Hesperidin Is a Potential Inhibitor against SARS-CoV-2 Infection
Hesperidin (HD) is a common flavanone glycoside isolated from citrus fruits and possesses great potential for cardiovascular protection. Hesperetin (HT) is an aglycone metabolite of HD with high bioavailability. Through the docking simulation, HD and HT have shown their potential to bind to two cell...
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| Veröffentlicht in: | Nutrients 2021-08, Vol.13 (8), p.2800 |
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| container_title | Nutrients |
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| creator | Cheng, Fang-Ju Huynh, Thanh-Kieu Yang, Chia-Shin Hu, Dai-Wei Shen, Yi-Cheng Tu, Chih-Yen Wu, Yang-Chang Tang, Chih-Hsin Huang, Wei-Chien Chen, Yeh Ho, Chien-Yi |
| description | Hesperidin (HD) is a common flavanone glycoside isolated from citrus fruits and possesses great potential for cardiovascular protection. Hesperetin (HT) is an aglycone metabolite of HD with high bioavailability. Through the docking simulation, HD and HT have shown their potential to bind to two cellular proteins: transmembrane serine protease 2 (TMPRSS2) and angiotensin-converting enzyme 2 (ACE2), which are required for the cellular entry of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Our results further found that HT and HD suppressed the infection of VeroE6 cells using lentiviral-based pseudo-particles with wild types and variants of SARS-CoV-2 with spike (S) proteins, by blocking the interaction between the S protein and cellular receptor ACE2 and reducing ACE2 and TMPRSS2 expression. In summary, hesperidin is a potential TMPRSS2 inhibitor for the reduction of the SARS-CoV-2 infection. |
| doi_str_mv | 10.3390/nu13082800 |
| format | Article |
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Hesperetin (HT) is an aglycone metabolite of HD with high bioavailability. Through the docking simulation, HD and HT have shown their potential to bind to two cellular proteins: transmembrane serine protease 2 (TMPRSS2) and angiotensin-converting enzyme 2 (ACE2), which are required for the cellular entry of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Our results further found that HT and HD suppressed the infection of VeroE6 cells using lentiviral-based pseudo-particles with wild types and variants of SARS-CoV-2 with spike (S) proteins, by blocking the interaction between the S protein and cellular receptor ACE2 and reducing ACE2 and TMPRSS2 expression. In summary, hesperidin is a potential TMPRSS2 inhibitor for the reduction of the SARS-CoV-2 infection.</description><identifier>ISSN: 2072-6643</identifier><identifier>EISSN: 2072-6643</identifier><identifier>DOI: 10.3390/nu13082800</identifier><identifier>PMID: 34444960</identifier><language>eng</language><publisher>Basel: MDPI AG</publisher><subject>ACE2 ; Angiotensin ; Angiotensin-converting enzyme 2 ; Bioavailability ; Cellular proteins ; Citrus ; Citrus fruits ; Coronaviruses ; COVID-19 ; Disease transmission ; Enzymes ; Health aspects ; Hesperidin ; High-definition television ; Infections ; Metabolites ; Peptides ; Peptidyl-dipeptidase A ; Proteases ; Protein binding ; Proteins ; Respiratory diseases ; Serine ; Serine proteinase ; Severe acute respiratory syndrome ; Severe acute respiratory syndrome coronavirus 2 ; Simulation</subject><ispartof>Nutrients, 2021-08, Vol.13 (8), p.2800</ispartof><rights>COPYRIGHT 2021 MDPI AG</rights><rights>2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.</rights><rights>2021 by the authors. 2021</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c450t-8936eef637d1aa743766ed483987b2e2ec140d7d19bb9a43b61072555f4549243</citedby><cites>FETCH-LOGICAL-c450t-8936eef637d1aa743766ed483987b2e2ec140d7d19bb9a43b61072555f4549243</cites><orcidid>0000-0002-7113-8352 ; 0000-0001-6467-8716</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC8401008/pdf/$$EPDF$$P50$$Gpubmedcentral$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC8401008/$$EHTML$$P50$$Gpubmedcentral$$Hfree_for_read</linktohtml><link.rule.ids>230,314,727,780,784,885,27923,27924,53790,53792</link.rule.ids></links><search><creatorcontrib>Cheng, Fang-Ju</creatorcontrib><creatorcontrib>Huynh, Thanh-Kieu</creatorcontrib><creatorcontrib>Yang, Chia-Shin</creatorcontrib><creatorcontrib>Hu, Dai-Wei</creatorcontrib><creatorcontrib>Shen, Yi-Cheng</creatorcontrib><creatorcontrib>Tu, Chih-Yen</creatorcontrib><creatorcontrib>Wu, Yang-Chang</creatorcontrib><creatorcontrib>Tang, Chih-Hsin</creatorcontrib><creatorcontrib>Huang, Wei-Chien</creatorcontrib><creatorcontrib>Chen, Yeh</creatorcontrib><creatorcontrib>Ho, Chien-Yi</creatorcontrib><title>Hesperidin Is a Potential Inhibitor against SARS-CoV-2 Infection</title><title>Nutrients</title><description>Hesperidin (HD) is a common flavanone glycoside isolated from citrus fruits and possesses great potential for cardiovascular protection. Hesperetin (HT) is an aglycone metabolite of HD with high bioavailability. Through the docking simulation, HD and HT have shown their potential to bind to two cellular proteins: transmembrane serine protease 2 (TMPRSS2) and angiotensin-converting enzyme 2 (ACE2), which are required for the cellular entry of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Our results further found that HT and HD suppressed the infection of VeroE6 cells using lentiviral-based pseudo-particles with wild types and variants of SARS-CoV-2 with spike (S) proteins, by blocking the interaction between the S protein and cellular receptor ACE2 and reducing ACE2 and TMPRSS2 expression. In summary, hesperidin is a potential TMPRSS2 inhibitor for the reduction of the SARS-CoV-2 infection.