Setnikar I, Cereda R, Pacini M A, Revel L
Rotta Research Laboratorium S.p.A., Monza, Italy.
Arzneimittelforschung. 1991 Feb;41(2):157-61.
Glucosamine (CAS 3416-24-8) is an aminomonosaccharide naturally occurring in the human body. It was tested for antiinflammatory activities and it showed to protect against the edema provoked in the rat paw by carrageenin, dextran, formalin, but not against the edema provoked by specific inflammation mediators, such as bradykinin, serotonin, histamine. Glucosamine protected against pleurities provoked in the rat by carrageenin, but not against that provoked by bradykinin. Furthermore glucosamine protected against peritonitis provoked in the rat by formalin and in the mouse by acetic acid. Glucosamine did not show antinoceptive properties against writings provoked by i.p. phenylquinone in the mouse. Glucosamine did not show inhibiting activities on cyclooxygenase or on the proteolytic enzymes in the inflamed paw of the rat, but it was able to inhibit in vitro superoxide generation and lysosomial enzymes of the liver. The potency of glucosamine on the antiinflammatory tests was lower than that of acetylsalicylic acid and much lower than that of indomethacin. Its acute toxicity, however, and notably the toxicity on the gastrointestinal tract is very low, practically absent. The pharmacological therapeutic index of glucosamine with regard to the antiinflammatory activities seems therefore comparable or superior to that of the known non-steroidal anti-inflammatories.
氨基葡萄糖(CAS 3416-24-8)是一种天然存在于人体中的氨基单糖。对其抗炎活性进行了测试,结果表明它能预防角叉菜胶、右旋糖酐、福尔马林诱发的大鼠足爪水肿,但对缓激肽、5-羟色胺、组胺等特定炎症介质诱发的水肿无效。氨基葡萄糖能预防角叉菜胶诱发的大鼠胸膜炎,但对缓激肽诱发的胸膜炎无效。此外,氨基葡萄糖能预防福尔马林诱发的大鼠腹膜炎以及乙酸诱发的小鼠腹膜炎。氨基葡萄糖对小鼠腹腔注射苯醌诱发的扭体反应没有镇痛作用。氨基葡萄糖对大鼠炎症足爪中的环氧化酶或蛋白水解酶没有抑制活性,但它能够在体外抑制肝脏中超氧化物的产生和溶酶体酶的活性。氨基葡萄糖在抗炎试验中的效力低于乙酰水杨酸,远低于吲哚美辛。然而,其急性毒性,尤其是对胃肠道的毒性非常低,几乎不存在。因此,就抗炎活性而言,氨基葡萄糖的药理学治疗指数似乎与已知的非甾体抗炎药相当或更高。