Lehrstuhl für Anorganische Chemie I-Bioanorganische Chemie, Fakultät für Chemie und Biochemie, Ruhr-Universität Bochum, Universitätsstrasse 150, 44801 Bochum, Germany.
Chembiochem. 2011 Feb 11;12(3):371-6. doi: 10.1002/cbic.201000576. Epub 2011 Jan 11.
Organometallic complexes possess great potential for imaging applications in biology, due to their kinetic stability and often favourable intrinsic properties. In this work we present a new class of Re(I) -tricarbonyl complexes with a substituted bis(phenanthridinylmethyl)amine (bpm) ligand. The complex Re(CO)(3) (R-bpm) could be conveniently prepared by microwave synthesis from [Re(CO)(3)(H(2)O)(3) ]Br and a suitably substituted bis(phenanthridinylmethyl)amine (R-bpm). Complex 5, with R=CH(2)-CO(2)-CH(3) , was characterized by a single-crystal X-ray structure. Complex 6 (R=CH(2)-C(6)H(4)-CO(2)H) was used in solid-phase peptide synthesis (SPPS) to label the neurotensin(8-13) (NT) fragment N-terminally. The complexes show luminescence emission with large Stokes shifts (λ(ex) =350 nm, λ(em) =570 nm). Cellular uptake and intracellular localization studies in several cell lines demonstrate the utility of the new Re(CO)(3) (R-bpm) complexes for fluorescence imaging and reveal significant differences between the simple methyl ester 5 and the NT bioconjugate 7.
金属有机配合物由于其动力学稳定性和通常有利的固有特性，在生物学成像应用中具有巨大的潜力。在这项工作中，我们提出了一类新的含有取代的双（菲啶基甲基）胺（bpm）配体的 Re(I) -三羰基配合物。配合物 Re(CO)(3) (R-bpm) 可以通过微波合成从 [Re(CO)(3)(H(2)O)(3) ]Br 和适当取代的双（菲啶基甲基）胺（R-bpm）方便地制备。具有 R=CH(2)-CO(2)-CH(3) 的配合物 5 通过单晶 X 射线结构进行了表征。配合物 6（R=CH(2)-C(6)H(4)-CO(2)H）用于固相肽合成（SPPS）中标记 N 端神经降压素（8-13）（NT）片段。这些配合物表现出具有大斯托克斯位移（λ(ex)=350nm，λ(em)=570nm）的发光发射。在几种细胞系中的细胞摄取和细胞内定位研究表明，新的 Re(CO)(3) (R-bpm) 配合物可用于荧光成像，并揭示了简单甲酯 5 和 NT 生物缀合物 7 之间的显著差异。
