Thrombin Inhibitors from the Freshwater Cyanobacterium Anabaena compacta

Bioassay-guided investigation of the cyanobacterium Anabaena compacta extracts afforded spumigin J (1) and the known thrombin inhibitor spumigin A (2). The absolute configuration of 1 was analyzed by advanced Marfey’s methodology. Compounds 1 and 2 inhibited thrombin with EC50 values of 4.9 and 2.1...

Full description

Saved in:
Bibliographic Details
Published in:Journal of natural products (Washington, D.C.) D.C.), 2012-09, Vol.75 (9), p.1546-1552
Main Authors: Anas, Andrea Roxanne J, Kisugi, Takaya, Umezawa, Taiki, Matsuda, Fuyuhiko, Campitelli, Marc R, Quinn, Ronald J, Okino, Tatsufumi
Format: Article
Language:English
Subjects:
Anabaena
Anabaena - chemistry
Cyanobacteria
Fresh Water - microbiology
Molecular Structure
Nuclear Magnetic Resonance, Biomolecular
Proline - analogs & derivatives
Proline - chemistry
Thrombin - antagonists & inhibitors
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Bioassay-guided investigation of the cyanobacterium Anabaena compacta extracts afforded spumigin J (1) and the known thrombin inhibitor spumigin A (2). The absolute configuration of 1 was analyzed by advanced Marfey’s methodology. Compounds 1 and 2 inhibited thrombin with EC50 values of 4.9 and 2.1 μM, and 0.7 and 0.2 μM in the cathepsin B inhibitory assay, respectively. The MM-GBSA methodology predicted spumigin A with 2S-4-methylproline as the better thrombin inhibitor.
ISSN:0163-3864
1520-6025
DOI:10.1021/np300282a