鱼藤素及其衍生物的研究进展  

Research progress of deguelin and its derivatives

作　　者：郑骏意 缪迎羚 李明慧 叶颖丹 吴沅欣 李启鑫 夏诗咏 孙明娜 ZHENG Junyi;MIAO Yingling;LI Minghui;YE Yingdan;WU Yuanxin;LI Qixin;XIA Shiyong;SUN Mingna(Key Laboratory of Molecular Target&Clinical Pharmacology and the State Key Laboratory of Respiratory Disease,School of Pharmaceutical Sciences,Guangzhou Medical University,Guangzhou 511436,China;The Affiliated Traditional Chinese Medicine Hospital,Guangzhou Medical University,Guangzhou 511000,China)

机构地区：[1]广州医科大学药学院广东省分子靶标与临床药理学重点实验室/呼吸疾病国家重点实验室,广东广州511436 [2]广州医科大学附属中医医院,广东广州510000

出　　处：《沈阳药科大学学报》2025年第1期10-25,共16页Journal of Shenyang Pharmaceutical University

基　　金：广州医科大学科研能力提升项目(02-410-2405014);广州医科大学大学生科研创新能力提升项目(02-408-240603029);国家自然科学基金青年项目(32101105);广州医科大学2023年学科建设项目(02-445-2301196XM);广州医科大学2023—2024年度大学生科技创新项目(2022A113);2023年广东省级大学生创新创业训练计划(S202310570077,S202310570078)。

摘　　要：鱼藤素是大量存在于豆科植物中的一种鱼藤酮类化合物,具有多种生物学活性,如杀虫、抗肿瘤、抗炎、抗病毒、抗糖尿病神经病变以及抗骨质疏松等。然而,高剂量的鱼藤素可导致呼吸抑制、心脏毒性和神经传导阻断等剂量相关的不良影响,这推动了负载鱼藤素的新制剂和鱼藤素结构修饰类似物的不断发展。本文通过检索SciFinder、Web of science、PubMed、CNKI等数据库中已发表的关于鱼藤素及其衍生物的相关文献资料,对鱼藤素的来源、生物活性、毒性、及其衍生物的研究进展,特别是针对其抗肿瘤活性的结构修饰与优化研究进行了综述,经分析和归纳总结发现针对鱼藤素的结构修饰主要集中于B、C、E环骨架和A环上的取代基,其目的主要是提高抗肿瘤活性并降低毒性,所得衍生物多数是作为Hsp90 C端抑制剂而表现出优良的抗肿瘤活性。本综述研究将为后续基于鱼藤素的生物活性研究和新药研发,特别是关于鱼藤素及其衍生物在抗肿瘤领域的深入研究和探索提供一定的借鉴和参考。Deguelin is a kind of rotenone compound,existing in a large number of leguminous plants.Plenty of experiments have suggested that deguelin has a variety of biological activities,such as insecticidal,anti-tumor,anti-inflammatory,antiviral,anti-diabetic neuropathy,and anti-osteoporosis.However,high doses of deguelin could lead to adverse effects such as respiratory depression,cardiotoxicity,and nerve conduction blockade,which has driven the continuous development of new formulations loaded with deguelin and its structural modification.This article reviewed the literatures on deguelin and its derivatives published in databases such as SciFinder,Web of Science,PubMed,and CNKI,covering the sources,biological activities,toxicity of deguelin,and the research progress of its derivatives,with a focus on the structural modifications and optimization for their antitumor activities.Through analysis and summarization,it was found that structural modifications of deguelin mainly focused on the B,C,and E ring skeletons and the substituents on the A ring.The aim was primarily to enhance antitumor activity and reduce toxicity and the resulting derivatives were mostly excellent antitumor agents acting as Hsp90 C-terminal inhibitors.This review study might provide a certain reference and guidance for subsequent research on the biological activities of deguelin and the development of new drugs,especially for in-depth research and exploration of deguelin and its derivatives in the field of antitumor therapy.

关 键 词：鱼藤素 衍生物 生物活性 抗肿瘤 天然分子 

分 类 号：R914[医药卫生—药物化学]