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有机锡(IV)修饰的石墨烯量子点作为分子成像和三阴性乳腺癌治疗的双重平台。

Organotin(IV)-Decorated Graphene Quantum Dots as Dual Platform for Molecular Imaging and Treatment of Triple Negative Breast Cancer.

机构信息

Department of Condensed Matter Physics, Faculty of Science, Masaryk University, Kotlářská 2, 61137, Brno, Czech Republic.

Centro Interdisciplinar de Química e Bioloxía (CICA), Universidade da Coruña, Rúa as Carballeiras, 15071 A, Coruña, Spain.

出版信息

Chemistry. 2023 Oct 26;29(60):e202301845. doi: 10.1002/chem.202301845. Epub 2023 Sep 18.

Abstract

The pharmacological activity of organotin(IV) complexes in cancer therapy is well recognized but their large applicability is hampered by their poor water solubility. Hence, carbon dots, in particular nitrogen-doped graphene quantum dots (NGQDs), may be a promising alternative for the efficient delivery of organotin(IV) compounds as they have a substantial aqueous solubility, a good chemical stability, and non-toxicity as well as a bright photoluminescence that make them ideal for theranostic applications against cancer. Two different multifunctional nanosystems have been synthesized and fully characterized based on two fragments of organotin-based cytotoxic compounds and 4-formylbenzoic acid (FBA), covalently grafted onto the NGQDs surface. Subsequently, an in vitro determination of the therapeutic and theranostic potential of the achieved multifunctional systems was carried out. The results showed a high cytotoxic potential of the NGQDs-FBA-Sn materials against breast cancer cell line (MDA-MB-231) and a lower effect on a non-cancer cell line (kidney cells, HEK293T). Besides, thanks to their optical properties, the dots enabled their fluorescence molecular imaging in the cytoplasmatic region of the cells pointing towards a successful cellular uptake and a release of the metallodrug inside cancer cells (NGQDs-FBA-Sn).

摘要

有机锡(IV)配合物在癌症治疗中的药理活性已得到广泛认可,但由于其水溶性差,其应用受到限制。因此,碳点(特别是氮掺杂石墨烯量子点(NGQDs))可能是高效传递有机锡(IV)化合物的有前途的替代品,因为它们具有较大的水溶性、良好的化学稳定性和低毒性以及明亮的光致发光性,使其成为癌症治疗诊断应用的理想选择。基于两种不同的片段,合成了两种基于有机锡的细胞毒性化合物和 4-甲酰苯甲酸(FBA),并将其共价接枝到 NGQDs 表面,合成了两种不同的多功能纳米系统,并对其进行了全面表征。随后,对所得到的多功能系统的治疗和治疗潜力进行了体外测定。结果表明,NGQDs-FBA-Sn 材料对乳腺癌细胞系(MDA-MB-231)具有很高的细胞毒性,对非癌细胞系(肾细胞,HEK293T)的影响较小。此外,由于其光学特性,这些点能够在细胞的细胞质区域进行荧光分子成像,表明成功地摄取了细胞,并将金属药物释放到癌细胞内(NGQDs-FBA-Sn)。

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