Many natural
terpenoid compounds from plants exhibit antinociceptive property but very few studies have addressed their efficacy in visceral models of nociception. The present study evaluated the antinociceptive potential of
oleanolic acid, a pentacyclic
triterpene in the mouse model of colonic nociception induced by mustard oil. We further examined the possible participation of
opioid, alpha2-adrenergic, and transient receptor potential vanilloid 1 (TRPV1)-receptors in its mechanism. Mice were pretreated orally with
oleanolic acid (3, 10, 30 mg/kg) or vehicle, and the
pain-related behavioral responses to intracolonic injection of mustard oil was analysed.
Oleanolic acid significantly suppressed the mustard oil-induced nociceptive behaviors at test doses of 10 and 30 mg/kg, in a dose-related manner. The antinociceptive effect of
oleanolic acid (30 mg/kg) was significantly blocked by pretreatment with the
opioid antagonist,
naloxone (2 mg/kg, i.p.), while the alpha2-adrenoceptor antagonist,
yohimbine (2 mg/kg, s.c.), had no effect. Pretreatment with
ruthenium red (3 mg/kg, s.c.), a non-competitive TRPV1 antagonist alone caused significant inhibition of mustard oil-induced nociception but its co-administration with
oleanolic acid produced neither antagonism nor potentiation of
oleanolic acid antinociception. In the open-field test that detects
sedative or motor abnormality, mice received 30 mg/kg
oleanolic acid did not show any per se influence, but significantly inhibited the mustard oil-induced decrease in ambulation frequency. These data demonstrate the visceral antinociceptive potential of
oleanolic acid that involves an
opioid mechanism and possibly a modulatory influence on
vanilloid-receptors, which needs further study.