Safety and efficacy of acarbose in the treatment of diabetes in Chinese patients

He, Ke; Shi, Jun-Cheng; Mao, Xiao‐Ming

doi:10.2147/tcrm.s50362

Cited by 31 publications

(19 citation statements)

References 53 publications

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“…Moreover, in previous studies, these fatty acids showed remarkable inhibition on α-glucosidase enzyme, which was significantly higher than acarbose [27,35]. Therefore, C. indica fruits could be predicted as having potential for anti-α-glucosidase activity, which is involved in the prevention of hyperglycemia [36]. If that is the case, a comprehensive solution for type 2 diabetes avoidance could be exploited from C. indica fruits.…”

Section: Discussionmentioning

confidence: 98%

Antioxidant and α-amylase Inhibitory Activities and Phytocompounds of Clausena indica Fruits

et al. 2020

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Background: Clausena indica fruit is commonly used for food ingredients and traditional medicines in tropical countries, however, information about its biological activities and chemical profiles has been inadequately reported. Methods: In this study, a bio-guided fractionation of antioxidants and α-amylase inhibitors from hexane (MH) and ethyl acetate (ME) extracts of C. indica fruit (pericarp and seed) was carried out. Eleven fractions from MH (D1–D11) and 17 fractions from ME (T1–T17) were obtained from column chromatography over silica gel, which were then examined for anti-radical capacity by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays, and pancreatic α-amylase inhibition, a key enzyme linked to type 2 diabetes. Results: Of isolated fractions, the fraction T4 revealed the most potent anti-DPPH activity (IC50 = 0.13 mg/mL), whereas T2 exhibits the strongest ABTS cation scavenging ability (IC50 = 0.31 mg/mL). In the enzymatic assay, the fractions D3 and T4 significantly inhibit the α-amylase reaction with IC50 values of 0.34 and 0.86 mg/mL, respectively. Remarkably, α-amylase suppression of T4 is close to acarbose and over four times stronger than palmitic acid, which are the well-known α-amylase inhibitors (IC50 = 0.07 and 1.52 mg/mL, respectively). The active constituents from fractions were identified by gas chromatography-mass spectrometry (GC-MS). The results show that the fraction D3 contains five major compounds, which are grouped in five classes consisting of fatty acids, phenols, benzodioxoles, alcohols, and sesquiterpenes. Among them, palmitic acid is the most dominant compound (32.64%), followed by 2R-acetoxymethyl-1,3,3-trimethyl-4t-(3-methyl-2-buten-1-yl)-1t-cyclohexanol (16.69%). Whilst, six major compounds belonging to fatty acid and coumarin classes are identified in the fraction T4. The most abundant compound in T4 is dentatin (47.32%), followed by palmitic acid (15.11%). Conclusions: This is the first finding that C. indica fruit can be a promising source for the development of natural antioxidant and antidiabetic agents. Additionally, the outcome reveals that dentatin, a known natural antineoplastic agent, can be feasibly exploited from C. indica fruit.

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Section: Discussionmentioning

confidence: 98%

Antioxidant and α-amylase Inhibitory Activities and Phytocompounds of Clausena indica Fruits

et al. 2020

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“…The α-glucosidase inhibitors (AGIs) primarily reduce postprandial plasma glucose concentrations through the competitive and reversible inhibition of α-glucosidase located in the brush border of the small intestine 60. Following nutrient ingestion, α-glucosidase hydrolyzes complex carbohydrates to monosaccharides for absorption.…”

Section: Actions Of Commonly Used Antidiabetes Medicationsmentioning

confidence: 99%

“…Following nutrient ingestion, α-glucosidase hydrolyzes complex carbohydrates to monosaccharides for absorption. Thus, AGIs obstruct the degradation of starches and sucrose and delay carbohydrate reabsorption in a nonsystemic manner 60. However, a patient’s diet may alter efficacy.…”

Section: Actions Of Commonly Used Antidiabetes Medicationsmentioning

confidence: 99%

“…However, a patient’s diet may alter efficacy. Studies indicate that AGIs may have a more potent effect in patients who consume a typical Eastern diet (whole grains, vegetables, fruits) compared with patients whose diet is characterized as Western (processed meat, high-fat dairy products, refined grains) 60,61…”

Section: Actions Of Commonly Used Antidiabetes Medicationsmentioning

confidence: 99%

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Practical combination therapy based on pathophysiology of type 2 diabetes

Levin

2016

DMSO

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Type 2 diabetes is a complex, chronic, and progressive condition that often necessitates the use of multiple medications to achieve glycemic goals. Clinical guidelines generally recommend intensifying pharmacotherapy if glycemic goals are not achieved after 3 months of treatment. However, for many patients with type 2 diabetes, treatment intensification is delayed or does not occur. Initiating combination therapy early in the disease course has the potential to delay disease progression and improve patient outcomes. Guidelines generally provide a list of agents that may be used in combination regimens and emphasize individualization of treatment. The purpose of this review is to discuss the rationale for combination therapy, considering treatment effects on pathophysiologic aspects of type 2 diabetes and individual drug profiles. The combination of newer antidiabetes therapies with complementary mechanisms of action provides the opportunity to target multiple sites of tissue, organ, and cellular dysfunction.

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“…Acarbose is a type of noninsulinotropic oral antidiabetic drug molecule, which mainly used to treat type two diabetes [1]. It is mainly used with a proper diet supplemented food and regular exercise to control the blood sugar in humans [2]. Acarbose also helps to prevent kidney damage, blindness, nerve cord problem, and other performance via controlling high blood sugar.…”

Section: Introductionmentioning

confidence: 99%

Spectroscopic and thermodynamic interaction studies of anti-diabetic drug with globular proteins

2019

Biointerface Res Appl Chem

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Drug-protein interaction is a fundamental problem in estimating the serious side effects of the drug. Hence, the main objective of this study was to study the interaction of acarbose with three different globular proteins i.e.; bovine serum albumin (BSA), human serum albumin (HSA), and hemoglobin (Hb) via UV-Visible absorption spectroscopic analysis. We were determined physicochemical parameters, binding constant, distribution constant and thermodynamic parameters activation energy, enthalpy, entropy, and Gibbs free energy by using UV-visible data. These both properties of acarbose-protein complexes indicated that the hydrogen bonding and weak van der Waals force played a major role in the interaction for complexation. The binding of acarbose with different proteins leads to change in the structure of protein folding which confirms by physicochemical and thermodynamic analysis.

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Safety and efficacy of acarbose in the treatment of diabetes in Chinese patients

Cited by 31 publications

References 53 publications

Antioxidant and α-amylase Inhibitory Activities and Phytocompounds of Clausena indica Fruits

Antioxidant and α-amylase Inhibitory Activities and Phytocompounds of Clausena indica Fruits

Practical combination therapy based on pathophysiology of type 2 diabetes

Spectroscopic and thermodynamic interaction studies of anti-diabetic drug with globular proteins

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