THE ACTIVITY OF 2-SUBSTITUTED QUINOLINE ALKALOIDS IN BALB/C MICE INFECTED WITH LEISHMANIA-DONOVANI

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 antileishmanial 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-infected 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. © 1994 The British Society for Antimicrobial Chemotherapy.