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Esculetin: A review of its pharmacology and pharmacokinetics
Phytotherapy Research ( IF 6.1 ) Pub Date : 2021-11-22 , DOI: 10.1002/ptr.7311
Linlin Zhang 1 , Qingxuan Xie 1 , Xiaofang Li 1
Affiliation  

Esculetin is a natural dihydroxy coumarin; it is mainly extracted from twig skin and the trunk bark of the Chinese herbal medicine Fraxinus rhynchophylla Hance. Emerging evidence suggests that esculetin has a wide range of pharmacological activities. Based on its fundamental properties, including antioxidant, antiinflammatory, antiapoptotic, anticancer, antidiabetic, neuroprotective, and cardiovascular protective activities, as well as antibacterial activity, among others, esculetin is expected to be a therapeutic drug for specific disease indications, such as cancer, diabetes, atherosclerosis, Alzheimer's disease (AD), Parkinson's disease (PD), nonalcoholic fatty liver disease (NAFLD), and other diseases. The oral bioavailability of esculetin was shown by studies to be low. The extensive glucuronidation was described to be the main metabolic pathway of esculetin and C-7 phenolic hydroxyl to be its major metabolic site. With the development of scientific research technology, the pharmacological effects of esculetin are identified and its potential for the treatment of diseases is demonstrated. The underlining mechanisms of action and biological activities as well as the pharmacokinetic data of the analyzed compound reported so far are highlighted in this review with the aim of becoming a proven, and applicable insight and reference for further studies on the utilization of esculetin.

中文翻译:

Esculetin:药理学和药代动力学综述

Esculetin 是一种天然二羟基香豆素;主要从中草药白蜡树的枝皮和树干皮中提取。汉斯。新出现的证据表明,七叶苷具有广泛的药理活性。基于其基本特性,包括抗氧化、抗炎、抗凋亡、抗癌、抗糖尿病、神经保护和心血管保护活性,以及​​抗菌活性等,预计七叶苷将成为特定疾病适应症的治疗药物,如癌症、糖尿病、动脉粥样硬化、阿尔茨海默病 (AD)、帕金森病 (PD)、非酒精性脂肪肝 (NAFLD) 和其他疾病。研究表明七叶树苷的口服生物利用度很低。广泛的葡萄糖醛酸化被描述为七叶苷的主要代谢途径,C-7酚羟基是其主要代谢位点。随着科研技术的发展,确定了 esculetin 的药理作用,并证明了其治疗疾病的潜力。本综述重点介绍了迄今为止报告的分析化合物的作用机制和生物活性以及药代动力学数据,旨在为进一步研究七叶苷的利用提供经过验证的、适用的见解和参考。
更新日期:2022-01-21
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