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基于苯并咪唑/2,2'-联吡啶的双核三元过渡金属配合物的DNA/溶菌酶结合倾向及核酸酶特性

DNA/lysozyme binding propensity and nuclease properties of benzimidazole/2,2'-bipyridine based binuclear ternary transition metal complexes.

作者信息

Mansour Ahmed M, Ragab Mona S

机构信息

Department of Chemistry, Faculty of Science, Cairo University Gamma Street, Giza Cairo 12613 Egypt

出版信息

RSC Adv. 2019 Sep 30;9(53):30879-30887. doi: 10.1039/c9ra07188a. eCollection 2019 Sep 26.

Abstract

In the present contribution, new binuclear ternary complexes; M(bpy)L (M = Co(ii) (1) and Ni(ii) (2); bpy = 2,2'-bipyridine; L = 1,1'-(hexane-1,6-diyl)bis[2-(pyridin-2-yl)1-benzimidazole] and Cu(bpy)(OH)L (3) were synthesized, characterized and screened for their antimicrobial activity and cytotoxicity against human liver carcinoma cells (HepG-2) as well as non-malignant human embryonic kidney cells (HEK-293). The structural studies were complemented by density functional theory (DFT) calculations. DNA binding of 1-3 was spectrophotometrically studied. The DNA cleavage ability of 1-3 towards the supercoiled plasmid DNA (pBR322 DNA) was examined through gel electrophoresis. Compound 3 has the highest cytotoxic activity (IC = 3.5 μg mL) against HepG-2 among the investigated complexes and is non cytotoxic to noncancerous HEK-293. Complexes (1 and 2) exhibited toxicity to HEK-293 with IC values of 30.3 and 23.5 μg mL in that order. While compound 1 showed antifungal activity against , complex 2 exhibited its toxicity against .

摘要

在本论文中,合成了新型双核三元配合物;M(bpy)L(M = Co(ii)(1)和Ni(ii)(2);bpy = 2,2'-联吡啶;L = 1,1'-(己烷-1,6-二基)双[2-(吡啶-2-基)-1-苯并咪唑])和Cu(bpy)(OH)L(3),对其进行了表征,并筛选了它们对人肝癌细胞(HepG-2)以及非恶性人胚胎肾细胞(HEK-293)的抗菌活性和细胞毒性。通过密度泛函理论(DFT)计算对结构研究进行了补充。用分光光度法研究了1-3与DNA的结合。通过凝胶电泳检测了1-3对超螺旋质粒DNA(pBR322 DNA)的DNA切割能力。在所研究的配合物中,化合物3对HepG-2具有最高的细胞毒性活性(IC = 3.5 μg mL),对非癌性的HEK-293无细胞毒性。配合物(1和2)对HEK-293表现出毒性,IC值分别为30.3和23.5 μg mL。虽然化合物1对……显示出抗真菌活性,但配合物2对……表现出毒性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6abc/9072361/125edd159db6/c9ra07188a-s1.jpg

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