Wan Jiafeng, Xu Shiqing, Li Jing, Yu Mengliu, Zhang Kai, Wei Gang, Su Zhiqiang
State Key Laboratory of Chemical Resource Engineering, Beijing Key Laboratory of Advanced Functional Polymer Composites, Beijing University of Chemical Technology, 100029 Beijing, China.
Dental Medical Center, China-Japan Friendship Hospital, Beijing 100029, China.
Nanoscale. 2022 Aug 11;14(31):11359-11368. doi: 10.1039/d2nr03321f.
Drug-derived carbon dots (CDs) not only have excellent photoluminescence properties of CDs, but also maintain pharmacological effects of original drugs, so as to realize extended applications for both bioimaging and chemotherapy. In this work, metformin (Met)-derived CDs (Met-CDs) as multifunctional nanocarriers with tumor cell imaging and cancer therapy are synthesized using Met and citric acid as precursors. The created Met-CDs exhibit obvious resistance to photobleaching, significant pH sensitivity in acidic environments, good pH stability in alkaline environments, and high temperature sensitivity. In addition, we further investigate the biological activity of Met-CDs using diabetic cell models, which demonstrate the ability of Met-CDs to treat diabetes and reduce the production of reactive oxygen species in diseased cells. Subsequently, human alveolar adenocarcinoma basal epithelial cells (A549) are cultured in both normal glucose and low glucose media, and different concentrations of Met and Met-CDs are added to investigate the effect of Met-CDs on A549 cells. Finally, we successfully utilize the prepared Met-CDs to image live A549 cells in normal glucose medium. The Met-CDs prepared in this work reveal high potential to be used as both fluorescent probes and drug agents for tumor therapy, realizing controllable integrated diagnosis and treatment of diseases.
药物衍生的碳点（CDs）不仅具有碳点优异的光致发光特性，还保留了原药物的药理作用，从而实现了生物成像和化疗的扩展应用。在这项工作中，以二甲双胍（Met）和柠檬酸为前体，合成了具有肿瘤细胞成像和癌症治疗功能的多功能纳米载体——二甲双胍衍生碳点（Met-CDs）。所制备的Met-CDs表现出明显的抗光漂白性能、在酸性环境中显著的pH敏感性、在碱性环境中良好的pH稳定性以及高温敏感性。此外，我们使用糖尿病细胞模型进一步研究了Met-CDs的生物活性，结果表明Met-CDs具有治疗糖尿病和减少病变细胞中活性氧产生的能力。随后，在正常葡萄糖和低葡萄糖培养基中培养人肺泡腺癌基底上皮细胞（A549），并添加不同浓度的Met和Met-CDs，以研究Met-CDs对A549细胞的影响。最后，我们成功利用制备的Met-CDs对正常葡萄糖培养基中的活A549细胞进行成像。这项工作中制备的Met-CDs显示出作为肿瘤治疗的荧光探针和药物制剂的巨大潜力，实现了疾病的可控一体化诊断和治疗。
