当前位置: X-MOL 学术J. Inorg. Biochem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Anti-cancer and anti-inflammatory activities of a new family of coordination compounds based on divalent transition metal ions and indazole-3-carboxylic acid
Journal of Inorganic Biochemistry ( IF 3.9 ) Pub Date : 2020-11-11 , DOI: 10.1016/j.jinorgbio.2020.111308
Antonio A García-Valdivia 1 , Fatin Jannus 2 , Amalia García-García 1 , Duane Choquesillo-Lazarte 3 , Belén Fernández 4 , Marta Medina-O'donnell 5 , José A Lupiáñez 2 , Javier Cepeda 6 , Fernando J Reyes-Zurita 2 , Antonio Rodríguez-Diéguez 1
Affiliation  

A new family of mononuclear coordination compounds has been synthetized and characterized: [M(3-ind)2(H2O)2] (M = Co (1), Ni (2), Zn (3), Fe (4), Mn (5); 3-ind = indazole-3-carboxylate). These materials are mononuclear coordination compounds that possess strong hydrogen bond interactions. The anti-inflammatory effects of these compounds were assayed in lipopolysaccharide activated RAW 264.7 macrophages by inhibition of NO production. Moreover, the cytotoxicity of the complexes and the ligand in RAW 264.7 cells were determined for the first time. The most significant results were obtained for the compounds 4 and 5 reaching values of NO inhibition close to 80% at 48 h, and above to 90% at 72 h of treatment. The highest inhibitory effects on NO production were showed at the range 7–23 μg/mL for compounds 4 and 5. As a consequence, compounds 4 and 5 could be potential drugs due to the interesting anti-inflammatory properties showed. The anti-cancer potential of these compounds has been also tested against different tumor cell lines. The cytotoxicity of the ligand and of compounds 2 and 3 were assayed in three cell lines: HT29, colon cancer cells, Hep-G2, hepatoma cells and B16-F10 melanoma cells. The best results have been achieved with compound 2 in HepG2 and B16-F10 cell lines, being between 1.5 and 2 times more effective that the ligand in HepG2 cells, and B16-F10 cells. All in all, indazole-3-carboxylic acid is a promising ligand for the formation of coordination compounds with biochemical properties.



中文翻译:

基于二价过渡金属离子和吲唑-3-羧酸的新型配位化合物家族的抗癌和抗炎活性

合成并表征了一个新的单核配位化合物家族:[M(3-ind) 2 (H 2 O) 2 ] (M = Co ( 1 ), Ni ( 2 ), Zn ( 3 ), Fe ( 4 ) , Mn ( 5 );3-ind = 吲唑-3-羧酸盐)。这些材料是具有强氢键相互作用的单核配位化合物。通过抑制 NO 产生,在脂多糖激活的 RAW 264.7 巨噬细胞中测定了这些化合物的抗炎作用。此外,首次确定了复合物和配体在 RAW 264.7 细胞中的细胞毒性。对于化合物4获得了最显着的结果5达到 NO 抑制值在 48 小时时接近 80%,在处理 72 小时时达到 90% 以上。对于化合物45,在 7–23 μg/mL 范围内显示出对 NO 产生的最高抑制作用。因此,由于显示出有趣的抗炎特性,化合物45可能是潜在的药物。这些化合物的抗癌潜力也已针对不同的肿瘤细胞系进行了测试。在三种细胞系中测定了配体以及化合物23的细胞毒性:HT29、结肠癌细胞、Hep-G2、肝癌细胞和 B16-F10 黑色素瘤细胞。使用化合物2取得了最好的结果在 HepG2 和 B16-F10 细胞系中,比 HepG2 细胞和 B16-F10 细胞中的配体有效 1.5 到 2 倍。总而言之,吲唑-3-羧酸是一种很有前途的配体,可用于形成具有生化特性的配位化合物。

更新日期:2020-11-12
down
wechat
bug