Diosgenin from Dioscorea bulbifera: novel hit for treatment of type II diabetes mellitus with inhibitory activity against α-amylase and α-glucosidase
Diabetes mellitus is a multifactorial metabolic disease characterized by post-prandial hyperglycemia (PPHG). α-amylase and α-glucosidase inhibitors aim to explore novel therapeutic agents. Herein we report the promises of Dioscorea bulbifera and its bioactive principle, diosgenin as novel α-amylase...
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| Veröffentlicht in: | PloS one 2014-09, Vol.9 (9), p.e106039 |
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| creator | Ghosh, Sougata More, Piyush Derle, Abhishek Patil, Ajay B Markad, Pramod Asok, Adersh Kumbhar, Navanath Shaikh, Mahemud L Ramanamurthy, Boppana Shinde, Vaishali S Dhavale, Dilip D Chopade, Balu A |
| description | Diabetes mellitus is a multifactorial metabolic disease characterized by post-prandial hyperglycemia (PPHG). α-amylase and α-glucosidase inhibitors aim to explore novel therapeutic agents. Herein we report the promises of Dioscorea bulbifera and its bioactive principle, diosgenin as novel α-amylase and α-glucosidase inhibitor. Among petroleum ether, ethyl acetate, methanol and 70% ethanol (v/v) extracts of bulbs of D. bulbifera, ethyl acetate extract showed highest inhibition upto 72.06 ± 0.51% and 82.64 ± 2.32% against α-amylase and α-glucosidase respectively. GC-TOF-MS analysis of ethyl acetate extract indicated presence of high diosgenin content. Diosgenin was isolated and identified by FTIR, 1H NMR and 13C NMR and confirmed by HPLC which showed an α-amylase and α-glucosidase inhibition upto 70.94 ± 1.24% and 81.71 ± 3.39%, respectively. Kinetic studies confirmed the uncompetitive mode of binding of diosgenin to α-amylase indicated by lowering of both Km and Vm. Interaction studies revealed the quenching of intrinsic fluorescence of α-amylase in presence of diosgenin. Similarly, circular dichroism spectrometry showed diminished negative humped peaks at 208 nm and 222 nm. Molecular docking indicated hydrogen bonding between carboxyl group of Asp300, while hydrophobic interactions between Tyr62, Trp58, Trp59, Val163, His305 and Gln63 residues of α-amylase. Diosgenin interacted with two catalytic residues (Asp352 and Glu411) from α-glucosidase. This is the first report of its kind that provides an intense scientific rationale for use of diosgenin as novel drug candidate for type II diabetes mellitus. |
| doi_str_mv | 10.1371/journal.pone.0106039 |
| format | Article |
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Herein we report the promises of Dioscorea bulbifera and its bioactive principle, diosgenin as novel α-amylase and α-glucosidase inhibitor. Among petroleum ether, ethyl acetate, methanol and 70% ethanol (v/v) extracts of bulbs of D. bulbifera, ethyl acetate extract showed highest inhibition upto 72.06 ± 0.51% and 82.64 ± 2.32% against α-amylase and α-glucosidase respectively. GC-TOF-MS analysis of ethyl acetate extract indicated presence of high diosgenin content. Diosgenin was isolated and identified by FTIR, 1H NMR and 13C NMR and confirmed by HPLC which showed an α-amylase and α-glucosidase inhibition upto 70.94 ± 1.24% and 81.71 ± 3.39%, respectively. Kinetic studies confirmed the uncompetitive mode of binding of diosgenin to α-amylase indicated by lowering of both Km and Vm. Interaction studies revealed the quenching of intrinsic fluorescence of α-amylase in presence of diosgenin. Similarly, circular dichroism spectrometry showed diminished negative humped peaks at 208 nm and 222 nm. Molecular docking indicated hydrogen bonding between carboxyl group of Asp300, while hydrophobic interactions between Tyr62, Trp58, Trp59, Val163, His305 and Gln63 residues of α-amylase. Diosgenin interacted with two catalytic residues (Asp352 and Glu411) from α-glucosidase. This is the first report of its kind that provides an intense scientific rationale for use of diosgenin as novel drug candidate for type II diabetes mellitus.