Otorhinolaryngology Hospital, The First Affiliated Hospital of Zhengzhou University, Zhengzhou, 450052, China; Translational Medicine Center, The First Affiliated Hospital of Zhengzhou University, Zhengzhou, 450052, China.
Department of Chemistry and Biochemistry, University of Maryland, College Park, MD, 20740, USA.
Eur J Med Chem. 2023 Nov 5;259:115704. doi: 10.1016/j.ejmech.2023.115704. Epub 2023 Aug 2.
Limonoids, a class of abundant natural tetracyclic triterpenoids, present diverse biological activity and provide a versatile platform amenable by chemical modifications for clinical use. Among all of the limonoids isolated from natural sources, obacunone, nomilin, and limonin are the primary hub of limonoid-based chemical modification research. To date, more than 800 limonoids analogs have been synthesized, some of which possess promising biological activities. This review not only discusses the synthesis of limonoid derivatives as promising therapeutic candidates and details the pharmacological studies of their underlying mechanisms from 2002 to 2022, but also proposes a preliminary limonoid synthetic structure-activity relationship (SAR) and provides future direction of limonoid derivatization research.
柠檬苦素类化合物是一类丰富的天然四环三萜类化合物，具有多种生物活性，并为临床应用提供了一个化学修饰的多功能平台。在从天然来源分离的所有柠檬苦素中，obacunone、nomilin 和 limonin 是基于柠檬苦素的化学修饰研究的主要核心。迄今为止，已经合成了 800 多种柠檬苦素类似物，其中一些具有有前途的生物活性。本综述不仅讨论了作为有前途的治疗候选物的柠檬苦素衍生物的合成，并详细介绍了其潜在机制的药理学研究，从 2002 年到 2022 年，还提出了初步的柠檬苦素合成结构-活性关系 (SAR)，并为柠檬苦素衍生化研究提供了未来的方向。
