随着癌症的日益普遍以及合成药物的有毒副作用，天然产物正在被作为有希望的治疗方法进行开发。葛根皂苷是一种天然存在的三萜类类固醇皂苷，具有多种治疗活性。它作为主要化合物从不同的薯蓣属植物中提取得到。本综述旨在总结有关葛根皂苷的抗癌活性研究进展，重点关注其潜在的细胞和分子机制，以及其药代动力学特征。数据收集自2023年5月1日之前各种可靠和可信的文献，包括PubMed、Springer Link、Scopus、Wiley Online、Web of Science、ScienceDirect和Google学术。研究结果表明，葛根皂苷通过多种分子机制展示了有希望的抗癌效果，包括抗炎作用、细胞凋亡、氧化应激的诱导、细胞毒性、基因毒性的诱导、细胞周期阻滞、抗增殖作用、自噬、糖酵解的抑制和癌细胞迁移的阻断。此外，本综述还强调了葛根皂苷的药代动力学特征，表明其口服生物利用度较低。总结而言，可提出葛根皂苷可能作为一个有希望的化疗药物。然而，进一步广泛的临床研究被推荐以确定其在癌症治疗中的安全性、疗效和治疗潜力。© 2023 Wiley-VCH GmbH.

With the increasing prevalence of cancer and the toxic side effects of synthetic drugs, natural products are being developed as promising therapeutic approaches. Gracillin is a naturally occurring triterpenoid steroidal saponin with several therapeutic activities. It is obtained as a major compound from different Dioscorea species. This review was designated to summarize the research progress on the anti-cancer activities of gracillin focusing on the underlying cellular and molecular mechanisms, as well as its pharmacokinetic features. The data were collected (up to date as of May 1, 2023) from various reliable and authentic literatures comprising PubMed, Springer Link, Scopus, Wiley Online, Web of Science, ScienceDirect, and Google Scholar. The findings demonstrated that gracillin displays promising anticancer effects through various molecular mechanisms, including anti-inflammatory effects, apoptotic cell death, induction of oxidative stress, cytotoxicity, induction of genotoxicity, cell cycle arrest, anti-proliferative effect, autophagy, inhibition of glycolysis, and blocking of cancer cell migration. Additionally, this review highlighted the pharmacokinetic features of gracillin, indicating its lower oral bioavailability. As a conclusion, it can be proposed that gracillin could serve as a hopeful chemotherapeutic agent. However, further extensive clinical research is recommended to establish its safety, efficacy, and therapeutic potential in cancer treatment.© 2023 Wiley-VCH GmbH.