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DNA/bovine serum albumin binding and cytotoxicity of transition metal ternary complexes based on sulfamethazine and bromazepam drugs
Applied Organometallic Chemistry ( IF 3.7 ) Pub Date : 2020-09-11 , DOI: 10.1002/aoc.5995
Ahmed M. Mansour 1 , Nour T. Abdel‐Ghani 1 , Mona S. Ragab 1
Affiliation  

Similar to the antibiotic mixing strategies, which depend on reducing the worth of diffusion of the resistant bacteria to new host, in this contribution, we explicit new mixed‐ligand complexes of the type [M(SMZ)2(BZM)] (M = Co(II), Ni(II) and Cu(II)) based on two drugs: sulfamethazine (SMZ) and bromazepam (BZM). The novelty aspect of the present work relies on combining two drugs in a single molecule via the synthesis of the ternary complexes. The ternary complexes were characterized by spectroscopic and analytical tools with the aid of the quantum chemical calculations. Copper(II) complex has the highest DNA intrinsic binding constant (2.20 × 105 M−1), induces extensively DNA cleavage compared to the other complexes, and exhibits the highest cytotoxicity (IC50 = 0.67 μM) against human liver cancer cell line (HepG2). Exciting, Cu(II) compound exhibits no toxicity to the nonmalignant human foetal lung fibroblast (WI‐38). Alternatively, the low cytotoxicity of the Co(II) complex correlates well with the high affinity of the compound to human serum albumin (Kb = 4.58 × 105) compared to 1.93 × 105 and 2.14 × 105 M−1 for Ni (II) and Cu (II) complexes, respectively.

中文翻译:

磺胺二甲嘧啶和溴马西m药物对过渡金属三元配合物的DNA /牛血清白蛋白结合及细胞毒性

与抗生素混合策略类似,后者依赖于降低抗药性细菌向新宿主扩散的价值,在此贡献中,我们明确了[M(SMZ)2(BZM)]类型的新混合配体复合物(M =基于以下两种药物的Co(II),Ni(II)和Cu(II):磺胺二甲嘧啶(SMZ)和溴马西epa(BZM)。本工作的新颖性在于通过三元复合物的合成将两种药物结合在一个分子中。通过光谱学和分析工具借助量子化学计算来表征三元配合物。铜(II)配合物具有最高的DNA内部结合常数(2.20×10 5 M -1),与其他复合物相比可广泛诱导DNA切割,并且对人肝癌细胞系(HepG2)表现出最高的细胞毒性(IC 50 = 0.67μM)。令人兴奋的是,Cu(II)化合物对非恶性人类胎儿肺成纤维细胞(WI-38)没有毒性。另外,与Ni的1.93×10 5和2.14×10 5 M -1相比,Co(II)复合物的低细胞毒性与该化合物对人血清白蛋白的高亲和力密切相关(K b = 4.58×10 5)。 (II)和Cu(II)配合物。
更新日期:2020-11-06
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