Reference : Reversal of Chloroquine and Mefloquine Resistance in Plasmodium Falciparum by the Two Mo...
Scientific journals : Article
Human health sciences : Pharmacy, pharmacology & toxicology
http://hdl.handle.net/2268/13893
Reversal of Chloroquine and Mefloquine Resistance in Plasmodium Falciparum by the Two Monoindole Alkaloids, Icajine and Isoretuline
English
Frederich, Michel mailto [Université de Liège - ULg > Département de pharmacie > Pharmacognosie >]
Hayette, Marie-Pierre mailto [Université de Liège - ULg > > Microbiologie médicale >]
Tits, Monique mailto [Université de Liège - ULg > Département de pharmacie > Phytochimie et phytothérapie >]
De Mol, Patrick mailto [Université de Liège - ULg > Département des sciences biomédicales et précliniques > Microbiologie médicale et virologie médicale]
Angenot, Luc mailto [Université de Liège - ULg > Département de pharmacie > Pharmacognosie >]
Aug-2001
Planta Medica
67
6
523-7
Yes (verified by ORBi)
International
0032-0943
[en] Eight naturally occurring monoindole alkaloids were evaluated in vitro for their ability to inhibit Plasmodium falciparum growth and, in drug combination, to reverse the resistance of a chloroquine-resistant strain of Plasmodium falciparum. None of these indole alkaloids has significant intrinsic antiplasmodial activity (IC(50) > 10 microM or 5 microg/ml). Nevertheless, three alkaloids (icajine, isoretuline and strychnobrasiline) did reverse chloroquine resistance at concentrations between 2.5 and 25 microg/ml (IF of 12.82 for isoretuline on W2 strain). The Interaction Factor (IF) equals 2, < 2, or > 2 for additive, antagonistic or synergistic effects of alkaloids on chloroquine inhibition, respectively. Icajine and isoretuline were also assessed in vitro for their mefloquine potentiating activity on a mefloquine-resistant strain of Plasmodium falciparum. Only icajine proved to be synergistic with mefloquine (IF = 15.38).
http://hdl.handle.net/2268/13893

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