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槲皮素对COVID-19的治疗和预防潜力:临床研究、创新组合物及专利文献展望

The Therapeutic and Prophylactic Potential of Quercetin against COVID-19: An Outlook on the Clinical Studies, Inventive Compositions, and Patent Literature.

作者信息

Imran Mohd, Thabet Hamdy Khamees, Alaqel Saleh I, Alzahrani Abdullah R, Abida Abida, Alshammari Mohammed Kanan, Kamal Mehnaz, Diwan Anupama, Asdaq Syed Mohammed Basheeruddin, Alshehri Sultan

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Northern Border University, Rafha 91911, Saudi Arabia.

Department of Chemistry, Faculty of Arts and Science, Northern Border University, Rafha 91911, Saudi Arabia.

出版信息

Antioxidants (Basel). 2022 Apr 29;11(5):876. doi: 10.3390/antiox11050876.

Abstract

Quercetin is a phenolic flavonol compound with established antioxidant, anti-inflammatory, and immuno-stimulant properties. Recent studies demonstrate the potential of quercetin against COVID-19. This article highlighted the prophylactic/therapeutic potential of quercetin against COVID-19 in view of its clinical studies, inventions, and patents. The literature for the subject matter was collected utilizing different databases, including PubMed, Sci-Finder, Espacenet, Patentscope, and USPTO. Clinical studies expose the potential of quercetin monotherapy, and also its combination therapy with other compounds, including zinc, vitamin C, curcumin, vitamin D3, masitinib, hydroxychloroquine, azithromycin, and ivermectin. The patent literature also examines claims that quercetin containing nutraceuticals, pharmaceuticals, and dietary supplements, alone or in combination with other drugs/compounds, including favipiravir, remdesivir, molnupiravir, navitoclax, dasatinib, disulfiram, rucaparib, tamarixin, iota-carrageenan, and various herbal extracts (aloe, poria, rosemary, and sphagnum) has potential for use against COVID-19. The literature reveals that quercetin exhibits anti-COVID-19 activity because of its inhibitory effect on the expression of the human ACE2 receptors and the enzymes of SARS-CoV-2 (MPro, PLPro, and RdRp). The USFDA designated quercetin as a "Generally Recognized as Safe" substance for use in the food and beverage industries. It is also an inexpensive and readily available compound. These facts increase the possibility and foreseeability of making novel and economical drug combinations containing quercetin to prevent/treat COVID-19. Quercetin is an acidic compound and shows metabolic interaction with some antivirals, antibiotics, and anti-inflammatory agents. Therefore, the physicochemical and metabolic drug interactions between quercetin and the combined drugs/compounds must be better understood before developing new compositions.

摘要

槲皮素是一种具有抗氧化、抗炎和免疫刺激特性的酚类黄酮醇化合物。最近的研究表明槲皮素对新冠病毒具有潜在作用。鉴于其临床研究、发明和专利,本文重点介绍了槲皮素对新冠病毒的预防/治疗潜力。利用不同数据库收集了该主题的文献,包括PubMed、Sci-Finder、Espacenet、Patentscope和美国专利商标局数据库。临床研究揭示了槲皮素单一疗法及其与其他化合物联合疗法的潜力,这些化合物包括锌、维生素C、姜黄素、维生素D3、马西替尼、羟氯喹、阿奇霉素和伊维菌素。专利文献还审查了含有槲皮素的营养保健品、药品和膳食补充剂的相关权利要求,这些产品单独或与其他药物/化合物联合使用,包括法匹拉韦、瑞德西韦、莫努匹拉韦、维托克洛克斯、达沙替尼、双硫仑、鲁卡帕尼、他马利新、ι-卡拉胶以及各种草药提取物(芦荟、茯苓、迷迭香和水苔),具有对抗新冠病毒的潜在用途。文献表明,槲皮素由于对人类血管紧张素转换酶2(ACE2)受体以及新冠病毒(M蛋白酶、木瓜蛋白酶样蛋白酶和RNA依赖性RNA聚合酶)的酶表达具有抑制作用,从而展现出抗新冠病毒活性。美国食品药品监督管理局将槲皮素指定为食品和饮料行业中“普遍认为安全”的物质。它也是一种价格低廉且易于获取的化合物。这些事实增加了开发含有槲皮素的新型经济药物组合以预防/治疗新冠病毒的可能性和可预测性。槲皮素是一种酸性化合物,与一些抗病毒药物、抗生素和抗炎药存在代谢相互作用。因此,在开发新组合物之前,必须更好地了解槲皮素与联合使用的药物/化合物之间的物理化学和代谢药物相互作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce87/9137692/22552f897abd/antioxidants-11-00876-g001.jpg

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