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一种来自大叶井口边草蕨的磺基糖脂及其对人中性粒细胞中血小板活化因子受体的作用。

A sulphonoglycolipid from the fern Polypodium decumanum and its effect on the platelet activating-factor receptor in human neutrophils.

作者信息

Vasänge M, Rolfsen W, Bohlin L

机构信息

Department of Pharmacy, Uppsala University, Sweden.

出版信息

J Pharm Pharmacol. 1997 May;49(5):562-6. doi: 10.1111/j.2042-7158.1997.tb06842.x.

Abstract

The South American fern Polypodium decumanum, traditional name calaguala, has documented clinical use in oral treatment of skin disorders, including psoriasis. The inflammatory mediator platelet-activating factor (PAF), has been implicated in the pathogenesis of psoriasis. A constituent of a calaguala extract has been shown to have inhibitory activity in a PAF-induced exocytosis model in human neutrophils. The compound was identified as the sulphoquinovosyl diacylglycerol 1,2-di-O-palmitoyl-3-O-(6-sulpho-alpha-D-quinovopyranosyl)-glycero l by spectroscopic means. When subsequently studied in an in-vitro model for [3H]PAF binding in neutrophils from man the compound caused dose-dependent displacement of [3H]PAF from its receptor with an IC50 value of 2 microM. It is suggested that the compound acts through PAF receptor antagonism in intact human neutrophils.

摘要

南美洲蕨类植物大叶骨牌蕨,传统名称为卡拉瓜拉,有文献记载其在口服治疗包括牛皮癣在内的皮肤疾病方面的临床应用。炎症介质血小板活化因子(PAF)与牛皮癣的发病机制有关。卡拉瓜拉提取物的一种成分已被证明在人中性粒细胞的PAF诱导的胞吐模型中具有抑制活性。通过光谱手段鉴定该化合物为磺基奎诺糖基二酰基甘油1,2 - 二 - O - 棕榈酰基 - 3 - O -(6 - 磺基 - α - D - 奎诺吡喃糖基) - 甘油。随后在人中性粒细胞的[3H]PAF结合体外模型中进行研究时,该化合物导致[3H]PAF从其受体上剂量依赖性地置换,IC50值为2 microM。提示该化合物通过拮抗完整人中性粒细胞中的PAF受体发挥作用。

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