College of Pharmacy, Chengdu University of Traditional Chinese Medicine, Wenjiang, Chengdu, 611137, China.
Metabonomics Synergy Innovation Laboratory, School of Medicine and Nursing, Chengdu University, Longquan, Chengdu, 610106, China.
Biomed Pharmacother. 2020 May;125:109955. doi: 10.1016/j.biopha.2020.109955. Epub 2020 Jan 31.
Costunolide (COS) and dehydrocostus lactone (DEH) are two natural sesquiterpene lactones with potential antitcancer activity against a range of cancer cell types both in vitro and in vivo, particularly for breast cancer and leukemia. There are many researches that have been taken to characterize these pathways and to reveal their anticancer mechanisms of action of COS and DEH. However, while there is a great deal of evidence detailing the effects of COS and DEH on considerable signaling pathways and cellular functions, a global view of their mechanism of action remains elusive. This review systematically summarizes the antitumor activity and mechanism of COS and DEH in the recent reports, and discusses the effect of the key active part (α-methylene-γ-butyrolactone) of COS and DEH against cancer. Moreover, we also discuss the antineoplastic activity of COS and DEH derivatives to improve the cytotoxicity and safety index. We believe this review can provide a systemic reference to develop COS and DEH as anticancer agents.
标题:Costunolide(COS)和脱氢木香内酯(DEH):具有抗癌活性的天然倍半萜内酯
摘要:Costunolide (COS) 和 dehydrocostus lactone (DEH) 是两种天然倍半萜内酯,具有体外和体内抗多种癌细胞类型的潜在抗癌活性,特别是对乳腺癌和白血病。已经有许多研究致力于表征这些途径并揭示 COS 和 DEH 的抗癌作用机制。然而,尽管有大量证据详细说明了 COS 和 DEH 对相当多的信号通路和细胞功能的影响,但它们作用机制的全貌仍然难以捉摸。本综述系统总结了 COS 和 DEH 在最近报道中的抗肿瘤活性和机制,并讨论了 COS 和 DEH 的关键活性部分(α-亚甲基-γ-丁内酯)对癌症的影响。此外,我们还讨论了 COS 和 DEH 衍生物的抗肿瘤活性,以提高细胞毒性和安全指数。我们相信,这篇综述可以为开发 COS 和 DEH 作为抗癌药物提供系统的参考。