Biochemical and biological assessment of the inhibitory potency of extracts from vinification byproducts of Vitis vinifera extracts against glycogen phosphorylase
[Display omitted] •Antidiabetic potency of 13 polyphenolic extracts from vinification byproducts of Greek varieties of Vitis vinifera assessed.•All extract display strong inhibitory potency against glycogen phosphorylase.•X-ray crystallography screening revealed that quercetin is the most bioactive...
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creator | Kantsadi, Anastassia L. Apostolou, Anna Theofanous, Stavroula Stravodimos, George A. Kyriakis, Efthimios Gorgogietas, Vyron A. Chatzileontiadou, Demetra S.M. Pegiou, Kalliope Skamnaki, Vassiliki T. Stagos, Dimitrios Kouretas, Dimitrios Psarra, Anna-Maria G. Haroutounian, Serkos A. Leonidas, Demetres D. |
description | [Display omitted]
•Antidiabetic potency of 13 polyphenolic extracts from vinification byproducts of Greek varieties of Vitis vinifera assessed.•All extract display strong inhibitory potency against glycogen phosphorylase.•X-ray crystallography screening revealed that quercetin is the most bioactive compound.•The most potent extract has a moderate effect on glycogenolysis in the cellular lever with IC50=17.35μg/mL.
The inhibitory potency of thirteen polyphenolic extracts obtained from vinification byproducts of Greek varieties of Vitis vinifera against glycogen phosphorylase (GP) has been studied by kinetic experiments. GP is an enzyme involved in glucose homeostasis and a molecular target for the discovery of new hypoglycemic agents. Studies have shown that all extracts display significant inhibitory potency for GP in vitro with IC50 values in the range of low μg/mL. X-ray crystallographic analysis of GP crystals soaked with two of these extracts revealed that the most active ingredient is quercetin which binds at novel binding site, distinct from the other known sites of the enzyme. One of the most potent of the studied extracts had also a moderate effect on glycogenolysis in the cellular lever with an IC50 value of 17.35μg/mL. These results highlight the importance of natural resources in the quest for the discovery of new hypoglycemic agents, while at the same time they can serve as the starting point for their exploitation for antidiabetic usage and the development of novel biofunctional foods. |
doi_str_mv | 10.1016/j.fct.2014.01.055 |
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•Antidiabetic potency of 13 polyphenolic extracts from vinification byproducts of Greek varieties of Vitis vinifera assessed.•All extract display strong inhibitory potency against glycogen phosphorylase.•X-ray crystallography screening revealed that quercetin is the most bioactive compound.•The most potent extract has a moderate effect on glycogenolysis in the cellular lever with IC50=17.35μg/mL.
The inhibitory potency of thirteen polyphenolic extracts obtained from vinification byproducts of Greek varieties of Vitis vinifera against glycogen phosphorylase (GP) has been studied by kinetic experiments. GP is an enzyme involved in glucose homeostasis and a molecular target for the discovery of new hypoglycemic agents. Studies have shown that all extracts display significant inhibitory potency for GP in vitro with IC50 values in the range of low μg/mL. X-ray crystallographic analysis of GP crystals soaked with two of these extracts revealed that the most active ingredient is quercetin which binds at novel binding site, distinct from the other known sites of the enzyme. One of the most potent of the studied extracts had also a moderate effect on glycogenolysis in the cellular lever with an IC50 value of 17.35μg/mL. These results highlight the importance of natural resources in the quest for the discovery of new hypoglycemic agents, while at the same time they can serve as the starting point for their exploitation for antidiabetic usage and the development of novel biofunctional foods.