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一种来源于澳大利亚海绵 Ianthella flabelliformis 的具有强效和选择性 δ-阿片受体结合亲和力的bastadin。

A bastadin with potent and selective delta-opioid receptor binding affinity from the Australian sponge Ianthella flabelliformis.

机构信息

Eskitis Institute, Griffith University, Brisbane, Queensland, 4111, Australia.

出版信息

J Nat Prod. 2010 Jun 25;73(6):1173-6. doi: 10.1021/np100010z.

DOI:10.1021/np100010z
PMID:20575589
Abstract

Three new bastadins, bastadin 25 (1), 15-O-sulfonatobastadin 11 (2), and bastadin 26 (3), were isolated from a MeOH extract of the Australian marine sponge Ianthella flabelliformis. Their structures were determined by interpretation of 1D and 2D NMR spectra and mass spectrometry. Bastadin 26 (3) showed potent affinity for the guinea pig delta-opioid receptors with a K(i) value of 100 nM. The other two bastadins had a 100-fold lower affinity. The three compounds were also tested for their affinity to guinea pig micro- and kappa-opioid receptors and shown to have either no affinity or only very weak affinity toward both of these opioid receptors.

摘要

三种新的巴斯塔丁,巴斯塔丁 25(1)、15-O-磺酸钠巴斯塔丁 11(2)和巴斯塔丁 26(3),从澳大利亚海洋海绵 Ianthella flabelliformis 的甲醇提取物中分离得到。通过一维和二维 NMR 光谱和质谱解析确定了它们的结构。巴斯塔丁 26(3)对豚鼠 δ-阿片受体具有很强的亲和力,Ki 值为 100 nM。另外两种巴斯塔丁的亲和力低 100 倍。这三种化合物还测试了它们对豚鼠 μ-和 κ-阿片受体的亲和力,结果表明它们对这两种阿片受体均无亲和力或仅有非常弱的亲和力。

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