Roymahapatra Gourisannkar, Dinda Joydev, Mishra Anjan, Mahapatra Ambikesh, Hwang Wen-Shu, Mandal Santi M
Central Research Facility, Indian Institute of Technology Kharagpur, Kharagpur, India.
J Cancer Res Ther. 2015 Jan-Mar;11(1):105-13. doi: 10.4103/0973-1482.150416.
To study the cytotoxic potency of self-assembled Ruthenium(II)-NHC complexes with 2,6-di-(N-methylimidazolylidene/benzimidazolylidene)pyrazine ligands.
Ru(II)-N-heterocyclic (Ru-NHC) complexes, Bis-[2,6-di-(N-methylimidazol-2-ylidene)pyrazine]ruthenium(II) hexaflurophosphate (3), Bis-[2,6-di-(N-methylbenzimidazol-2-ylidene)pyrazine]ruthenium(II) hexaflurophosphate (4) have been synthesized from corresponding ligands 2,6-di-(N-methylimidazolium)pyrazine dichloride (1); 2,6-di-(N-methylbenzimidazolium)pyrazine dichloride (2). Complexes were studied to determine their pro-apoptotic activity against HCT15 and Hep2 cell lines, and antimicrobial activity against Pseudomonas aeruginosa, Staphylococcus epidermidis and Candida albicans.
Both, complex 3 and 4, formed a nanosphere structure in aqueous growth medium. Cytotoxicity study revealed that complex 3 was more effective than complex 4. Complexes mainly target cellular DNA and bacterial cell wall.
This is the first report on the formation of nanoball structure of Ru(II)-NHC complexes. Thus, complex 3 provides a new insight to develop antitumor or antimicrobial drug.
研究具有2,6 - 二 -（N - 甲基咪唑亚基/苯并咪唑亚基）吡嗪配体的自组装钌（II）-NHC配合物的细胞毒性效力。
已由相应的配体二氯化2,6 - 二 -（N - 甲基咪唑鎓）吡嗪（1）；二氯化2,6 - 二 -（N - 甲基苯并咪唑鎓）吡嗪（2）合成了钌（II）-N - 杂环（Ru - NHC）配合物双[2,6 - 二 -（N - 甲基咪唑 - 2 - 亚基）吡嗪]钌（II）六氟磷酸盐（3）；双[2,6 - 二 -（N - 甲基苯并咪唑 - 2 - 亚基）吡嗪]钌（II）六氟磷酸盐（4）。研究了这些配合物对HCT15和Hep2细胞系的促凋亡活性以及对铜绿假单胞菌、表皮葡萄球菌和白色念珠菌的抗菌活性。
配合物3和4在水性生长培养基中均形成纳米球结构。细胞毒性研究表明配合物3比配合物4更有效。配合物主要靶向细胞DNA和细菌细胞壁。
这是关于Ru（II）-NHC配合物形成纳米球结构的首次报道。因此，配合物3为开发抗肿瘤或抗菌药物提供了新的见解。
