Quorum sensing and nf-κb inhibition of synthetic coumaperine derivatives from Piper nigrum

Yael Kadosh, Subramani Muthuraman, Karin Yaniv, Yifat Baruch, Jacob Gopas, Ariel Kushmaro, Rajendran Saravana Kumar

Research output: Contribution to journalArticlepeer-review


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.

Original languageAmerican English
Article number2293
Issue number8
StatePublished - 1 Jan 2021


  • Amide alkaloids
  • Antibacterial
  • Coumaperine
  • NF-kB
  • Piper nigrum
  • Plant natural-based compounds
  • Quorum sensing

All Science Journal Classification (ASJC) codes

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry


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