Evaluation of the Trypanocidal, Cytotoxic and Genotoxic Activity of Styrylquinoline Analogs

被引：4
|
作者：
Garcia, P. [1 ]
Genes, C. [1 ]
Molano, P. [2 ]
Torres, O. [2 ]
Saez, J. [3 ]
Triana, O. [1 ]
机构：
[1] Univ Antioquia, Grp Biol & Control Enfermedades Infecciosas, Medellin, Colombia
[2] Univ Cordoba, Dept Quim, Monteria, Colombia
[3] Univ Antioquia, Inst Quim, Lab Quim Plantas Colombianas, Medellin, Colombia
来源：
JOURNAL OF CHEMOTHERAPY | 2010年 / 22卷 / 03期
关键词：
Trypanosoma cruzi; styrylquinolines; sensitivity; toxicity; genetic variation; TRYPANOSOMA-CRUZI; CHAGAS-DISEASE; COMET ASSAY; IN-VITRO; 2-SUBSTITUTED QUINOLINES; DNA-DAMAGE; PLANT; ANTIPROTOZOAL; STRAINS; DRUGS;
D O I：
10.1179/joc.2010.22.3.169
中图分类号：
R73 [肿瘤学];
学科分类号：
100214 ;
摘要：
Styrylquinolines isolated from Galipea longiflora have shown leishmanicidal, trypanocidal, nematocidal and antimalarial activity. Here, we propose to use analogs of these styrylquinolines to enhance the activity against Trypanosoma cruzi. Three compounds in a reduced and oxidized state were synthesized, and the activity against epimastigotes and trypomastigotes was evaluated. In addition, the cytotoxic activity and genotoxic effect were also determined. The results indicated that epimastigotes from different T. cruzi I stocks were highly sensitive to the three compounds. The PQM4 compound presented promising activity against trypomastigotes and low cytotoxic and genotoxic effects. Finally, we observed that the double-bond reduction of the lateral chain of the three carbons made on these compounds improved the activity and substantially diminished the toxicity of the compounds.
引用
收藏
页码：169 / 174
页数：6
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