%0 Journal Article %9 ACL : Articles dans des revues avec comité de lecture non répertoriées par l'AERES %A Fournet, Alain %A Ferreira, M.E. %A Rojas de Arias, A. %A Torres de Ortiz, S. %A Fuentes, S. %A Nakayama, H. %A Schinini, A. %A Hocquemiller, R. %T In vivo efficacy of oral and intralesional administration of 2-substituted quinolines in experimental treatment of new world cutaneous leishmaniasis caused by Leishmania amazonensis %D 1996 %L fdi:010009661 %G ENG %J Antimicrobial Agents and Chemotherapy %@ 0066-4804 %K LEISHMANIOSE ; TRAITEMENT MEDICAL ; EFFICACITE ; ETUDE EXPERIMENTALE ; PLANTE MEDICINALE ; ANIMAL DE LABORATOIRE %K QUINOLINE ; METHYLGLUCAMINE %N 11 %P 2447-2451 %U https://www.documentation.ird.fr/hor/fdi:010009661 %> https://horizon.documentation.ird.fr/exl-doc/pleins_textes/pleins_textes_6/b_fdi_45-46/010009661.pdf %V 40 %W Horizon (IRD) %X The antileishmanial efficacies of 2-n-propylquinoline, chimanines B and D, 2-n-pentylquinoline, 2-phenylquinoline, 2-(3,4-methylenedioxyphenylethyl)quinoline, and two total alkaloidal extracts of #Galipea longiflora$ were evaluated in BALB/c mice infected with #Leishmania amazonensis$ or #Leishmania venezuelensis$. Animals were treated for 4 to 6 weeks postinfection with a quinoline by the oral route at 50 mg/kg of body weight twice daily for 15 days or by five intralesional injections at intervals of 4 days with a quinoline at 50 mg/kg of body weight. The reference drug, N-methylglucamine antimonate (Glucantime), was administered by subcutaneous or intralesional injection (regimens of 14, 28, or 56 mg of pentavalent antimony per kg of body weight daily). Twice-daily oral treatment with chimanine B at 50 mg/kg resulted in a decrease in lesion weight by 70% (P < 0.001) and a decrease in the parasite loads by 95% (P < 0.001). Five injections of chimanine B at intervals of 4 days reduced the lesion weight by 74% and the parasite loads in the lesion by 90% compared with the values for the group of untreated mice. Subcutaneous administration of N-methylglucamine antimonate at 28 mg of pentavalent antimony kg per day for 15 days reduced the parasite burden by 95% (P < 0.001) and five intralesional injections at the same concentration reduced the parasite burden by 96% (P < 0.001). Other 2-substituted quinolines, 2-n-propylquinoline administered by the oral and intralesional routes, 2-phenylquinoline administered by the oral route, 2-n-pentylquinoline administered by intralesional injection, and two total alkaloidal extracts of #G. longiflora$ administered by the oral route, had intermediate effects. These findings suggest that chimanine B may be chosen as a lead molecule in the development of oral therapy against leishmaniasis. (Résumé d'auteur) %$ 052PHLEIS03 ; 076PLAMED03