Screening and pharmacodynamic evaluation of the antirespiratory syncytial virus activity of steroidal pyridine compounds in vitro and in vivo
© 2020 Wiley Periodicals LLC..
Respiratory syncytial virus (RSV) causes serious lower respiratory tract infections and there are currently no safer or more effective drugs available. It is important to find novel medications for RSV infection. A series of steroidal pyridines were synthesized for screening and evaluation of their antiviral activity and investigation of their antiviral mechanism of action. Compound 3l had the highest antiviral activity, with a half-maximal effective concentration (EC50 ) of 3.13 μM. Compound 3l was explored for its effects in vitro on RSV 2 h before infection (pretreatment), at the time of infection (competition), and 2 h after infection (postinfection). Toll-like receptor (TLR)-3, retinoic acid-inducible gene (RIG)-I, interleukin (IL)-6, and interferon (IFN)-β were suppressed at the cellular level. Mouse lung tissue was subjected to hematoxylin and eosin (HE) staining and immunohistochemistry, which showed that RSV antigen and M gene expression could be reduced by compound 3l. Decreased expression of TLR-3, RIG-I, IL-6, IFN-β, and IL-10 was also found in vivo. The results indicated that compound 3l exerted its antiviral effects mainly through inhibition of viral replication and downregulation of inflammatory factors.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2021 |
|---|---|
| Erschienen: |
2021 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:93 |
|---|---|
| Enthalten in: |
Journal of medical virology - 93(2021), 6 vom: 16. Juni, Seite 3428-3438 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Wang, Zhenya [VerfasserIn] |
|---|
| Links: |
|---|
| Themen: |
9008-11-1 |
|---|
| Anmerkungen: |
Date Completed 08.10.2021 Date Revised 11.10.2023 published: Print-Electronic Citation Status MEDLINE |
|---|
| doi: |
10.1002/jmv.26604 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM316337900 |
|---|
| LEADER | 01000naa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM316337900 | ||
| 003 | DE-627 | ||
| 005 | 20231225160850.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231225s2021 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.1002/jmv.26604 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n1054.xml |
| 035 | |a (DE-627)NLM316337900 | ||
| 035 | |a (NLM)33064304 | ||
| 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 Screening and pharmacodynamic evaluation of the antirespiratory syncytial virus activity of steroidal pyridine compounds in vitro and in vivo |
| 264 | 1 | |c 2021 | |
| 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 Completed 08.10.2021 | ||
| 500 | |a Date Revised 11.10.2023 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a © 2020 Wiley Periodicals LLC. | ||
| 520 | |a Respiratory syncytial virus (RSV) causes serious lower respiratory tract infections and there are currently no safer or more effective drugs available. It is important to find novel medications for RSV infection. A series of steroidal pyridines were synthesized for screening and evaluation of their antiviral activity and investigation of their antiviral mechanism of action. Compound 3l had the highest antiviral activity, with a half-maximal effective concentration (EC50 ) of 3.13 μM. Compound 3l was explored for its effects in vitro on RSV 2 h before infection (pretreatment), at the time of infection (competition), and 2 h after infection (postinfection). Toll-like receptor (TLR)-3, retinoic acid-inducible gene (RIG)-I, interleukin (IL)-6, and interferon (IFN)-β were suppressed at the cellular level. Mouse lung tissue was subjected to hematoxylin and eosin (HE) staining and immunohistochemistry, which showed that RSV antigen and M gene expression could be reduced by compound 3l. Decreased expression of TLR-3, RIG-I, IL-6, IFN-β, and IL-10 was also found in vivo. The results indicated that compound 3l exerted its antiviral effects mainly through inhibition of viral replication and downregulation of inflammatory factors | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a antiviral activity | |
| 650 | 4 | |a inflammatory factor | |
| 650 | 4 | |a respiratory syncytial virus | |
| 650 | 4 | |a steroidal pyridines | |
| 650 | 7 | |a Antiviral Agents |2 NLM | |
| 650 | 7 | |a Cytokines |2 NLM | |
| 650 | 7 | |a Pyridines |2 NLM | |
| 650 | 7 | |a Interferons |2 NLM | |
| 650 | 7 | |a 9008-11-1 |2 NLM | |
| 700 | 1 | |a Hou, Duoduo |e verfasserin |4 aut | |
| 700 | 1 | |a Fang, Jieyu |e verfasserin |4 aut | |
| 700 | 1 | |a Zhu, Li |e verfasserin |4 aut | |
| 700 | 1 | |a Sun, Yingying |e verfasserin |4 aut | |
| 700 | 1 | |a Tan, Yayun |e verfasserin |4 aut | |
| 700 | 1 | |a Gu, Zichen |e verfasserin |4 aut | |
| 700 | 1 | |a Shan, Lihong |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Journal of medical virology |d 1990 |g 93(2021), 6 vom: 16. Juni, Seite 3428-3438 |w (DE-627)NLM000285676 |x 1096-9071 |7 nnns |
| 773 | 1 | 8 | |g volume:93 |g year:2021 |g number:6 |g day:16 |g month:06 |g pages:3428-3438 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.1002/jmv.26604 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 93 |j 2021 |e 6 |b 16 |c 06 |h 3428-3438 | ||