Anti-trypanosomal activity of helenalin and some structurally related sesquiterpene lactones.
The anti-trypanosomal activity of six sesquiterpene lactones (helenalin, mexicanin I, 11alpha,13-dihydrohelenalin acetate, chamissonolide, ivalin and isoalantolactone) against the African Trypanosoma brucei rhodesiense and American T. cruzi was investigated. All tested compounds were found active towards both parasites, the former being generally more sensitive. Helenalin was the most active compound in the series with IC50 values of 0.051 and 0.695 microM against T. brucei rhodesiense and T. cruzi, respectively. The low IC50 value for T. b. rhodesiense indicates that helenalin type compounds may be interesting candidates for further evaluation.
Schmidt
Thomas J
TJ
Institut für Pharmazeutische Biologie der Heinrich-Heine-Universität, Düsseldorf, Germany. schmidtt@uni-duesseldorf.de
Brun
Reto
R
Willuhn
Günter
G
Khalid
Sami A
SA
D000818:Animals; D018650:Arnica / Q000737:chemistry; D020128:Inhibitory Concentration 50; D007783:Lactones / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D010946:Plants, Medicinal / Q000737:chemistry; D012717:Sesquiterpenes / Q000737:chemistry / Q000494:pharmacology*; D045789:Sesquiterpenes, Guaiane; D014344:Trypanocidal Agents / Q000737:chemistry / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects*
D007783:Lactones; D012717:Sesquiterpenes; D045789:Sesquiterpenes, Guaiane; D014344:Trypanocidal Agents; C001329:helenalin