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米拉巴美定 E-H,来源于海绵 Stelletta clavosa 的具有抗 HIV 活性的环肽。

Mirabamides E-H, HIV-inhibitory depsipeptides from the sponge Stelletta clavosa.

机构信息

Department of Medicinal Chemistry, University of Utah, Salt Lake City, Utah 84112, USA.

出版信息

J Nat Prod. 2011 Feb 25;74(2):185-93. doi: 10.1021/np100613p. Epub 2011 Jan 31.

DOI:10.1021/np100613p
PMID:21280591
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3072293/
Abstract

Four new depsipeptides, mirabamides E-H (1-4), and the known depsipeptide mirabamide C (5) have been isolated from the sponge Stelletta clavosa, collected from the Torres Strait. The planar structures were determined on the basis of extensive 1D and 2D NMR and HRESIMS. The absolute configurations were established by the advanced Marfey's method, NMR, and GC-MS. The four new compounds all showed strong inhibition of HIV-1 in a neutralization assay with IC(50) values of 121, 62, 68, and 41 nM, respectively.

摘要

从托雷斯海峡采集的海绵 Stelletta clavosa 中分离得到了 4 种新的 depsipeptides,米拉巴米德 E-H(1-4)和已知的 depsipeptide 米拉巴米德 C(5)。基于广泛的 1D 和 2D NMR 和 HRESIMS,确定了平面结构。通过先进的 Marfey 法、NMR 和 GC-MS 确定了绝对构型。这四种新化合物在中和测定中均显示出强烈抑制 HIV-1 的作用,IC50 值分别为 121、62、68 和 41 nM。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f9fa/3072293/7014e8edc507/nihms269406f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f9fa/3072293/b2f7c2c9ede2/nihms269406f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f9fa/3072293/7014e8edc507/nihms269406f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f9fa/3072293/b2f7c2c9ede2/nihms269406f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f9fa/3072293/7014e8edc507/nihms269406f2.jpg

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