</description><identifier>ISSN: 1932-6203</identifier><identifier>EISSN: 1932-6203</identifier><identifier>DOI: 10.1371/journal.pone.0106039</identifier><identifier>PMID: 25216353</identifier><language>eng</language><publisher>United States: Public Library of Science</publisher><subject>Acetic acid ; alpha-Amylases - antagonists & inhibitors ; alpha-Amylases - metabolism ; alpha-Glucosidases - metabolism ; Amylases ; Animals ; Biochemistry ; Bioinformatics ; Biology and Life Sciences ; Biotechnology ; Bonding ; Carboxyl group ; Catalysis ; Catalytic Domain ; Chemical bonds ; Chemical compounds ; Chemistry ; Circular Dichroism ; Diabetes ; Diabetes mellitus ; Diabetes Mellitus, Experimental - drug therapy ; Diabetes Mellitus, Experimental - enzymology ; Diabetes Mellitus, Experimental - pathology ; Dichroism ; Dioscorea - chemistry ; Dioscorea bulbifera ; Dioscorea dumetorum ; Dioscorea polygonoides ; Diosgenin - chemistry ; Diosgenin - pharmacology ; Diosgenin - therapeutic use ; Enzyme Inhibitors - isolation & purification ; Enzyme Inhibitors - pharmacology ; Enzyme Inhibitors - therapeutic use ; Enzymes ; Ethanol ; Ethyl acetate ; Fluorescence ; Glucosidase ; Herbal medicine ; High-performance liquid chromatography ; Hydrogen ; Hydrogen bonding ; Hydrophobicity ; Hyperglycemia ; Inhibition ; Intestines - enzymology ; Kinetics ; Liquid chromatography ; Medicine and Health Sciences ; Mice ; Molecular docking ; Molecular Docking Simulation ; NMR ; Nuclear magnetic resonance ; Petroleum ether ; Pharmacology ; Plant Extracts - pharmacology ; Plant Extracts - therapeutic use ; Potassium ; Protein Binding - drug effects ; Quenching ; Residues ; Science ; Spectrometry ; Spectrometry, Fluorescence ; Studies ; Sus scrofa ; α-Amylase ; α-Glucosidase</subject><ispartof>PloS one, 2014-09, Vol.9 (9), p.e106039</ispartof><rights>2014 Ghosh et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License: http://creativecommons.org/licenses/by/4.0/ (the “License”), which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.</rights><rights>2014 Ghosh et al 2014 Ghosh et al</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c526t-4b687c3bfe6343fe6693a07960fb9096f64e9c97c8fc37bf8cbdf8c243bf030d3</citedby><cites>FETCH-LOGICAL-c526t-4b687c3bfe6343fe6693a07960fb9096f64e9c97c8fc37bf8cbdf8c243bf030d3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC4162539/pdf/$$EPDF$$P50$$Gpubmedcentral$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC4162539/$$EHTML$$P50$$Gpubmedcentral$$Hfree_for_read</linktohtml><link.rule.ids>230,314,723,776,780,860,881,2096,2915,23845,27901,27902,53766,53768,79342,79343</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/25216353$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Ghosh, Sougata</creatorcontrib><creatorcontrib>More, Piyush</creatorcontrib><creatorcontrib>Derle, Abhishek</creatorcontrib><creatorcontrib>Patil, Ajay B</creatorcontrib><creatorcontrib>Markad, Pramod</creatorcontrib><creatorcontrib>Asok, Adersh</creatorcontrib><creatorcontrib>Kumbhar, Navanath</creatorcontrib><creatorcontrib>Shaikh, Mahemud L</creatorcontrib><creatorcontrib>Ramanamurthy, Boppana</creatorcontrib><creatorcontrib>Shinde, Vaishali S</creatorcontrib><creatorcontrib>Dhavale, Dilip D</creatorcontrib><creatorcontrib>Chopade, Balu A</creatorcontrib><title>Diosgenin from Dioscorea bulbifera: novel hit for treatment of type II diabetes mellitus with inhibitory activity against α-amylase and α-glucosidase</title><title>PloS one</title><addtitle>PLoS One</addtitle><description>Diabetes mellitus is a multifactorial metabolic disease characterized by post-prandial hyperglycemia (PPHG). α-amylase and α-glucosidase inhibitors aim to explore novel