acacetin and Pain

Acacetin is a bioflavonoid with pharmacological properties such as antinociceptive/anti-inflammatory activities. However, scientific evidence of its spectrum activity and mechanisms of action is unknown.. Acacetin administered via i.p. was assessed using several nociceptive experimental models such as the writhing test, the formalin test and carrageenan paw oedema in the thermal plantar tests (Hargreaves method) in mice, as well as the pain-induced functional impairment model in rat (PIFIR model).. Acacetin produced a significant and dose-dependent inhibition of the writhes with an ED50 = 20 mg/kg. Furthermore, acacetin inhibited licking and shaking associated with nociceptive behaviour mainly in the inflammatory phase of the formalin test. No significant differences were observed in the plantar test in mice, but a minor response was obtained in the PIFIR model. Animals receiving pre-treatment of WAY100635 (0.1 mg/kg, s.c.), flumazenil (3 mg/kg, i.p.) or naloxone (1 mg/kg, i.p.) partially reduced the antinociceptive response of acacetin in the writhing test. Presence of the inhibitors in the NO-cGMP-K(+) channel pathway did not modify the antinociceptive effect of acacetin in the writhing or the formalin test.. Our data showed that systemic administration of acacetin decreased visceral and inflammatory nociception and prevented the formalin-induced oedema. In the mechanism of the acacetin antinociceptive effect, 5-HT1A, GABA/BDZs and opioid receptors but not the NO-cGMP-K(+) channel pathway seem to be involved. The data presented prove acacetin to be potentially useful in the therapy of pain-related diseases.

Topics: Analgesics; Animals; Anti-Inflammatory Agents; Disease Models, Animal; Flavones; Inflammation; Male; Mice; Pain; Pain Measurement; Rats; Treatment Outcome

Fever and pain management is a very challenging job for the clinician as the available synthetic agents are causing serious side effects. The present research article deals with the antipyretic and antinociceptive activity of extract/fractions of Potentilla evestita and acacetin isolated from the chloroform fraction of the plant.. Various chromatographic and spectroscopic techniques were used for the isolation and characterizion of compound. In-vivo yeast induced fibrile mice were used for antipyretic activity while acetic acid induced writhing and formalin tests were used for antinociceptive.. The extract/fractions of P. evestita caused marked antipyretic effect during various assessment times in which chloroform was the most prominent followed by ethyl acetate. When acacetin was injected, it produced marked effect with maximum activity of 33.28% and 55.01% at 5 and 10 mg/kg i.p respectively. When studied in acetic acid induced writhing test, the extract/fractions evoked significant antinociceptive effect in which chloroform was the most effective fraction followed by ethyl acetate. Acacetin showed significant antinociceptive effect with 44.77% and 67.03% reduction in abdominal constriction at 5 and 10 mg/kg i.p., respectively. Similarly, it evoked significant dose dependent reduction in noxious stimulation with 42.07% and 64.57% pain attenuation at 5 and 10 mg/kg i.p., respectively in initial phase. In the late phase, it illustrated more dominant effect with 46.32% and 67.29% reduction of painful sensation.. In conclusion, the extract/fractions of P. evestita as well as the isolated compound, acacetin showed strong antipyretic and antinociceptive activity in various animal models possibly mediated through both peripheral and central mechanism.

Topics: Acetic Acid; Analgesics; Animals; Antipyretics; Disease Models, Animal; Fever; Flavones; Male; Mice, Inbred BALB C; Pain; Pain Measurement; Plant Extracts; Plant Leaves; Potentilla; Rats, Wistar