Anti-inflammatory and antioxidant activity of coumarins designed as potential fluorescent zinc sensors

J Enzyme Inhib Med Chem. 2007 Jun;22(3):287-92. doi: 10.1080/14756360601073914.

Abstract

A series of coumarin analogs, designed and synthesised as potential fluorescent zinc probes were evaluated for their biological activity as anti-inflammatory and antioxidant agents. The effect of the synthesised compounds on inflammation, using the carrageenin-induced rat paw oedema model, was studied. In general, the compounds were found to be potent anti-inflammatory agents (26.5-64%). Compound 5 was found to interact significantly with 1,1-diphenyl-2-picryl-hydrazyl stable free radical (DPPH) whereas the remainder were inactive in this assay. The compounds inhibit in general the soybean lipoxygenase and scavenge superoxide anion radicals. The anti-inflammatory activity seems to be connected with their reducing activity. Their RM values were determined as an expression of their lipophilicity. Theoretical calculations of their lipophilicity as clog P were performed indicating that only a poor relationship exists between their lipophilicity and anti-inflammatory activity.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry*
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Antioxidants / chemistry*
  • Antioxidants / pharmacology*
  • Biphenyl Compounds
  • Carrageenan / toxicity
  • Coumarins / chemistry*
  • Coumarins / pharmacology*
  • Drug Evaluation, Preclinical
  • Edema / chemically induced
  • Edema / drug therapy
  • Female
  • Fluorescent Dyes
  • Free Radical Scavengers / chemistry
  • Free Radical Scavengers / pharmacology
  • Glycine max / enzymology
  • Hydrazines
  • Lipoxygenase / drug effects
  • Male
  • Picrates
  • Rats
  • Rats, Inbred F344
  • Structure-Activity Relationship
  • Zinc

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Antioxidants
  • Biphenyl Compounds
  • Coumarins
  • Fluorescent Dyes
  • Free Radical Scavengers
  • Hydrazines
  • Picrates
  • Carrageenan
  • 1,1-diphenyl-2-picrylhydrazyl
  • lipoxygenase L-1
  • Lipoxygenase
  • Zinc