Gill Martin R, Cecchin Denis, Walker Michael G, Mulla Raminder S, Battaglia Giuseppe, Smythe Carl, Thomas Jim A
Department of Chemistry , University of Sheffield , Sheffield , UK . Email:
Department of Chemistry , University College London , London , UK . Email:
Chem Sci. 2013 Dec 28;4(12):4512-4519. doi: 10.1039/c3sc51725j. Epub 2013 Oct 16.
The characterization and bioactivity of the dinuclear ruthenium(ii) complex [(Ru(DIP))(tpphz)] (DIP = 4,7-diphenyl-1,10-phenanthroline and tpphz = tetrapyrido[3,2-:2',3'-:3'',2''-:2''',3'''-]phenazine) is reported. This new complex is found to be luminescent in acetonitrile, where excitation into MLCT (metal-to-ligand charge-transfer) bands in the visible area of the spectrum ( = 450 nm, = 45 000 M cm) result in red emission ( = 620 nm, = 0.017). Aqueous binding studies indicate that this complex binds to duplex DNA with an affinity of 1.8 × 10 M through a non-classical groove-binding interaction, however, unlike the parent complex [(Ru(phen))(tpphz)] (phen = 1,10-phenanthroline), it also displays an increase in MLCT luminescence on addition of liposomes. Confocal microscopy and TEM studies show that this lipophilic complex targets the endoplasmic reticulum of eukaryotic cells, where it functions as an imaging agent for this organelle, and cytotoxicity studies in human cancer cell lines indicate a comparable potency to the anti-cancer drug cisplatin.
报道了双核钌（II）配合物[(Ru(DIP))(tpphz)]（DIP = 4,7-二苯基-1,10-菲咯啉，tpphz = 四吡啶并[3,2 - :2',3' - :3'',2'' - :2''',3'''-]菲嗪）的表征及生物活性。发现这种新配合物在乙腈中具有发光性，在光谱的可见光区域激发进入MLCT（金属到配体电荷转移）带（λ = 450 nm，ε = 45000 M⁻¹ cm⁻¹）会产生红色发射（λ = 620 nm，ε = 0.017）。水相结合研究表明，该配合物通过非经典的沟槽结合相互作用以1.8×10⁸ M的亲和力与双链DNA结合，然而，与母体配合物[(Ru(phen))(tpphz)]（phen = 1,10 - 菲咯啉）不同的是，加入脂质体后它的MLCT发光也会增强。共聚焦显微镜和透射电子显微镜研究表明，这种亲脂性配合物靶向真核细胞的内质网，在那里它作为该细胞器的成像剂发挥作用，并且在人类癌细胞系中的细胞毒性研究表明其效力与抗癌药物顺铂相当。
