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Biocatalyzed Synthesis of Antidiabetic Drugs
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Voglibose (Fig. 11.53, 191), ATC Code A10BF03, DrugBank Code DB04878 (trade name Voglib, marketed by Mascot Health Series), an N-substituted derivative of valiolamine 192, is a branched-chain aminocyclitol, or pseudo-amino sugar, whose N-substituted moiety is derived from glycerol. Voglibose is an alpha-glucosidase inhibitor used for lowering post-prandial blood glucose levels in people with diabetes mellitus (Kawamori et al., 2009; Derosa and Maffioli, 2012; Campo et al., 2013). The chemical synthesis of 191 starting from 192 has been described by different methodologies (Chen et al., 2006); on the other hand, 192 was first isolated from the fermentation broth of Streptomyces hygroscopicus subsp. Limoneus IFO12703 (Kameda et al., 1984), although it can be also be obtained either through stereoselective transformation of valienamine 193 or validamine 194 (Horii et al., 1985), or by chemical total syntheses starting from different natural precursors (Shing and Cheng, 2008; Ji et al., 2013; Quan et al., 2013). Finally, 193 can be obtained from biocatalytic hydrolysis of naturally occurring validoxylamine A 195 or validamycin 196 (Zheng et al., 2006; Xue et al., 2007); on the other hand, 193 is one of the components of acarbose 197, a pseudotetrasaccharide in which this polyhydroxylated aminocyclohexene portion is linked via its nitrogen atom to an acarviosine unit, constituted by 6-deoxyglucose α-1,4-linked to a maltose moiety. Acarbose (ATC Code A10BF01, DrugBank Code DB00284) is generic sold in Europe and China as Glucobay (Bayer AG), in North America as Precose (Bayer Pharmaceuticals), and in Canada as Prandase (Bayer AG). Some aminocylclitol-type of glycosidase inhibitors.
Some of the organic ligand transition metal complexes can serve as potent α-glucosidase inhibitors: in-vitro, kinetics and in-silico studies
Published in Inorganic and Nano-Metal Chemistry, 2023
Syed Majid Bukhari, Rizwana Sarwar, Asma Zaidi, Majid Ali, Farhan A. Khan, Umar Farooq, Jalal Uddin, Aliya Ibrar, Ajmal Khan, Ahmed Al-Harrasi
The α-glucosidase is a membrane bound enzyme which is located in epithelium of the small intestine. It has vital importance in the functioning of carbohydrase and in digestion process of glycolipids, lyco-proteins and is involved in several other metabolic pathways.[1] It releases α-D-glucose (monosaccharide unit) by hydrolyzing non-reducing, terminal 1, 4-linked α-D-glucose (oligosaccharides and polysaccharides) to maintain postprandial blood glucose level.[2,3] The α-glucosidase inhibitors have been shown to possess therapeutic potential against type-2 diabetes mellitus, human immunodeficiency virus infection, obesity and metastatic cancer.[3–5] There are only three α-glucosidase inhibitors (acarbose, miglitol and voglibose) which are clinically used today for the treatment of type-2 diabetes. These inhibitors lower the rate of carbohydrase absorption and suppress postprandial hyperglycemia.[4]
Determination of biological activity of Carduus lanuginosus: an endemic plant in Turkey
Published in International Journal of Environmental Health Research, 2021
Diabetes mellitus is a multifactorial metabolic disorder characterized with high blood glucose levels known as hyperglycemia (Hu et al. 2013). The most effective approach for managing the type 2 DM is the inhibition of α-amylase and α-glucosidase (Krentz and Bailey 2005) because α-amylase and α-glucosidase, which are called key enzymes, can hydrolyze to carbohydrates (Gray 1995). However, the drugs used as key enzyme inhibitors (voglibose, acarbose, and miglitol) were found to have several adverse effects (abdominal distraction, bloating, meteorism, diarrhea, and flatulence, etc.) (Chiasson et al. 2002). It is important to consider the antidiabetic properties of therapeutic plants and products to obtain alternative compounds have poor toxic and side effects in diabetes mellitus. Therefore, the plant extracts were investigated with regard to the enzyme inhibition activities. Acarbose was used as the positive control for both inhibition activities.