In vitro anti-leishmania evaluation of nickel complexes with a triazolopyrimidine derivative against Leishmania infantum and Leishmania braziliensis

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• 作者：Inmaculada Ram&iacute ; rez-Mac&iacute ; as^a ; Carmen R. Maldonado^b ; ¹ ; ^{carmen.r.maldonado@ed.ac.uk} ; ^{quimicarmen@ugr.es} ; Clotilde Mar&iacute ; n^a ; Francisco Olmo^a ; Ramó ; n Gutié ; rrez-Sá ; nchez^c ; Mar&iacute ; a J. Rosales^a ; Miguel Quiró ; s^b ; Juan M. Salas^b ; Manuel Sá ; nchez-Moreno^a ; ^{msanchem@ugr.es}
• 关键词：Nickel complexes ; H-bonds ; Triazolopyrimidines ; Leishmania infantum ; Leishmania braziliensis ; Biological activity
• 刊名：Journal of Inorganic Biochemistry
• 出版年：2012
• 期刊代码：53_01620134
• 类别：ch
• 出版时间：July, 2012
• 卷：112
• 期：Complete
• 页码：1-9
• 文件大小：1956 K

摘要

Studies on the anti-proliferative activity in vitro of seven ternary nickel (II) complexes with a triazolopyrimidine derivative and different aliphatic or aromatic amines as auxiliary ligands against promastigote and amastigote forms of Leishmania infantum and Leishmania braziliensis have been carried out. These compounds are not toxic for the host cells and two of them are effective at lower concentrations than the reference drug used in the present study (Glucantime). In general, the in vitro growth rate of Leishmania spp. was reduced, its capacity to infect cells was negatively affected and the multiplication of the amastigotes decreased. Ultrastructural analysis and metabolism excretion studies were executed in order to propose a possible mechanism for the action of the assayed compounds. Our results show that the potential mechanism is at the level of organelles membranes, either by direct action on the microtubules or by their disorganization, leading to vacuolization, degradation and ultimately cell death.