Phytosterol supplements do not inhibit dipeptidyl peptidase-4.
Diabetes Metab Syndr
; 14(5): 1475-1478, 2020.
Article
em En
| MEDLINE
| ID: mdl-32771921
ABSTRACT
BACKGROUND AND AIMS:
Several commercially available phytosterol supplements are promoted for their cholesterol-lowering effects. However, limited information is available about their potential anti-hyperglycaemic effects. This study aimed to evaluate the dipeptidyl peptidase-4 (DPP-4) inhibitory effects of phytosterol supplements in silico and in vitro to determine their potential for anti-diabetic activity.METHODS:
Docking studies were carried out in silico to evaluate the potential for interactions between three major phytosterol compounds (stigmasterol, ß-sitosterol, campesterol) and the DPP-4 enzyme, the enzyme that is inhibited by the anti-diabetic gliptins. Gas chromatography-tandem mass spectrometry (GC-MS/MS) was used to analyse three different supplements for phytosterol content. DPP-4 inhibitory activity was tested in vitro for these phytosterol supplements and two major phytosterol standards.RESULTS:
In silico calculations predicted free binding energies for DPP-4 with the phytosterols to be stigmasterol -8.78 kcal/mol; ß-sitosterol -8.70 kcal/mol; campesterol -8.40 kcal/mol. These binding energies indicated a potential for significant DPP-4 inhibition. However, these results were not supported by the in vitro studies. Stigmasterol and ß-sitosterol had an IC50 > 50 mg/ml (maximum tested concentration) and the Thompson's Cholesterol Manager® and Mega Strength Beta Sitosterol® supplements gave an IC50 > 100 mg/ml (maximum tested concentration). Blackmores Cholesterol Health® gave an IC50 value of 40 mg/ml which was attributed to ß-carotene content.CONCLUSIONS:
Phytosterol supplements do not appear to offer any anti-diabetic activity potential via pathways that involve the inhibition of DPP-4.Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Fitosteróis
/
Dipeptidil Peptidase 4
/
Suplementos Nutricionais
/
Inibidores da Dipeptidil Peptidase IV
Idioma:
En
Ano de publicação:
2020
Tipo de documento:
Article