therapeutic agents. Herein we report the promises of Dioscorea bulbifera and its bioactive principle, diosgenin as novel α-amylase and α-glucosidase inhibitor. Among petroleum ether, ethyl acetate, methanol and 70% ethanol (v/v) extracts of bulbs of D. bulbifera, ethyl acetate extract showed highest inhibition upto 72.06 ± 0.51% and 82.64 ± 2.32% against α-amylase and α-glucosidase respectively. GC-TOF-MS analysis of ethyl acetate extract indicated presence of high diosgenin content. Diosgenin was isolated and identified by FTIR, 1H NMR and 13C NMR and confirmed by HPLC which showed an α-amylase and α-glucosidase inhibition upto 70.94 ± 1.24% and 81.71 ± 3.39%, respectively. Kinetic studies confirmed the uncompetitive mode of binding of diosgenin to α-amylase indicated by lowering of both Km and Vm. Interaction studies revealed the quenching of intrinsic fluorescence of α-amylase in presence of diosgenin. Similarly, circular dichroism spectrometry showed diminished negative humped peaks at 208 nm and 222 nm. Molecular docking indicated hydrogen bonding between carboxyl group of Asp300, while hydrophobic interactions between Tyr62, Trp58, Trp59, Val163, His305 and Gln63 residues of α-amylase. Diosgenin interacted with two catalytic residues (Asp352 and Glu411) from α-glucosidase. This is the first report of its kind that provides an intense scientific rationale for use of diosgenin as novel drug candidate for type II diabetes mellitus.</description><subject>Acetic acid</subject><subject>alpha-Amylases - antagonists & inhibitors</subject><subject>alpha-Amylases - metabolism</subject><subject>alpha-Glucosidases - metabolism</subject><subject>Amylases</subject><subject>Animals</subject><subject>Biochemistry</subject><subject>Bioinformatics</subject><subject>Biology and Life Sciences</subject><subject>Biotechnology</subject><subject>Bonding</subject><subject>Carboxyl group</subject><subject>Catalysis</subject><subject>Catalytic Domain</subject><subject>Chemical bonds</subject><subject>Chemical compounds</subject><subject>Chemistry</subject><subject>Circular Dichroism</subject><subject>Diabetes</subject><subject>Diabetes mellitus</subject><subject>Diabetes Mellitus, Experimental - drug therapy</subject><subject>Diabetes Mellitus, Experimental - enzymology</subject><subject>Diabetes Mellitus, Experimental - pathology</subject><subject>Dichroism</subject><subject>Dioscorea - chemistry</subject><subject>Dioscorea bulbifera</subject><subject>Dioscorea dumetorum</subject><subject>Dioscorea polygonoides</subject><subject>Diosgenin - chemistry</subject><subject>Diosgenin - pharmacology</subject><subject>Diosgenin - therapeutic use</subject><subject>Enzyme Inhibitors - isolation & purification</subject><subject>Enzyme Inhibitors - pharmacology</subject><subject>Enzyme Inhibitors - therapeutic use</subject><subject>Enzymes</subject><subject>Ethanol</subject><subject>Ethyl acetate</subject><subject>Fluorescence</subject><subject>Glucosidase</subject><subject>Herbal medicine</subject><subject>High-performance liquid chromatography</subject><subject>Hydrogen</subject><subject>Hydrogen bonding</subject><subject>Hydrophobicity</subject><subject>Hyperglycemia</subject><subject>Inhibition</subject><subject>Intestines - enzymology</subject><subject>Kinetics</subject><subject>Liquid chromatography</subject><subject>Medicine and Health Sciences</subject><subject>Mice</subject><subject>Molecular docking</subject><subject>Molecular Docking Simulation</subject><subject>NMR</subject><subject>Nuclear magnetic resonance</subject><subject>Petroleum ether</subject><subject>Pharmacology</subject><subject>Plant Extracts - pharmacology</subject><subject>Plant Extracts - therapeutic use</subject><subject>Potassium</subject><subject>Protein Binding - drug