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Synthetic surfactin analogues have improved anti-PEDV properties
Surfactin has antiviral activity against various enveloped viruses by inhibiting viral membrane fusion. However, the potential utility of surfactin as an antiviral drug is limited by its cytotoxicity. In this study, 10 surfactin analogues were obtained by chemical synthesis and evaluated to determin...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Public Library of Science
2019
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6459484/ https://www.ncbi.nlm.nih.gov/pubmed/30973929 http://dx.doi.org/10.1371/journal.pone.0215227 |
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author | Yuan, Lvfeng Zhang, Shuai Peng, Jie Li, Yuchen Yang, Qian |
author_facet | Yuan, Lvfeng Zhang, Shuai Peng, Jie Li, Yuchen Yang, Qian |
author_sort | Yuan, Lvfeng |
collection | PubMed |
description | Surfactin has antiviral activity against various enveloped viruses by inhibiting viral membrane fusion. However, the potential utility of surfactin as an antiviral drug is limited by its cytotoxicity. In this study, 10 surfactin analogues were obtained by chemical synthesis and evaluated to determine their anti-PEDV activities, hemolytic activities, and critical micelle concentrations. The main goal of our study was to develop a safer drug; a surfactin analogue with high anti-PEDV activity and low hemolytic activity. Compared with surfactin, one of the analogues we developed, SLP5, has lower hemolytic activity, with the same antiviral activity. The selectivity index of SLP5 is 52, while the SI for surfactin is 4, in other words, the safe and effective concentration range of SLP5 is 12 times greater than that of surfactin. Like surfactin, SLP5 has a direct antiviral effect on PEDV. Structurally, SLP5 is a linear lipopeptide with three carboxyl groups. Surfactin derivatives similar to SLP5 could be obtained by lactone bond hydrolyzation of surfactin, as well as total synthesis. |
format | Online Article Text |
id | pubmed-6459484 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | Public Library of Science |
record_format | MEDLINE/PubMed |
spelling | pubmed-64594842019-05-03 Synthetic surfactin analogues have improved anti-PEDV properties Yuan, Lvfeng Zhang, Shuai Peng, Jie Li, Yuchen Yang, Qian PLoS One Research Article Surfactin has antiviral activity against various enveloped viruses by inhibiting viral membrane fusion. However, the potential utility of surfactin as an antiviral drug is limited by its cytotoxicity. In this study, 10 surfactin analogues were obtained by chemical synthesis and evaluated to determine their anti-PEDV activities, hemolytic activities, and critical micelle concentrations. The main goal of our study was to develop a safer drug; a surfactin analogue with high anti-PEDV activity and low hemolytic activity. Compared with surfactin, one of the analogues we developed, SLP5, has lower hemolytic activity, with the same antiviral activity. The selectivity index of SLP5 is 52, while the SI for surfactin is 4, in other words, the safe and effective concentration range of SLP5 is 12 times greater than that of surfactin. Like surfactin, SLP5 has a direct antiviral effect on PEDV. Structurally, SLP5 is a linear lipopeptide with three carboxyl groups. Surfactin derivatives similar to SLP5 could be obtained by lactone bond hydrolyzation of surfactin, as well as total synthesis. Public Library of Science 2019-04-11 /pmc/articles/PMC6459484/ /pubmed/30973929 http://dx.doi.org/10.1371/journal.pone.0215227 Text en © 2019 Yuan et al http://creativecommons.org/licenses/by/4.0/ This is an open access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/) , which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. |
spellingShingle | Research Article Yuan, Lvfeng Zhang, Shuai Peng, Jie Li, Yuchen Yang, Qian Synthetic surfactin analogues have improved anti-PEDV properties |
title | Synthetic surfactin analogues have improved anti-PEDV properties |
title_full | Synthetic surfactin analogues have improved anti-PEDV properties |
title_fullStr | Synthetic surfactin analogues have improved anti-PEDV properties |
title_full_unstemmed | Synthetic surfactin analogues have improved anti-PEDV properties |
title_short | Synthetic surfactin analogues have improved anti-PEDV properties |
title_sort | synthetic surfactin analogues have improved anti-pedv properties |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6459484/ https://www.ncbi.nlm.nih.gov/pubmed/30973929 http://dx.doi.org/10.1371/journal.pone.0215227 |
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