脱水穿心莲内酯琥珀酸半酯的药理作用研究Ⅰ.抗炎作用
PHARMACOLOGICAL STUDIES ON 14-DEOXY-11,12-DIDEHYDROANDROGRAPHOLIDE-3,19-DISUCCINATE Ⅰ.Anti-inflammatory Activity
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摘要: 腹腔注射或皮下注射本品128~250 mg/kg,对二甲苯、组织胺、醋酸等所致小白鼠皮肤或腹腔毛细血管通透性增高、蛋清所致大鼠足肿胀及巴豆油所致炎性渗出均有明显的抑制作用,但对肉芽组织增生无明显影响。由于去除肾上腺后其抗炎作用消失,本品也不能延长去肾上腺幼年大白鼠的生存时间,但可引起幼年小白鼠胸腺萎缩、明显降低大白鼠肾上腺中维生素C的含量,多次给药并可增加垂体前叶中ACTH的含量,因此说明本品不具有肾上腺皮质激素样作用,但能兴奋垂体——肾上腺皮质系统功能,这一作用是在于促进了垂体前叶ACTH的合成和释放。继以大白鼠肾上腺中维生素C含量降低为指标,分析了本品作用的部位,结果表明,动物去除垂体后,此作用消失,戊巴比妥钠麻醉,作用仍然存在,但在戊巴比妥钠麻醉的基础上,吗啡、地塞米松、氯丙嗪等均能完全阻断本品降低肾上腺中维生素C含量的作用,上述结果提示本品兴奋垂体——肾上腺皮质系统功能的作用部位可能在皮层下中枢。Abstract: The monopotassium salt of 14-Deoxy-11, 12-didehydroandrographolide-3,19-disuccinate (DAS) neutralized with equivalentamount of sodium bicarbonate is an aqueous soluble preparation derived from andrographolide which is the principal composition of Andrographis paniculata Ness. DAS was reported to have therapeutic effect on pneumonia and upper respiratory tract infection of virus origin. We investigated its anti-inflammatory activity in mice and rats. The experimental results showed that DAS significantly inhibited the increase of capillary permeabilities induced by various phlogistic stimulations and exudation induced by croton oil, but had no effect on granuloma formation around cotton pellet or in granuloma pouch. DAS was found to inhibit egg-white induced edema of the hind paw in intact rats but not in adrenalectomized animals. DAS induced marked involution of the thymus in immature mice and significantly depleted the content of adrenal ascorbic acid of rats. However, this action of DAS was abolished by hypophysecton(?)y. After five consecutive daily injections of DAS the ACTH content of the pituitary gland some increased with significant depletion of adrenal ascorbic acid content in rats. These results indicate that the anti-inflammatory activity of DAS is presumably due to increasing synthesis and release of ACTH of the pituitary gland.
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