Young apple polyphenols as natural α-glucosidase inhibitors: In vitro and in silico studies

Gong, Tian; Yang, Xi; Bai, Fangting; Li, Dan; Zhao, Ting; Zhang, Jiangtao; Sun, Lijun; Guo, Yurong

doi:10.1016/j.bioorg.2020.103625

Cited by 46 publications

(35 citation statements)

References 36 publications

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“…At a certain excitation wavelength, the presence of tryptophan (Trp), tyrosine (Tyr), and phenylalanine (Phe) can cause fluorescent properties in α-glucosidase and α-amylase ( 45 ). Trp and Tyr residues are excited at 280 nm, and the microenvironment in which these residues are located affects fluorescence intensity and position ( 46 ). Figure 5 shows the fluorescence spectra of α-glucosidase ( Figure 5A ) and α-amylase ( Figure 5B ) with different EGC concentrations.…”

Section: Resultsmentioning

confidence: 99%

Structural changes and molecular mechanism study on the inhibitory activity of epigallocatechin against α-glucosidase and α-amylase

Man

Feng²,

Xiao³

et al. 2022

Front. Nutr.

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In this study, the inhibition and mechanism of epigallocatechin (EGC) on two key glycoside hydrolases (α-glucosidase, α-amylase) were explored from the molecular structure level. The chemical structure of EGC was characterized by X-ray diffraction, Fourier transform infrared (FTIR) spectroscopy, and proton nuclear magnetic resonance spectroscopy. EGC’s inhibition on these enzymes was colorimetrically determined. The effects of EGC on the chemical structure and spatial configuration of the enzymes were explored via FTIR spectroscopy, fluorescence spectroscopy, and molecular docking techniques. The results showed that EGC exhibited the inhibition of α-glucosidase and α-amylase in a non-competitive manner, showing a continuous upward trend as EGC’s concentration increased. There was a fluorescence quenching effect of EGC on α-glucosidase and α-amylase. Molecular docking confirmed that EGC can bind to amino acid residues in the enzyme through intermolecular hydrogen bonds and hydrophobic interactions, resulting in the changed chemical structure and spatial conformation of the enzymes. This decreased enzyme activity. This result suggested that EGC has the potential to inhibit two key glycoside hydrolases, and it would be beneficial to incorporate EGC into functional foods for diabetics.

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Section: Resultsmentioning

confidence: 99%

Structural changes and molecular mechanism study on the inhibitory activity of epigallocatechin against α-glucosidase and α-amylase

Man

Feng²,

Xiao³

et al. 2022

Front. Nutr.

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“…A smaller K ic value means a more tightly binding of inhibitor to free α‐glucosidases. As in previous reports, the K ic values were 144.93 ± 2.84 and 1204.80 ± 5.03 mg/mL from some natural compounds (apple polyphenols and tannic acid) (Gong et al ., 2020), showing that curcumin has a stronger competitive inhibitory intensity than those compounds. Of course, the inhibitory effect of curcumin on α‐glucosidases is still relatively weak as compared with some drugs such as acarbose or voglibose.…”

Section: Resultsmentioning

confidence: 99%

Curcumin as a mild natural α‐glucosidase inhibitor: a study on its mechanism in vitro

Liu

Zhu

et al. 2021

Int J of Food Sci Tech

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Curcumin, natural dietary ingredient, is considered as mild effective inhibitors for α-glucosidase to prevent type 2 diabetes. In this work, spectroscopic techniques combined with molecular simulation were used to further understand the inhibition kinetic mechanism of curcumin on α-glucosidase. Curcumin showed a mild inhibition effect (IC 50 =20.54 AE 1.02 mg/ml) for α-glucosidases through a competitive inhibition mechanism, and it led to fluorescence quenching as well as energy transfer by binding behaviour (average binding distance, r 0 = 2.43 nm). Hydrogen bonds and steric hindrance were the main interactions between curcumin and the activity site of α-glucosidases, as revealed by molecular docking. Circular dichroism spectroscopy results also indicate that curcumin affected the denaturation temperature of α-glucosidases, which dropped from 74 °C to 68 °C, resulting in inhibition. The findings can contribute to a better understanding of the development and application of curcumin in functional dietary food.

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“…Although many literatures are focused on the antibacterial effects of apple polyphenols, there are few literatures on thinned young apple polyphenols. We extracted and purified polyphenols from ‘Fuji’ thinned young apples according to the methods of our previous publication ( Gong et al, 2020 ) and analyzed the extracted YAP by HPLC. The higher contents of individual phenols in thinned young apples were chlorogenic acid and phlorizin.…”

Section: Discussionmentioning

confidence: 99%

“…The YAP were extracted and purification according to our previous method ( Gong et al, 2020 ). Briefly, the thinned young apples were crashed into 3–4-mm particles.…”

Section: Methodsmentioning

confidence: 99%

Thinned-Young Apple Polyphenols Inhibit Halitosis-Related Bacteria Through Damage to the Cell Membrane

et al. 2022

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The thinned young apple is a by-product and is generally discarded in the orchard during fruit thinning. The polyphenol content of thinned young apples is about 10 times more than that of ripe apples. In our study, the antibacterial effect of thinned young apple polyphenols (YAP) on the halitosis-related bacteria including Porphyromonas gingivalis, Prevotella intermedius, and Fusobacterium nucleatum was investigated. The minimum inhibitory concentrations of YAP against P. gingivalis, P. intermedia, and F. nucleatum were 8.0, 8.0, and 12.0 mg/ml, while the minimum bactericidal concentrations were 10.0, 10.0, and 14.0 mg/ml, respectively. The scanning electron microscopy and transmission electron microscopy analyses showed that after YAP treatment, the membrane surface of halitosis-related bacterial cells was coarse and the cell wall and membrane were separated and eventually ruptured. The integrity of the cell membrane was determined by flow cytometry, indicating that the cells with the integrity membrane significantly reduced as the YAP concentration treatment increased. The release of proteins and nucleic acids into the cell suspension significantly increased, and the membrane potential reduced after the YAP treatment. This research illustrated the antibacterial mechanism of YAP against halitosis-related bacteria and provided a scientific basis of utilizing the polyphenols from the discarded thinned young apples.

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Young apple polyphenols as natural α-glucosidase inhibitors: In vitro and in silico studies

Cited by 46 publications

References 36 publications

Structural changes and molecular mechanism study on the inhibitory activity of epigallocatechin against α-glucosidase and α-amylase

Structural changes and molecular mechanism study on the inhibitory activity of epigallocatechin against α-glucosidase and α-amylase

Curcumin as a mild natural α‐glucosidase inhibitor: a study on its mechanism in vitro

Thinned-Young Apple Polyphenols Inhibit Halitosis-Related Bacteria Through Damage to the Cell Membrane

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