Determination of the anticancer properties of cis- and trans-diadamanthylcarboxylates of dirhenium(III)

N. Shtemenko, K. Polokhina, A. Golichenko, S. Babiy, A. Shtemenko
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引用次数: 1

Abstract

The aim of the study. The aim of the work was to investigate in vivo anticancer activity of cis- and trans-diadamanthylcarboxylates of dirhenium(III) alone and together with cisplatin in form of nanobins.Materials and methods. Model of tumor growth, Guerin’s carcinoma; intraperitoneal administration of cisplatin, dirhenium(III) compounds in liposomes and of binary liposomes, containing both cytostatics; volumes and final weights of tumors were measured.Results. In vivo antitumor properties of two dirhenium(III) dicarboxylates with 1-adamantanecarboxylic acid moieties as ligands with cis- (I) and trans- (II) orientation of the carboxylic groups around a cluster fragment alone and together with cisplatin were presented; an attempt to understand differences in a possible mechanism of anticancer activity of the substances were undertaken. Antiradical and DNA-binding properties of I and II were the matter of consideration.Conclusions. Cis- and trans- compounds of dirhenium I and II had close antitumor activity in vivo with a little bit superiority of the cis- analog. Mechanisms of anticancer activity of I and II are different and may also include monofunctional adduct formation and subsequent interstrand cross-linking for the II substance, formation of protein-DNA cross-links, etc.
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dihenium (III)顺式和反式二金刚烷基羧酸酯抗癌性能的测定
研究的目的。这项工作的目的是研究单独的dihenium (III)的顺式和反式双金刚烷基羧酸盐以及与纳米形式的顺铂一起的体内抗癌活性。材料和方法。Guerin癌的肿瘤生长模型;腹腔内给药顺铂,含dihenium (III)化合物的脂质体和含有这两种细胞抑制剂的二元脂质体;测量肿瘤的体积和最终重量。以1-金刚烷烷羧酸为配体,羧基在簇片段周围呈顺式(I)和反式(II)取向的两种二羧酸dihenium (III)的体内抗肿瘤性能,并与顺铂一起进行了研究;试图了解这些物质抗癌活性的可能机制的差异。I和II的抗自由基和dna结合特性是需要考虑的问题。I和II的顺式和反式化合物在体内具有相近的抗肿瘤活性,比其顺式类似物略显优势。I和II的抗癌活性机制不同,也可能包括单功能加合物的形成和随后的II物质的链间交联,蛋白质- dna交联的形成等。
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6 weeks
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