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Evaluation of New Palladium Cages as Potential Delivery Systems for the Anticancer Drug Cisplatin

机译:评价新型钯笼作为抗癌药顺铂的潜在给药系统

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摘要

Self-assembled metallocages are very promising drug-delivery systems among supramolecular complexes. Thus, exo-functionalized Pd2L4 (L=ligand) cages were synthesized and characterized, and the encapsulation of the anticancer drug cisplatin in their cavity has been documented. The antiproliferative effects of the metallocages and their combination with cisplatin were examined in vitro in cancer cell lines, while fluorescence microscopy was used to monitor their uptake. Notably, the hydroxymethyl-functionalized Pd-II cage encapsulating cisplatin showed improved cytotoxic effect against human ovarian cancer cells compared to free cisplatin. The toxicity of Pd2L4 cages was evaluated for the first time ex vivo in healthy rat-liver tissues using the precision cut-tissue slices technology, demonstrating in some cases scarce effects on liver viability. These results further highlight the potential of self-assembled Pd2L4 cages for biological applications.
机译:自组装金属位点是超分子复合物中非常有前途的药物递送系统。因此,合成并表征了外功能化的Pd2L4(L =配体)笼,并已证明抗癌药顺铂在其腔中的包封。在癌细胞系中体外检测了金属定位蛋白及其与顺铂的组合的抗增殖作用,而荧光显微镜用于监测其摄取。值得注意的是,与游离顺铂相比,封装顺铂的羟甲基官能化的Pd-II笼显示出对人卵巢癌细胞的改善的细胞毒性作用。使用精密切割组织切片技术首次在健康的大鼠肝组织中对Pd2L4笼子的毒性进行了体外评估,表明在某些情况下对肝脏生存力的影响很小。这些结果进一步突出了自组装的Pd2L4笼在生物应用中的潜力。

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