Antileishmanial activity of ruthenium(II)tetraammine nitrosyl complexes

被引：45

作者：

Melo Pereira, Jose Clayston ^{[1
]}

Carregaro, Vanessa ^{[2
]}

Costa, Diego Luis ^{[2
]}

da Silva, Joao Santana ^{[2
]}

Cunha, Fernando Q. ^{[3
]}

Franco, Douglas Wagner ^{[1
]}

机构：

[1] Univ Sao Paulo, Dept Quim & Fis Mol, Inst Quim Sao Carlos, Sao Carlos, SP, Brazil

[2] Univ Sao Paulo, Fac Med Ribeirao Preto, Dept Bioquim & Imunol, Ribeirao Preto, SP, Brazil

[3] Univ Sao Paulo, Fac Med Ribeirao Preto, Dept Farmacol, Ribeirao Preto, SP, Brazil

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 09期

基金：

巴西圣保罗研究基金会;

关键词：

Nitric oxide; Ruthenium complexes; Nitroxyl; Leishmania major; NITRIC-OXIDE; NITROXYL HNO; NO; TOXICITY; REACTIVITY; CHEMISTRY; CYTOTOXICITY; ASSAY;

D O I：

10.1016/j.ejmech.2010.06.010

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The complexes trans-[Ru(NO)(NH3)(4)L](X)(3) (X = BF4-, PF6- or Cl- and L = N-heterocyclic ligands, P (OEt)(3), SO3-2), and [Ru(NO)Hedta)] were shown to exhibit IC50pro in the range of 36 (L = imN) to 5000 mu M (L = imC). The inhibitory effects of trans-[Ru(NO)(NH3)(4)imN](BF4)(3) and of the Angeli's salt on the growth of the intramacrophage amastigote form studied were found to be similar while the trans-[Ru(NH3)(4)imN(H2O)](2+) complex was found not to exhibit any substantial antiamastigote effect. The trans-[Ru(NO)(NH3)(4)imN](BF4)(3) compound, administered (500 nmol kg(-1) day(-1)) in BALB/c mice infected with Leishmania major, was found to exhibit a 98% inhibition on the parasite growth. Furthermore, this complex proved to be at least 66 times more efficient than glucantime in in vivo experiments. (C) 2010 Elsevier Masson SAS. All rights reserved.

引用

页码：4180 / 4187

页数：8

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