Mbikay Majambu, Chrétien Michel
Functional Endoproteolysis Laboratory, Montreal Clinical Research Institute, Montreal, QC, Canada.
Front Pharmacol. 2022 Mar 2;13:830205. doi: 10.3389/fphar.2022.830205. eCollection 2022.
Isoquercetin and quercetin are secondary metabolites found in a variety of plants, including edible ones. Isoquercetin is a monoglycosylated derivative of quercetin. When ingested, isoquercetin accumulates more than quercetin in the intestinal mucosa where it is converted to quercetin; the latter is absorbed into enterocytes, transported to the liver, released in circulation, and distributed to tissues, mostly as metabolic conjugates. Physiologically, isoquercetin and quercetin exhibit antioxidant, anti-inflammatory, immuno-modulatory, and anticoagulant activities. Generally isoquercetin is less active than quercetin and , whereas it is equally or more active , suggesting that it is primarily a more absorbable precursor to quercetin, providing more favorable pharmacokinetics to the latter. Isoquercetin, like quercetin, has shown broad-spectrum antiviral activities, significantly reducing cell infection by influenza, Zika, Ebola, dengue viruses among others. This ability, together with their other physiological properties and their safety profile, has led to the proposition that administration of these flavonols could prevent infection by severe acute respiratory syndrome-coronavirus-2 (SARS-CoV-2), or arrest the progression to severity and lethality of resulting coronavirus disease of 2019 (Covid-19). screening of small molecules for binding affinity to proteins involved SARS-CoV-2 life cycle has repeatedly situated quercetin and isoquercetin near to top of the list of likely effectors. If experiments in cells and animals confirm these predictions, this will provide additional justifications for the conduct of clinical trials to evaluate the prophylactic and therapeutic efficacy of these flavonols in Covid-19.
异槲皮素和槲皮素是在包括可食用植物在内的多种植物中发现的次生代谢产物。异槲皮素是槲皮素的单糖基化衍生物。摄入后,异槲皮素在肠黏膜中的积累量比槲皮素多,在肠黏膜中它会转化为槲皮素;后者被吸收进入肠细胞,运输到肝脏,释放到循环系统中,并分布到组织中,主要以代谢共轭物的形式存在。在生理上,异槲皮素和槲皮素具有抗氧化、抗炎、免疫调节和抗凝活性。一般来说,异槲皮素的活性比槲皮素低 ,而在 方面它具有同等活性或更高活性 ,这表明它主要是槲皮素更易吸收的前体,为后者提供了更有利的药代动力学。与槲皮素一样,异槲皮素也具有广谱抗病毒活性,能显著减少流感病毒、寨卡病毒、埃博拉病毒、登革热病毒等对细胞的感染。这种能力,连同它们的其他生理特性和安全性,使得人们提出,服用这些黄酮醇可以预防严重急性呼吸综合征冠状病毒 2(SARS-CoV-2)感染,或阻止由此导致的 2019 冠状病毒病(Covid-19)发展为重症和致死性疾病。对与 SARS-CoV-2 生命周期相关蛋白质具有结合亲和力的小分子进行筛选,结果多次表明槲皮素和异槲皮素几乎位于可能的效应物名单前列。如果细胞和动物实验证实这些预测,这将为开展临床试验以评估这些黄酮醇在 Covid-19 中的预防和治疗效果提供更多依据。