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林可霉素类 8-10,弹性蛋白酶抑制剂,具有来源于海洋蓝藻 Lyngbya semiplena 的环状 depsipeptide 支架。

Lyngbyastatins 8-10, elastase inhibitors with cyclic depsipeptide scaffolds isolated from the marine cyanobacterium Lyngbya semiplena.

机构信息

Department of Medicinal Chemistry, University of Florida, 1600 SW Archer Road, Gainesville, FL 32610, USA.

出版信息

Mar Drugs. 2009 Nov 3;7(4):528-38. doi: 10.3390/md7040528.

Abstract

Investigation of an extract from the marine cyanobacterium Lyngbya semiplena, collected in Tumon Bay, Guam, led to the identification of three new cyclodepsipeptides, lyngbyastatins 8-10 (1-3). The structures of 1-3 were determined by NMR, MS, ESIMS fragmentation and chemical degradation. Compounds 1-3 are closely related to lyngbyastatins 4-7. Like the latter compounds, we found 1-3 to inhibit porcine pancreatic elastase, with IC(50) values of 123 nM, 210 nM and 120 nM, respectively.

摘要

从关岛图蒙湾采集的海洋蓝藻 Lyngbya semiplena 提取物的研究,鉴定出三种新型环二肽,即 Lyngbyastatin 8-10(1-3)。通过 NMR、MS、ESIMS 碎裂和化学降解确定了 1-3 的结构。化合物 1-3 与 Lyngbyastatin 4-7 密切相关。与后一种化合物一样,我们发现 1-3 抑制猪胰弹性蛋白酶,其 IC50 值分别为 123 nM、210 nM 和 120 nM。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/060f/2810234/c9bb17e89b02/marinedrugs-07-00528f1.jpg

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