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Palmyrolide A,一种来自帕劳环礁蓝藻的具有不同寻常稳定性的神经活性大环内酯。

Palmyrolide A, an unusually stabilized neuroactive macrolide from Palmyra Atoll cyanobacteria.

机构信息

Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography and Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, La Jolla, California 92037, USA.

出版信息

Org Lett. 2010 Oct 15;12(20):4490-3. doi: 10.1021/ol101752n.

Abstract

Palmyrolide A (1) is a new neuroactive macrolide isolated from a marine cyanobacterial assemblage composed of Leptolyngbya cf. and Oscillatoria spp. collected from Palmyra Atoll. It features a rare N-methyl enamide and an intriguing t-butyl branch; the latter renders the adjacent lactone ester bond resistant to hydrolysis. Consistent with its significant suppression of calcium influx in cerebrocortical neurons (IC(50) = 3.70 μM), palmyrolide A (1) showed a relatively potent sodium channel blocking activity in neuro-2a cells (IC(50) = 5.2 μM), without appreciable cytotoxicity.

摘要

棕榈醇 A(1)是一种从海洋蓝藻共生体中分离得到的新型神经活性大环内酯,该共生体由来自帕尔米拉环礁的 Leptolyngbya cf. 和 Oscillatoria spp. 组成。它具有罕见的 N-甲基烯酰胺和有趣的叔丁基支链;后者使相邻的内酯酯键不易水解。棕榈醇 A(1)显著抑制大脑皮质神经元中的钙内流(IC(50)=3.70 μM),因此具有相对较强的神经-2a 细胞钠通道阻断活性(IC(50)=5.2 μM),且无明显细胞毒性。

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