Bioactive flavonoids from Rubus corchorifolius inhibit α-glucosidase and α-amylase to improve postprandial hyperglycemia

Tian, Jinlong; Si, Xu; Wang, Yuehua; Gong, Ersheng; Xie, Xu; Zhang, Ye; Li, Bin; Shu, Chi

doi:10.1016/j.foodchem.2020.128149

Cited by 69 publications

(77 citation statements)

References 32 publications

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“…Starch digestion is an important target for controlling blood glucose. It has been reported that postprandial hyperglycemia may be alleviated by polyphenols by inhibiting the activities of starch-hydrolyzing enzymes such as α-amylase [ 9 , 31 , 53 ]. In this study, the interaction and possible mechanism between MPPs and α-amylase were investigated preliminarily.…”

Section: Resultsmentioning

confidence: 99%

Inhibitory Effects against Alpha-Amylase of an Enriched Polyphenol Extract from Pericarp of Mangosteen (Garcinia mangostana)

Chen

Jia

et al. 2022

Foods

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The pericarp of mangosteen, a by-product of the mangosteen, is rich in polyphenols. In this study, an efficient and environmentally friendly method for preparative enrichment of polyphenols from mangosteen pericarp (MPPs) was developed, and the inhibitory effects on starch digestion were also evaluated. It was found that the optimal extract method of MPPs was at a solid to solvent ratio of 1:50 g/mL, pH of 2, and at 80 °C for 2 h. The IC50 of MPPs for α-amylase was 0.28 mg/mL. Based on the fluorescence quenching results, we presumed that MPPs could alter the natural structure of α-amylase, resulting in inhibitory activity on α-amylase. In addition, MPPs significantly reduced the blood glucose peak and AUC of glucose responses in rats after ingestion of the starch solution. Taken together, MPPs may have the potential as a functional supplement for blood glucose control and diabetes prevention.

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Section: Resultsmentioning

confidence: 99%

Inhibitory Effects against Alpha-Amylase of an Enriched Polyphenol Extract from Pericarp of Mangosteen (Garcinia mangostana)

Chen

Jia

et al. 2022

Foods

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“…The 4‴–OH and 5‴–OH both interacted with Asp69. Hydrogen bonding and van der Waals forces were the main interaction driving forces, forcing the formation of α‐glucosidase–GUB complex, van der Waals was detected between GUB and nine amino acid residues of α‐glucosidase (Pro312, Arg446, His351, Arg213, Phe178, Glu277, Val216, Gln279, and Gln353), π–π stacking between the aromatic ring of GUB and Tyr72, His280, Arg315 further enhanced the affinity of α‐glucosidase with GUB (Tian et al, 2020). This further verified and complemented the results of thermodynamic analysis.…”

Section: Resultsmentioning

confidence: 99%

“…These results suggested that GUB inhibited α‐glucosidase in a reversible pattern (Chanda et al, 2020). Up to date, reversible inhibition is the major manner of polyphenols against the activity of α‐glucosidase (Tian et al, 2020).…”

Section: Resultsmentioning

confidence: 99%

Inhibitory activity and mechanism of guavinoside B from guava fruits against α‐glucosidase: Insights by spectroscopy and molecular docking analyses

Zhang

et al. 2022

Journal of Food Biochemistry

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Guavinoside B (GUB) is the main active substance in guava fruit and shows promising biological activities. In this study, the inhibitory activity and mechanism of GUB on α-glucosidase were studied by using spectroscopic techniques, kinetic analysis, and molecular docking. Results indicated that GUB possessed significant inhibition ability on α-glucosidase, which was about 10 times that of acarbose. The GUB was a mixed-type inhibitor, which suppressed the activity of α-glucosidase through a reversible process. Fluorescence analysis revealed that GUB quenched the fluorescence of α-glucosidase statically, the formation of GUBα-glucosidase complex was a spontaneous and exothermic process, van der Waals forces, hydrogen bonding, and hydrophobic interaction were the predominant driving forces, only one single-binding site on α-glucosidase was involved in the binding process. GUB inserted into the hydrophobic pocket of α-glucosidase with 11 hydrogen bonds and two π-π stacking formed. The presence of GUB changed the microenvironment near the fluorescent amino acids of α-glucosidase, and the structure of α-glucosidase was slightly changed, eventually leading to the decrease of α-glucosidase activity. Practical applicationsDiabetes mellitus (DM) is a worldwide chronic metabolic disease threatening human health seriously. Guava fruit is a popular fruit, and its extracts were reported to show many biological activities. GUB is the main benzophenone glycoside in guava fruits.However, the inhibitory activity and mechanism of its specific active compound GUB are still unclear. Studies have shown that GUB could reversibly inhibit the activity of α-glucosidase, and its inhibitory ability was about 10 times that of acarbose. The kinetics and mechanism of inhibition were revealed. These will facilitate the further research and application of guava fruit and GUB in functional and healthy foods against hyperglycinaemia or even DM.

