Ma Shaofang, Zhang Yan, Zhu Zihan, Wang Deping, Zhou Xin, Wang Jing, Bian Wei, Tang Xinjing
School of Basic Medical Science and Key Laboratory of Cellular Physiology, Shanxi Medical University, Taiyuan 030001, China.
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
Mol Pharm. 2025 Feb 3;22(2):958-971. doi: 10.1021/acs.molpharmaceut.4c01211. Epub 2024 Dec 30.
The low cure rate and high mortality associated with cancer pose significant threats to human health. Photodynamic and photothermal therapies have emerged as promising treatment strategies for various types of cancers. In this study, we successfully synthesized a novel type of carbon dot (CD) using 1,2,4-aminobenzene and ethylenediamine as precursors. Surprisingly, these CDs exhibited outstanding nucleolus-targeting capabilities coupled with a remarkable photothermal effect. Through the integration of these nucleolus-targeting CDs with indocyanine green (ICG) and folic acid (FA), we created CDs-ICG-FA nanocomplexes suitable for combined photodynamic and photothermal therapy. In vitro experiments demonstrated that CDs-ICG-FA maintained a robust photothermal ability, achieving a conversion efficiency of up to 34.3%. Furthermore, CDs-ICG-FA generated abundant reactive oxygen species, effectively inducing cancer cell death and demonstrating its potential for photodynamic therapy. In MCF-7 cancer cells, CDs-ICG-FA exhibited a pronounced synergistic photothermal/photodynamic anticancer effect. Subsequent in vivo experiments in mice revealed that CDs-ICG-FA could selectively accumulate at tumor sites, significantly inhibiting tumor growth upon exposure to an 808 nm laser. These findings suggest that the developed nucleolus-targeting CDs-ICG-FA hold promising potential for cancer targeting and the application of combined photothermal/photodynamic therapy.
癌症的低治愈率和高死亡率对人类健康构成了重大威胁。光动力疗法和光热疗法已成为治疗各类癌症的有前景的治疗策略。在本研究中，我们以1,2,4-氨基苯和乙二胺为前驱体成功合成了一种新型碳点（CD）。令人惊讶的是，这些碳点表现出出色的核仁靶向能力以及显著的光热效应。通过将这些核仁靶向碳点与吲哚菁绿（ICG）和叶酸（FA）整合，我们制备了适用于光动力和光热联合治疗的碳点-ICG-FA纳米复合物。体外实验表明，碳点-ICG-FA保持了强大的光热能力，转换效率高达34.3%。此外，碳点-ICG-FA产生了大量活性氧，有效诱导癌细胞死亡，显示出其光动力治疗的潜力。在MCF-7癌细胞中，碳点-ICG-FA表现出显著的光热/光动力协同抗癌效果。随后在小鼠体内进行的实验表明，碳点-ICG-FA可以选择性地在肿瘤部位积聚，在暴露于808 nm激光时显著抑制肿瘤生长。这些发现表明，所开发的核仁靶向碳点-ICG-FA在癌症靶向以及光热/光动力联合治疗的应用方面具有广阔的前景。
