IngentaConnect Antinociceptive effect of proanthocyanidins from Croton celtidifo...

Authors: DalBó, Silvia¹; Jürgensen, Sofia¹; Horst, Heros²; Ruzza, Abreve ngelo Adolfo²; Soethe, Douglas Nihues³; Santos, Adair Roberto Soares³; Pizzolatti, Moacir Geraldo²; Ribeiro-do-Valle, Rosa Maria¹

Source: Journal of Pharmacy and Pharmacology, Volume 57, Number 6, June 2005 , pp. 765-772(8)

Publisher: Pharmaceutical Press

Abstract:

The chemical composition of the chromatography 63 subfraction (63SF) from the ethyl acetate soluble fraction of the crude extract of Croton celtidifolius bark presented a high content of total proanthocyanidins (75.0 ± 2.3%). HPLC analysis of 63SF revealed a dimeric profile (e.g.catechin-(4 alpha

8)-catechin and gallocatechin-(4 alpha

8)-catechin) and polymeric proanthocyanidins. In pharmacological investigations, 63SF administered intraperitoneally exhibited dose-dependent antinociceptive activity against several chemical stimuli, including the intraperitoneal injection of acetic acid (ID50 (the dose of 63SF which was able to reduce the nociceptive response by 50% relative to the control value) = 0.9 (0.5–1.6)) and the intraplantar injection of capsaicin (ID50 = 13.0 (10.0–17.0)), glutamate (ID50 = 4.0 (2.0–7.0)) and formalin (ID50 first phase = 36.0 (24.0–53.0) and late phase = 11.0 (8.0–14.0)). 63SF administered orally exhibited an antinociceptive effect in the formalin test (ID50 first phase = 125.0 (89.0–177.0) and late phase = 65.0 (33.0–95.0)). In the same test, 63SF was effective when given soon after the first phase, as well as exhibiting therapeutic activity. Furthermore, 63SF was effective in models of thermal nociception including tail-flick and hot-plate tests. When the mice were treated in the neonatal period with capsaicin, the antinociceptive effect of 63SF in the first phase of the formalin test was abolished, but pretreatment with naltrexone did not change the antinociceptive effect of 63SF. Together, these results provide evidence that 63SF exerted a pronounced systemic antinociception against chemical (acetic acid, formalin, glutamate and capsaicin tests) and thermal (hot-plate and tail-flick tests) nociceptive models of pain in mice at a dose that did not interfere with the locomotor activity. The mechanism by which this sub-fraction produced antinociception remains unclear, but it is unlikely to involve the activation of the opioid system. However, unmyelinated C-fibres sensitive to treatment with capsaicin are likely to participate in antinociception caused by 63SF.

Document Type: Research article

DOI: 10.1211/0022357056091

Affiliations: 1: Departamento de Farmacologia, Centro de Ciências Biológicas, Bloco D, UFSC, Campus Universitário, Trindade, Florianópolis, SC, Brazil, CEP 88040-900 2: Departamento de Química, CFM, UFSC, Campus Universitário, Trindade, Florianópolis, SC, Brazil, CEP 88040-900 3: Departamento de Ciências Fisiológicas, CCB, UFSC, Campus Universitário, Trindade, Florianópolis, SC, Brazil, CEP 88040-900

The full text electronic article is available for purchase. You will be able to download the full text electronic article after payment.

$38.49 plus tax Refund Policy

Antinociceptive effect of proanthocyanidins from Croton celtidifolius bark