Synthesis, characterization and biological studies of a cobalt(III) complex of sulfathiazole

被引:10
作者
Pontoriero, Ana [1 ]
Mosconi, Natalia [1 ]
Monti, Laura [1 ]
Bellu, Sebastian [1 ]
Williams, Patricia A. M. [2 ]
Raimondi, Marcela [3 ]
Lima, Beatriz [4 ]
Egly Feresin, Gabriela [4 ]
Nerli, Bibiana [1 ]
Rizzotto, Marcela [1 ]
机构
[1] Univ Nacl Rosario, Fac Ciencias Bioquim & Farmaceut, CONICET, Inst Quim Rosario IQUIR, Suipacha 531, RA-2000 Rosario, Santa Fe, Argentina
[2] Univ Nacl La Plata, Fac Ciencias Exactas, Dept Quim, Ctr Quim Inorgan CEQUINOR,CONICET, 47 & 115 CC 962,B1900AVV, RA-1900 La Plata, Buenos Aires, Argentina
[3] Univ Nacl Rosario, Fac Cs Med, Area Microbiol, Santa Fe 3100, RA-2000 Rosario, Santa Fe, Argentina
[4] UNSJ, IBT, Ave Libertador Gral,San Martin 1109, Oeste, San Juan, Argentina
关键词
Sulfadrug metal complex; BSA; Antimicrobial properties; Ames test; Allium test; SCHIFF-BASE COMPLEXES; BOVINE SERUM-ALBUMIN; ANTIMICROBIAL ACTIVITY; CRYSTAL-STRUCTURE; PSEUDOMONAS-AERUGINOSA; ANTIBACTERIAL ACTIVITY; CO(III) COMPLEXES; METAL-COMPLEXES; X-RAY; LIGANDS;
D O I
10.1016/j.cbi.2017.10.004
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The emergence of old and new antibiotic resistance created in the last decades revealed a substantial medical need for new classes of antimicrobial agents. The antimicrobial activity of sulfa drugs is often enhanced by complexation with metal ions, which is in concordance with the well-known importance of metal ions in biological systems. Besides, sulfonamides and its derivatives constitute an important class of drugs, with several types of pharmacological agents possessing antibacterial, anti-carbonic anhydrase, diuretic, hypoglycemic, antithyroid, antiviral and anticancer activities, among others. The purpose of this work has been the obtainment, characterization and determination of biological properties (antibacterial, antifungal, mutagenicity and phytotoxicity) of a new Co(III)-sulfathiazole complex: Costz, besides of its interaction with bovine serum albumin (BSA). The reaction between sodium sulfathiazole (Nastz) and cobalt(II) chloride in the presence of H2O2 leads to a brown solid, [CoIII(stz) 2OH(H2O)(3)], (Costz). The structure of this compound has been examined by means of elemental analyses, FT-IR, H-1 NMR, UV-Visible spectrometric methods and thermal studies. The Co(III) ion, which exhibits a distorted octahedral environment, could coordinate with the N thiazolic atom of sulfathiazolate. The complex quenched partially the native fluorescence of bovine serum albumin (BSA), suggesting a specific interaction with the protein. The Costz complex showed, in vitro, a moderate antifungal activity against Aspergillus fumigatus and A. flavus. As antibacterial, Costz displayed, in vitro, enhanced activity respective to the ligand against Pseudomonas aeruginosa. Costz did not show mutagenic properties with the Ames test. In the Allium cepa test the complex showed cytotoxic properties but not genotoxic ones. These results may be auspicious, however, further biological studies are needed to consider the complex Costz as a possible drug in the future.
引用
收藏
页码:152 / 161
页数:10
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