Cargando…

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...

Descripción completa

Detalles Bibliográficos
Autores principales: Kadosh, Yael, Muthuraman, Subramani, Yaniv, Karin, Baruch, Yifat, Gopas, Jacob, Kushmaro, Ariel, Kumar, Rajendran Saravana
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
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
_version_ 1783683687656718336
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
work_keys_str_mv AT kadoshyael quorumsensingandnfkbinhibitionofsyntheticcoumaperinederivativesfrompipernigrum
AT muthuramansubramani quorumsensingandnfkbinhibitionofsyntheticcoumaperinederivativesfrompipernigrum
AT yanivkarin quorumsensingandnfkbinhibitionofsyntheticcoumaperinederivativesfrompipernigrum
AT baruchyifat quorumsensingandnfkbinhibitionofsyntheticcoumaperinederivativesfrompipernigrum
AT gopasjacob quorumsensingandnfkbinhibitionofsyntheticcoumaperinederivativesfrompipernigrum
AT kushmaroariel quorumsensingandnfkbinhibitionofsyntheticcoumaperinederivativesfrompipernigrum
AT kumarrajendransaravana quorumsensingandnfkbinhibitionofsyntheticcoumaperinederivativesfrompipernigrum