TY - JOUR
T1 - Quorum sensing and nf-κb inhibition of synthetic coumaperine derivatives from piper nigrum
AU - Kadosh, Yael
AU - Muthuraman, Subramani
AU - Yaniv, Karin
AU - Baruch, Yifat
AU - Gopas, Jacob
AU - Kushmaro, Ariel
AU - Kumar, Rajendran Saravana
N1 - Funding Information:
Acknowledgments: S.M. thanks VIT Chennai for his Ph.D. fellowship. S.M. and R.S.K. extend thanks to the Chemistry Division, VIT Chennai, for infrastructure and instrumentation facilities (CHN analysis, GC–MS and FTIR). The skillful technical assistance from SAIF, VIT Vellore is gratefully acknowledged. Y.K. thanks her Ph.D. fellowship from the Israel Ministry of Science & Technology. We thank Esti Kramarsky-Winter for scientific comments and editing. For technical assistance we also thank Alon Zilha from The Ilse Katz Centre for Meso and Nanoscale Science and Technology and NIBN, Ben-Gurion University of the Negev, Israel.
Funding Information:
Funding: This research was funded by an Interdisciplinary Faculty Grant BGU. YK was supported by a fellowship from the Israel Ministry of Science & Technology.
Publisher Copyright:
© 2021 by the authors. Licensee MDPI, Basel, Switzerland.
PY - 2021/1/1
Y1 - 2021/1/1
N2 - 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.
AB - 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.
KW - Amide alkaloids
KW - Antibacterial
KW - Coumaperine
KW - NF-kB
KW - Piper nigrum
KW - Plant natural-based compounds
KW - Quorum sensing
UR - http://www.scopus.com/inward/record.url?scp=85105132401&partnerID=8YFLogxK
U2 - 10.3390/molecules26082293
DO - 10.3390/molecules26082293
M3 - Article
C2 - 33921056
AN - SCOPUS:85105132401
VL - 26
JO - Molecules
JF - Molecules
SN - 1420-3049
IS - 8
M1 - 2293
ER -