</description><identifier>ISSN: 0278-6915</identifier><identifier>EISSN: 1873-6351</identifier><identifier>DOI: 10.1016/j.fct.2014.01.055</identifier><identifier>PMID: 24556570</identifier><identifier>CODEN: FCTOD7</identifier><language>eng</language><publisher>Oxford: Elsevier Ltd</publisher><subject>Bioactive polyphenols ; Biological and medical sciences ; Biological effects of radiation ; Diabetes. Impaired glucose tolerance ; Endocrine pancreas. Apud cells (diseases) ; Endocrinopathies ; Etiopathogenesis. Screening. Investigations. Target tissue resistance ; Food toxicology ; Fundamental and applied biological sciences. Psychology ; Glycogen metabolism ; Glycogen phosphorylase ; Glycogen Phosphorylase - antagonists & inhibitors ; Ionizing radiations ; Medical sciences ; Models, Molecular ; Plant Extracts - chemistry ; Plant Extracts - pharmacology ; Tissues, organs and organisms biophysics ; Toxicology ; Type 2 diabetes ; Vinification byproducts ; Vitis - chemistry ; Vitis vinifera ; X-ray crystallography</subject><ispartof>Food and chemical toxicology, 2014-05, Vol.67, p.35-43</ispartof><rights>2014 Elsevier Ltd</rights><rights>2015 INIST-CNRS</rights><rights>Copyright © 2014 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c416t-de197ca5856757df26c6fe2e435784268e9a94ebf25bafc6f4a47685548ebe9e3</citedby><cites>FETCH-LOGICAL-c416t-de197ca5856757df26c6fe2e435784268e9a94ebf25bafc6f4a47685548ebe9e3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.fct.2014.01.055$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=28423682$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/24556570$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kantsadi, Anastassia L.</creatorcontrib><creatorcontrib>Apostolou, Anna</creatorcontrib><creatorcontrib>Theofanous, Stavroula</creatorcontrib><creatorcontrib>Stravodimos, George A.</creatorcontrib><creatorcontrib>Kyriakis, Efthimios</creatorcontrib><creatorcontrib>Gorgogietas, Vyron A.</creatorcontrib><creatorcontrib>Chatzileontiadou, Demetra S.M.</creatorcontrib><creatorcontrib>Pegiou, Kalliope</creatorcontrib><creatorcontrib>Skamnaki, Vassiliki T.</creatorcontrib><creatorcontrib>Stagos, Dimitrios</creatorcontrib><creatorcontrib>Kouretas, Dimitrios</creatorcontrib><creatorcontrib>Psarra, Anna-Maria G.</creatorcontrib><creatorcontrib>Haroutounian, Serkos A.</creatorcontrib><creatorcontrib>Leonidas, Demetres D.</creatorcontrib><title>Biochemical and biological assessment of the inhibitory potency of extracts from vinification byproducts of Vitis vinifera extracts against glycogen phosphorylase</title><title>Food and chemical toxicology</title><addtitle>Food Chem Toxicol</addtitle><description>[Display omitted]
•Antidiabetic potency of 13 polyphenolic extracts from vinification byproducts of Greek varieties of Vitis vinifera assessed.•All extract display strong inhibitory potency against glycogen phosphorylase.•X-ray crystallography screening revealed that quercetin is the most bioactive compound.•The most potent extract has a moderate effect on glycogenolysis in the cellular lever with IC50=17.35μg/mL.
The inhibitory potency of thirteen polyphenolic extracts obtained from vinification byproducts of Greek varieties of Vitis vinifera against glycogen phosphorylase (GP) has been studied by kinetic experiments. GP is an enzyme involved in glucose homeostasis and a molecular target for the discovery of new hypoglycemic agents. Studies have shown that all extracts display significant inhibitory potency for GP in vitro with IC50 values in the range of low μg/mL. X-ray crystallographic analysis of GP crystals soaked with two of these extracts revealed that the most active ingredient is quercetin which binds at novel binding site, distinct from the other known sites of the enzyme. One of the most potent of the studied extracts had also a moderate effect on glycogenolysis in the cellular lever with an IC50 value of 17.35μg/mL. These results highlight the importance of natural resources in the quest for the discovery of new hypoglycemic agents, while at the same time they can serve as the starting point for their exploitation for antidiabetic usage and the development of novel biofunctional foods.