In vitro and in vivo antileishmanial efficacy of a new nitrilquinoline against Leishmania donovani
In vitro and in vivo antileishmanial efficacy of a new nitrilquinoline against Leishmania donovani
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DOI：
10.1016/j.biopha.2007.02.001
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发表时间：
2007-02-01
影响因子：
7.5
通讯作者：
Loiseau, P. M.
中科院分区：
文献类型：
--
作者：
Nakayama, H.;Desrivot, J.;Loiseau, P. M.
The in vitro activity of a new analogue of 2-alkenylquinoline (2-nitrilquinoline or NQ) against Leishmania donovani was compared to oral reference drug miltefosine (HePC). IC50 of NQ was found at 38.6 mu M against promastigotes and 2.4 mu M against intramacrophage amastigotes. In vivo evaluation in the L. donovani Balb/c mice model indicated that oral treatments at 12.5 and 25 mg/kg for 10 consecutive days significantly reduced the parasite burden in the liver by 68.9 and 68.5%, respectively. This activity was similar to those of HePC at 7.5 mg/kg for 10 days which reduced the parasite burden in liver by 72.5%. The present study shows the positive contribution of a nitril substitute being added into the alkenyl chain branched at the 2-position of the quinoline ring to the antileishmanial activity. In addition, any apparent toxicological disorder was observed during the experiments. (c) 2007 Elsevier Masson SAS. All rights reserved.
