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川陈皮素:对其药理活性、作用机制及毒性的深入了解

Sinensetin: An Insight on Its Pharmacological Activities, Mechanisms of Action and Toxicity.

作者信息

Han Jie Lee, Jantan Ibrahim, Yusoff Syaratul Dalina, Jalil Juriyati, Husain Khairana

机构信息

Drug and Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur, Malaysia.

Institute of Systems Biology, Universiti Kebangsaan Malaysia, Bangi, Malaysia.

出版信息

Front Pharmacol. 2021 Jan 20;11:553404. doi: 10.3389/fphar.2020.553404. eCollection 2020.

Abstract

Sinensetin, a plant-derived polymethoxylated flavonoid found in var. and several citrus fruits, has been found to possess strong anticancer activities and a variety of other pharmacological benefits and promising potency in intended activities with minimal toxicity. This review aims to compile an up-to-date reports of published scientific information on sinensetin pharmacological activities, mechanisms of action and toxicity. The present findings about the compound are critically analyzed and its prospect as a lead molecule for drug discovery is highlighted. The databases employed for data collection are mainly through Google Scholar, PubMed, Scopus and Science Direct. and studies showed that sinensetin possessed strong anticancer activities and a wide range of pharmacological activities such as anti-inflammatory, antioxidant, antimicrobial, anti-obesity, anti-dementia and vasorelaxant activities. The studies provided some insights on its several mechanisms of action in cancer and other disease states. However, more detail mechanistic studies are needed to understand its pharmacological effects. More studies in various animal models including toxicity, pharmacokinetic, pharmacodynamic and bioavailability studies are required to assess its efficacy and safety before submission to clinical studies. In this review, an insight on sinensetin pharmacological activities and mechanisms of action serves as a useful resource for a more thorough and comprehensive understanding of sinensetin as a potential lead candidate for drug discovery.

摘要

橙皮素是一种在中药材石蒜和多种柑橘类水果中发现的植物源多甲氧基黄酮,已被发现具有强大的抗癌活性以及多种其他药理益处,并且在预期活性中具有显著效力,毒性极小。本综述旨在汇编有关橙皮素药理活性、作用机制和毒性的已发表科学信息的最新报告。对该化合物的现有研究结果进行了批判性分析,并强调了其作为药物发现先导分子的前景。用于数据收集的数据库主要通过谷歌学术、PubMed、Scopus和科学Direct。多项研究表明,橙皮素具有强大的抗癌活性以及广泛的药理活性,如抗炎、抗氧化、抗菌、抗肥胖、抗痴呆和血管舒张活性。这些研究为其在癌症和其他疾病状态下的多种作用机制提供了一些见解。然而,需要更详细的机制研究来了解其药理作用。在提交临床研究之前,需要在各种动物模型中进行更多研究,包括毒性、药代动力学、药效学和生物利用度研究,以评估其疗效和安全性。在本综述中,对橙皮素药理活性和作用机制的深入了解为更全面、深入地理解橙皮素作为药物发现潜在先导候选物提供了有用的资源。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d34f/7898666/b076da04841e/fphar-11-553404-g001.jpg

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