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In vitro and in vivoactivity of series of cationic dinuclearPt(II) complexes
Journal of Inorganic Biochemistry ( IF 3.8 ) Pub Date : 2021-09-23 , DOI: 10.1016/j.jinorgbio.2021.111619
Ivana Vasić 1 , Snežana Rajković 2 , Aleksandar Arsenijević 3 , Marija Milovanović 3 , Nebojša Arsenijević 3 , Jelena Milovanović 4 , Marija D Živković 1
Affiliation  

The antitumour potential of nine dinuclear platinum(II) complexes of the type [{Pt(L)Cl}2(μ-X)]2+(where L represents two NH3 or different bidentantly coordinated diamine ligand - ethylenediamine, en; (±)-1,2-propylenediamine, 1,2-pn; isobutylenediamine, ibn; trans-(±)-1,2-diaminocyclohexane, dach; 1,3-propylenediamine, 1,3-pd; 2,2-dimethyl-1,3-propylenediamine, 2,2-diMe-1,3-pd; (±)-1,3-pentanediamine,1,3-pnd, and X is a bridging pyrazine (pz) or pyridazine (pydz) ligand) were determined by in vitro and in vivo assays using the CT26 cell line and a murine model of heterotopic colon cancer tumour induced in immunocompetent BALB/c mice. This study concludes that complexes Pt1, Pt2 and Pt7 possess significant in vitro cytotoxic activity against mouse colon carcinoma CT26 cells, while all these complexes show moderate apoptotic effect. Complexes Pt1 and Pt7 arrested CT26 cells in G2/M phase of cell cycle, while, evaluated by detection of Ki67 expressing cells, complexes Pt5 and Pt6 exerted the highest antiproliferative effect. Complexes Pt1 and Pt2 exerted significant in vivo antitumour effects. These complexes reduced the growth of primary tumour and the incidence of lung and liver metastases without causing the significant hepato- and nephro- toxicity. Our data indicate considerable antitumour activity of platinum(II) complexes against CT26 cells in vitro and in vivo and imply possible further investigations on their role as potential chemotherapeutic agents.



中文翻译:


系列阳离子双核Pt(II)配合物的体外和体内活性



[{Pt( L )Cl} 2 ( μ -X)] 2+类型的九种双核铂(II)配合物的抗肿瘤潜力(其中L代表两个NH 3或不同的双齿配位二胺配体-乙二胺,en;( ±)-1,2-丙二胺,1,2-pn;异丁二胺,ibn;反式-(±)-1,2-二氨基环己烷,dach;1,3-丙二胺,2,2-二甲基; -1,3-丙二胺,2,2-diMe-1,3-pd;(±)-1,3-戊二胺,1,3-pnd,X是桥联吡嗪(pz)或哒嗪(pydz)配体)通过使用 CT26 细胞系和在免疫活性 BALB/c 小鼠中诱导的异位结肠癌肿瘤小鼠模型进行体外体内测定来确定。本研究得出的结论是,复合物Pt1Pt2Pt7对小鼠结肠癌CT26细胞具有显着的体外细胞毒活性,同时所有这些复合物都显示出中等的细胞凋亡作用。复合物Pt1Pt7将CT26细胞阻滞在细胞周期的G2/M期,而通过检测Ki67表达细胞进行评估,复合物Pt5Pt6发挥了最高的抗增殖作用。复合物Pt1Pt2在体内发挥显着的抗肿瘤作用。这些复合物减少了原发肿瘤的生长以及肺和肝转移的发生率,而不引起显着的肝和肾毒性。 我们的数据表明,铂(II)络合物在体外体内对 CT26 细胞具有相当大的抗肿瘤活性,这意味着可能需要对其作为潜在化疗剂的作用进行进一步研究。

更新日期:2021-09-29
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