Mehner Christian, Müller Daniela, Kehraus Stefan, Hautmann Stephanie, Gütschow Michael, König Gabriele M
Institute for Pharmaceutical Biology, University of Bonn, Nussallee 6, 53115 Bonn, Germany.
Chembiochem. 2008 Nov 3;9(16):2692-703. doi: 10.1002/cbic.200800415.
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 was the most potent compound with an IC(50) value of 85 nM (K(i) value of 36 nM).
从蓝藻门的岛屿念珠藻中获得了8种新的蓝藻肽（胰岛肽A - H）。它们的分离是基于对目标酶人白细胞弹性蛋白酶的生物活性、分子生物学研究以及基质辅助激光解吸电离飞行时间（MALDI - TOF）分析。这些肽是人类白细胞弹性蛋白酶的选择性抑制剂，活性在纳摩尔范围内。胰岛肽D是最有效的化合物，IC(50)值为85 nM（K(i)值为36 nM）。
