Inhibition of α-glucosidase activity and non-enzymatic glycation by tannic acid: Inhibitory activity and molecular mechanism

Huang, Qian; Chai, Wei-Ming; Ma, Zuo-Yuan; Ou-Yang, Chong; Wei, Qiming; Song, Shuang; Zou, Zhengrong; Peng, Yiyuan

doi:10.1016/j.ijbiomac.2019.09.010

Cited by 52 publications

(36 citation statements)

References 40 publications

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“…4(D)). PCH peptides might induce conformational changes or prevent the substrate from entering the active site of the enzyme, thus inhibiting the catalytic activity of α‐glucosidase 28 . These two types of peptide exert their actions on α‐glucosidase to provide synergistic hypoglycemic activity.…”

Section: Discussionmentioning

confidence: 99%

Hypoglycemic peptide‐enriched hydrolysates of Corbicula fluminea and Chlorella sorokiniana possess synergistic hypoglycemic activity through inhibiting α‐glucosidase and dipeptidyl peptidase‐4 activity

et al. 2021

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BACKGROUND The prevalence of diabetes mellitus worldwide has increased in recent decades. Maintaining the level of blood glucose is the most basic and important issue for diabetics. This study aimed to investigate the hypoglycemic activity of a combination of hypoglycemic peptide‐enriched hydrolysates of Corbicula fluminea (ACH) and Chlorella sorokiniana (PCH). RESULTS Combined supplementation of ACH and PCH synergistically inhibited α‐glucosidase and DPP4 activities in vitro. After 4 weeks of treatment with ACH and/or PCH, the plasma glucose concentration and insulin, homeostasis model assessment‐estimated insulin resistance (HOMA‐IR), total cholesterol (TC) and triglyceride (TG) levels significantly decreased. The hypoglycemic peptides in ACH and PCH were purified and assayed for α‐glucosidase and DPP4 activity. The hypoglycemic peptides in ACH and PCH effectively decreased α‐glucosidase and DPP4 activities. In silico assays showed that these two peptide types have different docking poses, which determined their inhibitory effect against α‐glucosidase and DPP4 activity. CONCLUSION Combined treatment with hypoglycemic peptide‐enriched ACH and PCH could modulate blood glucose by synergistically inhibiting α‐glucosidase and DPP4 activities. © 2021 Society of Chemical Industry.

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Section: Discussionmentioning

confidence: 99%

Hypoglycemic peptide‐enriched hydrolysates of Corbicula fluminea and Chlorella sorokiniana possess synergistic hypoglycemic activity through inhibiting α‐glucosidase and dipeptidyl peptidase‐4 activity

et al. 2021

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“…Inhibitory kinetic mechanisms of α‐glucosidase by T 1 – T 3 were determined using Lineweaver–Burk plots, with methods similar to those previously reported [31,47] . Inhibition kinetics were performed by varying concentrations of T 1 – T 3 and detecting different concentrations of the inhibitor substrate.…”

Section: Methodsmentioning

confidence: 99%

Natural Triterpenoids Isolated from Akebia trifoliata Stem Explants Exert a Hypoglycemic Effect via α‐Glucosidase Inhibition and Glucose Uptake Stimulation in Insulin‐Resistant HepG2 Cells

