Young apple polyphenols as natural α-glucosidase inhibitors: In vitro and in silico studies.
Bioorg Chem
; 96: 103625, 2020 03.
Article
em En
| MEDLINE
| ID: mdl-32028059
ABSTRACT
In this study, the inhibitory activity of young apple polyphenols (YAP) on α-glucosidase was investigated. Composition and inhibition analyses suggested that tannic acid (TA), (-)-epicatechin (EC) and phlorizin (PH) were the main active constituents in YAP showing α-glucosidase inhibition. PH was a competitive inhibitor, while YAP, TA and EC were the mixed-type ones. YAP, TA, PH and EC quenched the fluorescence spectrum of α-glucosidase significantly. Interestingly, the constants that indicate binding interaction between α-glucosidase and TA, PH, EC, including reciprocal of competitive inhibition constant (1/Kic), fluorescence quenching constant (KFQ) and binding energy (Eb), were shown similar orders as TA > PH > EC, contrary to IC50 values. This indicates that binding interactions between polyphenols and α-glucosidase caused the enzyme inhibition. Additionally, potential enzyme unfolding by polyphenols interactions indicated by red-shift of maximum emission wavelength is supported by the decrease in α-helix and ß-sheet contents of the enzyme. Conclusively, the α-glucosidase inhibition indicates that YAP may have potentials in alleviation of type 2 diabetes symptom.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Malus
/
Polifenóis
/
Inibidores de Glicosídeo Hidrolases
Limite:
Humans
Idioma:
En
Revista:
Bioorg Chem
Ano de publicação:
2020
Tipo de documento:
Article