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Allopathic Medicines
Published in Varma H. Rambaran, Nalini K. Singh, Alternative Medicines for Diabetes Management, 2023
Varma H. Rambaran, Nalini K. Singh
Alpha-glucosidase inhibitors (AGIs), such as acarbose (Glucobay) (Figure 2.9a), miglitol (Figure 2.9b), and voglibose (Figure 2.9c), form a new class of “suppressing-based” therapy that target the enzyme, α-glucosidase (AG). AG is an exo-type carbohydrase that is responsible for breaking down complex carbohydrates to glucose in the upper gastrointestinal tract (Kumar, Narwal et al. 2011, Lebovitz 1998). As such, the inhibition of the AG enzyme results in a decrease in complex carbohydrate catabolism, which as a consequence, retards the rise in postprandial BG levels (Lebovitz 1998).Structural formulae of α-glucosidase inhibitors: (a) acarbose, (b) miglitol, and (c) voglibose.
Heterocyclic Drugs from Plants
Published in Rohit Dutt, Anil K. Sharma, Raj K. Keservani, Vandana Garg, Promising Drug Molecules of Natural Origin, 2020
Debasish Bandyopadhyay, Valeria Garcia, Felipe Gonzalez
A pyrrole derivative isolated from Grifolafrondosa showed activity both in diabetes and cancer. This derivative inhibits the alpha-glucosidase to demonstrate hypoglycemic effect (Chen et al., 2018). This derivative also works by inhibiting the protein, which promotes the cell growth and migration. G. frondosa is a mushroom and consumption of this mushroom increases preventative qualities (Ma et al., 2014). Acquiring this pyrrole derivative would be relatively cost effective, in contrasting the prices of current available treatments for both cancer and diabetes. Thus far, the pyrrole derivative found in G. frondosa showed capable antitumor properties and positive hypoglycemic effect. It improved the insulin resistance in various animal studies and it would be a much better and cost-effective method of treating diabetes in contrast to currently available expensive insulin pens and anti-diabetic medications. Such treatments cost patients up to plenty of dollars a month. A cost-effective method could mean less hospitalizations, amputations, and deaths of so many. The implications of developing a drug with concomitant preventative and curative properties are great, as it could potentially save both resources and lives.
Structure-Function Elucidation of Flavonoids by Modern Technologies
Published in Dilip Ghosh, Pulok K. Mukherjee, Natural Medicines, 2019
Ritu Varshney, Neeladrisingha Das, Rutusmita Mishra, Partha Roy
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).
Careful use to minimize adverse events of oral antidiabetic medications in the elderly
Published in Expert Opinion on Pharmacotherapy, 2021
Alpha-glucosidase inhibitors reduce postprandial hyperglycemia and have a moderate effect on fasting plasma glucose levels, resulting in a significant but only moderate reduction in HbA1c levels. Both acarbose [58] and miglitol [59] are generally well tolerated and safe in the elderly. One major advantage of alpha-glucosidase inhibitors in comparison with insulin-secretagogues is the absence of hypoglycemia. As alpha-glucosidase inhibitors reduce postprandial hyperglycemia and may reduce the risk of delayed hypoglycemia, these agents may contribute to dampen the overall glycemic variability. They are considered as a useful and relatively safe therapeutic option in elderly patients with T2D [60]. As in younger individuals, most discontinuations after initiation of alpha-glucosidase inhibitors were due to gastrointestinal side effects such as flatulence and diarrhea. Of note, however, a few case reports of paralytic ileus were reported between 1996 and 2006, all in Japan, in elderly (but also in middle-aged) diabetic patients treated with acarbose and voglibose [61]. Despite the potential advantages of alpha-glucosidase inhibitors in elderly patients with T2D, there is a lack of studies focusing specifically on that population and no studies with hard clinical outcomes that demonstrated a protection against diabetic complications.
Meta-inhibition of ocular and gastrointestinal dysfunctions by phenolic-rich fraction of Croton zambsicus leaves in a rat model exposed to chronic mixed metals
Published in Cutaneous and Ocular Toxicology, 2021
J. K. Akintunde, O. R. Omoniyi, O. E. Folorunsho, C. A. Moses
Carbohydrate in the gut is metabolically catabolized into disaccharide and monosaccharide units by alpha-amylase and alpha-glucosidase, respectively to give energy45. The uncontrolled turnover rate of monosaccharide-glucose by these enzymes could be linked to certain pathological conditions including type 2 diabetes, hyperglycaemia and diabetic retinopathy46,47. Results of this study showed that chronic exposure of rats to 0.5 mL EOMABRSL for 98 days and 70 days to rats strongly increased the metabolic activity of colon α-glucosidase and α- amylase enzymes, with indication of chronic diabetic oculopathy47. This further suggests that intestinal disruption by the complex metals with increased carbohydrate metabolising enzymes could be connected to colon inflammatory diseases and its metabolic disorders, which eventually degenerate into visual impairment and hypertension, if not treated at early stage48–50. The results of this study therefore supported the view that administration of 400 mg/kg of phenolic C-ZAMB fraction protected the colon or intestinal dysfunctions caused by complex mixture of environmental metals, evidently seen by the decrease in the activities of alpha-amylase and alpha-glucosidase enzymes in the treated rats51,52.
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].