部分合成(-)-立方宾衍生物(-)-o苄基立方宾的镇痛和抗炎活性。

Bollettino chimico farmaceutico Pub Date : 2004-03-01
H dos S Coimbra, V de A Royo, V A de Souza, A C Pereira, G H B de Souza, R da Silva, P M Donate, M L A Silva, W R Cunha, J C T Carvalho, J K Bastos
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引用次数: 0

摘要

用不同的动物模型研究了(-)-立方宾与苄基溴反应得到的苄基立方宾衍生物的抗炎和抗伤作用。(-)-邻苯并立方宾对角菜胶致大鼠足部水肿的抗炎作用(16.2%)低于立方宾(57%)和吲哚美辛(77%),但对醋酸致小鼠扭体的抑制作用(80%)高于(-)-立方宾(41%),剂量分别为10、20和40 mg/kg时呈剂量效应相关。此外,该衍生物在大鼠热板实验和细胞迁移实验中均无活性。总的来说,结果表明,立方素的苄基化仅能有效增强其镇痛活性。
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Analgesic and anti-inflammatory activities of (-)-o benzyl cubebin, a (-)-cubebin derivative, obtained by partial synthesis.

The anti-inflammatory and antinociceptive effects of the benzylated cubebin derivative, obtained by reaction of (-)-cubebin with benzyl bromide, were investigated using different animal models. The (-)-o-benzyl cubebin showed a low anti-inflammatory effect (16.2%) in relation to cubebin (57%) and indomethacin (77%) in the carrageenin-induced paw edema in rats, but on the other hand it was more effective (80%) than (-)-cubebin (41%) in inhibiting acetic acid-induced writhing in mice, producing dose-response correlation with doses of 10, 20 and 40 mg/kg, respectively. Moreover, this derivative compound did not show activity in both the hot plate and the cell migration test in rats. Overall, the results showed that the benzylation of cubebin were efficient in enhancing only its analgesic activity.

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