Cailotto Simone, Amadio Emanuele, Facchin Manuela, Selva Maurizio, Pontoglio Enrico, Rizzolio Flavio, Riello Pietro, Toffoli Giuseppe, Benedetti Alvise, Perosa Alvise
Department of Molecular Sciences and Nanosystems, Università Ca' Foscari Venezia, Via Torino 155, 30172 Venezia Mestre, Italy.
Experimental and Clinical Pharmacology Unit, C.R.O. National Cancer Institute, 33081 Aviano, Italy.
ACS Med Chem Lett. 2018 Jul 16;9(8):832-837. doi: 10.1021/acsmedchemlett.8b00240. eCollection 2018 Aug 9.
There is the need for reproducible, simple, high-yielding synthetic protocols aimed at obtaining carbon dots (CDs) with controlled fluorescence, photothermal and photochemical behavior, surface properties, biocompatibility, tumor targeting ability, drug absorption biodistribution, and tumor uptake. This Letter describes a systematic study on the effect of glucose, fructose, and ascorbic acid as starting materials for the preparation of highly luminescent CDs, characterized by a blue emission. Their composition and morphology are investigated by titration of OH surface groups, spectroscopic techniques, and high-resolution transmission electron microscopy (HR-TEM), and their toxicity was tested toward HeLa cells. CDs made using fructose were toxic, while those made from glucose and ascorbic acid showed good biocompatibility. The reproducible and simple synthetic procedure yields luminescent biomass-derived CDs for combined cancer therapy and diagnostics. Their doxorubicin (DOX) drug uptake was measured by spectrofluorimetry, indicating a crucial role of the morphologies of the CDs in controlling DOX loading. The glucose derived CDs showed up to 28% w/w of DOX loading.
需要有可重复、简单且高产的合成方案，以获得具有可控荧光、光热和光化学行为、表面性质、生物相容性、肿瘤靶向能力、药物吸收生物分布以及肿瘤摄取的碳点（CDs）。本文描述了一项关于以葡萄糖、果糖和抗坏血酸作为起始原料制备高发光CDs（以蓝色发射为特征）效果的系统研究。通过滴定OH表面基团、光谱技术和高分辨率透射电子显微镜（HR-TEM）研究了它们的组成和形态，并测试了它们对HeLa细胞的毒性。使用果糖制备的CDs具有毒性，而由葡萄糖和抗坏血酸制备的CDs表现出良好的生物相容性。这种可重复且简单的合成方法产生了用于联合癌症治疗和诊断的发光生物质衍生CDs。通过荧光光谱法测量了它们对阿霉素（DOX）的药物摄取，表明CDs的形态在控制DOX负载方面起着关键作用。葡萄糖衍生的CDs显示出高达28% w/w的DOX负载量。
