New Peptolides from the Cyanobacterium Nostoc insulare as Selective and Potent Inhibitors of Human Leukocyte Elastase

被引：26

作者：

Mehner, Christian ^{[1
]}

Mueller, Daniela ^{[1
]}

Kehraus, Stefan ^{[1
]}

Hautmann, Stephanie ^{[2
]}

Guetschow, Michael ^{[2
]}

Koenig, Gabriele M. ^{[1
]}

机构：

[1] Univ Bonn, Inst Pharmaceut Biol, D-53115 Bonn, Germany

[2] Univ Bonn, D-53121 Bonn, Germany

来源：

CHEMBIOCHEM | 2008年 / 9卷 / 16期

关键词：

cyanobacteria; enzymes; natural products; peptides; structure elucidation;

D O I：

10.1002/cbic.200800415

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Eight new cyanopeptolins (insulapeptolides A-H) were obtained from the cyanobacterium Nostoc insulare. Their isolation was guided by their bioactivity toward the target enzyme human leukocyte elastase, molecular biological investigations, and MALDI-TOF analysis. These peptides are selective inhibitors of human leukocyte elastase with activities in the nanomolar range. Insulapeptolide D (4) was the most potent compound with an IC50 value of 85 nM (K-i value of 36 nM).

引用

页码：2692 / 2703

页数：12

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