首页|In vitro and in vivo inhibitory effect of anthocyanin-rich bilberry extract on alpha-glucosidase and alpha-amylase

In vitro and in vivo inhibitory effect of anthocyanin-rich bilberry extract on alpha-glucosidase and alpha-amylase

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The inhibition of glycosidase activity is regarded as an effective treatment for diabetes mellitus. Bilberry (Vaccinium myrtillus L.) fruit has a high content of anthocyanins with various biological activities. The objective of this study was to investigate the inhibitory activity of anthocyanin-rich bilberry extract (BE) on alpha-glucosidase and alpha-amylase and their interaction mechanisms in vitro. The IC50 values of BE with regard to alpha-glucosidase and alpha-amylase inhibition were 0.31 +/- 0.02 and 4.06 +/- 0.12 mg/mL, respectively. The enzyme kinetics revealed that BE acts as a mixed-type inhibitor against alpha-glucosidase and alpha-amylase. Moreover, the fluorescence of two glucosidases showed significant quenching by BE. FTIR spectra and differential scanning calorimetry (DSC) indicated that BE changed the enzyme structure and decreased its stability. A morphological observation of starch granules found that BE inhibited the activity of alpha-amylase to postpone the hydrolysis of starch. Furthermore, the in vivo study further showed that BE had a hypoglycaemic effect. The most suitable conformation (main anthocyanidins of BE) and optimal binding site (alpha-glucosidase, alpha-amylase) were assayed by molecular docking. In conclusion, this study revealed that BE could be a potential glycosidase inhibitor.

alpha-glucosidasealpha-amylaseBilberry extractInhibitory mechanism

Zhao, Jiang、Li, Heyu、Li, Liwei、Zhang, Hua、Wang, Hao、Ji, Yanglin、Liu, Dong、Jin, Yan、Zhao, Juan

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Tianjin Univ Sci & Technol, State Key Lab Food Nutr & Safety, Tianjin 300457, Peoples R China

Tianjin Ubasio Biotechnol Grp Co Ltd, Tianjin 300457, Peoples R China

Yunnan Tasly Deepure Biol Tea Grp Co Ltd, Simao 665000, Yunnan, Peoples R China

Tianjin Inspect & Quarantine Bur, Anim & Plant & Food Inspect Ctr Tianjin Customs, Tianjin 300461, Peoples R China

Tianjin Univ Sci & Technol, Res Ctr Modern Anal Technol, Tianjin 300457, Peoples R China

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2021

LWT-Food Science & Technology

LWT-Food Science & Technology

ISSN:0023-6438
年,卷(期):2021.145
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