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甾体生物碱苷类化合物托替宁的抗炎活性。

Anti-inflammatory activity of the steroid alkaloid glycoside, toatine.

作者信息

Filderman R B, Kovacs B A

出版信息

Br J Pharmacol. 1969 Nov;37(3):748-55. doi: 10.1111/j.1476-5381.1969.tb08514.x.

Abstract
  1. Tomatine, isolated from extracts of crown gall-infected tomato plants or obtained commercially, was tested for anti-inflammatory activity using three different methods.2. Tomatine administered to intact rats intramuscularly in a dose range of 1-10 mg/kg or orally in doses of 15-30 mg/kg exerted a significant dose dependent inhibition of carrageenan induced paw oedema. The inhibitory effect of tomatine when given in a dose of 10 mg/kg intramuscularly to intact rats lasted more than 24 hr.3. In adrenalectomized rats significant dose-related inhibition of paw oedema was obtained with tomatine and the inhibition at each dose level (0.5-10 mg/kg) was found to be greater than that found in intact animals.4. Tomatine administered subcutaneously to intact rats daily for 7 days in doses of 5 or 10 mg/kg exerted a significant, dose dependent inhibition of granulation tissue formation induced by the subcutaneous implantation of carrageenan impregnated cotton pellets.5. Tomatine administered to intact mice in a dose of 10 mg/kg subcutaneously 1 hr before the intraperitoneal injection of acidified saline and intravenous pontamine sky blue significantly decreased the leakage of the protein bound dye into the peritoneal cavity.6. Tomatidine, the aglycone of tomatine, was not effective at dose levels of 10-20 mg/kg in any of the three tests.
摘要
  1. 从感染冠瘿病的番茄植株提取物中分离得到或通过商业途径获得的番茄碱,采用三种不同方法对其抗炎活性进行了测试。

  2. 给完整大鼠肌肉注射剂量范围为1 - 10毫克/千克的番茄碱,或口服剂量为15 - 30毫克/千克的番茄碱,对角叉菜胶诱导的爪肿胀产生了显著的剂量依赖性抑制作用。当以10毫克/千克的剂量给完整大鼠肌肉注射番茄碱时,其抑制作用持续超过24小时。

  3. 在肾上腺切除的大鼠中,番茄碱对角叉菜胶诱导的爪肿胀产生了显著的剂量相关抑制作用,并且发现在每个剂量水平(0.5 - 10毫克/千克)的抑制作用都大于在完整动物中观察到的抑制作用。

  4. 给完整大鼠每天皮下注射剂量为5或10毫克/千克的番茄碱,连续注射7天,对皮下植入角叉菜胶浸渍棉球诱导的肉芽组织形成产生了显著的剂量依赖性抑制作用。

  5. 在腹腔注射酸化盐水和静脉注射丽春红天蓝前1小时,给完整小鼠皮下注射剂量为10毫克/千克的番茄碱,显著降低了蛋白质结合染料向腹腔内的渗漏。

  6. 番茄碱的糖苷配基番茄胺,在三种测试中的任何一种中,在剂量水平为10 - 20毫克/千克时均无效。

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