Novel β-carboline-tripeptide conjugates attenuate mesenteric ischemia/reperfusion injury in the rat

Eur J Med Chem. 2011 Jun;46(6):2441-52. doi: 10.1016/j.ejmech.2011.03.029. Epub 2011 Mar 21.

Abstract

We have synthesized a series of new β-carboline-tripeptide conjugates, and examined their anti-inflammatory properties in a mouse model of xylene-induced ear edema. The analgesic capacity of these compounds was further evaluated in a rodent tail flick assay. Our results indicate that β-carboline conjugate 4a manifests potent anti-inflammatory and analgesic activity while exerting a protective effect against mesenteric ischemia/reperfusion (I/R) injury in the rat.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Carbolines / chemistry*
  • Crystallography, X-Ray
  • Dose-Response Relationship, Drug
  • Edema / chemically induced
  • Edema / prevention & control
  • Male
  • Mesenteric Arteries / drug effects*
  • Mesenteric Arteries / pathology
  • Mice
  • Mice, Inbred ICR
  • Models, Molecular
  • Molecular Dynamics Simulation
  • Molecular Structure
  • Oligopeptides / chemical synthesis
  • Oligopeptides / chemistry
  • Oligopeptides / pharmacology*
  • Rats
  • Rats, Wistar
  • Reperfusion Injury / drug therapy*
  • Reperfusion Injury / pathology
  • Stereoisomerism
  • Xylenes / antagonists & inhibitors

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Carbolines
  • Oligopeptides
  • Xylenes