The activity of 2-substituted quinoline alkaloids in BALB/c mice infected with Leishmanis donovani
Fecha
1994Autor
Fournet, A
Gantier, JC
Gautheret, A
Leysalles, L
Munos, MH
Mayrargue, J
Moskowitz, H
Cavé, A
Hocquemiller, R
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Abstract.
Potent antileishmanial activity has recently been described in vivo when certain 2-substituted quinoline alkaloids are administered to mice with cutaneous leishmaniasis. We now report the ahtileishmanial activity of four 2-substituted quinoline alkaloids, namely chimanine D or 2-(1',2'-trans-epoxypropyl) quinoline (I). 2-n- propylquinoline (II), 2-styrylquinoline (III) and 2-(2'-hydroxypropyl) quinoline (IV), for experimental treatment of visceral leishmaniasis in infected BALB/c mice. Subcutaneous treatment with chimanine D for 10 days at 0-54 mmol/kg per day resulted in 86.6% parasite suppression in the liver. Oral administration of 0-54 mmol/kg of 2-n-propylquinoline once daily for 5 or 10 days to L. donovani-nfected mice suppressed parasite burdens in liver by 87.8 and 99.9%. respectively. Cutaneous administration of meglumine antimonate for 10 days resulted in 97.4% parasite suppression in the liver. This study is, to our knowledge, the first to demonstrate the activity of 2-substituted quinoline alkaloids in experimental treatment of visceral leishmaniasis. Further biological and chemical studies of these products might yet prove helpful for the development of new antileishmanial drugs.