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一种新型合成类维生素A化合物(一种聚戊烯酸衍生物,E-5166)可抑制表皮生长因子刺激的花生四烯酸释放。

A novel synthetic vitamin A-like compound (a polyprenoic acid derivative, E-5166) inhibits the release of arachidonic acid stimulated by epidermal growth factor.

作者信息

Suya H, Aoyagi T, Koizumi H, Fukaya T, Nemoto O

出版信息

J Invest Dermatol. 1987 May;88(5):630-3. doi: 10.1111/1523-1747.ep12470238.

Abstract

Little is known about the mechanisms of anti-inflammatory activity of retinoids. A new synthetic vitamin A-like compound (polyprenoic acid derivative, E-5166) has a strong in vitro binding affinity to intracellular binding proteins for acidic retinoids. In order to elucidate the anti-inflammatory activity of E-5166, we studied the effect of E-5166 on the epidermal growth factor (EGF)-stimulated arachidonic acid (AA) release of pig epidermis. E-5166 significantly inhibited the EGF-stimulated AA release and this inhibitory effect of E-5166 required a longer incubation than hydrocortisone did. Furthermore, E-5166 inhibited the EGF-stimulated phosphatidylinositol (PI) turnover of pig epidermis. These results indicate that E-5166 inhibited the EGF-stimulated AA release through the inhibition of the EGF-stimulated PI turnover.

摘要

关于类视黄醇抗炎活性的机制人们所知甚少。一种新的合成类维生素A化合物(聚戊烯酸衍生物,E-5166)对酸性类视黄醇的细胞内结合蛋白具有很强的体外结合亲和力。为了阐明E-5166的抗炎活性,我们研究了E-5166对表皮生长因子(EGF)刺激的猪表皮花生四烯酸(AA)释放的影响。E-5166显著抑制了EGF刺激的AA释放,且E-5166的这种抑制作用比氢化可的松需要更长的孵育时间。此外,E-5166抑制了EGF刺激的猪表皮磷脂酰肌醇(PI)周转。这些结果表明,E-5166通过抑制EGF刺激的PI周转来抑制EGF刺激的AA释放。

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