Quercetin and Its Metabolites Inhibit Recombinant Human Angiotensin-Converting Enzyme 2 (ACE2) Activity
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...
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| Veröffentlicht in: | Journal of agricultural and food chemistry 2020-11, Vol.68 (47), p.13982-13989 |
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| container_issue | 47 |
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| container_title | Journal of agricultural and food chemistry |
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| creator | Liu, Xiaocao Raghuvanshi, Ruma Ceylan, Fatma Duygu Bolling, Bradley W |
| description | 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-O-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 IC50 of 4.48 μM. Thus, quercetin, its metabolites, and polyphenols with 3′,4′-hydroxylation inhibited rhACE2 activity at physiologically relevant concentrations in vitro. |
| doi_str_mv | 10.1021/acs.jafc.0c05064 |
| format | Article |
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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-O-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 IC50 of 4.48 μM. 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Agric. Food Chem</addtitle><date>2020-11-25</date><risdate>2020</risdate><volume>68</volume><issue>47</issue><spage>13982</spage><epage>13989</epage><pages>13982-13989</pages><issn>0021-8561</issn><eissn>1520-5118</eissn><abstract>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-O-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 IC50 of 4.48 μM. Thus, quercetin, its metabolites, and polyphenols with 3′,4′-hydroxylation inhibited rhACE2 activity at physiologically relevant concentrations in vitro.</abstract><pub>American Chemical Society</pub><pmid>33179911</pmid><doi>10.1021/acs.jafc.0c05064</doi><tpages>8</tpages><orcidid>https://orcid.org/0000-0002-4222-2467</orcidid><oa>free_for_read</oa></addata></record> |
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| source | American Chemical Society Journals |
| subjects | Functional Structure/Activity Relationships |
| title | Quercetin and Its Metabolites Inhibit Recombinant Human Angiotensin-Converting Enzyme 2 (ACE2) Activity |
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