Journal ArticleDOI
The Search for Novel Human Pancreatic α‐Amylase Inhibitors: High‐Throughput Screening of Terrestrial and Marine Natural Product Extracts
Chris A. Tarling,Katherine Woods,Ran Zhang,Harry C. Brastianos,Gary D. Brayer,Raymond J. Andersen,Stephen G. Withers +6 more
TLDR
A family of three glycosylated acyl flavonols, montbretins A–C, was thereby identified and characterized as competitive amylase inhibitors, with Ki values ranging from 8.1–6100 nM, which suggest a binding mode for these inhibitors.Abstract:
Specific inhibitors of human pancreatic alpha-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 30 000 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 bioassay-guided purification. A family of three glycosylated acyl flavonols, montbretins A-C, 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.read more
Citations
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Glycosylation in health and disease.
TL;DR: The broad role of glycans in immunity, cancer, xenotransplantation and glomerular filtration and the potential of ‘glycomedicine’ are discussed.
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Alginate: Current Use and Future Perspectives in Pharmaceutical and Biomedical Applications
TL;DR: The present use and future possibilities ofAlginates as a tool in drug formulation are discussed and biological and pharmacological activity of alginates are described.
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Mechanistic insights into glycosidase chemistry.
TL;DR: The enzymatic hydrolysis of the glycosidic bond continues to gain importance, reflecting the critically important roles complex glycans play in health and disease as well as the rekindled interest in enzymic biomass conversion.
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Potent α-amylase inhibitory activity of Indian Ayurvedic medicinal plants
TL;DR: Results suggests that extracts of Linum usitatisumum, Morus alba and Ocimum tenuiflorum act effectively as PPA inhibitors leading to a reduction in starch hydrolysis and hence eventually to lowered glucose levels.
Journal ArticleDOI
Evaluation of Traditional Indian Antidiabetic Medicinal Plants for Human Pancreatic Amylase Inhibitory Effect In Vitro
TL;DR: Analysis of Ayurvedic Indian medicinal plants subjected to sequential solvent extraction revealed the presence of alkaloids, proteins, tannins, cardiac glycosides, flavonoids, saponins and steroids as probable inhibitory compounds.
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