Inhibition of the carbohydrate-hydrolyzing enzymes α-amylase and α-glucosidase by hydroxylated xanthones

Santos, Clementina M.M.; Proença, Carina; Freitas, Marisa; Araújo, Alberto N.; Silva, Artur M. S.; Fernandes, Eduarda

doi:10.1039/d2fo00023g

Cited by 18 publications

(10 citation statements)

References 47 publications

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“…This also corresponds to the level of serum glucose results that showed these two groups as well as the NC have the lowest serum glucose level. This aligns with various reports showing that inhibitors of these starch hydrolyzing enzymes are effective in managing T2D (Oboh et al, 2015, Ademiluyi & Oboh, 2013, Santos et al, 2022). Furthermore, the GI value of these samples as earlier mentioned showed a positive correlation to the pancreatic α‐amylase activity; the sample having the highest GI (25:75 BL) also had the highest α‐amylase activity.…”

Section: Discussionsupporting

confidence: 91%

“…During digestion, carbohydrate content in a food sample is broken down into glucose and this produces a rise in the blood glucose level. Two major enzymes have been implicated in the metabolism of carbohydrates; α‐amylase and α‐glucosidase (Santos et al, 2022). The enzyme, α‐amylase degrades starch, a polysaccharide, by acting on the α‐1,4 glycosidic bonds present in the starch molecules and hydrolyzing them to small‐chain dextrins.…”

Section: Discussionmentioning

confidence: 99%

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Glycemic indices and effect of bitter leaf ( Vernonia amygdalina ) flavored non‐alcoholic wheat beer ( NAWB ) on key carbohydrate metabolizing enzymes in high fat diet fed ( HFD )/ STZ ‐induced diabetic Wistar rats

Akerele

Adedayo

Oboh

et al. 2022

Journal of Food Biochemistry

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In a bid to make the use of functional food easier in the management and prevention of diseases, product development and fortification from/with functional foods have become the recent focus of research. This study, therefore, sought to exploit the recent trend in the brewing industry on the production of non‐alcoholic beers by investigating the possibility of having a non‐alcoholic beer flavored with bitter leaf, a known plant widely reported to have a strong hypoglycemic effect, as against the traditional use of hops, and the effect of the produced beer on the glycemic indices and various diabetic biochemical parameters that serve as biomarkers for type‐2 diabetes (T2D). The glycemic indices, as well as the inhibitory potentials of bitter leaf‐flavored Non‐alcoholic wheat beer (NAWB) in ratios of 100%HP, 100%BL, 75:25BL, 50:50BL, and 25:75BL, on enzymes linked to a high‐fat diet/streptozocin (HFD/STZ)‐induced T2D albino Wistar rats were investigated. There were no significant difference (p > .05) between the starch (1.72–1.77 mg/100 mL), amylose (0.22–0.24 mg/100 mL), and amylopectin (1.49–1.53 mg/100 mL) contents of the various samples. The Glycemic Index (GI) of the samples ranged from 36 to 73 with 75:25Bl and 50:50BL have the lowest (36) values. The samples reduced blood glucose levels and inhibited pancreatic α‐amylase, lipase, and intestinal α‐glucosidase activity. The inhibitory potentials of these beer samples on α‐amylase and α‐glucosidase as well as their ability to reduce blood glucose levels in diabetic rats thus making the bitter leaf flavored NAWB a suitable healthy beverage for better glycemic control in diabetics. Practical applications This study revealed the potential of producing non‐alcoholic wheat beer flavored with bitter leaves as a possible substitute for hops. The potential inherent in bitter leaf in the management of type 2 diabetes can thus be made available through a far‐reaching beverage medium such as non‐alcoholic beer to help in the treatment/management of T2D. The results of this research could be an eye‐opener to the possible utilization of bitter leaf and by extension other plants that have been reported in the management of T2D. The use of the bitter leaf as a substitute for hops in the production of non‐alcoholic beer in the brewing industry could help in a health‐oriented campaign for safe drinks that could be helpful in the control of blood glucose levels of diabetic patients.

