College of Chinese Medicine, Weifang Medical University, Weifang, China.
College of First Clinical Medicine, Shandong University of Traditional Chinese Medicine, Jinan 250022, China.
Biomed Pharmacother. 2023 Dec;168:115707. doi: 10.1016/j.biopha.2023.115707. Epub 2023 Oct 18.
In Chinese medicine, the Cucurbitaceae family contains many compounds known as cucurbitacins, which have been categorized into 12 classes ranging from A to T and more than 200 derivatives. Cucurbitacins are a class of highly oxidized tetracyclic triterpenoids with potent anticancer properties. The eight components of cucurbitacins with the strongest anticancer activity are cucurbitacins B, D, E, I, IIa, L-glucoside, Q, and R. Cucurbitacins have also been reported to suppress JAK-STAT 3, mTOR, VEGFR, Wnt/β-catenin, and MAPK signaling pathways, all of which are crucial for the survival and demise of cancer cells. In this paper, we review the progress in research on cucurbitacin-induced apoptosis, autophagy, cytoskeleton disruption, cell cycle arrest, inhibition of cell proliferation, inhibition of invasion and migration, inhibition of angiogenesis, epigenetic alterations, and synergistic anticancer effects in tumor cells. Recent studies have identified cucurbitacins as promising molecules for therapeutic innovation with broad versatility in immune response. Thus, cucurbitacin is a promising class of anticancer agents that can be used alone or in combination with chemotherapy and radiotherapy for the treatment of many types of cancer.Therefore, based on the research reports in the past five years at home and abroad, we further summarize and review the structural characteristics, chemical and biological activities, and studies of cucurbitacins based on the previous studies to provide a reference for further development and utilization of cucurbitacins.
在中医药中，葫芦科植物含有许多被称为葫芦素的化合物，这些化合物已被分为从 A 到 T 的 12 类，并有 200 多种衍生物。葫芦素是一类高度氧化的四环三萜类化合物，具有很强的抗癌特性。具有最强抗癌活性的葫芦素的八个成分是葫芦素 B、D、E、I、IIa、L-葡糖苷、Q 和 R。据报道，葫芦素还能抑制 JAK-STAT3、mTOR、VEGFR、Wnt/β-catenin 和 MAPK 信号通路，所有这些信号通路对癌细胞的存活和死亡都至关重要。在本文中，我们综述了葫芦素诱导细胞凋亡、自噬、细胞骨架破坏、细胞周期停滞、抑制细胞增殖、抑制侵袭和迁移、抑制血管生成、表观遗传改变以及在肿瘤细胞中协同抗癌作用的研究进展。最近的研究表明，葫芦素作为治疗创新的有前途的分子，在免疫反应中具有广泛的多功能性。因此，葫芦素是一类很有前途的抗癌药物，可以单独使用或与化疗和放疗联合用于治疗多种类型的癌症。因此，基于国内外过去五年的研究报告，我们进一步总结和综述了葫芦素的结构特征、化学和生物活性以及研究情况，为进一步开发和利用葫芦素提供参考。
