Untapped diamonds for untamed diabetes: The α-glucosidase inhibitors

Kalra, Sanjay; Chadha, Manoj; Sharma, Swati; Unnikrishnan, AG

doi:10.4103/2230-8210.129102

Cited by 9 publications

(4 citation statements)

References 11 publications

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“…One class of drugs to treat DM is α-glucosidase inhibitors, which can prevent the carbohydrate digestion and, consequently, defer glucose absorption and suppress postprandial hyperglycemia. , Therefore, the inhibitors of α-glucosidase have been recommended as first-line agents for the treatment of DM. They can be used alone or in combination with other antidiabetic agents for the treatment of type 2 DM and can also be used for patients with type 1 DM . Inhibitors of α-glucosidase, such as voglibose, miglitol, and acarbose, are currently used clinically, but their use may be limited as a result of side effects, such as diarrhea, abdominal cramping, flatulence, and vomiting. , Therefore, much effort has been devoted to developing a lead compound by searching for effective α-glucosidase inhibitors from natural sources.…”

Section: Introductionmentioning

confidence: 99%

“…They can be used alone or in combination with other antidiabetic agents for the treatment of type 2 DM and can also be used for patients with type 1 DM. 5 Inhibitors of αglucosidase, such as voglibose, miglitol, and acarbose, are currently used clinically, but their use may be limited as a result of side effects, such as diarrhea, abdominal cramping, flatulence, and vomiting. 6,7 Therefore, much effort has been devoted to developing a lead compound by searching for effective α-glucosidase inhibitors from natural sources.…”

Section: ■ Introductionmentioning

confidence: 99%

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Resveratroloside Alleviates Postprandial Hyperglycemia in Diabetic Mice by Competitively Inhibiting α-Glucosidase

Zhao

Tao

Zhang

et al. 2019

J. Agric. Food Chem.

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The regulation of postprandial blood glucose (PBG) levels is an effective therapeutic method to treat diabetes and prevent diabetes-related complications. Resveratroloside is a monoglucosylated form of stilbene that is present in red wine, grapes, and several traditional medicinal plants. In our study, the effect of resveratroloside on reducing PBG was studied in vitro and in vivo. In comparison to the starch treatment alone, the oral administration of resveratroloside−starch complexes significantly inhibited the PBG increase in a dose-dependent pattern in normal and diabetic mice. The PBG level treated with resveratrol (30 mg/kg) was not lower than that of resveratroloside. Further analyses demonstrated that resveratroloside strongly and effectively inhibited α-glucosidase, with an 50% inhibitory concentration value of 22.9 ± 0.17 μM, and its inhibition was significantly stronger than those of acarbose and resveratrol (264 ± 3.27 and 108 ± 2.13 μM). Moreover, a competitive inhibition mechanism of resveratroloside on α-glucosidase was determined by enzyme kinetic assays and molecular docking experiments. The molecular docking of resveratroloside with α-glucosidase demostrated the competitive inhibitory effect of resveratroloside, which occupies the catalytic site and forms strong hydrogen bonds with the residues of α-glucosidase. Resveratrol was also determined to be a competitive inhibition mechanism on α-glucosidase by enzyme kinetic assays and molecular docking experiments. This study suggested that resveratroloside had the ability to regulate PBG levels and can be considered a potential agent for the treatment of diabetes mellitus.

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Section: Introductionmentioning

confidence: 99%

Section: ■ Introductionmentioning

confidence: 99%

Resveratroloside Alleviates Postprandial Hyperglycemia in Diabetic Mice by Competitively Inhibiting α-Glucosidase

Zhao

Tao

Zhang

et al. 2019

J. Agric. Food Chem.

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“…With the significant delay of intestinal glucose absorption, α-glucosidase inhibitors can reduce postprandial hyperglycemia to lower the risk of late diabetic complications . As a result of its tolerability and cardiovascular benefits, the International Diabetes Federation (IDF) has recommended α-glucosidase inhibitors as a first-line therapy for DM …”

Section: Introductionmentioning

confidence: 99%

“…14 As a result of its tolerability and cardiovascular benefits, the International Diabetes Federation (IDF) has recommended αglucosidase inhibitors as a first-line therapy for DM. 15 Many sugar derivatives, such as sugar alcohols, as a result of their low-energy character, have been developed into food additives as substitutes for glucose. 16 The sugar alcohol erythritol exists naturally in algae, wine, sake, beer, pears, grapes, watermelons, and mushrooms and is a C4 polyol, which was approved in 1997 by the U.S. Food and Drug Administration (FDA) to be listed on the generally recognized as safe (GRAS) list.…”

Section: ■ Introductionmentioning

confidence: 99%

Erythritol Attenuates Postprandial Blood Glucose by Inhibiting α-Glucosidase

Wen

Tang

Stewart

et al. 2018

J. Agric. Food Chem.

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Diabetes mellitus (DM) is a serious metabolic disorder, where impaired postprandial blood glucose regulation often leads to severe health complications. The natural chemical erythritol is a C4 polyol approved by the U.S. Food and Drug Administration for use as a sweetener. Here, we examined a potential role for erythritol in the control of postprandial blood glucose levels in DM. An anti-postprandial hyperglycemia effect upon erythritol administration (500 mg kg) was demonstrated in alloxan-induced DM model mice by monitoring changes in blood glucose after intragastric administration of drugs and starch. We also found that erythritol most likely exerts its anti-postprandial hyperglycemic activities by inhibiting α-glucosidase in a competitive manner. This was supported by enzyme activity assays and molecular modeling experiments. In the latter experiments, it was possible to successfully dock erythritol into the catalytic pocket of α-glucosidase, with the resultant interaction likely driven by electrostatic interactions involving Asp215, Asp69, and Arg446 residues. This study suggests that erythritol may not only serve as a glucose substitute but also be a useful agent in the treatment of DM to help manage postprandial blood glucose levels.

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