</description><subject>Bioactive polyphenols</subject><subject>Biological and medical sciences</subject><subject>Biological effects of radiation</subject><subject>Diabetes. Impaired glucose tolerance</subject><subject>Endocrine pancreas. Apud cells (diseases)</subject><subject>Endocrinopathies</subject><subject>Etiopathogenesis. Screening. Investigations. Target tissue resistance</subject><subject>Food toxicology</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Glycogen metabolism</subject><subject>Glycogen phosphorylase</subject><subject>Glycogen Phosphorylase - antagonists & inhibitors</subject><subject>Ionizing radiations</subject><subject>Medical sciences</subject><subject>Models, Molecular</subject><subject>Plant Extracts - chemistry</subject><subject>Plant Extracts - pharmacology</subject><subject>Tissues, organs and organisms biophysics</subject><subject>Toxicology</subject><subject>Type 2 diabetes</subject><subject>Vinification byproducts</subject><subject>Vitis - chemistry</subject><subject>Vitis vinifera</subject><subject>X-ray crystallography</subject><issn>0278-6915</issn><issn>1873-6351</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2014</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kcuO1DAQRSMEYpqBD2CDvEFik8ZO_EjEihnxkkZiA2wtxyl3u5XYjcs9Ir_Dl-JWGmbHwrKse25VuW5VvWR0yyiTbw9bZ_O2oYxvKdtSIR5VG9aptpatYI-rDW1UV8ueiavqGeKBUqqYkk-rq4YLIYWim-r3jY92D7O3ZiImjGTwcYq79YkIiDOETKIjeQ_Eh70ffI5pIceYIdjlrMCvnIzNSFyKM7n3wbvizz4GMizHFMfTWSzgD589rgAk8-AzO-MDZrKbFht3EMhxH7GctEwG4Xn1xJkJ4cXlvq6-f_zw7fZzfff105fb93e15UzmegTWK2tEJ6QSanSNtNJBA7wVquON7KA3PYfBNWIwrmjccCU7IXgHA_TQXldv1rpl5J8nwKxnjxamyQSIJ9RMKtnyntKuoGxFbYqICZw-Jj-btGhG9TkafdAlGn2ORlOmSzTF8-pS_jTMMP5z_M2iAK8vgMGyfpdMsB4fuPKJVnZN4d6tHJRl3HtIGq0vWcDoE5SmY_T_GeMP9nexOA</recordid><startdate>20140501</startdate><enddate>20140501</enddate><creator>Kantsadi, Anastassia L.</creator><creator>Apostolou, Anna</creator><creator>Theofanous, Stavroula</creator><creator>Stravodimos, George A.</creator><creator>Kyriakis, Efthimios</creator><creator>Gorgogietas, Vyron A.</creator><creator>Chatzileontiadou, Demetra S.M.</creator><creator>Pegiou, Kalliope</creator><creator>Skamnaki, Vassiliki T.</creator><creator>Stagos, Dimitrios</creator><creator>Kouretas, Dimitrios</creator><creator>Psarra, Anna-Maria G.</creator><creator>Haroutounian, Serkos A.</creator><creator>Leonidas, Demetres D.</creator><general>Elsevier Ltd</general><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7U7</scope><scope>C1K</scope></search><sort><creationdate>20140501</creationdate><title>Biochemical and biological assessment of the inhibitory potency of extracts from vinification byproducts of Vitis vinifera extracts against glycogen phosphorylase</title><author>Kantsadi, Anastassia L. ; Apostolou, Anna ; Theofanous, Stavroula ; Stravodimos, George A. ; Kyriakis, Efthimios ; Gorgogietas, Vyron A. ; Chatzileontiadou, Demetra S.M. ; Pegiou, Kalliope ; Skamnaki, Vassiliki T. ; Stagos, Dimitrios ; Kouretas, Dimitrios ; Psarra, Anna-Maria G. ; Haroutounian, Serkos A. ; Leonidas, Demetres D.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c416t-de197ca5856757df26c6fe2e435784268e9a94ebf25bafc6f4a47685548ebe9e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2014</creationdate><topic>Bioactive polyphenols</topic><topic>Biological and medical sciences</topic><topic>Biological effects of radiation</topic><topic>Diabetes. Impaired glucose tolerance</topic><topic>Endocrine pancreas. Apud cells (diseases)</topic><topic>Endocrinopathies</topic><topic>Etiopathogenesis. Screening. Investigations. Target tissue resistance</topic><topic>Food toxicology</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>Glycogen metabolism</topic><topic>Glycogen phosphorylase</topic><topic>Glycogen Phosphorylase - antagonists & inhibitors</topic><topic>Ionizing radiations</topic><topic>Medical sciences</topic><topic>Models, Molecular</topic><topic>Plant Extracts - chemistry</topic><topic>Plant Extracts - pharmacology</topic><topic>Tissues, organs and organisms biophysics</topic><topic>Toxicology</topic><topic>Type 2 diabetes</topic><topic>Vinification byproducts</topic><topic>Vitis - chemistry</topic><topic>Vitis vinifera</topic><topic>X-ray crystallography</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kantsadi, Anastassia L.</creatorcontrib><creatorcontrib>Apostolou, Anna</creatorcontrib><creatorcontrib>Theofanous, Stavroula</creatorcontrib><creatorcontrib>Stravodimos, George A.</creatorcontrib><creatorcontrib>Kyriakis, Efthimios</creatorcontrib><creatorcontrib>Gorgogietas, Vyron A.