Supramolecular hybrids of carbon dots and dihydroartemisinin for enhanced anticancer activity and mechanism analysis,Journal of Materials Chemistry B

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Supramolecular hybrids of carbon dots and dihydroartemisinin for enhanced anticancer activity and mechanism analysis
Journal of Materials Chemistry B ( IF 6.1 ) Pub Date : 2020-09-18 , DOI: 10.1039/d0tb01826k
Yawei Li ₁ , Nianqiu Shi ₁ , Wei Zhang ₁ , Hong Zhang ₁ , Yu Song ₁ , Wenhe Zhu ₁ , Xianmin Feng ₁

Affiliation

Dihydroartemisinin (DHA) has been regarded as a potential anticancer agent in recent years. Nevertheless, the clinical applications of DHA are seriously restricted as a result of its intrinsic characteristics, such as poor water solubility, instability, and fast clearance. Herein, a type of fluorescent nanoparticles was successfully fabricated via supramolecular assembling of carbon dots (CDs) and DHA. The formulated CDs–DHA fluorescent nanoparticles not only significantly improve the solubility and stability of DHA, but also possess favorable biocompatibility and pH-dependent drug release behavior. In particular, the hybrids of CDs and DHA as nanocarriers can effectively promote the endocytosis of DHA and exhibit enhanced antitumor effects compared with free DHA in vitro and in vivo. In addition, we also explore the possible action mechanism of CDs–DHA through flow cytometric assay, transfection and western blot analysis. The results indicate that CDs–DHA nanoparticles suppress the progression of hepatic carcinoma through inducing apoptosis and inhibiting glucose metabolism, and the mechanism is related to the downregulation of PKM2 expression and the suppression of the Akt/mTOR signaling pathway, which may provide a potential therapeutic target for hepatic carcinoma treatment. This work emphasizes the great potential of utilizing CDs as a safe and convenient platform to deliver DHA for efficient cancer therapy, and the study on the anticancer mechanism can also offer theoretical support for the clinical application of DHA.

中文翻译：

用于增强抗癌活性和机制分析的碳点和双氢青蒿素的超分子杂化物

近年来，双氢青蒿素（DHA）被认为是一种潜在的抗癌药物。然而，DHA因其水溶性差、不稳定、清除快等固有特性而严重限制了其临床应用。在此，通过碳点 (CD) 和 DHA 的超分子组装成功制造了一种荧光纳米粒子。配制的CDs-DHA荧光纳米粒子不仅显着提高了DHA的溶解性和稳定性，而且具有良好的生物相容性和pH依赖性药物释放行为。特别是，CDs和DHA的杂交体作为纳米载体可以有效地促进DHA的内吞作用，并在体外和体外与游离DHA相比表现出增强的抗肿瘤作用。体内。此外，我们还通过流式细胞术、转染和蛋白质印迹分析探索了 CDs-DHA 的可能作用机制。结果表明，CDs-DHA纳米粒通过诱导细胞凋亡和抑制糖代谢抑制肝癌的进展，其机制与下调PKM2表达和抑制Akt/mTOR信号通路有关，可能提供潜在的治疗作用。肝癌治疗的靶点。这项工作强调了利用CDs作为一种安全便捷的平台来传递DHA进行高效癌症治疗的巨大潜力，抗癌机制的研究也可以为DHA的临床应用提供理论支持。

更新日期：2020-10-07

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