Analgesic and anti-inflammatory activities evaluation of (-)-O-acetyl, (-)-O-methyl, (-)-O-dimethylethylamine cubebin and their preparation from (-)-cubebin |
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Authors: | Souza G H B da Silva Filho A A de Souza V A Pereira A C Royo V de A e Silva M L A da Silva R Donate P M Carvalho J C T Bastos J K |
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Institution: | Faculdade de Ciências Farmacêuticas de Ribeir?o Preto, Universidade de S?o Paulo, Avenida do Cafe S/N, Ribeir?o Preto, 14040 903, S?o Paulo, Brazil. |
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Abstract: | The anti-inflammatory and antinociceptive effects of the acetylated (2), methylated (3) and aminated (4) derivatives of cubebin (1), obtained by its reaction with acetic anhydride, methyl iodide and dimethylethylamine chloride, respectively, were investigated, using different animal models. The compound (2) was the most effective anti-inflammatory one in the carrageenin-induced paw edema in rats and was the only one which showed dose-response correlation for this assay with r = 0.993 and Y = 64.58x + 0.22. Besides, compounds (2) and (4) were more effective than cubebin in inhibiting acetic acid-induced writhing in mice, producing dose-response correlation with doses of 10, 20 and 30 mg/kg, respectively. Regarding the hot plate and the cell migration tests in rats, none of the four tested compounds showed activity. Overall, the results showed that the acetylation and amination of cubebin were efficient in enhancing its analgesic activity, as well as its anti-inflammatory activity. |
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Keywords: | (-)-Cubebin O-acetyl cubebin" target="_blank">(-)-O-acetyl cubebin O-methyl cubebin" target="_blank">(-)-O-methyl cubebin O-dimethylethylamine cubebin" target="_blank">(-)-O-dimethylethylamine cubebin Anti-inflammatory activity Analgesic activity Piper cubeba |
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