Towards Water Soluble Mitochondria-Targeting Theranostic Osmium(II) Triazole-Based Complexes.
Towards Water Soluble Mitochondria-Targeting Theranostic Osmium(II) Triazole-Based Complexes.
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DOI：
10.3390/molecules21101382
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发表时间：
2016-10-18
期刊：
影响因子：
--
通讯作者：
Elliott PI
中科院分区：
文献类型：
--
作者：
Omar SA;Scattergood PA;McKenzie LK;Bryant HE;Weinstein JA;Elliott PI
合成并表征了配合物[Os（btzpy）2][PF 6]2（1，btzpy = 2，6-bis（1-phenyl-1，2，3-triazol-4-yl）pyridine）.配合物1表现出磷光（λem = 595 nm，τ = 937 ns，φem = 9.3%，在脱气乙腈中），与其已知的钌（II）类似物形成对比，其在室温下不发光。该络合物经历显着的氧依赖性淬灭的发射与脱气和充气乙腈溶液之间的发光强度降低43倍，表明其潜在的单线态氧敏化剂。配合物1进行对位复分解，得到[Os（btzpy）2] Cl 2（1Cl），其显示出与1的那些几乎相同的光学吸收和发射光谱。在空气平衡的乙腈溶液中，直接测定了~ 1Cl敏化的单线态氧产率（φ（~ 1 O ~ 2）= 57%）。在这些生物物理性质的基础上，进行了初步的细胞摄取和发光显微成像研究。复合物1Cl容易进入癌细胞系HeLa和U2 OS，观察到线粒体染色和强烈发射，允许在低至1 μM的浓度下成像。长期毒性结果表明，在HeLa细胞中毒性较低，LD 50>100 μM。因此，基于1的锇（II）配合物为开发具有抗癌活性的新型治疗诊断剂提供了一个很好的平台。
The complex [Os(btzpy)2][PF6]2 (1, btzpy = 2,6-bis(1-phenyl-1,2,3-triazol-4-yl)pyridine) has been prepared and characterised. Complex 1 exhibits phosphorescence (λem = 595 nm, τ = 937 ns, φem = 9.3% in degassed acetonitrile) in contrast to its known ruthenium(II) analogue, which is non-emissive at room temperature. The complex undergoes significant oxygen-dependent quenching of emission with a 43-fold reduction in luminescence intensity between degassed and aerated acetonitrile solutions, indicating its potential to act as a singlet oxygen sensitiser. Complex 1 underwent counterion metathesis to yield [Os(btzpy)2]Cl2 (1Cl), which shows near identical optical absorption and emission spectra to those of 1. Direct measurement of the yield of singlet oxygen sensitised by 1Cl was carried out (φ (1O2) = 57%) for air equilibrated acetonitrile solutions. On the basis of these photophysical properties, preliminary cellular uptake and luminescence microscopy imaging studies were conducted. Complex 1Cl readily entered the cancer cell lines HeLa and U2OS with mitochondrial staining seen and intense emission allowing for imaging at concentrations as low as 1 μM. Long-term toxicity results indicate low toxicity in HeLa cells with LD50 >100 μM. Osmium(II) complexes based on 1 therefore present an excellent platform for the development of novel theranostic agents for anticancer activity.
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影响因子：
20.6
作者：
Baggaley, Elizabeth;Weinstein, Julia A.;Williams, J. A. Gareth
通讯作者：
Williams, J. A. Gareth
影响因子：
1.8
作者：
Costa, Ruben D.;Orti, Enrique;Bolink, Henk J.
通讯作者：
Bolink, Henk J.
影响因子：
4.6
作者：
Fortage, Jerome;Dupeyre, Gregory;Campagna, Sebastiano
通讯作者：
Campagna, Sebastiano
影响因子：
4.4
作者：
BECKE, AD
通讯作者：
BECKE, AD
DOI：
10.1007/bf01114537
发表时间：
1990-04-01
期刊：
THEORETICA CHIMICA ACTA
影响因子：
--
作者：
ANDRAE, D;HAUSSERMANN, U;PREUSS, H
通讯作者：
PREUSS, H