Structure-Function Elucidation of Flavonoids by Modern Technologies
Dilip Ghosh, Pulok K. Mukherjee in Natural Medicines, 2019
Alpha-glucosidase (α-glucosidase) is an important enzyme that catalyses the final step of starch digestion in the small intestine. The α-glucosidase inhibitors help to lower the postprandial blood glucose and insulin levels in diabetic patients (van de Laar 2008). Acarbose and miglitol are extensively studied α-glucosidase inhibitors and have been found to be effective in lowering blood glucose level in type 1 and type 2 diabetic patients. In older type 2 diabetic patients, acarbose also showed increased insulin sensitivity (Sugihara et al. 2014). The α-glucosidase inhibitory activity of phytochemicals can be determined as illustrated by Walker et al. (1993). Some examples of the flavonoids already known for their α-glucosidase inhibition activity are rutin (Li et al. 2009; Oboh et al. 2015), quercetin (Tadera et al. 2006; Li et al. 2009; Oboh et al. 2015; Semaan et al. 2017), myricetin (Tadera et al. 2006; Kang et al. 2015), kaempferol (Peng et al. 2016), luteolin (Kim et al. 2000; Tadera et al. 2006), fisetin (Tadera et al. 2006), isoquercetin (Li et al. 2009), naringenin (Tadera et al. 2006; Priscilla et al. 2014) and epigallocatechin-3-gallate (EGCG; Tadera et al. 2006).
Potential of Diet and Dietary Supplementation to Ameliorate the Chronic Clinical Perturbations of Metabolic Syndrome
Stephen T. Sinatra, Mark C. Houston in Nutritional and Integrative Strategies in Cardiovascular Medicine, 2015
To be absorbed, CHO must be broken down into monosaccharides. At a minimum, two major enzymes are involved in this process. Alpha-amylase from saliva and pancreatic juice decomposes starches into monosaccharide, disaccharide, trisaccharide, and oligosaccharide units. Alpha-glucosidases bound in the brush border of the small intestines further divide the remaining larger units into monosaccharides.87 To give an example, sucrose, commonly referred to as “table sugar‚” is a disaccharide of linked glucose and fructose. Sucrase, an alpha-glucosidase, breaks down sucrose into glucose and fructose. Different monosaccharides are absorbed by different transport mechanisms.87 As a general principal, the smaller the CHO molecule, the more rapid is the absorption (high glycemic index). This rapid absorption has been connected to the harm that excess sugar intake (high glycemic load) induces.84,85
Therapeutic Potential of Marine Foods: A Review
Hafiz Ansar Rasul Suleria, Megh R. Goyal in Health Benefits of Secondary Phytocompounds from Plant and Marine Sources, 2021
The α-Glucosidase activity is prohibited through callyspongynic acid (also known as polyacetylenic acid) that is derived from sponge Callyspongia truncate [103]. To prevent the glycogen hydrolysis, α-Glucosidase is interfaced within the mechanism because it is responsible to keep the concentration of glucose in the blood at a desirable low level [181]. Another polybromodiphenyl ether compound isolated from Indonesian marine sponge (Lamellodysidea herbacea) inhibits protein tyrosine phosphatase 1B (an important target for diabetes treatment) [166]. Marine omega-3 FAs show beneficial effects on the prevention of T2D in the Asian population, which suggests an association between consumption of fish or fish oil and the development of Type-2 diabetes on geographical location [183].
Benzonate derivatives of acetophenone as potent α-glucosidase inhibitors: synthesis, structure–activity relationship and mechanism
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
Wen-Jia Dan, Qiang Zhang, Fan Zhang, Wei-Wei Wang, Jin-Ming Gao
Diabetes mellitus is one of the major chronic diseases1. The incidence and prevalence of diabetes have risen sharply in recent years, and 642 million people might be suffering from diabetes until 20402,3. α-Glucosidase is a type of glycoside hydrolase, which favors in absorption of carbohydrates. By inhibiting its activity, the absorption of small intestine carbohydrates could be delayed, which bring on the reduction of postprandial blood glucose4,5. Moreover, the inhibition of α-glucosidase also has positive effects to treat some diseases such as virosis, cancer, and chronic heart failure etc6,7. Nowadays, the α-glucosidase inhibitors have been recognised as an efficient therapy in the treatment of type-II diabetes (T2D)8. They inhibit membrane bound α-glucosidase in the cells lining the small intestine, which in turn decreases the digestion of starch and additional dietary sugars, helping to avoid hyperglycemia and maintain normal blood sugar levels9. Therefore, it is significant to discover new classes of α-glucosidase inhibitors and to investigate the action mechanism of these inhibitors.
Synthesis, in vitro inhibitory activity, kinetic study and molecular docking of novel N-alkyl–deoxynojirimycin derivatives as potential α-glucosidase inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Ping Lin, Jia-Cheng Zeng, Ji-Guang Chen, Xu-Liang Nie, En Yuan, Xiao-Qiang Wang, Da-Yong Peng, Zhong-Ping Yin
α-Glucosidase is a type of glucosidases that acts on 1,4-α-bonds, which locate on the brush edge of the small intestine and play a critical role in digestion and absorption of carbohydrates1. Inhibition of α-glucosidase is one approach to delay the absorption of glucose and decrease the postprandial blood glucose level2. Therefore, α-glucosidase inhibitors are widely used for the prevention and treatment of typeII diabetes millitus3. Besides, α-glucosidase participates in other physical and biological processes as well and may also be used as a therapeutic agent for other diseases, such as cancer4 and HIV5. Today, several types of α-glucosidase inhibitors are being clinically used for the treatment of typeII diabetes millitus, such as acarbose, voglibose, and miglitol6. However, these medications also have adverse effects, including abdominal discomfort, diarrhoea, and flatulence7. So, developing novel α-glucosidase inhibitors is critical and attractive.
Prominent and emerging anti-diabetic molecular targets
Published in Journal of Drug Targeting, 2021
Faezeh Almasi, Fatemeh Mohammadipanah
Alpha-glucosidase, located in the cells lining the small intestine, liberates glucose by cleaving α (1→4) bonds in starch and disaccharides. Acarbose and miglitol are commercially available alpha-glucosidase inhibitors (AGIs) that decrease glucose uptake through the intestine. These types of inhibitors are studied vastly due to a more effective reduction of glucose variability compared to other anti-diabetic drugs [9,10]. In addition to glycemic control, acarbose also has some additive effects, such as glycemic excursions, reducing pro-inflammatory cytokines, stabilising carotid plaque, and reversing impaired glucose tolerance [11]. Acarbose as the most widely prescribed α-glucosidase inhibitor is not a drug of first choice and is less effective than metformin (the most common prescribed individual drug) on reducing glucose levels [12].
Related Knowledge Centers
- Alglucosidase Alfa
- Cellulase
- Glycogen Debranching Enzyme
- Maltase
- Rhodnius Prolixus
- Maltase-Glucoamylase
- Glucosidases
- Brush Border
- Β-Glucosidase
- Glycogen Storage Disease Type II