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The search for novel human pancreatic alpha-amylase inhibitors: High-throughput screening of terrestrial and marine natural product extracts

TitleThe search for novel human pancreatic alpha-amylase inhibitors: High-throughput screening of terrestrial and marine natural product extracts
Publication TypeJournal Article
Year of Publication2008
AuthorsTarling, CA, Woods, K, Zhang, R, Brastianos, HC, Brayer, GD, Andersen, RJ, Withers, SG
JournalChembiochem
Volume9
Pagination433-438
Date PublishedJan
ISBN Number1439-4227
Abstract

Specific inhibitors of human pancreatic a-amylase (HPA) have potential as oral agents for the control of blood glucose levels in the treatment of diabetes and obesity. In a search for novel inhibitors, a library of 30000 crude biological extracts of terrestrial and marine origin has been screened. A number of inhibitory extracts were identified, of which the most potent was subjected to 1 bioassay-guided purification. A family of three glycosylated acyl flavonols, montbretins A-C-1 was thereby identified and characterized as competitive amylase inhibitors, with K-i values ranging from 8.1-6100 nm. Competitive inhibition by myricetin, which corresponds to the flavone core, and noncompetitive inhibition by a second fragment, ethyl caffeiate, suggest a binding mode for these inhibitors.

URL<Go to ISI>://000253460000016