Please use this identifier to cite or link to this item:
https://hdl.handle.net/10321/5148
DC Field | Value | Language |
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dc.contributor.author | Rampadarath, Athika | en_US |
dc.contributor.author | Balogun, Fatai Oladunni | en_US |
dc.contributor.author | Pillay, Charlene | en_US |
dc.contributor.author | Sabiu, Saheed | en_US |
dc.date.accessioned | 2024-02-15T12:27:34Z | - |
dc.date.available | 2024-02-15T12:27:34Z | - |
dc.date.issued | 2022-06-24 | - |
dc.identifier.citation | Rampadarath, A. et al. 2022. Identification of flavonoid C-glycosides as promising antidiabetics targeting protein tyrosine phosphatase 1B. Journal of Diabetes Research: 6233217-. doi:10.1155/2022/6233217 | en_US |
dc.identifier.issn | 2314-6745 | - |
dc.identifier.issn | 2314-6753 (Online) | - |
dc.identifier.other | isidoc: 2R1YR | - |
dc.identifier.other | pubmed: 35782627 | - |
dc.identifier.uri | https://hdl.handle.net/10321/5148 | - |
dc.description.abstract | Protein tyrosine phosphatase 1B (PTP1B), a negative regulator of the insulin signaling pathway, has gained attention as a validated druggable target in the management of type 2 diabetes mellitus (T2DM). The lack of clinically approved PTP1B inhibitors has continued to prompt research in plant-derived therapeutics possibly due to their relatively lesser toxicity profiles. Flavonoid C-glycosides are one of the plant-derived metabolites gaining increased relevance as antidiabetic agents, but their possible mechanism of action remains largely unknown. This study investigates the antidiabetic potential of flavonoid C-glycosides against PTP1B <i>in silico</i> and <i>in vitro</i>. Of the seven flavonoid C-glycosides docked against the enzyme, three compounds (apigenin, vitexin, and orientin) had the best affinity for the enzyme with a binding score of -7.3 kcal/mol each, relative to -7.4 kcal/mol for the reference standard, ursolic acid. A further probe (in terms of stability, flexibility, and compactness) of the complexes over a molecular dynamics time study of 100 ns for the three compounds suggested orientin as the most outstanding inhibitor of PTP1B owing to its overall -34.47 kcal/mol binding energy score compared to ursolic acid (-19.24 kcal/mol). This observation was in accordance with the <i>in vitro</i> evaluation result, where orientin had a half maximal inhibitory concentration (IC<sub>50</sub>) of 0.18 mg/ml relative to 0.13 mg/ml for the reference standard. The kinetics of inhibition of PTP1B by orientin was mixed-type with <i>V</i> <sub>max</sub> and <i>K</i> <sub><i>m</i></sub> values of 0.004 <i>μ</i>M/s and 0.515 <i>μ</i>M. Put together, the results suggest orientin as a potential PTP1B inhibitor and could therefore be further explored in the management T2DM as a promising therapeutic agent. | en_US |
dc.format.extent | 11 p | en_US |
dc.format.medium | Electronic-eCollection | - |
dc.language.iso | en | en_US |
dc.publisher | Hindawi Limited | en_US |
dc.relation.ispartof | Journal of Diabetes Research; Vol. 2022 | en_US |
dc.subject | 1116 Medical Physiology | en_US |
dc.subject.mesh | Humans | - |
dc.subject.mesh | Diabetes Mellitus, Type 2 | - |
dc.subject.mesh | Flavonoids | - |
dc.subject.mesh | Glycosides | - |
dc.subject.mesh | Enzyme Inhibitors | - |
dc.subject.mesh | Hypoglycemic Agents | - |
dc.subject.mesh | Protein Tyrosine Phosphatase, Non-Receptor Type 1 | - |
dc.subject.mesh | Diabetes Mellitus, Type 2 | - |
dc.subject.mesh | Enzyme Inhibitors | - |
dc.subject.mesh | Flavonoids | - |
dc.subject.mesh | Glycosides | - |
dc.subject.mesh | Humans | - |
dc.subject.mesh | Hypoglycemic Agents | - |
dc.subject.mesh | Protein Tyrosine Phosphatase, Non-Receptor Type 1 | - |
dc.title | Identification of flavonoid C-glycosides as promising antidiabetics targeting protein tyrosine phosphatase 1B | en_US |
dc.type | Article | en_US |
dc.date.updated | 2024-02-09T09:11:49Z | - |
dcterms.dateAccepted | 2022-6-8 | - |
dc.identifier.doi | 10.1155/2022/6233217 | - |
local.sdg | SDG03 | - |
item.cerifentitytype | Publications | - |
item.fulltext | With Fulltext | - |
item.openairetype | Article | - |
item.grantfulltext | open | - |
item.languageiso639-1 | en | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
Appears in Collections: | Research Publications (Applied Sciences) |
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JDR Copyright clearance.docx | Copyirght clearance | 141.12 kB | Microsoft Word XML | View/Open |
Rampadarath et al_2022.pdf | 1.03 MB | Adobe PDF | View/Open |
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