INHIBITION OF RAT ACUTE INFLAMMATORY PAW EDEMA BY DIHEMIPHTHALATE OF GLYCYRRHETINIC ACID-DERIVATIVES - COMPARISON WITH GLYCYRRHETINIC ACID
INHIBITION OF RAT ACUTE INFLAMMATORY PAW EDEMA BY DIHEMIPHTHALATE OF GLYCYRRHETINIC ACID-DERIVATIVES - COMPARISON WITH GLYCYRRHETINIC ACID
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DOI：
10.1111/j.2042-7158.1993.tb07182.x
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发表时间：
1993-12-01
影响因子：
3.3
通讯作者：
SHIBATA, S
中科院分区：
文献类型：
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作者：
INOUE, H;INOUE, K;SHIBATA, S
将甘草次酸衍生物的二半邻苯二甲酸酯化合物对各种血管活性剂诱导的急性大鼠爪水肿的抗炎作用与母体化合物进行比较。三种二半邻苯二甲酸酯化合物（18β-齐墩果-12-烯-3β,30-二醇二-O-半邻苯二甲酸酯、18β-齐墩果-9(11),12-二酮-3β,30-二醇二-O-半邻苯二甲酸酯和齐墩果-11,13(18)-二烯-3β,30-二醇的二钠盐 二邻半邻苯二甲酸酯）在前3小时内显着抑制角叉菜胶诱导的大鼠足水肿的发展（ED50分别为70、90和108 mg kg（-1），口服），而甘草次酸（ED50，200 mg kg（-1））在角叉菜胶治疗后3小时显示出对足水肿的显着抑制。剂量低于 100 mg kg(-1) 的二半邻苯二甲酸酯化合物还可以抑制由组胺、缓激肽和 PAF 乙醚引起的小鼠爪水肿。然而，这些化合物未能抑制 5-HT 诱导的小鼠爪水肿。甘草次酸对上述刺激物引起的小鼠足爪炎症作用不大。 10(-7)-10(-4) M 的三种化合物抑制组胺诱导的豚鼠离体回肠收缩。然而。 5-HT 和缓激肽的浓度-反应曲线是化合物。这些结果表明，二半邻苯二甲酸酯化合物调节由内源性血管活性剂引起的血管通透性，作为抗炎机制之一。该作用与甘草次酸有很大不同。
The anti-inflammatory profile of dihemiphthalate compounds of glycyrrhetinic acid derivatives in acute rat paw oedema induced by various vasoactive agents was compared with the parent compound. Three dihemiphthalate compounds (the di-sodium salt of 18 beta-olean-12-ene-3 beta,30-diol di-O-hemiphthalate, 18 beta-olean-9(11),12-dione-3 beta,30-diol di-O-hemiphthalate and olean-11,13(18)-diene-3 beta,30-diol di-O-hemiphthalate), significantly inhibited development of carrageenan-induced rat paw oedema during the first 3 h (ED50 70, 90, and 108 mg kg(-1) respectively, p.o.), while glycyrrhetinic acid (ED50, 200 mg kg(-1)) showed a significant inhibition of paw oedema 3 h after carrageenan treatment. The dihemiphthalate compounds also suppressed mouse paw oedema induced by histamine, bradykinin, and PAF acether at doses of less than 100 mg kg(-1). However, these compounds failed to inhibit 5-HT-induced mouse paw oedema. Glycyrrhetinic acid had little effect on mouse paw inflammation induced by the above irritants. The three compounds at 10(-7)-10(-4) M, inhibited histamine-induced contraction of guinea-pig isolated ileum. However. concentration-response curves to 5-HT and bradykinin were compounds. These results suggest that the dihemiphthalate compounds modulate vascular permeability caused by endogenous vasoactive agents as one of the anti-inflammatory mechanisms. This action is quite different from that of glycyrrhetinic acid.