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Cytotoxicity and DNA/BSA binding ability of copper(II) complexes with dimethylbithiazole

机译:铜(II)与二甲基噻唑配合物的细胞毒性和DNA / BSA结合能力

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The interaction of two copper(II) complexes [Cu(dmbt)(2)NO3](NO3) and [CuCl(dmbt)(mu-Cl)](2) with calf-thymus DNA has been explored by using absorption, emission, and thermal denaturation. Both complexes illustrate high interaction ability with calf-thymus DNA, with intrinsic binding constants K (b) of 1.7 x 10(5) and 1.4 x 10(5) M-1 at 298 K, respectively, which is in the range of those found for typical classical intercalators. The intermolecular interaction between Cu complexes and bovine serum albumin (BSA) under imitated physiological conditions was investigated using UV-Vis and fluorescence. Tryptophan quenching experiment showed that both complexes bind BSA strongly, with dynamic quenching constants of 1.16 x 10(5) M-1 s(-1) and 1.64 x 10(5) M-1 s(-1), respectively, at 298 K, and a single class of binding site for the complexes on BSA. Both Cu complexes were also used for in vitro cytotoxicity evaluation against four cultures, NIH-3T3, Caco-2, HT-29, and T47D by MTT assay. Interestingly, nitrate contained complex illustrated no toxicity on normal cell line (NIH-3T3), with twice antitumor activity against colon carcinoma (HT-29), comparing with cisplatin.
机译:利用吸收,发射研究了两种铜(II)配合物[Cu(dmbt)(2)NO3](NO3)和[CuCl(dmbt)(mu-Cl)](2)与小牛胸腺DNA的相互作用。以及热变性。两种复合物均显示出与小牛胸腺DNA的高相互作用能力,在298 K时的固有结合常数K(b)分别为1.7 x 10(5)和1.4 x 10(5)M-1。适用于典型的经典嵌入剂。利用紫外-可见光和荧光技术研究了铜复合物与牛血清白蛋白(BSA)在模拟生理条件下的分子间相互作用。色氨酸猝灭实验表明,两种复合物均能牢固结合BSA,在298的动态猝灭常数分别为1.16 x 10(5)M-1 s(-1)和1.64 x 10(5)M-1 s(-1)。 K,以及BSA上复合物的一类结合位点。两种铜配合物还用于通过MTT分析针对四种培养物NIH-3T3,Caco-2,HT-29和T47D进行体外细胞毒性评估。有趣的是,硝酸盐所含的复合物对正常细胞系(NIH-3T3)无毒,与顺铂相比对结肠癌(HT-29)具有两倍的抗肿瘤活性。

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