一种新型双核配位化合物,设计无氧化损伤和毒理学作用

IF 0.5 4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY
Jamerson da Silva, André Galembeck, Mônica Belian, Wagner Silva, Jandyson Santos, Jacinto Silva Neto, J. Aguiar, T. Gonçalves
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引用次数: 0

摘要

一种新的双核配位化合物,设计无氧化损伤和毒理学效应。本文报道了一种新型双核铂(2+)复合物- [Pt(DACH-κ 2n)µ-(c4h2o2 -κ 40o)Pt(DACH-κ 2n)] -的合成、表征、急性毒性、抗肿瘤活性和组织病理学分析。通过急性毒性试验,可以根据经合组织议定书对铂配合物进行分类。双核复合物归为2类(顺铂- 1类;分析dsDNA与双核配合物的相互作用时,观察到Tm增加,提示双核配合物与dsDNA的相互作用可能是通过链间形式进行的。从接种了埃利希癌的小鼠中提取的肿瘤块的评估显示,顺铂和奥沙利铂的肿瘤抑制率相似,但在统计上不同,双核复合物的情况下更优越。顺铂和奥沙利铂的抑制率分别为41.4%和40.8%,而双核复合物的抑制率为66.3%。组织病理学分析显示,顺铂治疗组出现更明显的组织损伤、中度肝脂肪变性和肾炎。用双核复合物治疗的动物肝脏、脾脏和肾脏均在正常范围内,无组织病变,无转移。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
UM NOVO COMPOSTO DE COORDENAÇÃO DINUCLEAR PROJETADO PARA NÃO APRESENTAR DANOS OXIDATIVOS E EFEITOS TOXICOLÓGICOS
A NEW DINUCLEAR COORDINATION COMPOUND DESIGNED TO HAVE NO OXIDATIVE DAMAGE AND TOXICOLOGICAL EFFECTS. The synthesis, characterization, acute toxicity, antitumor activity, and histopathological analysis of a novel dinuclear platinum(2+) complex − [Pt(DACH-κ2N)µ-(C4H2O6-κ4O)Pt(DACH-κ2N)] − is reported. Through acute toxicity tests, it was possible to place the platinum complexes into categories according to the OECD protocol. The dinuclear complex was classified in category 2 (cisplatin - category 1; and oxaliplatin - category 2). Analyzing the interaction between dsDNA and dinuclear complex was observed an Tm increase, suggesting that the dinuclear complex-dsDNA interact probably through of the interstrand form. Evaluations of tumor masses extracted from mice inoculated with Ehrlich carcinoma demonstrated a percent of tumor inhibition similar for cisplatin and oxaliplatin, but statistically different and superior for the case of the dinuclear complex. Cisplatin and oxaliplatin showed 41.4 and 40.8% inhibition, respectively, while the dinuclear complex presented 66.3%. The histopathological analysis demonstrated that the group treated with cisplatin showed more significant tissue damage, moderate hepatic steatosis, and nephritis. The livers, spleens, and kidneys of the animals treated with the dinuclear complex were within the normality range with no tissue lesions, and absence of metastasis.
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来源期刊
Quimica Nova
Quimica Nova 化学-化学综合
CiteScore
1.60
自引率
12.50%
发文量
72
审稿时长
2-4 weeks
期刊介绍: Química Nova publishes in portuguese, spanish and english, original research articles, revisions, technical notes and articles about education in chemistry. All the manuscripts submitted to QN are evaluated by, at least, two reviewers (from Brazil and abroad) of recognized expertise in the field of chemistry involved in the manuscript. The Editorial Council can be eventually asked to review manuscripts. Editors are responsible for the final edition of QN.
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