / isolation & purification
  • Trypanocidal Agents / pharmacology*
  • Trypanosoma brucei brucei / drug effects*

Substances

  • Diterpenes
  • Terpenes
  • Trypanocidal Agents
  • Suramin
  • Eflornithine