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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Towards cancer cell-specific phototoxic organometallic rhenium(I) complexes?
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Towards cancer cell-specific phototoxic organometallic rhenium(I) complexes?

机译：面向癌细胞的光毒性有机金属rh（I）配合物？

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Over the recent years, several Re(I) organometallic compounds have been shown to be toxic to various cancer cell lines. However, these compounds lacked sufficient selectivity towards cancer tissues to be used as novel chemotherapeutic agents. In this study, we probe the potential of two known N,N-bis(quinolinoyl) Re(I) tricarbonyl complex derivatives, namely Re(I) tricarbonyl [N,N-bis(quinolin-2-ylmethyl)- amino]-4-butane-1-amine (Re–NH_2) and Re(I) tricarbonyl [N,N-bis(quinolin-2-ylmethyl)amino]-5-valeric acid (Re–COOH), as photodynamic therapy (PDT) photosensitizers. Re–NH_2 and Re–COOH proved to be excellent singlet oxygen generators in a lipophilic environment with quantum yields of about 75%. Furthermore, we envisaged to improve the selectivity of Re–COOH via conjugation to two types of peptides, namely a nuclear localization signal (NLS) and a derivative of the neuropeptide bombesin, to form Re–NLS and Re–Bombesin, respectively. Fluorescent microscopy on cervical cancer cells (HeLa) showed that the conjugation of Re–COOH to NLS significantly enhanced the compound’s accumulation into the cell nucleus and more specifically into its nucleoli. Importantly, in view of PDT applications, the cytotoxicity of the Re complexes and their bioconjugates increased significantly upon light irradiation. In particular, Re–Bombesin was found to be at least 20-fold more toxic after light irradiation. DNA photocleavage studies demonstrated that all compounds damaged DNA via singlet oxygen and, to a minor extent, superoxide production.
机译：近年来，几种Re（I）有机金属化合物已显示出对各种癌细胞系的毒性。但是，这些化合物对癌症组织缺乏足够的选择性以用作新型化学治疗剂。在这项研究中，我们探讨了两种已知的N，N-双（喹啉基）Re（I）三羰基络合物衍生物的潜力，即Re（I）三羰基[N，N-双（quinolin-2-ylmethyl）-氨基]-作为光动力疗法（PDT）的4-丁烷-1-胺（Re–NH_2）和Re（I）三羰基[N，N-双（喹啉-2-基甲基）氨基] -5-戊酸（Re–COOH）光敏剂。在亲脂环境中，Re–NH_2和Re–COOH被证明是极好的单线态氧产生剂，其量子产率约为75％。此外，我们设想通过结合两种类型的肽（分别是核定位信号（NLS）和神经肽蛙皮素的衍生物）来分别形成Re-NLS和Re-Bombesin来提高Re-COOH的选择性。宫颈癌细胞（HeLa）的荧光显微镜显示，Re-COOH与NLS的结合显着增强了该化合物在细胞核中的积累，尤其是在其核仁中的积累。重要的是，鉴于PDT的应用，Re配合物及其生物结合物的细胞毒性在光照射下显着增加。特别是，光照射后，Re-Bombesin的毒性至少增加了20倍。 DNA光裂解研究表明，所有化合物均通过单线态氧破坏DNA，并在较小程度上破坏超氧化物的产生。

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