Department of Pharmacy, Xiangya Hospital, Central South University, Changsha, China; National Clinical Research Center for Geriatric Disorders, Xiangya Hospital, Central South University, Changsha 42008, China; The Hunan Institute of Pharmacy Practice and Clinical Research, Changsha, China.
Department of Pharmacy, Xiangya Hospital, Central South University, Changsha, China; National Clinical Research Center for Geriatric Disorders, Xiangya Hospital, Central South University, Changsha 42008, China; The Hunan Institute of Pharmacy Practice and Clinical Research, Changsha, China.
Bioorg Med Chem. 2024 Nov 1;113:117895. doi: 10.1016/j.bmc.2024.117895. Epub 2024 Sep 4.
Rhein, as a plant antibiotic, demonstrates a broad spectrum of pharmacological effects. Nevertheless, its limited water solubility, low bioavailability, and potential hepatotoxicity and nephrotoxicity making it difficult to directly become a medicine, thereby imposing significant constraints on its clinical application. In recent decades, extensive researches have been proceeded on the multifaceted structural modifications of rhein, resulting in notable improvements on pharmacological activities and druggabilities. This review offers a comprehensive overview and advanced update on the biological potential and structural-activity relationships (SARs) of various rhein derivatives, delineating the sites of structural modification and corresponding activity trends of rhein derivatives for future.
大黄作为一种植物抗生素，具有广泛的药理作用。然而，其水溶性有限、生物利用度低以及潜在的肝毒性和肾毒性，使其难以直接成为药物，从而对其临床应用造成了重大限制。在过去的几十年中，人们对大黄的多方面结构修饰进行了广泛的研究，从而显著改善了其药理活性和药物可开发性。本文综述了各种大黄衍生物的生物学潜力和结构-活性关系（SARs），全面概述和更新了大黄衍生物的结构修饰部位和相应的活性趋势，为未来的研究提供了参考。
