首页> 外文期刊>European Journal of Pharmacology: An International Journal >Effect of triterpenoids on the inflammation induced by protein kinase C activators, neuronally acting irritants and other agents.
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Effect of triterpenoids on the inflammation induced by protein kinase C activators, neuronally acting irritants and other agents.

机译:三萜类化合物对蛋白激酶C激活剂,神经元刺激物和其他药物诱导的炎症的影响。

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摘要

In order to establish the mode of the anti-inflammatory activity of triterpenoids, 11 naturally occurring compounds were assayed on mouse ear oedema induced by the protein kinase C activators, mezerein, 12-O-tetradecanoylphorbol-13-acetate (TPA), two 12-deoxyphorbol-13-monoesters (13-tetradecanoate (DPT) and 13-phenylacetate (DPP)) and bryostatin 1, and by resiniferatoxin, xylene and arachidonic acid. The effects on bradykinin-induced paw oedema and on the rat skin inflammation caused by hydrogen peroxide were also examined. The oedema induced by mezerein and DPT was reduced to different extents by the triterpenoids administered epicutaneously (0.5 mg per ear). Against DPT-induced oedema, lupane and oleanane derivatives were the most effective compounds. Oleananes and lupanes possessing a carboxyl group were active against bryostatin 1-induced oedema. Most of the triterpenoids were ineffective against the neurogenic inflammation caused by resiniferatoxin and xylene. Many triterpenoids, especially oleanane and lupane alcoholic derivatives, were active against the plantar oedema induced by bradykinin and on the intradermal inflammation induced by hydrogen peroxide. In conclusion, the anti-inflammatory activity of triterpenoids may depend on inhibition of protein kinase C, without any involvement of neurogenic inflammatory mechanisms.
机译:为了建立三萜类化合物的抗炎活性模式,对11种天然存在的化合物进行了测定,这些化合物是由蛋白激酶C激活剂,美塞瑞因,12-O-十四烷酰佛波醇13-乙酸盐(TPA)诱导的,两个12 -脱氧佛波醇13-单酯(13-十四烷酸酯(DPT)和13-苯乙酸酯(DPP))和bryostatin 1,并由树脂毒素,二甲苯和花生四烯酸。还检查了对缓激肽诱导的爪水肿和过氧化氢引起的大鼠皮肤炎症的影响。皮下注射三萜类化合物(每只耳朵0.5毫克)可减轻美塞瑞因和DPT引起的水肿程度。针对DPT引起的水肿,卢烷和齐墩果烷衍生物是最有效的化合物。带有羧基的齐墩果烷和羽扇豆具有抑制bryostatin 1诱导的水肿的作用。大多数三萜类化合物对由树脂毒素和二甲苯引起的神经性炎症无效。许多三萜类化合物,特别是齐墩果烷和羽扇烷醇衍生物,对缓激肽引起的足底水肿和过氧化氢引起的皮内炎症具有活性。总之,三萜类化合物的抗炎活性可能取决于对蛋白激酶C的抑制作用,而没有任何神经源性炎症机制的参与。

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