引言: 青蒿素的衍生物青蒿酸具有抗疟疾作用，并且近年来也被报道具有抗肿瘤活性。然而，其抗肿瘤机制尚不明确。方法: 在本研究中，我们重点研究了青蒿酸通过靶向Hsp90来抑制肿瘤细胞增殖的作用，我们采用免疫沉淀、增殖实验、流式细胞术、免疫印迹法、肿瘤异种移植动物模型和免疫组织化学等方法进行研究。此外，为了研究青蒿酸的抗肿瘤效果，我们使用了青蒿酸包裹的PLGA-PEG纳米颗粒在裸鼠中进行实验。结果: 研究发现，青蒿酸与Hsp90的结合降低了其客体蛋白AKT、ERK、p-AKT、p-ERK和EGFR的表达，从而阻断了淋巴瘤细胞在G0/G1→S阶段的细胞周期，并诱导细胞凋亡。此外，肿瘤异种移植实验结果显示，青蒿酸降低了肿瘤组织中AKT和ERK蛋白的表达，抑制了肿瘤增殖，减小了肿瘤的大小和重量。此外，纳米颗粒封装被证明能增强青蒿酸的抗癌活性。讨论: 因此，我们证实了青蒿酸通过靶向Hsp90来抑制淋巴瘤细胞增殖，我们相信这种化合物具有作为一种新型抗肿瘤药物的开发潜力。版权 © 2023元策，琪，宏阳，彦雯，玉梅，碧娟和君林。

Introduction: Artesunate, a derivative of artemisinin, has anti-malarial effects, and in recent years has also been reported to have anti-tumor activity. However, its anti-tumor mechanisms are not well understood. Methods: In this study, we focused on the targeting of Hsp90 by artesunate to inhibit tumor cell proliferation, which we examined using immunoprecipitation, a proliferation assay, flow cytometry, western blotting, a tumor xenograft animal model, and immunohistochemistry. Furthermore, to examine the tumor-suppressive effects of artesunatein nude mice, we used artesunate-loaded PLGA-PEG nanoparticles. Results: The binding of artesunate to Hsp90 was found to reduce the expression of its client proteins AKT, ERK, p-AKT, p-ERK, and EGFR, thereby blocking the cell cycle at the G0/G1 → S stage in lymphoma cells and inducing apoptosis. In addition, the results of tumor xenograft experiments revealed that artesunate reduced the expression of AKT and ERK proteins in tumor tissues, inhibited tumor proliferation, and reduced tumor size and weight. Furthermore, nanoparticle encapsulation was demonstrated to enhance the anti-cancer activity of artesunate. Discussion: We thus established that artesunate inhibits the proliferation of lymphoma cells by targeting the Hsp90 protein, and we accordingly believe that this compound has potential for development as a novelanti-tumor drug.Copyright © 2023 Yuan-Ce, Qi, Hong-Yang, Yan-Wen, Yu-Mei, Bi-Juan and Jun-Lin.