title: Trypanocidal, leishmanicidal and cytotoxic effects of anthecotulide-type linear sesquiterpene lactones from Anthemis auriculata.
abstract: Trypanosomiasis and leishmaniasis pose major public health threats for many countries, particularly those in sub-Saharan Africa and South America. In the present study, we evaluated the in vitro antiprotozoal activity of three irregular, linear sesquiterpene lactones recently isolated from Greek Anthemis auriculata, namely anthecotulide (1), 4-hydroxyanthecotulide (2) and 4-acetoxyanthecotulide (3). Trypomastigote forms of Trypanosoma brucei rhodesiense and T. cruzi as well as axenic amastigotes of Leishmania donovani were used for testing. The cytotoxic potential of the compounds was also assessed against mammalian (rat) skeletal myoblasts (L6 cells). All compounds showed potent trypanocidal and leishmanicidal activity. 4-Hydroxyanthecotulide (2) appeared to be the most active compound against all parasites, particularly towards T. b. rhodesiense (IC(50) 0.56 microg/ml), whereas 4-acetoxyanthecotulide (3) was the least active. All three metabolites possessed toxicity on mammalian cells, which might limit their use as antiprotozoal agents.
authors.affiliation: Department of Pharmacognosy and Chemistry of Natural Products, School of Pharmacy, University of Athens, Athens, Greece.
authors.forename: Anastasia
authors.initials: A
authors.lastname: Karioti
authors.forename: Helen
authors.initials: H
authors.lastname: Skaltsa
authors.forename: Marcel
authors.initials: M
authors.lastname: Kaiser
authors.forename: Deniz
authors.initials: D
authors.lastname: Tasdemir
mesh_terms: D000818:Animals; D031166:Anthemis / Q000737:chemistry*; D002460:Cell Line; D007783:Lactones / Q000302:isolation & purification / Q000494:pharmacology* / Q000633:toxicity; D007893:Leishmania donovani / Q000187:drug effects; D008018:Life Cycle Stages; D032446:Myoblasts / Q000187:drug effects; D021261:Parasitic Sensitivity Tests; D035261:Plant Components, Aerial; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D010946:Plants, Medicinal / Q000737:chemistry; D051381:Rats; D012717:Sesquiterpenes / Q000302:isolation & purification / Q000494:pharmacology* / Q000633:toxicity; D014344:Trypanocidal Agents / Q000302:isolation & purification / Q000494:pharmacology* / Q000633:toxicity; D016833:Trypanosoma brucei rhodesiense / Q000187:drug effects; D014349:Trypanosoma cruzi / Q000187:drug effects
chemical_list: C510711:4-hydroxyanthecotulide; D007783:Lactones; D010936:Plant Extracts; D012717:Sesquiterpenes; D014344:Trypanocidal Agents; C499300:anthecotulide