Abstract
Glycogen phosphorylase (GP) is a validated pharmaceutical target for the development of antihyperglycaemic agents. Phytogenic polyphenols, mainly flavonoids and pentacyclic triterpenes, have been found to be potent inhibitors of GP. These compounds have both pharmaceutical and nutraceutical potential for glycemic control in diabetes type 2. This review focuses mainly on the most successful (potent) of these compounds discovered to date. The protein-ligand interactions that form the structural basis of their potencies are discussed, highlighting the potential for exploitation of their scaffolds in the future design of new GP inhibitors.
Keywords: Alpha-glucosidases, antioxidants, diabetes, glycogen phosphorylase, flavonoids, pentacyclic triterpenes.
Current Medicinal Chemistry
Title:Phytogenic Polyphenols as Glycogen Phosphorylase Inhibitors: The Potential of Triterpenes and Flavonoids for Glycaemic Control in Type 2 Diabetes
Volume: 24 Issue: 4
Author(s): George A. Stravodimos, Ben A. Chetter, Efthimios Kyriakis, Anastassia L. Kantsadi, Demetra S.M. Chatzileontiadou, Vassiliki T. Skamnaki, Atsushi Kato, Joseph M. Hayes and Demetres D. Leonidas
Affiliation:
Keywords: Alpha-glucosidases, antioxidants, diabetes, glycogen phosphorylase, flavonoids, pentacyclic triterpenes.
Abstract: Glycogen phosphorylase (GP) is a validated pharmaceutical target for the development of antihyperglycaemic agents. Phytogenic polyphenols, mainly flavonoids and pentacyclic triterpenes, have been found to be potent inhibitors of GP. These compounds have both pharmaceutical and nutraceutical potential for glycemic control in diabetes type 2. This review focuses mainly on the most successful (potent) of these compounds discovered to date. The protein-ligand interactions that form the structural basis of their potencies are discussed, highlighting the potential for exploitation of their scaffolds in the future design of new GP inhibitors.
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Stravodimos A. George, Chetter A. Ben, Kyriakis Efthimios, Kantsadi L. Anastassia, Chatzileontiadou S.M. Demetra, Skamnaki T. Vassiliki, Kato Atsushi, Hayes M. Joseph and Leonidas D. Demetres, Phytogenic Polyphenols as Glycogen Phosphorylase Inhibitors: The Potential of Triterpenes and Flavonoids for Glycaemic Control in Type 2 Diabetes, Current Medicinal Chemistry 2017; 24 (4) . https://dx.doi.org/10.2174/0929867324666161118122534
DOI https://dx.doi.org/10.2174/0929867324666161118122534 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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