Back to Search Start Over

Quorum Sensing and NF-κB Inhibition of Synthetic Coumaperine Derivatives from Piper nigrum

Authors :
Yael Kadosh
Subramani Muthuraman
Karin Yaniv
Yifat Baruch
Jacob Gopas
Ariel Kushmaro
Rajendran Saravana Kumar
Source :
Molecules, Vol 26, Iss 8, p 2293 (2021)
Publication Year :
2021
Publisher :
MDPI AG, 2021.

Abstract

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.

Details

Language :
English
ISSN :
14203049
Volume :
26
Issue :
8
Database :
Directory of Open Access Journals
Journal :
Molecules
Publication Type :
Academic Journal
Accession number :
edsdoj.9aa5337447e4c3c850fa93bb27c8f7f
Document Type :
article
Full Text :
https://doi.org/10.3390/molecules26082293