effects</subject><subject>Quenching</subject><subject>Residues</subject><subject>Science</subject><subject>Spectrometry</subject><subject>Spectrometry, Fluorescence</subject><subject>Studies</subject><subject>Sus scrofa</subject><subject>α-Amylase</subject><subject>α-Glucosidase</subject><issn>1932-6203</issn><issn>1932-6203</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2014</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>BENPR</sourceid><sourceid>DOA</sourceid><recordid>eNptUkuOEzEQbSEQMwzcAIElNmw62O1uf1ggoeEXaSQ2sLZst504ctvBdgflJJyDi3AmnElmNIPYlOvz3nNVqZrmOYILhCl6s4lzCtIvtjGYBUSQQMwfNOeI464lHcQP7_hnzZOcNxAOmBHyuDnrhg4RPODz5tcHF_PKBBeATXECh1DHZCRQs1fOmiTfghB3xoO1K8DGBEqtlsmEAqIFZb81YLkEo5PKFJPBZLx3Zc7gpytr4MLaKVdi2gOpi9u5Up2VdCEX8Od3K6e9l9kAGcZDuPKzjtmNNfW0eWSlz-bZ6b1ovn_6-O3yS3v19fPy8v1Vq4eOlLZXhFGNlTUE97hawrGElBNoFYecWNIbrjnVzGpMlWVajdV0faVADEd80bw86m59zOK00yzQQOqCekZxRSyPiDHKjdgmN8m0F1E6cZ2IaSVkKk57I4yEnI6EDoyqnjHDLLPKcqLp0A8MdVXr3em3WU1m1HWJSfp7ovcrwa3FKu5Ej0g3YF4FXp8EUvwxm1zE5LKuK5fBxPm6767vKBpohb76B_r_6fojSqeYczL2thkExeHObljicGfidGeV9uLuILekm8PCfwEfvNXY</recordid><startdate>20140912</startdate><enddate>20140912</enddate><creator>Ghosh, Sougata</creator><creator>More, Piyush</creator><creator>Derle, Abhishek</creator><creator>Patil, Ajay B</creator><creator>Markad, Pramod</creator><creator>Asok, Adersh</creator><creator>Kumbhar, Navanath</creator><creator>Shaikh, Mahemud L</creator><creator>Ramanamurthy, Boppana</creator><creator>Shinde, Vaishali S</creator><creator>Dhavale, Dilip D</creator><creator>Chopade, Balu A</creator><general>Public Library of Science</general><general>Public Library of Science (PLoS)</general><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>3V.</scope><scope>7QG</scope><scope>7QL</scope><scope>7QO</scope><scope>7RV</scope><scope>7SN</scope><scope>7SS</scope><scope>7T5</scope><scope>7TG</scope><scope>7TM</scope><scope>7U9</scope><scope>7X2</scope><scope>7X7</scope><scope>7XB</scope><scope>88E</scope><scope>8AO</scope><scope>8C1</scope><scope>8FD</scope><scope>8FE</scope><scope>8FG</scope><scope>8FH</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABJCF</scope><scope>ABUWG</scope><scope>AEUYN</scope><scope>AFKRA</scope><scope>ARAPS</scope><scope>ATCPS</scope><scope>AZQEC</scope><scope>BBNVY</scope><scope>BENPR</scope><scope>BGLVJ</scope><scope>BHPHI</scope><scope>C1K</scope><scope>CCPQU</scope><scope>D1I</scope><scope>DWQXO</scope><scope>FR3</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>H94</scope><scope>HCIFZ</scope><scope>K9.</scope><scope>KB.</scope><scope>KB0</scope><scope>KL.</scope><scope>L6V</scope><scope>LK8</scope><scope>M0K</scope><scope>M0S</scope><scope>M1P</scope><scope>M7N</scope><scope>M7P</scope><scope>M7S</scope><scope>NAPCQ</scope><scope>P5Z</scope><scope>P62</scope><scope>P64</scope><scope>PATMY</scope><scope>PDBOC</scope><scope>PIMPY</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>PTHSS</scope><scope>PYCSY</scope><scope>RC3</scope><scope>7X8</scope><scope>5PM</scope><scope>DOA</scope></search><sort><creationdate>20140912</creationdate><title>Diosgenin from Dioscorea bulbifera: novel hit for treatment of type II diabetes mellitus with inhibitory activity against α-amylase and α-glucosidase</title><author>Ghosh, Sougata ; More, Piyush ; Derle, Abhishek ; Patil, Ajay B ; Markad, Pramod ; Asok, Adersh ; Kumbhar, Navanath ; Shaikh, Mahemud L ; Ramanamurthy, Boppana ; Shinde, Vaishali S ; Dhavale, Dilip D ; Chopade, Balu A</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c526t-4b687c3bfe6343fe6693a07960fb9096f64e9c97c8fc37bf8cbdf8c243bf030d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2014</creationdate><topic>Acetic acid</topic><topic>alpha-Amylases - 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drug effects</topic><topic>Quenching</topic><topic>Residues</topic><topic>Science</topic><topic>Spectrometry</topic><topic>Spectrometry, Fluorescence</topic><topic>Studies</topic><topic>Sus