Lyngbyastatins 8-10, Elastase Inhibitors with Cyclic Depsipeptide Scaffolds Isolated from the Marine Cyanobacterium Lyngbya semiplena

被引:69
作者
Kwan, Jason C. [1 ]
Taori, Kanchan [1 ]
Paul, Valerie J. [2 ]
Luesch, Hendrik [1 ]
机构
[1] Univ Florida, Dept Med Chem, Gainesville, FL 32610 USA
[2] Smithsonian Marine Stn, Ft Pierce, FL 34949 USA
关键词
lyngbyastatins; cyanobacteria; Lyngbya semiplena; cyclic depsipeptides; elastase inhibitors; SERINE-PROTEASE INHIBITORS; MICROCYSTIS-AERUGINOSA; POTENT; N-GREATER-THAN-3; CONFERVOIDES; CYTOTOXIN; PEPTIDES; SPECTRA; NMR;
D O I
10.3390/md7040528
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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 IC50 values of 123 nM, 210 nM and 120 nM, respectively.
引用
收藏
页码:528 / 538
页数:11
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