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Self-assembly and self-delivery of the pure nanodrug dihydroartemisinin for tumor therapy and mechanism analysis
Biomaterials Science ( IF 5.8 ) Pub Date : 2023-01-31 , DOI: 10.1039/d2bm01949c Yawei Li 1 , Wei Zhang 1 , Naiyuan Shi 1 , Wenqing Li 1 , Junxia Bi 1 , Xianmin Feng 1 , Nianqiu Shi 1 , Wenhe Zhu 1 , Zhigang Xie 2
Biomaterials Science ( IF 5.8 ) Pub Date : 2023-01-31 , DOI: 10.1039/d2bm01949c Yawei Li 1 , Wei Zhang 1 , Naiyuan Shi 1 , Wenqing Li 1 , Junxia Bi 1 , Xianmin Feng 1 , Nianqiu Shi 1 , Wenhe Zhu 1 , Zhigang Xie 2
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Dihydroartemisinin (DHA), a plant-derived natural product, has recently been proven to be an effective therapeutic agent for cancer treatment. Nevertheless, the poor water solubility and low bioavailability of DHA seriously impede its clinical applications. Herein, a simple and green strategy based on the self-assembly of DHA was developed to synthesize carrier-free nanoparticles (NPs). The resulting nanodrug (DHA NPs) was formed by the self-assembly of DHA molecules via hydrogen bonding and hydrophobic interactions. The DHA NPs exhibited a near-spherical morphology with narrow size distribution, favorable drug encapsulation efficiency (>92%), excellent stability, and on-demand drug release behavior. Furthermore, the in vitro and in vivo experiments revealed that the DHA NPs exhibited significantly higher therapeutic efficacy than the DHA equivalent. In addition, we further explored the potential molecular mechanism of the DHA NPs by utilizing RNA-seq technology and western blotting analysis, which demonstrated that the p53 signaling pathway plays a crucial part in the process of inhibiting tumor cell growth and inducing apoptosis. This work not only reveals the rationale for developing pure nanodrugs via the self-assembly of natural small molecules for oncotherapy but also the investigation of the antitumor mechanism and provides novel theoretical support for the clinical usage of DHA.
中文翻译：
用于肿瘤治疗的纯纳米药物双氢青蒿素的自组装和自递送及其机制分析
双氢青蒿素 (DHA) 是一种源自植物的天然产物，最近已被证明是一种有效的癌症治疗剂。然而，DHA水溶性差、生物利用度低等问题严重阻碍了其临床应用。在此，开发了一种基于 DHA 自组装的简单绿色策略来合成无载体纳米粒子 (NPs)。由此产生的纳米药物 (DHA NPs) 是由 DHA 分子通过氢键和疏水相互作用自组装形成的。DHA NPs 表现出近球形形态，粒径分布窄，药物包封率良好（>92%），稳定性好，药物释放行为按需。此外，体外和体内实验表明，DHA NPs 的治疗效果明显高于 DHA 等效物。此外，我们利用RNA-seq技术和western blotting分析进一步探索了DHA NPs的潜在分子机制，证明p53信号通路在抑制肿瘤细胞生长和诱导细胞凋亡的过程中起着至关重要的作用。这项工作不仅揭示了通过天然小分子自组装开发用于肿瘤治疗的纯纳米药物的基本原理，还揭示了抗肿瘤机制的研究，并为 DHA 的临床应用提供了新的理论支持。
更新日期：2023-01-31
中文翻译：
用于肿瘤治疗的纯纳米药物双氢青蒿素的自组装和自递送及其机制分析
双氢青蒿素 (DHA) 是一种源自植物的天然产物，最近已被证明是一种有效的癌症治疗剂。然而，DHA水溶性差、生物利用度低等问题严重阻碍了其临床应用。在此，开发了一种基于 DHA 自组装的简单绿色策略来合成无载体纳米粒子 (NPs)。由此产生的纳米药物 (DHA NPs) 是由 DHA 分子通过氢键和疏水相互作用自组装形成的。DHA NPs 表现出近球形形态，粒径分布窄，药物包封率良好（>92%），稳定性好，药物释放行为按需。此外，体外和体内实验表明，DHA NPs 的治疗效果明显高于 DHA 等效物。此外，我们利用RNA-seq技术和western blotting分析进一步探索了DHA NPs的潜在分子机制，证明p53信号通路在抑制肿瘤细胞生长和诱导细胞凋亡的过程中起着至关重要的作用。这项工作不仅揭示了通过天然小分子自组装开发用于肿瘤治疗的纯纳米药物的基本原理，还揭示了抗肿瘤机制的研究，并为 DHA 的临床应用提供了新的理论支持。
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