槲皮素及其代谢物抑制重组人血管紧张素转换酶 2（ACE2）活性。
Quercetin and Its Metabolites Inhibit Recombinant Human Angiotensin-Converting Enzyme 2 (ACE2) Activity.
机构信息
College of Food Science and Engineering, South China University of Technology, Guangzhou 510640, China.
Department of Food Science, University of Wisconsin-Madison, 1605 Linden Drive, Madison, Wisconsin 53706, United States.
出版信息
J Agric Food Chem. 2020 Nov 25;68(47):13982-13989. doi: 10.1021/acs.jafc.0c05064. Epub 2020 Nov 12.
Angiotensin-converting enzyme 2 (ACE2) is a host receptor for severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Inhibiting the interaction between the envelope spike glycoproteins (S-proteins) of SARS-CoV-2 and ACE2 is a potential antiviral therapeutic approach, but little is known about how dietary compounds interact with ACE2. The objective of this study was to determine if flavonoids and other polyphenols with B-ring 3',4'-hydroxylation inhibit recombinant human (rh)ACE2 activity. rhACE2 activity was assessed with the fluorogenic substrate Mca-APK(Dnp). Polyphenols reduced rhACE2 activity by 15-66% at 10 μM. Rutin, quercetin-3--glucoside, tamarixetin, and 3,4-dihydroxyphenylacetic acid inhibited rhACE2 activity by 42-48%. Quercetin was the most potent rhACE2 inhibitor among the polyphenols tested, with an IC of 4.48 μM. Thus, quercetin, its metabolites, and polyphenols with 3',4'-hydroxylation inhibited rhACE2 activity at physiologically relevant concentrations .
血管紧张素转换酶 2（ACE2）是严重急性呼吸系统综合征冠状病毒 2（SARS-CoV-2）的宿主受体。抑制 SARS-CoV-2 包膜刺突糖蛋白（S 蛋白）与 ACE2 之间的相互作用是一种潜在的抗病毒治疗方法，但人们对膳食化合物如何与 ACE2 相互作用知之甚少。本研究旨在确定具有 B 环 3'、4'-羟基化的黄酮类化合物和其他多酚是否抑制重组人（rh）ACE2 活性。rhACE2 活性通过荧光底物 Mca-APK（Dnp）进行评估。多酚在 10 μM 时将 rhACE2 活性降低了 15-66%。芦丁、槲皮素-3-O-葡萄糖苷、柽柳素和 3,4-二羟基苯乙酸抑制 rhACE2 活性 42-48%。在测试的多酚中，槲皮素是最有效的 rhACE2 抑制剂，IC 为 4.48 μM。因此，槲皮素、其代谢物和具有 3'、4'-羟基化的多酚在生理相关浓度下抑制 rhACE2 活性。
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