Discovery and SAR Research for Antivirus Activity of Novel Butenolide on Influenza A Virus H1N1 In Vitro and In Vivo

[Image: see text] Influenza viruses (IV) cause substantial morbidity and mortality through routine seasonal spread and epidemics. A novel series of butenolides were discovered to be able to inhibit influenza H1N1 activity in vitro, and the SAR for anti-influenza activity was investigated. By optimiz...

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Autores principales: Wang, Zhenya, Hu, Xiaoning, Li, Yuanyuan, Mou, Xiaodong, Wang, Congcong, Chen, Xinli, Tan, Yayun, Wu, Chunli, Liu, Hongmin, Xu, Haiwei
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2019
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6705239/
https://www.ncbi.nlm.nih.gov/pubmed/31460454
http://dx.doi.org/10.1021/acsomega.9b01421
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author Wang, Zhenya
Hu, Xiaoning
Li, Yuanyuan
Mou, Xiaodong
Wang, Congcong
Chen, Xinli
Tan, Yayun
Wu, Chunli
Liu, Hongmin
Xu, Haiwei
author_facet Wang, Zhenya
Hu, Xiaoning
Li, Yuanyuan
Mou, Xiaodong
Wang, Congcong
Chen, Xinli
Tan, Yayun
Wu, Chunli
Liu, Hongmin
Xu, Haiwei
author_sort Wang, Zhenya
collection PubMed
description [Image: see text] Influenza viruses (IV) cause substantial morbidity and mortality through routine seasonal spread and epidemics. A novel series of butenolides were discovered to be able to inhibit influenza H1N1 activity in vitro, and the SAR for anti-influenza activity was investigated. By optimization of the hit compound, compound 37 was obtained with an EC(50) of 6.7 μM against influenza A virus H1N1 as an inhibitor of NA and with low cytotoxicity on MDCK cells. Also, it can inhibit the expression of the influenza A virus gene in the lung of SPF KM mice to show antivirus activity in vivo. These results suggested that compound 37 could inhibit the influenza A virus H1N1 via targeting NA.
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spelling pubmed-67052392019-08-27 Discovery and SAR Research for Antivirus Activity of Novel Butenolide on Influenza A Virus H1N1 In Vitro and In Vivo Wang, Zhenya Hu, Xiaoning Li, Yuanyuan Mou, Xiaodong Wang, Congcong Chen, Xinli Tan, Yayun Wu, Chunli Liu, Hongmin Xu, Haiwei ACS Omega [Image: see text] Influenza viruses (IV) cause substantial morbidity and mortality through routine seasonal spread and epidemics. A novel series of butenolides were discovered to be able to inhibit influenza H1N1 activity in vitro, and the SAR for anti-influenza activity was investigated. By optimization of the hit compound, compound 37 was obtained with an EC(50) of 6.7 μM against influenza A virus H1N1 as an inhibitor of NA and with low cytotoxicity on MDCK cells. Also, it can inhibit the expression of the influenza A virus gene in the lung of SPF KM mice to show antivirus activity in vivo. These results suggested that compound 37 could inhibit the influenza A virus H1N1 via targeting NA. American Chemical Society 2019-08-02 /pmc/articles/PMC6705239/ /pubmed/31460454 http://dx.doi.org/10.1021/acsomega.9b01421 Text en Copyright © 2019 American Chemical Society This is an open access article published under an ACS AuthorChoice License (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html) , which permits copying and redistribution of the article or any adaptations for non-commercial purposes.
spellingShingle Wang, Zhenya
Hu, Xiaoning
Li, Yuanyuan
Mou, Xiaodong
Wang, Congcong
Chen, Xinli
Tan, Yayun
Wu, Chunli
Liu, Hongmin
Xu, Haiwei
Discovery and SAR Research for Antivirus Activity of Novel Butenolide on Influenza A Virus H1N1 In Vitro and In Vivo
title Discovery and SAR Research for Antivirus Activity of Novel Butenolide on Influenza A Virus H1N1 In Vitro and In Vivo
title_full Discovery and SAR Research for Antivirus Activity of Novel Butenolide on Influenza A Virus H1N1 In Vitro and In Vivo
title_fullStr Discovery and SAR Research for Antivirus Activity of Novel Butenolide on Influenza A Virus H1N1 In Vitro and In Vivo
title_full_unstemmed Discovery and SAR Research for Antivirus Activity of Novel Butenolide on Influenza A Virus H1N1 In Vitro and In Vivo
title_short Discovery and SAR Research for Antivirus Activity of Novel Butenolide on Influenza A Virus H1N1 In Vitro and In Vivo
title_sort discovery and sar research for antivirus activity of novel butenolide on influenza a virus h1n1 in vitro and in vivo
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6705239/
https://www.ncbi.nlm.nih.gov/pubmed/31460454
http://dx.doi.org/10.1021/acsomega.9b01421
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