Quercetin Phytosome® as a potential drug for Covid-19.

F. Di Pierro, Amjad Khan, A. Bertuccioli, P. Maffioli, G. Derosa, Saeed Khan, B. Khan, Roohi Nigar, I. Ujjan, Bikha R Devraian
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引用次数: 8

Abstract

When looking for new antiviral compounds aimed to counteract the COVID-19, a disease caused by the recently identified novel coronavirus (SARS-CoV-2), the knowledge of the main viral proteins is fundamental. The major druggable targets of SARS-CoV-2 include 3-chymotrypsin-like protease (3CLpro), papain-like protease (PLpro), RNA-dependent 26 RNA polymerase, and spike (S) protein. Molecular docking studies have highlighted that quercetin, a natural polyphenol belonging to the flavonol class, inhibits 3CLpro, PLpro and S proteins. Biophysical technics have then very recently confirmed that quercetin is reasonably a potent inhibitor of 3CLpro. The likely antiviral properties of quercetin are anyway challenged by its very poor oral bioavailability profile and any attempt to overcome this limit should be welcome. A phospholipid complex of quercetin (Quercetin Phytosome®) has been recently tested in humans to evaluate a possible improvement in oral bioavailability. After hydrolysis of the conjugated form (mainly glucuronide) of quercetin found in human plasma, the pharmacokinetics results have demonstrated an increased bioavailability rate by about 20-fold for total quercetin. It has been also observed that the presence of specific glucuronidase could yield free systemic quercetin in human body. Taking also into considerations its anti-inflammatory and thrombin-inhibitory actions, a bioavailable form of quercetin, like Quercetin Phytosome®, should be considered a possible candidate to clinically face COVID-19.
槲皮素光敏体®作为Covid-19的潜在药物。
COVID-19是一种由最近发现的新型冠状病毒(SARS-CoV-2)引起的疾病,在寻找旨在对抗COVID-19的新型抗病毒化合物时,了解主要病毒蛋白是至关重要的。SARS-CoV-2的主要药物靶点包括3-凝糜蛋白酶样蛋白酶(3CLpro)、木瓜蛋白酶样蛋白酶(PLpro)、RNA依赖性26 RNA聚合酶和刺突(S)蛋白。分子对接研究表明,槲皮素是一种天然多酚,属于黄酮醇类,可抑制3CLpro、PLpro和S蛋白。生物物理技术最近证实槲皮素是一种有效的3CLpro抑制剂。槲皮素可能的抗病毒特性无论如何都受到其非常差的口服生物利用度的挑战,任何克服这一限制的尝试都应该受到欢迎。槲皮素的磷脂复合物(槲皮素光敏体®)最近在人体中进行了测试,以评估其可能改善口服生物利用度。在水解人血浆中槲皮素的共轭形式(主要是葡萄糖醛酸)后,药代动力学结果表明,总槲皮素的生物利用度提高了约20倍。研究还发现,特定葡糖苷酶的存在可在人体内产生游离的全身性槲皮素。考虑到槲皮素的抗炎和凝血酶抑制作用,槲皮素的一种生物可利用形式,如槲皮素光敏体®,应被视为临床应对COVID-19的可能候选物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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