CYTOTOXICITY AND ANTIMICROBIAL ACTIVITY OF MONO-, DI- AND TRINUCLEAR RUTHENIUM(II) POLYPYRIDINE COMPLEXES
CYTOTOXICITY AND ANTIMICROBIAL ACTIVITY OF MONO-, DI- AND TRINUCLEAR RUTHENIUM(II) POLYPYRIDINE COMPLEXES
复制标题
单核、二核和三核钌(II)聚吡啶配合物的细胞毒性和抗菌活性
DOI：
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发表时间：
2015
期刊：
影响因子：
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通讯作者：
Ignacimuthu Savrimuthu
中科院分区：
文献类型：
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作者：
Senthamarai Kannan Balakrishnan;Suresh Kumar Dass;Host Antony David Rajendran;Ignacimuthu Savrimuthu
目的：评价所合成的单核、双核和三核钌多吡啶配合物的体外细胞毒性、抗菌和抗真菌活性。研究方法：用96孔板法筛选了一系列合成的钌（II）配合物R1、R2和R3对HepG2癌细胞系的体外抗增殖活性。采用纸片扩散法进行抗菌活性测定。此外，通过肉汤微量稀释法进行抗真菌剂的测定。结果如下：配合物对HepG2细胞的IC50分别为14.52（R3）、19.53（R2）和22.32 μM（R1），呈剂量依赖性。所有配合物对革兰氏阳性菌（G +）如金黄色葡萄球菌（MRSA）、迟缓真杆菌（Eubacterium lentum）和枯草芽孢杆菌（Bacillus subtilis）均有一定的抑制作用，对革兰氏阴性菌（G ─）产气肠杆菌（Enterobacter aerogenes）有一定的抑制作用，但对解淀粉欧文氏菌（Erwinia amylovora）（MTCC 2760）无抑制作用，并显示出一定的抗真菌活性。结论：从这项研究中，我们可以提出，咪唑部分数量的系统性增加沿着钌（II）多吡啶络合物的共轭π电子系统的扩展云是导致抗增殖活性的原因，该活性以R1 < R2 < R3的顺序对HepG2癌细胞增加。结果表明，配合物对革兰氏阳性菌有较好的抗菌活性，对革兰氏阴性菌的抗菌活性较差或无抗菌活性，对真菌的抗菌活性较弱。
Objectives: To evaluate the in vitro cytotoxicity, antibacterial and antifungal activity of the synthesized mono-, di- and trinuclear ruthenium(II) polypyridine complexes. Methods: A series of synthesized ruthenium(II) complexes, R1, R2 and R3, are screened for in vitro antiproliferative activity against HepG2 cancer cell line using 96-well plate method. An assay of antimicrobial activity was performed by disc diffusion method. In addition an assay of an antifungal was performed by broth micro-dilution method. Results: The cytotoxicity of complexes revealed IC 50 values of 14.52 (R3), 19.53 (R2) and 22.32 μM (R1) against HepG2 cell line in a dose dependent manner. All the complexes inhibited moderately the growth of Gram positive bacteria (G + ) such as Staphylococcus aureus (MRSA), Eubacterium lentum, and Bacillus subtillis , quite meagerly the growth of the Gram negative bacterium (G ─ ), Enterobacter aerogenes, but did not inhibit at all the growth of Erwinia amylovora (MTCC 2760) and showed a slight antifungal activity. Conclusion: From this study, we could suggest that the systematic increase in number of imidazole moiety along with expanding cloud of conjugated π-electron system of ruthenium(II) polypyridine complexes is responsible for the antiproliferative activity which increases in the order, R1 < R2 < R3 against HepG2 cancer cells. Consecutively, the complexes show good antimicrobial activity against Gram positive bacteria, but show poor or no effect against Gram negative bacteria and exhibit a little antifungal activity.