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“…The digestive enzymes α-amylase and α-glucosidase hydrolyze α-1,4-glucosidic bonds in starch causing post-prandial hyperglycaemia in patients with diabetes mellitus type 2 (Spínola et al 2019;Tian et al 2021). Despite this being the first report of the enzyme -inhibitory activity of R. discolor fruits, the α-amylase and α-glucosidase inhibitory activity of different Rubus species has been reported in several recently published papers (Salehi et al 2013;Grochowski et al 2019;Spínola et al 2019;Zengin et al 2019;Tian et al 2021). In the present study the examined extracts of R. discolor fruits showed low effi-cacy in inhibiting α-amylase activity.…”

Section: Discussionmentioning

confidence: 99%

“…Those findings are of particular interest because the strong inhibition of α-amylase leads to digestive disconformities due to the fermentation of undigested starch which are the main side effects of officially used drugs in the treatment of diabetes mellitus type 2. Therefore, the use of pharmaceuticals with high α-glucosidase and moderate or weak α-amylase inhibitory activity is highly recommended to control postprandial hyperglycaemia (Spínola et al 2019;Zengin et al 2019;Tian et al 2021).…”

Section: Discussionmentioning

confidence: 99%

Phenolic profile and biological potential of wild blackberry (Rubus discolor) fruits

et al. 2021

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The berries of Rubus discolor are considered a rich source of phytochemicals which could play an important role in the prevention of prevalent contemporary chronic diseases. Thus, the goal of the presented study was to determine the profile of phenolic acids and anthocyanins of aqueous and ethanol extracts of R. discolor fruit, and their free radical scavenging, antiproliferative, antidiabetic and antimicrobial activities. LC-MS/MS analyses confirmed the presence of 11 phenolic acids with protocatechuic and gallic acids being the major compounds. Additionally, cyanidin- glucoside/galactoside was the most abundant among the five identified anthocyanins. The ethanol extract was more efficient in scavenging free radicals than the aqueous extract. The absence of antiproliferative activity was observed for both extracts. However, they inhibited carbohydrate hydrolysing digestive enzymes associated with type-2 diabetes. Furthermore, the obtained results for ?-glucosidase inhibitory activity (IC50 values 44.52 and 80.72 ?g/mL, for the aqueous and ethanol extracts, respectively) indicate significantly higher activity than the positive control, GlucobayR (233.38 ?g/mL). The ethanol extract was more effective against all of the examined bacteria (Bacillus cereus, Staphylococcus aureus and Enterobacter cloacae) than the aqueous extract. On the contrary, the aqueous extract showed better antifungal properties, particularly against Trihoderma viride and Penicillium verrucosum var. cyclopium. The quantified phenolics and presented bioactivities of R. discolor fruit extracts candidate them as a potential source of bioactive compounds which might be used in the food, pharmacy and cosmetic industries.

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Bioactive flavonoids from Rubus corchorifolius inhibit α-glucosidase and α-amylase to improve postprandial hyperglycemia

Cited by 69 publications

References 32 publications

Inhibitory Effects against Alpha-Amylase of an Enriched Polyphenol Extract from Pericarp of Mangosteen (Garcinia mangostana)

Inhibitory Effects against Alpha-Amylase of an Enriched Polyphenol Extract from Pericarp of Mangosteen (Garcinia mangostana)

Inhibitory activity and mechanism of guavinoside B from guava fruits against α‐glucosidase: Insights by spectroscopy and molecular docking analyses

Phenolic profile and biological potential of wild blackberry (Rubus discolor) fruits

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