</creatorcontrib><creatorcontrib>Chatzileontiadou, Demetra S.M.</creatorcontrib><creatorcontrib>Pegiou, Kalliope</creatorcontrib><creatorcontrib>Skamnaki, Vassiliki T.</creatorcontrib><creatorcontrib>Stagos, Dimitrios</creatorcontrib><creatorcontrib>Kouretas, Dimitrios</creatorcontrib><creatorcontrib>Psarra, Anna-Maria G.</creatorcontrib><creatorcontrib>Haroutounian, Serkos A.</creatorcontrib><creatorcontrib>Leonidas, Demetres D.</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Toxicology Abstracts</collection><collection>Environmental Sciences and Pollution Management</collection><jtitle>Food and chemical toxicology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kantsadi, Anastassia L.</au><au>Apostolou, Anna</au><au>Theofanous, Stavroula</au><au>Stravodimos, George A.</au><au>Kyriakis, Efthimios</au><au>Gorgogietas, Vyron A.</au><au>Chatzileontiadou, Demetra S.M.</au><au>Pegiou, Kalliope</au><au>Skamnaki, Vassiliki T.</au><au>Stagos, Dimitrios</au><au>Kouretas, Dimitrios</au><au>Psarra, Anna-Maria G.</au><au>Haroutounian, Serkos A.</au><au>Leonidas, Demetres D.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Biochemical and biological assessment of the inhibitory potency of extracts from vinification byproducts of Vitis vinifera extracts against glycogen phosphorylase</atitle><jtitle>Food and chemical toxicology</jtitle><addtitle>Food Chem Toxicol</addtitle><date>2014-05-01</date><risdate>2014</risdate><volume>67</volume><spage>35</spage><epage>43</epage><pages>35-43</pages><issn>0278-6915</issn><eissn>1873-6351</eissn><coden>FCTOD7</coden><abstract>[Display omitted]
•Antidiabetic potency of 13 polyphenolic extracts from vinification byproducts of Greek varieties of Vitis vinifera assessed.•All extract display strong inhibitory potency against glycogen phosphorylase.•X-ray crystallography screening revealed that quercetin is the most bioactive compound.•The most potent extract has a moderate effect on glycogenolysis in the cellular lever with IC50=17.35μg/mL.
The inhibitory potency of thirteen polyphenolic extracts obtained from vinification byproducts of Greek varieties of Vitis vinifera against glycogen phosphorylase (GP) has been studied by kinetic experiments. GP is an enzyme involved in glucose homeostasis and a molecular target for the discovery of new hypoglycemic agents. Studies have shown that all extracts display significant inhibitory potency for GP in vitro with IC50 values in the range of low μg/mL. X-ray crystallographic analysis of GP crystals soaked with two of these extracts revealed that the most active ingredient is quercetin which binds at novel binding site, distinct from the other known sites of the enzyme. One of the most potent of the studied extracts had also a moderate effect on glycogenolysis in the cellular lever with an IC50 value of 17.35μg/mL. These results highlight the importance of natural resources in the quest for the discovery of new hypoglycemic agents, while at the same time they can serve as the starting point for their exploitation for antidiabetic usage and the development of novel biofunctional foods.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>24556570</pmid><doi>10.1016/j.fct.2014.01.055</doi><tpages>9</tpages></addata></record> |
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subjects | Bioactive polyphenols Biological and medical sciences Biological effects of radiation Diabetes. Impaired glucose tolerance Endocrine pancreas. Apud cells (diseases) Endocrinopathies Etiopathogenesis. Screening. Investigations. Target tissue resistance Food toxicology Fundamental and applied biological sciences. Psychology Glycogen metabolism Glycogen phosphorylase Glycogen Phosphorylase - antagonists & inhibitors Ionizing radiations Medical sciences Models, Molecular Plant Extracts - chemistry Plant Extracts - pharmacology Tissues, organs and organisms biophysics Toxicology Type 2 diabetes Vinification byproducts Vitis - chemistry Vitis vinifera X-ray crystallography |
title | Biochemical and biological assessment of the inhibitory potency of extracts from vinification byproducts of Vitis vinifera extracts against glycogen phosphorylase |
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