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Quorum Sensing and NF-κB Inhibition of Synthetic Coumaperine Derivatives from Piper nigrum
Bacterial communication, termed Quorum Sensing (QS), is a promising target for virulence attenuation and the treatment of bacterial infections. Infections cause inflammation, a process regulated by a number of cellular factors, including the transcription Nuclear Factor kappa B (NF-κB); this factor...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8071387/ https://www.ncbi.nlm.nih.gov/pubmed/33921056 http://dx.doi.org/10.3390/molecules26082293 |
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author | Kadosh, Yael Muthuraman, Subramani Yaniv, Karin Baruch, Yifat Gopas, Jacob Kushmaro, Ariel Kumar, Rajendran Saravana |
author_facet | Kadosh, Yael Muthuraman, Subramani Yaniv, Karin Baruch, Yifat Gopas, Jacob Kushmaro, Ariel Kumar, Rajendran Saravana |
author_sort | Kadosh, Yael |
collection | PubMed |
description | Bacterial communication, termed Quorum Sensing (QS), is a promising target for virulence attenuation and the treatment of bacterial infections. Infections cause inflammation, a process regulated by a number of cellular factors, including the transcription Nuclear Factor kappa B (NF-κB); this factor is found to be upregulated in many inflammatory diseases, including those induced by bacterial infection. In this study, we tested 32 synthetic derivatives of coumaperine (CP), a known natural compound found in pepper (Piper nigrum), for Quorum Sensing Inhibition (QSI) and NF-κB inhibitory activities. Of the compounds tested, seven were found to have high QSI activity, three inhibited bacterial growth and five inhibited NF-κB. In addition, some of the CP compounds were active in more than one test. For example, compounds CP-286, CP-215 and CP-158 were not cytotoxic, inhibited NF-κB activation and QS but did not show antibacterial activity. CP-154 inhibited QS, decreased NF-κB activation and inhibited bacterial growth. Our results indicate that these synthetic molecules may provide a basis for further development of novel therapeutic agents against bacterial infections. |
format | Online Article Text |
id | pubmed-8071387 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-80713872021-04-26 Quorum Sensing and NF-κB Inhibition of Synthetic Coumaperine Derivatives from Piper nigrum Kadosh, Yael Muthuraman, Subramani Yaniv, Karin Baruch, Yifat Gopas, Jacob Kushmaro, Ariel Kumar, Rajendran Saravana Molecules Article Bacterial communication, termed Quorum Sensing (QS), is a promising target for virulence attenuation and the treatment of bacterial infections. Infections cause inflammation, a process regulated by a number of cellular factors, including the transcription Nuclear Factor kappa B (NF-κB); this factor is found to be upregulated in many inflammatory diseases, including those induced by bacterial infection. In this study, we tested 32 synthetic derivatives of coumaperine (CP), a known natural compound found in pepper (Piper nigrum), for Quorum Sensing Inhibition (QSI) and NF-κB inhibitory activities. Of the compounds tested, seven were found to have high QSI activity, three inhibited bacterial growth and five inhibited NF-κB. In addition, some of the CP compounds were active in more than one test. For example, compounds CP-286, CP-215 and CP-158 were not cytotoxic, inhibited NF-κB activation and QS but did not show antibacterial activity. CP-154 inhibited QS, decreased NF-κB activation and inhibited bacterial growth. Our results indicate that these synthetic molecules may provide a basis for further development of novel therapeutic agents against bacterial infections. MDPI 2021-04-15 /pmc/articles/PMC8071387/ /pubmed/33921056 http://dx.doi.org/10.3390/molecules26082293 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Kadosh, Yael Muthuraman, Subramani Yaniv, Karin Baruch, Yifat Gopas, Jacob Kushmaro, Ariel Kumar, Rajendran Saravana Quorum Sensing and NF-κB Inhibition of Synthetic Coumaperine Derivatives from Piper nigrum |
title | Quorum Sensing and NF-κB Inhibition of Synthetic Coumaperine Derivatives from Piper nigrum |
title_full | Quorum Sensing and NF-κB Inhibition of Synthetic Coumaperine Derivatives from Piper nigrum |
title_fullStr | Quorum Sensing and NF-κB Inhibition of Synthetic Coumaperine Derivatives from Piper nigrum |
title_full_unstemmed | Quorum Sensing and NF-κB Inhibition of Synthetic Coumaperine Derivatives from Piper nigrum |
title_short | Quorum Sensing and NF-κB Inhibition of Synthetic Coumaperine Derivatives from Piper nigrum |
title_sort | quorum sensing and nf-κb inhibition of synthetic coumaperine derivatives from piper nigrum |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8071387/ https://www.ncbi.nlm.nih.gov/pubmed/33921056 http://dx.doi.org/10.3390/molecules26082293 |
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