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Section: Discussionsupporting

confidence: 91%

Section: Discussionmentioning

confidence: 99%

Glycemic indices and effect of bitter leaf ( Vernonia amygdalina ) flavored non‐alcoholic wheat beer ( NAWB ) on key carbohydrate metabolizing enzymes in high fat diet fed ( HFD )/ STZ ‐induced diabetic Wistar rats

Akerele

Adedayo

Oboh

et al. 2022

Journal of Food Biochemistry

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“…In Figure 5c, with the increase of inhibitor (Cur), the K m value (−1/K m is the intercept of the x‐axis) increased. However, the maximum reaction speed, V max (1/V max is the y‐axis intercept), remained unchanged, which is a competitive inhibition dynamic process [34]. Cur may directly bond to the active fraction of α‐Glu and contend with p ‐NPG (the substrate) through the catalyst.…”

Section: Resultsmentioning

confidence: 99%

Inhibition of α‐glucosidase activity by curcumin loaded on ZnO@rGO nanocarrier for potential treatment of diabetes mellitus

Liu,

Wang,

Yap

et al. 2024

Luminescence

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Curcumin (Cur) is an acidic polyphenol with some effects on α‐glucosidase (α‐Glu), but Cur has disadvantages such as being a weak target, lacking passing the blood–brain barrier and having low bioavailability. To enhance the curative effect of Cur, the hybrid composed of ZnO nanoparticles decorated on rGO was used to load Cur (ZnO@rGO‐Cur). The use of the multispectral method and enzyme inhibition kinetics analysis certify the inhibitory effect and interaction mechanism of ZnO@rGO‐Cur with α‐Glu. The static quenching of α‐Glu with both Cur and ZnO@rGO‐Cur is primarily driven by hydrogen bond and van der Waals interactions. The conformation‐changing ability by binding to the neighbouring phenolic hydroxyl group of Cur increased their ability to alter the secondary structure of α‐Glu, resulting in the inhibition of enzyme activity. The inhibition constant (Ki, Cur > Kis,ZnO@rGO‐Cur) showed that the inhibition effect of ZnO@rGO‐Cur on α‐Glu was larger than that of Cur. The CCK‐8 experiments proved that ZnO@rGO nanocomposites have good biocompatibility. These results suggest that the therapeutic potential of ZnO@rGO‐Cur composite is an emerging nanocarrier platform for drug delivery systems for the potential treatment of diabetes mellitus.

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“…This difference in composition is a consideration for drug manufacturing, where compounds with a higher composition will cost less in the extraction and drug manufacturing processes. Based on research conducted by Santos et al [ 27 ] in 2022, the γ-mangostin compound had better α-glucosidase inhibitory activity than α-mangostin with a value of 11.4 ± 0.3 µM against 137 ± 2 µM, respectively. This value is in line with the MD simulation results, where the γ-mangostin compound had better free energy than α-mangostin (−15.2123 kcal/mol).…”

Section: Discussionmentioning

confidence: 99%

In Silico Study of Mangostin Compounds and Its Derivatives as Inhibitors of α-Glucosidase Enzymes for Anti-Diabetic Studies

Maulana

Sriwidodo

Rukayadi

et al. 2022

Biology

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Diabetes is a chronic disease with a high mortality rate worldwide and can cause other diseases such as kidney damage, narrowing of blood vessels, and heart disease. The concomitant use of drugs such as metformin, sulfonylurea, miglitol, and acarbose may cause side effects with long-term administration. Therefore, natural ingredients are the best choice, considering that their long-term side effects are not significant. One of the compounds that can be used as a candidate antidiabetic is mangostin; however, information on the molecular mechanism needs to be further analyzed through molecular docking, simulating molecular dynamics, and testing the in silico antidiabetic potential. This study focused on modeling the protein structure, molecular docking, and molecular dynamics simulations and analyses. This process produces RMSD values, free energies, and intermolecular hydrogen bonding. Based on the analysis results, all molecular dynamics simulations can occur under physiological conditions, and γ-mangostin is the best among the test compounds.

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Inhibition of the carbohydrate-hydrolyzing enzymes α-amylase and α-glucosidase by hydroxylated xanthones

Abstract: Xanthones are oxygen-containing heterocyclic compounds that exhibit a wide range of biological and pharmacological properties. Some natural and synthetic derivatives have been identified for their antidiabetic profile, mainly as α-glucosidase...

Cited by 18 publications

References 47 publications

Glycemic indices and effect of bitter leaf ( Vernonia amygdalina ) flavored non‐alcoholic wheat beer ( NAWB ) on key carbohydrate metabolizing enzymes in high fat diet fed ( HFD )/ STZ ‐induced diabetic Wistar rats

Glycemic indices and effect of bitter leaf ( Vernonia amygdalina ) flavored non‐alcoholic wheat beer ( NAWB ) on key carbohydrate metabolizing enzymes in high fat diet fed ( HFD )/ STZ ‐induced diabetic Wistar rats

Inhibition of α‐glucosidase activity by curcumin loaded on ZnO@rGO nanocarrier for potential treatment of diabetes mellitus

In Silico Study of Mangostin Compounds and Its Derivatives as Inhibitors of α-Glucosidase Enzymes for Anti-Diabetic Studies

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