scrofa</topic><topic>α-Amylase</topic><topic>α-Glucosidase</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ghosh, Sougata</creatorcontrib><creatorcontrib>More, Piyush</creatorcontrib><creatorcontrib>Derle, Abhishek</creatorcontrib><creatorcontrib>Patil, Ajay B</creatorcontrib><creatorcontrib>Markad, Pramod</creatorcontrib><creatorcontrib>Asok, Adersh</creatorcontrib><creatorcontrib>Kumbhar, Navanath</creatorcontrib><creatorcontrib>Shaikh, Mahemud L</creatorcontrib><creatorcontrib>Ramanamurthy, Boppana</creatorcontrib><creatorcontrib>Shinde, Vaishali S</creatorcontrib><creatorcontrib>Dhavale, Dilip D</creatorcontrib><creatorcontrib>Chopade, Balu A</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>ProQuest Central (Corporate)</collection><collection>Animal Behavior Abstracts</collection><collection>Bacteriology Abstracts (Microbiology B)</collection><collection>Biotechnology Research Abstracts</collection><collection>Nursing & Allied Health Database</collection><collection>Ecology Abstracts</collection><collection>Entomology Abstracts (Full archive)</collection><collection>Immunology Abstracts</collection><collection>Meteorological & Geoastrophysical Abstracts</collection><collection>Nucleic Acids Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>Agricultural Science Collection</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Medical Database (Alumni Edition)</collection><collection>ProQuest Pharma Collection</collection><collection>Public Health Database</collection><collection>Technology Research Database</collection><collection>ProQuest SciTech Collection</collection><collection>ProQuest Technology Collection</collection><collection>ProQuest Natural Science Collection</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>Materials Science & Engineering Collection</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest One Sustainability</collection><collection>ProQuest Central UK/Ireland</collection><collection>Advanced Technologies & Aerospace Collection</collection><collection>Agricultural & Environmental Science Collection</collection><collection>ProQuest Central Essentials</collection><collection>Biological Science Collection</collection><collection>ProQuest Central</collection><collection>Technology Collection</collection><collection>Natural Science Collection</collection><collection>Environmental Sciences and Pollution Management</collection><collection>ProQuest One Community College</collection><collection>ProQuest Materials Science Collection</collection><collection>ProQuest Central Korea</collection><collection>Engineering Research Database</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Central Student</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>SciTech Premium Collection</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Materials Science Database</collection><collection>Nursing & Allied Health Database (Alumni Edition)</collection><collection>Meteorological & Geoastrophysical Abstracts - 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Academic</collection><collection>PubMed Central (Full Participant titles)</collection><collection>DOAJ Directory of Open Access Journals</collection><jtitle>PloS one</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ghosh, Sougata</au><au>More, Piyush</au><au>Derle, Abhishek</au><au>Patil, Ajay B</au><au>Markad, Pramod</au><au>Asok, Adersh</au><au>Kumbhar, Navanath</au><au>Shaikh, Mahemud L</au><au>Ramanamurthy, Boppana</au><au>Shinde, Vaishali S</au><au>Dhavale, Dilip D</au><au>Chopade, Balu A</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Diosgenin from Dioscorea bulbifera: novel hit for treatment of type II diabetes mellitus with inhibitory activity against α-amylase and α-glucosidase</atitle><jtitle>PloS one</jtitle><addtitle>PLoS