title: Antiplasmodial and antitrypanosomal activity of pyrethrins and pyrethroids.
abstract: In a screen of 1800 plant and fungal extracts for antiplasmodial, antitrypanosomal, and leishmanicidal activity, the n-hexane extract of Chrysanthemum cinerariifolium (Trevir.) Vis. flowers showed strong activity against Plasmodium falciparum. We isolated the five pyrethrins [i.e., pyrethrin II (1), jasmolin II (2), cinerin II (3), pyrethrin I (4), and jasmolin I (5)] from this extract. These were tested together with 15 synthetic pyrethroids for their activity against P. falciparum and Trypanosoma brucei rhodesiense and for cytotoxicity in rat myoblast L6 cells. The natural pyrethrins showed antiplasmodial activity with IC(50)s between 4 and 12 μM, and antitrypanosomal activity with IC(50)s from 7 to 31 μM. The pyrethroids exhibited weaker antiplasmodial and antitrypanosomal activity than the pyrethrins. Both pyrethrins and pyrethroids showed moderate cytotoxicity against L6 cells. Pyrethrin II (1) was the most selective antiplasmodial compound, with a selectivity index of 24.
authors.affiliation: Department of Pharmaceutical Sciences, University of Basel, Klingelbergstrasse 50, 4056 Basel, Switzerland.
authors.forename: Yoshie
authors.initials: Y
authors.lastname: Hata
authors.forename: Stefanie
authors.initials: S
authors.lastname: Zimmermann
authors.forename: Melanie
authors.initials: M
authors.lastname: Quitschau
authors.forename: Marcel
authors.initials: M
authors.lastname: Kaiser
authors.forename: Matthias
authors.initials: M
authors.lastname: Hamburger
authors.forename: Michael
authors.initials: M
authors.lastname: Adams
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D011723:Chrysanthemum cinerariifolium / Q000737:chemistry*; D035264:Flowers / Q000737:chemistry*; D032448:Myoblasts, Skeletal / Q000187:drug effects; D010936:Plant Extracts / Q000737:chemistry; D010963:Plasmodium falciparum / Q000187:drug effects; D011722:Pyrethrins / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D016833:Trypanosoma brucei rhodesiense / Q000187:drug effects
chemical_list: D000962:Antimalarials; D000981:Antiprotozoal Agents; D010936:Plant Extracts; D011722:Pyrethrins