Bian

Yang

Elango

et al. 2021

Chemistry & Biodiversity

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The inhibition of α‐glucosidase activity is a prospective approach to attenuate postprandial hyperglycemia in the treatment of type 2 diabetes mellitus (T2DM). Herein, the inhibition of α‐glucosidase by three compounds T1–T3 of Akebia trifoliata stem, namely hederagenin (T1), 3‐epiakebonoic acid (T2), and arjunolic acid (T3) were investigated using enzyme kinetics and molecular docking analysis. The three triterpenoids exhibited excellent inhibitory activities against α‐glucosidase. T1–T3 showed the strongest inhibition with IC50 values of 42.1±5.4, 19.6±3.2, and 11.2±2.3 μM, respectively, compared to the acarbose positive control (IC50=106.3±8.2). Enzyme inhibition kinetics showed that triterpenoids T1–T3 demonstrated competitive, mixed, and noncompetitive‐type inhibition against α‐glucosidase, respectively. The inhibition constant (Ki) values were 21.21, 7.70, and 3.18 μM, respectively. Docking analysis determined that the interaction of ligands T1–T3 and α‐glucosidase was mainly forced by hydrogen bonds and hydrophobic interactions, which could result in improved binding to the active site of the target enzyme. The insulin resistant (IR)‐HepG2 cell model used in this study (HepG2 cells exposed to 10−7 M insulin for 24 h) and glucose uptake assays showed that compounds T1–T3 had no cytotoxicity with concentrations ranging from 6.25 to 25 μM and displayed significant stimulation of glucose uptake in IR‐HepG2 cells. Thus, triterpenoids T1–T3 showed dual therapeutic effects of α‐glucosidase inhibition and glucose uptake stimulation and could be used as potential medicinal resources to investigate new antidiabetic agents for the prevention or treatment of diabetes.

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“…Finally, tannic acid is a specific form of tannin, which is widely distributed in green tea, wine, grapes, and plants. It has strong antioxidant, anti-inflammatory, anticarcinogenic and antimutagenic activities [ 67 ] and anti-glycation activities [ 68 , 69 ].…”

Section: Methodsmentioning

confidence: 99%

Polyphenols Attenuate Highly-Glycosylated Haemoglobin-Induced Damage in Human Peritoneal Mesothelial Cells

et al. 2020

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We investigated the cytoprotective role of the dietary polyphenols on putative damage induced by Amadori adducts in Human Peritoneal Mesothelial Cells (HPMCs). Increased accumulation of early products of non-enzymatic protein glycation—Amadori adducts—in the peritoneal dialysis fluid due to their high glucose, induces severe damage in mesothelial cells during peritoneal dialysis. Dietary polyphenols reportedly have numerous health benefits in various diseases and have been used as an efficient antioxidant in the context of several oxidative stress-related pathologies. HPMCs isolated from different patients were exposed to Amadori adducts (highly glycated haemoglobin, at physiological concentrations), and subsequently treated with several polyphenols, mostly presented in our Mediterranean diet. We studied several Amadori-induced effects in pro-apoptotic and oxidative stress markers, as well as the expression of several pro-inflammatory genes (nuclear factor-kappaB, NF-kB; inducible Nitric Oxide synthetase, iNOS), different caspase-activities, level of P53 protein or production of different reactive oxygen species in the presence of different polyphenols. In fact, cytoprotective agents such as dietary polyphenols may represent an alternate approach to protect mesothelial cells from the cytotoxicity of Amadori adducts. The interference with the Amadori adducts-triggered mechanisms could represent a therapeutic tool to reduce complications associated with peritoneal dialysis in the peritoneum, helping to maintain peritoneal membrane function longer in patients undergoing peritoneal dialysis.

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Inhibition of α-glucosidase activity and non-enzymatic glycation by tannic acid: Inhibitory activity and molecular mechanism

Cited by 52 publications

References 40 publications

Hypoglycemic peptide‐enriched hydrolysates of Corbicula fluminea and Chlorella sorokiniana possess synergistic hypoglycemic activity through inhibiting α‐glucosidase and dipeptidyl peptidase‐4 activity

Hypoglycemic peptide‐enriched hydrolysates of Corbicula fluminea and Chlorella sorokiniana possess synergistic hypoglycemic activity through inhibiting α‐glucosidase and dipeptidyl peptidase‐4 activity

Natural Triterpenoids Isolated from Akebia trifoliata Stem Explants Exert a Hypoglycemic Effect via α‐Glucosidase Inhibition and Glucose Uptake Stimulation in Insulin‐Resistant HepG2 Cells

Polyphenols Attenuate Highly-Glycosylated Haemoglobin-Induced Damage in Human Peritoneal Mesothelial Cells

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