Discovery and SAR Research for Antivirus Activity of Novel Butenolide on Influenza A Virus H1N1 In Vitro and In Vivo
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 EC50 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.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2019 |
|---|---|
| Erschienen: |
2019 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:4 |
|---|---|
| Enthalten in: |
ACS omega - 4(2019), 8 vom: 20. Aug., Seite 13265-13269 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Wang, Zhenya [VerfasserIn] |
|---|
| Links: |
|---|
| Themen: |
|---|
| Anmerkungen: |
Date Revised 01.10.2020 published: Electronic-eCollection Citation Status PubMed-not-MEDLINE |
|---|
| doi: |
10.1021/acsomega.9b01421 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM300699875 |
|---|
| LEADER | 01000naa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM300699875 | ||
| 003 | DE-627 | ||
| 005 | 20231225103111.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231225s2019 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.1021/acsomega.9b01421 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n1002.xml |
| 035 | |a (DE-627)NLM300699875 | ||
| 035 | |a (NLM)31460454 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Wang, Zhenya |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Discovery and SAR Research for Antivirus Activity of Novel Butenolide on Influenza A Virus H1N1 In Vitro and In Vivo |
| 264 | 1 | |c 2019 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Revised 01.10.2020 | ||
| 500 | |a published: Electronic-eCollection | ||
| 500 | |a Citation Status PubMed-not-MEDLINE | ||
| 520 | |a 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 EC50 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 | ||
| 650 | 4 | |a Journal Article | |
| 700 | 1 | |a Hu, Xiaoning |e verfasserin |4 aut | |
| 700 | 1 | |a Li, Yuanyuan |e verfasserin |4 aut | |
| 700 | 1 | |a Mou, Xiaodong |e verfasserin |4 aut | |
| 700 | 1 | |a Wang, Congcong |e verfasserin |4 aut | |
| 700 | 1 | |a Chen, Xinli |e verfasserin |4 aut | |
| 700 | 1 | |a Tan, Yayun |e verfasserin |4 aut | |
| 700 | 1 | |a Wu, Chunli |e verfasserin |4 aut | |
| 700 | 1 | |a Liu, Hongmin |e verfasserin |4 aut | |
| 700 | 1 | |a Xu, Haiwei |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t ACS omega |d 2016 |g 4(2019), 8 vom: 20. Aug., Seite 13265-13269 |w (DE-627)NLM264243048 |x 2470-1343 |7 nnns |
| 773 | 1 | 8 | |g volume:4 |g year:2019 |g number:8 |g day:20 |g month:08 |g pages:13265-13269 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.1021/acsomega.9b01421 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 4 |j 2019 |e 8 |b 20 |c 08 |h 13265-13269 | ||