Root bark of Discaria americana attenuates pain: A pharmacological evidence of interaction with opioidergic system and TRP/ASIC channels

J Ethnopharmacol. 2018 Dec 5:227:258-267. doi: 10.1016/j.jep.2018.09.008. Epub 2018 Sep 7.

Abstract

Ethnopharmacological relevance: Discaria americana (Rhamnaceae) root bark infusion have been used in traditional medicine as antipyretic, tonic, ameliorative of stomach and skin diseases and diabetes. This study was designed to investigate whether the methanolic extract of the root bark of Discaria americana (MEDa) exhibits antinociceptive effects in mice. Furthermore, it was investigated the involvement of the opioidergic system in MEDa mechanism of action as well the interactions with TRP/ASIC channels in its effect.

Materials and methods: The antinociceptive effect of intra-gastric gavage (i.g.) of MEDa (0.3-300 mg/kg) was evaluated in mice subjected to acute chemical (acetic-acid, formalin, glutamate, capsaicin, cinnamaldehyde, and acidified saline) or thermal (hot plate) tests of pain. The involvement of opioid system was evaluated in the formalin test. A nonspecific effect of MEDa was observed by measuring locomotor activity and exploratory behavior in open field test.

Results: MEDa significantly reduced the number of writhing induced by acetic acid and inhibited the nociception in the two phases of formalin. These effects were inhibited by pretreatment with naloxone. The nociception induced by hot plate and intraplantar injection of glutamate, capsaicin, cinnamaldehyde and acidified saline were significantly inhibited by MEDa. Only the dose of 300 mg/kg altered the locomotor activity.

Conclusions: Our results demonstrated, for the first time, that the methanolic extract of the root bark of Discaria americana presents antinociceptive effect in chemical and thermal stimuli and its analgesic properties can be due activation of the opioidergic system. These results support the use of Discaria americana in traditional medicine and demonstrate that this plant presents a therapeutic potential for the development of phytomedicines with antinociceptive profile.

Keywords: Antinociceptive; Discaria Americana; Formalin; Glutamate; TRP/ASIC channels.

MeSH terms

  • Acid Sensing Ion Channel Blockers / pharmacology
  • Analgesics, Opioid / pharmacology
  • Analgesics, Opioid / therapeutic use*
  • Animals
  • Behavior, Animal / drug effects
  • Male
  • Mice
  • Naloxone / pharmacology
  • Narcotic Antagonists / pharmacology
  • Pain / drug therapy*
  • Phytotherapy
  • Plant Bark
  • Plant Extracts / pharmacology
  • Plant Extracts / therapeutic use*
  • Plant Roots
  • Rhamnaceae*
  • Transient Receptor Potential Channels / antagonists & inhibitors

Substances

  • Acid Sensing Ion Channel Blockers
  • Analgesics, Opioid
  • Narcotic Antagonists
  • Plant Extracts
  • Transient Receptor Potential Channels
  • Naloxone