Xiao Chen, Li Jiayuan, Wang Xing, Li Shiyou, Xu Chen, Zhang Zhijie, Hua Ao, Ding Ze-Yang, Zhang Bi-Xiang, Yang Xiangliang, Li Zifu
National Engineering Research Center for Nanomedicine, College of Life Science and Technology, Huazhong University of Science and Technology, Wuhan 430074, PR China.
Hepatic Surgery Center and Hubei Key Laboratory of Hepato-Pancreatic-Biliary Diseases, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, PR China.
J Control Release. 2023 Apr;356:288-305. doi: 10.1016/j.jconrel.2023.02.043. Epub 2023 Mar 8.
Cancer stem cells (CSCs) have been recognized as the culprit for tumor progression, treatment resistance, metastasis, and recurrence while redox homeostasis represents the Achilles' Heel of CSCs. However, few drugs or formulations that are capable of elevating oxidative stress have achieved clinical success for eliminating CSCs. Here, we report hydroxyethyl starch stabilized copper-diethyldithiocarbamate nanoparticles (CuET@HES NPs), which conspicuously suppress CSCs not only in vitro but also in numerous tumor models in vivo. Furthermore, CuET@HES NPs effectively inhibit CSCs in fresh tumor tissues surgically excised from hepatocellular carcinoma patients. Mechanistically, we uncover that hydroxyethyl starch stabilized copper-diethyldithiocarbamate nanocrystals via copper‑oxygen coordination interactions, thereby promoting copper-diethyldithiocarbamate colloidal stability, cellular uptake, intracellular reactive oxygen species production, and CSCs apoptosis. As all components are widely used in clinics, CuET@HES NPs represent promising treatments for CSCs-rich solid malignancies and hold great clinical translational potentials. This study has critical implications for design of CSCs targeting nanomedicines.
癌症干细胞(CSCs)被认为是肿瘤进展、治疗耐药、转移和复发的罪魁祸首,而氧化还原稳态是癌症干细胞的致命弱点。然而,很少有能够提高氧化应激的药物或制剂在消除癌症干细胞方面取得临床成功。在此,我们报道了羟乙基淀粉稳定的二乙基二硫代氨基甲酸铜纳米颗粒(CuET@HES NPs),其不仅在体外,而且在多种体内肿瘤模型中均能显著抑制癌症干细胞。此外,CuET@HES NPs能有效抑制从肝细胞癌患者手术切除的新鲜肿瘤组织中的癌症干细胞。从机制上讲,我们发现羟乙基淀粉通过铜 - 氧配位相互作用稳定二乙基二硫代氨基甲酸铜纳米晶体,从而促进二乙基二硫代氨基甲酸铜的胶体稳定性、细胞摄取、细胞内活性氧生成以及癌症干细胞凋亡。由于所有成分都在临床上广泛使用,CuET@HES NPs代表了针对富含癌症干细胞的实体恶性肿瘤的有前景的治疗方法,并具有巨大的临床转化潜力。这项研究对靶向癌症干细胞的纳米药物设计具有关键意义。