Studies on the inhibition of α-glucosidase by biflavonoids and their interaction mechanisms

Li, Huan; Yang, Jichen; Wang, Mengfan; Ma, Xiangzhao; Peng, Xin

doi:10.1016/j.foodchem.2023.136113

Cited by 36 publications

(11 citation statements)

References 40 publications

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“…The intestinal α-glucosidase secreted in the epithelium of the small intestine is essential for carbohydrate digestion and has been identified as a therapeutic target for managing postprandial hyperglycemia . Inhibiting the activity of this enzyme can help control blood glucose levels in the postprandial state . Our study aims to highlight major challenges in evaluating the consumption of various sweeteners, including both natural and artificial alternatives, in terms of their ability to inhibit intestinal α-glucosidase activity.…”

Section: Introductionmentioning

confidence: 79%

“…19 Inhibiting the activity of this enzyme can help control blood glucose levels in the postprandial state. 20 Our study aims to highlight major challenges in evaluating the consumption of various sweeteners, including both natural and artificial alternatives, in terms of their ability to inhibit intestinal α-glucosidase activity. Additionally, we examine any potential relationships between the use of sweeteners and the downstream glycemic responses.…”

Section: Introductionmentioning

confidence: 99%

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Natural Sweetener, Glycyrrhetinic Acid 3-O-Mono-beta-d-glucuronide, for Postprandial Hyperglycemia Management

Guo,

Zhang,

Fei

et al. 2024

J. Agric. Food Chem.

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This study examines the inhibitory effects of a range of sweeteners on α-glucosidase. Our findings revealed that only one natural sweetener, namely, glycyrrhetinic acid 3-O-mono-beta-d-glucuronide (GAMG), derived from licorice, exhibited a mixed-type inhibition against α-glucosidase with a IC50 value of 0.73 ± 0.05 mg/mL. The fluorescence intensity of α-glucosidase was quenched by GAMG in the formation of an α-glucosidase–GAMG complex. GAMG has been shown to induce conformational changes in α-glucosidase, likely through hydrogen bonding, van der Waals force, and alkyl–alkyl interactions with amino acid residues, including Arg 281, Leu 283, Trp 376, Asp 404, Asp 443, Trp 481, Asp 518, Phe 525, Ala 555, and Asp 616. Additional animal validation experiments demonstrated that GAMG slowed starch digestion, thereby attenuating the postprandial glycemic response. Taken together, these findings provide evidence that GAMG is a natural sweetener with potent inhibitory activity that selectively targets α-glucosidase. This study supports the use of GAMG as a natural sweetener, which holds a high biological value and may be beneficial for managing postprandial hyperglycemia.

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Section: Introductionmentioning

confidence: 79%

Section: Introductionmentioning

confidence: 99%

Natural Sweetener, Glycyrrhetinic Acid 3-O-Mono-beta-d-glucuronide, for Postprandial Hyperglycemia Management

Guo,

Zhang,

Fei

et al. 2024

J. Agric. Food Chem.

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“…The relationship between the structure and activity of phenolic compounds with α-glucosidase TA B L E 1 List of polyphenols from a dietary supplement that helps to inhibit diabetes-related enzymes. activity demonstrates that hydroxylation of flavonoids can be beneficial for increasing their inhibitory impact on the enzyme, whilst methoxylation, glycosylation, and reducing the C 2 = C 3 double bond may diminish the inhibitory activity (Li et al, 2023). Several naturally occurring and synthetic phenolic compounds; coumarins, chromones, and their derivatives, including luteolin, naringenin, anthocyanins, and baicalein, have been targeted as powerful AGIs (Al-Salahi et al, 2018).…”

Section: Inhibition Of α-Glucosidasementioning

confidence: 99%

“…Acarbose is a competitive inhibitor of α‐glucosidase with the inhibition dependent on substrate concentration, while the phenolic extracts of various plants show non‐competitive inhibition which is independent of substrate concentration (Zhang et al., 2015 ). The relationship between the structure and activity of phenolic compounds with α‐glucosidase activity demonstrates that hydroxylation of flavonoids can be beneficial for increasing their inhibitory impact on the enzyme, whilst methoxylation, glycosylation, and reducing the C 2 = C 3 double bond may diminish the inhibitory activity (Li et al., 2023 ). Several naturally occurring and synthetic phenolic compounds; coumarins, chromones, and their derivatives, including luteolin, naringenin, anthocyanins, and baicalein, have been targeted as powerful AGIs (Al‐Salahi et al., 2018 ).…”

Section: Roles Of Phenolic Compounds For Inhibition Of Enzymes Linked...mentioning

confidence: 99%

Dietary phenolic compounds as promising therapeutic agents for diabetes and its complications: A comprehensive review

Aryal,

Joshi,

Thapa

et al. 2024

Food Science & Nutrition

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In the middle of an ever‐changing landscape of diabetes care, precision medicine, and lifestyle therapies are becoming increasingly important. Dietary polyphenols are like hidden allies found in our everyday meals. These biomolecules, found commonly in fruits, vegetables, and various plant‐based sources, hold revolutionary potential within their molecular structure in the way we approach diabetes and its intimidating consequences. There are currently numerous types of diabetes medications, but they are not appropriate for all patients due to limitations in dosages, side effects, drug resistance, a lack of efficacy, and ethnicity. Currently, there has been increased interest in practicing herbal remedies to manage diabetes and its related complications. This article aims to summarize the potential of dietary polyphenols as a foundation in the treatment of diabetes and its associated consequences. We found that most polyphenols inhibit enzymes linked to diabetes. This review outlines the potential benefits of selected molecules, including kaempferol, catechins, rosmarinic acid, apigenin, chlorogenic acid, and caffeic acid, in managing diabetes mellitus as these compounds have exhibited promising results in in vitro, in vivo, in silico, and some preclinical trials study. This encompassing exploration reveals the multifaceted impact of polyphenols not only in mitigating diabetes but also in addressing associated conditions like inflammation, obesity, and even cancer. Their mechanisms involve antioxidant functions, immune modulation, and proinflammatory enzyme regulation. Furthermore, these molecules exhibit anti‐tumor activities, influence cellular pathways, and activate AMPK pathways, offering a less toxic, cost‐effective, and sustainable approach to addressing diabetes and its complications.

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“…From molecular docking it was speculated that compound 5 could produce a hydrophobic force with α-glucosidase by binding to the active sites (Ile262, Val266, Ile272). It was reported that hydrogen-bond formation could increase the stability of the enzyme-substrate complex, 33 thereby binding the inhibitor more tightly to the enzyme and enhancing its inhibition activity (Table 4).…”

Section: Molecular Dockingmentioning

confidence: 99%

Polyketides with α-glucosidase inhibitory and neuroprotective activities from Aspergillus versicolor associated with Pedicularis sylvatica

Jiang,

Zhai,

Wang

et al. 2024

Org. Biomol. Chem.

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Studies on the inhibition of α-glucosidase by biflavonoids and their interaction mechanisms

Cited by 36 publications

References 40 publications

Natural Sweetener, Glycyrrhetinic Acid 3-O-Mono-beta-d-glucuronide, for Postprandial Hyperglycemia Management

Natural Sweetener, Glycyrrhetinic Acid 3-O-Mono-beta-d-glucuronide, for Postprandial Hyperglycemia Management

Dietary phenolic compounds as promising therapeutic agents for diabetes and its complications: A comprehensive review

Polyketides with α-glucosidase inhibitory and neuroprotective activities from Aspergillus versicolor associated with Pedicularis sylvatica

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