Celastrol: A Review of Useful Strategies Overcoming its Limitation in Anticancer Application.

Celastrol: A Review of Useful Strategies Overcoming its Limitation in Anticancer Application.
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DOI:
10.3389/fphar.2020.558741
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发表时间:
2020
影响因子:
5.6
通讯作者:
Fu C
Fu C
中科院分区:
医学2区
文献类型:
--
作者:
Shi J;Li J;Xu Z;Chen L;Luo R;Zhang C;Gao F;Zhang J;Fu C

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雷公藤红素是雷公藤中的一种天然活性成分,对肝癌、乳腺癌、前列腺癌、多发性骨髓瘤、神经胶质瘤等多种肿瘤具有显著的广谱抗癌活性,但其水稳定性差、生物利用度低、治疗窗窄、副作用大等缺点限制了其临床应用。为了解决这一问题,采取了一些策略来提高雷公藤红素的抗癌功效并减少其副作用。本文综述了雷公藤红素的抗癌功效和给药途径,以及雷公藤红素的联合治疗、结构衍生物和纳米/微系统开发等方面的研究进展。使用雷公藤红素介导的这些策略的具体优势。最后,讨论了该领域面临的挑战和未来的研究方向。为开发天然抗癌化合物用于肿瘤治疗提供参考。
Celastrol, a natural bioactive ingredient derived from Tripterygium wilfordii Hook F, exhibits significant broad-spectrum anticancer activities for the treatment of a variety of cancers including liver cancer, breast cancer, prostate tumor, multiple myeloma, glioma, etc. However, the poor water stability, low bioavailability, narrow therapeutic window, and undesired side effects greatly limit its clinical application. To address this issue, some strategies were employed to improve the anticancer efficacy and reduce the side-effects of celastrol. The present review comprehensively focuses on the various challenges associated with the anticancer efficiency and drug delivery of celastrol, and the useful approaches including combination therapy, structural derivatives and nano/micro-systems development. The specific advantages for the use of celastrol mediated by these strategies are presented. Moreover, the challenges and future research directions are also discussed. Based on this review, it would provide a reference to develop a natural anticancer compound for cancer treatment.
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