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Citrus bioflavonoids dipeptidyl peptidase-4 inhibition compared with gliptin antidiabetic medications.
- Source :
-
Biochemical and biophysical research communications [Biochem Biophys Res Commun] 2018 Sep 03; Vol. 503 (1), pp. 21-25. Date of Electronic Publication: 2018 Jun 09. - Publication Year :
- 2018
-
Abstract
- This study compared dipeptidyl peptidase-4 (DPP-4) inhibitory activity of citrus bioflavonoid nutraceuticals compared with three gliptins. Citrus bioflavonoid standards and three commercially available citrus bioflavonoid supplements (Thompson's Super Bioflavonoid Complex <superscript>®</superscript> (SB), Ethical Nutrients Bioflavonoids Plus Vitamin C <superscript>®</superscript> (EN), and Country Life Citrus Bioflavonoids and Rutin <superscript>®</superscript> (CB)) were considered in this study. Ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) analysis was undertaken to identify and quantitate the citrus bioflavonoids present in each supplement. The DPP-4 inhibitory activity was determined by fluorometric assay. All of the tested individual citrus flavonoids demonstrated DPP-4 inhibitory activity, with IC <subscript>50</subscript> values ranging from 485 μM (rutin) to 5700 μM (hesperitin and eriodictyol). Similarly, the flavonoid supplements had IC <subscript>50</subscript> values of 16.9 mg/mL (EN), 3.44 mg/mL (SB) and 2.72 mg/mL (CB). These values compare with gliptin IC <subscript>50</subscript> values of 0.684 μM (sitagliptin), 0.707 μM (saxagliptin) and 2.286 μM (vildagliptin). The supplement flavonoid content varied from 11.98% (CB) to 5.26% (EN) and 14.51% (SB) of tablet mass, corresponding to daily flavonoid doses of around 300, 150 and 400 mg, respectively, with CB and SB containing rutin at levels of 7.0% and 7.5% of tablet mass, respectively. While our data demonstrated that citrus bioflavonoid based supplements do possess DPP-4 inhibitory activity, they are several orders of magnitude less potent than gliptins. Further studies using higher concentrations of citrus bioflavonoids, as well as investigations into antioxidant properties which may add additional benefit are warranted.<br /> (Copyright © 2018 Elsevier Inc. All rights reserved.)
- Subjects :
- Adamantane analogs & derivatives
Adamantane chemistry
Adamantane pharmacology
Computer Simulation
Diabetes Mellitus, Type 2 blood
Diabetes Mellitus, Type 2 drug therapy
Dipeptides chemistry
Dipeptides pharmacology
Dipeptidyl Peptidase 4 chemistry
Dipeptidyl-Peptidase IV Inhibitors administration & dosage
Flavonoids administration & dosage
Humans
Hypoglycemic Agents administration & dosage
In Vitro Techniques
Molecular Docking Simulation
Nitriles chemistry
Nitriles pharmacology
Pyrrolidines chemistry
Pyrrolidines pharmacology
Sitagliptin Phosphate chemistry
Sitagliptin Phosphate pharmacology
Spectrometry, Fluorescence
Tandem Mass Spectrometry
Vildagliptin
Citrus chemistry
Dipeptidyl-Peptidase IV Inhibitors chemistry
Dipeptidyl-Peptidase IV Inhibitors pharmacology
Flavonoids chemistry
Flavonoids pharmacology
Hypoglycemic Agents chemistry
Hypoglycemic Agents pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1090-2104
- Volume :
- 503
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Biochemical and biophysical research communications
- Publication Type :
- Academic Journal
- Accession number :
- 29698678
- Full Text :
- https://doi.org/10.1016/j.bbrc.2018.04.156