Anti-inflammatory and anticholinesterase activity of six flavonoids isolated from Polygonum and Dorstenia species

Arch Pharm Res. 2017 Oct;40(10):1129-1134. doi: 10.1007/s12272-015-0612-9. Epub 2015 May 8.

Abstract

This study was aimed at investigating the anti-inflammatory and anticholinesterase activity of six naturally occurring flavonoids: (-) pinostrobin (1), 2',4'-dihydroxy-3',6'-dimethoxychalcone (2), 6-8-diprenyleriodictyol (3), isobavachalcone (4), 4-hydroxylonchocarpin (5) and 6-prenylapigenin (6). These compounds were isolated from Dorstenia and Polygonum species used traditionally to treat pain. The anti-inflammatory activity was determined by using the Griess assay and the 15-lipoxygenase inhibitory activity was determined with the ferrous oxidation-xylenol orange assay. Acetylcholinesterase inhibition was determined by the Ellman's method. At the lowest concentration tested (3.12 µg/ml), compounds 2, 3 and 4 had significant NO inhibitory activity with 90.71, 84.65 and 79.57 % inhibition respectively compared to the positive control quercetin (67.93 %). At this concentration there was no significant cytotoxicity against macrophages with 91.67, 72.86 and 70.86 % cell viability respectively, compared to 73.1 % for quercetin. Compound 4 had the most potent lipoxygenase inhibitory activity (IC50 of 25.92 µg/ml). With the exception of (-) pinostrobin (1), all the flavonoids had selective anticholinesterase activity with IC50 values ranging between 5.93 and 8.76 µg/ml compared to the IC50 4.94 µg/ml of eserine the positive control. These results indicate that the studied flavonoids especially isobavachalcone are potential anti-inflammatory natural products that may have the potential to be developed as therapeutic agents against inflammatory conditions and even Alzheimer's disease.

Keywords: 15-Lipoxygenase; Anticholinesterase; Flavonoids; Nitric oxide production inhibition.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / isolation & purification
  • Anti-Inflammatory Agents / pharmacology*
  • Cameroon
  • Cell Culture Techniques
  • Cell Line
  • Cell Survival / drug effects
  • Cholinesterase Inhibitors / isolation & purification
  • Cholinesterase Inhibitors / pharmacology*
  • Dose-Response Relationship, Drug
  • Flavonoids / isolation & purification
  • Flavonoids / pharmacology*
  • Macrophages / drug effects
  • Macrophages / metabolism
  • Medicine, African Traditional
  • Mice
  • Molecular Structure
  • Moraceae / chemistry*
  • Moraceae / growth & development
  • Nitric Oxide / biosynthesis
  • Polygonum / chemistry*
  • Polygonum / growth & development

Substances

  • Anti-Inflammatory Agents
  • Cholinesterase Inhibitors
  • Flavonoids
  • Nitric Oxide