One</addtitle><date>2014-09-12</date><risdate>2014</risdate><volume>9</volume><issue>9</issue><spage>e106039</spage><pages>e106039-</pages><issn>1932-6203</issn><eissn>1932-6203</eissn><abstract>Diabetes mellitus is a multifactorial metabolic disease characterized by post-prandial hyperglycemia (PPHG). α-amylase and α-glucosidase inhibitors aim to explore novel therapeutic agents. Herein we report the promises of Dioscorea bulbifera and its bioactive principle, diosgenin as novel α-amylase and α-glucosidase inhibitor. Among petroleum ether, ethyl acetate, methanol and 70% ethanol (v/v) extracts of bulbs of D. bulbifera, ethyl acetate extract showed highest inhibition upto 72.06 ± 0.51% and 82.64 ± 2.32% against α-amylase and α-glucosidase respectively. GC-TOF-MS analysis of ethyl acetate extract indicated presence of high diosgenin content. Diosgenin was isolated and identified by FTIR, 1H NMR and 13C NMR and confirmed by HPLC which showed an α-amylase and α-glucosidase inhibition upto 70.94 ± 1.24% and 81.71 ± 3.39%, respectively. Kinetic studies confirmed the uncompetitive mode of binding of diosgenin to α-amylase indicated by lowering of both Km and Vm. Interaction studies revealed the quenching of intrinsic fluorescence of α-amylase in presence of diosgenin. Similarly, circular dichroism spectrometry showed diminished negative humped peaks at 208 nm and 222 nm. Molecular docking indicated hydrogen bonding between carboxyl group of Asp300, while hydrophobic interactions between Tyr62, Trp58, Trp59, Val163, His305 and Gln63 residues of α-amylase. Diosgenin interacted with two catalytic residues (Asp352 and Glu411) from α-glucosidase. This is the first report of its kind that provides an intense scientific rationale for use of diosgenin as novel drug candidate for type II diabetes mellitus.</abstract><cop>United States</cop><pub>Public Library of Science</pub><pmid>25216353</pmid><doi>10.1371/journal.pone.0106039</doi><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 1932-6203 |
| ispartof | PloS one, 2014-09, Vol.9 (9), p.e106039 |
| issn | 1932-6203 1932-6203 |
| language | eng |
| recordid | cdi_plos_journals_1561634873 |
| source | MEDLINE; DOAJ Directory of Open Access Journals; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; PubMed Central; Free Full-Text Journals in Chemistry; Public Library of Science (PLoS) |
| subjects | Acetic acid alpha-Amylases - antagonists & inhibitors alpha-Amylases - metabolism alpha-Glucosidases - metabolism Amylases Animals Biochemistry Bioinformatics Biology and Life Sciences Biotechnology Bonding Carboxyl group Catalysis Catalytic Domain Chemical bonds Chemical compounds Chemistry Circular Dichroism Diabetes Diabetes mellitus Diabetes Mellitus, Experimental - drug therapy Diabetes Mellitus, Experimental - enzymology Diabetes Mellitus, Experimental - pathology Dichroism Dioscorea - chemistry Dioscorea bulbifera Dioscorea dumetorum Dioscorea polygonoides Diosgenin - chemistry Diosgenin - pharmacology Diosgenin - therapeutic use Enzyme Inhibitors - isolation & purification Enzyme Inhibitors - pharmacology Enzyme Inhibitors - therapeutic use Enzymes Ethanol Ethyl acetate Fluorescence Glucosidase Herbal medicine High-performance liquid chromatography Hydrogen Hydrogen bonding Hydrophobicity Hyperglycemia Inhibition Intestines - enzymology Kinetics Liquid chromatography Medicine and Health Sciences Mice Molecular docking Molecular Docking Simulation NMR Nuclear magnetic resonance Petroleum ether Pharmacology Plant Extracts - pharmacology Plant Extracts - therapeutic use Potassium Protein Binding - drug effects Quenching Residues Science Spectrometry Spectrometry, Fluorescence Studies Sus scrofa α-Amylase α-Glucosidase |
| title | Diosgenin from Dioscorea bulbifera: novel hit for treatment of type II diabetes mellitus with inhibitory activity against α-amylase and α-glucosidase |
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