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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...

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Detalles Bibliográficos
Autores principales: Yuan, Lvfeng, Zhang, Shuai, Peng, Jie, Li, Yuchen, Yang, Qian
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Public Library of Science 2019
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.
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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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