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聚乙二醇化羰基钌配合物的亲水性一氧化碳释放材料

Hydrophilic CO-Releasing Material of PEGlyated Ruthenium Carbonyl Complex.

作者信息

Zhang Xiao, Guo Nan, Yang Shuhong, Khan Huma, Zhang Weiqiang

机构信息

Key Laboratory of Applied Surface and Colloid Chemistry Ministry of Education (MOE), School of Chemistry and Chemical Engineering, Shaanxi Normal University, Xi'an 710062, China.

School of Chemical Engineering, Northwest University, Xi'an 710127, China.

出版信息

Materials (Basel). 2022 May 18;15(10):3597. doi: 10.3390/ma15103597.

Abstract

The poor water-solubility and instability of Ru(II) carbonyl complex hamper the therapeutic application as CO releasing materials (CO-RMs). To enhance the hydrophilicity and bio-utility of CO, a robust Ru(I) carbonyl sawhorse skeleton was grafted with water-soluble PEGylated sidearm. In this case, 12 PEGylated sawhorse Ru(CO) complexes were prepared with satisfactory yields and characterized by IR and H- and C- NMR. X-ray diffraction analysis of CO-RM , and revealed the featured diruthenium sawhorse skeleton and PEGylated axial ligands. The flask-shaking method measures the water-solubility of CO-RMs, indicating that both bridging carboxylate ligands and PEGlyated axial ligands regulate the hydrophilicity of these CO-RMs. Under photolysis conditions, CO-RM - sustainable released therapeutic amounts of CO in the myoglobin assay. The correlation of the CO release kinetics and hydrophilicity of CO-RMs demonstrated that the more hydrophilic CO-RM released CO faster. The biological test found that the low cytotoxic CO-RM showed a specific anticancer activity toward HT-29 tumour cells.

摘要

钌(II)羰基配合物的低水溶性和不稳定性阻碍了其作为一氧化碳释放材料(CO-RMs)的治疗应用。为了提高CO的亲水性和生物利用度,在坚固的钌(I)羰基锯架骨架上接枝了水溶性聚乙二醇化侧链。在此情况下,制备了12种聚乙二醇化锯架钌(CO)配合物,产率令人满意,并通过红外光谱、氢核磁共振和碳核磁共振进行了表征。对CO-RM 、 和 的X射线衍射分析揭示了其特征性的双钌锯架骨架和聚乙二醇化轴向配体。摇瓶法测定了CO-RMs的水溶性,表明桥连羧酸酯配体和聚乙二醇化轴向配体均调节了这些CO-RMs的亲水性。在光解条件下,CO-RM 在肌红蛋白测定中可持续释放治疗量的CO。CO-RMs的CO释放动力学与亲水性之间的相关性表明,亲水性越强的CO-RM释放CO的速度越快。生物学测试发现,低细胞毒性的CO-RM 对HT-29肿瘤细胞具有特异性抗癌活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ccfb/9143562/577e8b5d02b4/materials-15-03597-sch001.jpg

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