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Acetilbergenina: obtenção e avaliação das atividades antinociceptiva e anti-inflamatória
(Universidade Federal do Pará, 2010-01-22) BORGES, Jaqueline Cibene Moreira; SOUSA, Pergentino José da Cunha; http://lattes.cnpq.br/9909053957915090; SANTOS, Lourivaldo da Silva; http://lattes.cnpq.br/3232898465948962
Endopleura uchi (Huber) Cuatrec. (Humiriaceae), a Brazilian Amazon plant, commonly known as “uxi”, is used in folk medicine for the treatment of several pathologies, such as arthritis. Bergenin, one of the chemical constituents of E. uchi, has several biological activities, including anti-inflammatory and antinociceptive activities. In order to obtain a more potent derivative than bergenin it has decided to acetyl this substance. Acetylbergenin was tested in nociception and inflammation models. Bergenin was isolated from the chromatographic fractionation of aqueous extract from stem bark of E. uchi and the acetylbergenin was obtained by acetylation of bergenin. The substances were identified based on spectral analysis of 1H NMR, 13C NMR, DEPT and COSY, and comparison with literature data. For nociception models were carried out the abdominal writhing test, hot plate test and formalin test, while in the inflammation models were carried out the croton oil-induced ear edema, rat paw edema induced by carrageenan and dextran, carragenin-induced peritonitis test. Furthermore, the model of gastric ulcer induced by stress was used to assess the potential ulcerogenic of the substance. In the abdominal writhing test induced by acetic acid 0.6%, acetilbergenin doses of 1, 5, 10, 15 and 25 mg / kg blocked the number of writhing in 28.2%, 52.7%, 61.1 %, 68.3% and 95.0%, respectively, and dose-dependent manner when compared to the control group. The calculated ED50 was 6.8mg/kg. In the hot plate test (55ºC), acetylbergenin (6.8 mg/kg) did not induce alterations in the latency time when compared to the control group. In the formalin test, acetylbergenin (6.8mg/kg) inhibited 88.30% the algic stimulus in the second phase (inflammatory) compared to the control group. Furthermore, naloxone reversed the effect of acetylbergenin the second phase of this test. In the croton oilinduced dermatitis, acetylbergenin (6.8 mg/kg) provoked inhibitory effect in 75.60% in comparison to the control group. In the paw edema induced by carrageenan, acetylbergenin (6.8 mg/kg) was able to reduce the development of edema from the 2nd to the 5th hours compared to the control group. In the paw edema induced by dextran, acetylbergenin (6.8 mg/kg) reduced edema at all times. In carragenininduced peritonitis, acetylbergenin (6.8mg/kg) blocked 70% of the neutrophils number compared to the control group. In the trial of gastric ulcer, acetylbergenin blocked 78.55% in the generation of gastric lesions by stress when compared to indomethacin. The results suggest that acetylbergenin has an antinociceptive and anti-inflammatory activity which, according to the tests employed, is probably of peripheral origin.