Jiang Wenjie, Zeng Jing, Guo Li, Shi Jianyou, Lei Yang
Department of Pharmacy, Personalized Drug Therapy Key Laboratory of Sichuan Province, Sichuan Academy of Medical Science and Sichuan Provincial People's Hospital, School of Medicine, University of Electronic Science and Technology of China, Chengdu, China.
School of Food and Bioengineering, Xihua University, Chengdu, Sichuan, China.
Front Pharmacol. 2025 Jun 26;16:1571452. doi: 10.3389/fphar.2025.1571452. eCollection 2025.
Deguelin is a natural isoflavone derived from the rotenone family, commonly found in plants belonging to the Derris and Grifola genera. Comprehensive research has underscored its considerable promise in oncological treatment. Deguelin demonstrates anticancer activity by suppressing cell proliferation and promoting apoptosis the modulation of critical signaling pathways, such as NF-κB, Wnt, and AMPK pathways. Moreover, deguelin demonstrates several biological activities, including cell cycle arrest, autophagy modulation, anti-angiogenic and anti-metastatic capabilities, along with antioxidant and anti-inflammatory actions. Notwithstanding these encouraging benefits, the practical utilization of deguelin has been impeded by its volatility, possible neurotoxicity, and other detrimental consequences. This review initially examines the antitumor biological actions of deguelin, incorporating recent discoveries regarding its methods of action. It subsequently consolidates studies on structural alterations intended to enhance the efficacy of deguelin while mitigating its toxicity, and offers a summary of the structure-activity connections of its derivatives. The review seeks to further research on deguelin and guide the development of more efficacious derivatives for prospective clinical applications. This study seeks to establish a robust basis for the advancement of deguelin as a potential chemopreventive agent for cancer.
鱼藤素是一种源自鱼藤酮家族的天然异黄酮，常见于鱼藤属和云芝属植物中。全面研究强调了其在肿瘤治疗方面的巨大潜力。鱼藤素通过抑制细胞增殖、促进凋亡以及调节关键信号通路（如NF-κB、Wnt和AMPK通路）来展现抗癌活性。此外，鱼藤素还具有多种生物学活性，包括细胞周期阻滞、自噬调节、抗血管生成和抗转移能力，以及抗氧化和抗炎作用。尽管有这些令人鼓舞的益处，但鱼藤素的挥发性、可能的神经毒性和其他有害后果阻碍了其实际应用。本综述首先研究鱼藤素的抗肿瘤生物学作用，纳入其作用机制的最新发现。随后汇总旨在提高鱼藤素疗效同时减轻其毒性的结构改造研究，并总结其衍生物的构效关系。本综述旨在推动对鱼藤素的进一步研究，并指导开发更有效的衍生物以供未来临床应用。本研究旨在为将鱼藤素发展成为一种潜在的癌症化学预防剂奠定坚实基础。
