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来自巴氏软珊瑚的bastadin 20和bastadin O - 硫酸酯:Ry1R FKBP12受体复合物的新型调节剂。

Bastadin 20 and bastadin O-sulfate esters from Ianthella basta: novel modulators of the Ry1R FKBP12 receptor complex.

作者信息

Franklin M A, Penn S G, Lebrilla C B, Lam T H, Pessah I N, Molinski T F

机构信息

Department of Chemistry, University of California, Davis 95616, USA.

出版信息

J Nat Prod. 1996 Dec;59(12):1121-7. doi: 10.1021/np960507g.

Abstract

New compounds bastadin 20 (9), 15,34-O-disulfatobastadin 7 (10), and 10-O-sulfatobastadin 3 (11) were isolated from Ianthella basta collected in Exmouth Gulf, Western Australia. Compounds 10 and 11 exhibited moderate differential activity as SR Ca2+ channel agonists (EC50 13.6 and 100 microM, respectively) of the Ry1R FKBP12 complex, while the potency of 9 was almost half that of 10 (EC50 20.6 microM). The problem of dereplication of bastadins was addressed using 1H-NMR "fingerprinting" of MeO signals in the corresponding permethyl bastadin derivatives.

摘要

从采集于西澳大利亚埃克斯茅斯湾的巴氏软珊瑚(Ianthella basta)中分离出了新化合物bastadin 20(9)、15,34 - O - 二硫酸化bastadin 7(10)和10 - O - 硫酸化bastadin 3(11)。化合物10和11作为兰尼碱受体1(Ry1R)FKBP12复合物的肌浆网Ca2+通道激动剂表现出中等程度的差异活性(EC50分别为13.6和100微摩尔),而化合物9的效力几乎是化合物10的一半(EC50为20.6微摩尔)。利用相应全甲基化bastadin衍生物中MeO信号的1H - NMR“指纹图谱”解决了bastadins的重复鉴定问题。

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