</description><subject>ACE2</subject><subject>Angiotensin</subject><subject>Angiotensin-converting enzyme 2</subject><subject>Bioavailability</subject><subject>Cellular proteins</subject><subject>Citrus</subject><subject>Citrus fruits</subject><subject>Coronaviruses</subject><subject>COVID-19</subject><subject>Disease transmission</subject><subject>Enzymes</subject><subject>Health aspects</subject><subject>Hesperidin</subject><subject>High-definition television</subject><subject>Infections</subject><subject>Metabolites</subject><subject>Peptides</subject><subject>Peptidyl-dipeptidase A</subject><subject>Proteases</subject><subject>Protein binding</subject><subject>Proteins</subject><subject>Respiratory diseases</subject><subject>Serine</subject><subject>Serine proteinase</subject><subject>Severe acute respiratory syndrome</subject><subject>Severe acute respiratory syndrome coronavirus 2</subject><subject>Simulation</subject><issn>2072-6643</issn><issn>2072-6643</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2021</creationdate><recordtype>article</recordtype><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>AZQEC</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><sourceid>DWQXO</sourceid><recordid>eNptkVFr2zAQx8VoWUval30Cw15GwenZks_Wy1gIaxMorLTbXoVsnxMVR8oku7BvX5mWph07PUjo_7v_3XGMfcpgzrmESztmHKq8AvjATnMo8xRR8KM37xN2HsIDTFFCifwjO-EihkQ4Zd9WFPbkTWtssg6JTm7dQHYwuk_WdmtqMzif6I02NgzJ_eLuPl2632kexY6awTh7xo473Qc6f7ln7NfV95_LVXrz43q9XNykjShgSCvJkahDXraZ1qXgJSK1ouKyKuuccmoyAW0UZV1LLXiNWey_KIpOFELmgs_Y12ff_VjvqG1ik173au_NTvu_ymmj3ivWbNXGPapKQAZQRYMvLwbe_RkpDGpnQkN9ry25Mai8QAQOmZxqff4HfXCjt3G8iSpEJZDLA7XRPSljOxfrNpOpWpRYoEDkGKn5f6h4WtqZxlnqTPx_l3DxnNB4F4Kn7nXGDNS0cnVYOX8CjcKYNw</recordid><startdate>20210801</startdate><enddate>20210801</enddate><creator>Cheng, Fang-Ju</creator><creator>Huynh, Thanh-Kieu</creator><creator>Yang, Chia-Shin</creator><creator>Hu, Dai-Wei</creator><creator>Shen, Yi-Cheng</creator><creator>Tu, Chih-Yen</creator><creator>Wu, Yang-Chang</creator><creator>Tang, Chih-Hsin</creator><creator>Huang, Wei-Chien</creator><creator>Chen, Yeh</creator><creator>Ho, Chien-Yi</creator><general>MDPI AG</general><general>MDPI</general><scope>AAYXX</scope><scope>CITATION</scope><scope>3V.</scope><scope>7TS</scope><scope>7X7</scope><scope>7XB</scope><scope>88E</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BENPR</scope><scope>CCPQU</scope><scope>COVID</scope><scope>DWQXO</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>K9.</scope><scope>M0S</scope><scope>M1P</scope><scope>PIMPY</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>7X8</scope><scope>5PM</scope><orcidid>https://orcid.org/0000-0002-7113-8352</orcidid><orcidid>https://orcid.org/0000-0001-6467-8716</orcidid></search><sort><creationdate>20210801</creationdate><title>Hesperidin Is a Potential Inhibitor against SARS-CoV-2 Infection</title><author>Cheng, Fang-Ju ; 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Hesperetin (HT) is an aglycone metabolite of HD with high bioavailability. Through the docking simulation, HD and HT have shown their potential to bind to two cellular proteins: transmembrane serine protease 2 (TMPRSS2) and angiotensin-converting enzyme 2 (ACE2), which are required for the cellular entry of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Our results further found that HT and HD suppressed the infection of VeroE6 cells using lentiviral-based pseudo-particles with wild types and variants of SARS-CoV-2 with spike (S) proteins, by blocking the interaction between the S protein and cellular receptor ACE2 and reducing ACE2 and TMPRSS2 expression. In summary, hesperidin is a potential TMPRSS2 inhibitor for the reduction of the SARS-CoV-2 infection.</abstract><cop>Basel</cop><pub>MDPI AG</pub><pmid>34444960</pmid><doi>10.3390/nu13082800</doi><orcidid>https://orcid.org/0000-0002-7113-8352</orcidid><orcidid>https://orcid.org/0000-0001-6467-8716</orcidid><oa>free_for_read</oa></addata></record> |
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| subjects | ACE2 Angiotensin Angiotensin-converting enzyme 2 Bioavailability Cellular proteins Citrus Citrus fruits Coronaviruses COVID-19 Disease transmission Enzymes Health aspects Hesperidin High-definition television Infections Metabolites Peptides Peptidyl-dipeptidase A Proteases Protein binding Proteins Respiratory diseases Serine Serine proteinase Severe acute respiratory syndrome Severe acute respiratory syndrome coronavirus 2 Simulation |
| title | Hesperidin Is a Potential Inhibitor against SARS-CoV-2 Infection |
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