- A high-resolution α-glucosidase inhibition profiling for targeted identification of natural antidiabetic products from Lycopodiella cernua (L.) Pic. Serm and their inhibitory mechanism study. [Journal Article]Nat Prod Res. 2023 Jan 29 [Online ahead of print]NP
- The targeted identification of α-glucosidase inhibitors from the crude ethyl acetate of Lycopodiella cernua (L.) Pic. Serm (L.cernua) was guided by high-resolution inhibition profiling. The α-glucosidase inhibition profiling and HPLC-QTOF-MS showed tannins and serratenes were the corresponding antidiabetic constituents. Two new serratenes named 3β, 21β-dihydroxyserra-14-en-24-oic acid-3β-(4'-meth…
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- Design, synthesis, biological evaluation, and docking study of chromone-based phenylhydrazone and benzoylhydrazone derivatives as antidiabetic agents targeting α-glucosidase. [Journal Article]Bioorg Chem. 2023 Jan 20; 132:106384.BC
- To develop novel α-glucosidase inhibitors, a series of chromone-based phenylhydrazone and benzoylhydrazone derivatives were designed, synthesized, and evaluated their inhibitory effects on α-glucosidase. The target compounds were characterized using 1H NMR, 13C NMR, and high-resolution mass spectra. Some of the compounds showed a varying degree of α-glucosidase inhibitory activity with IC50 value…
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- Inhibition of α-Glycosidase by Lippia dulcis Trevir. (Verbenaceae) Preparations, Quantification of Verbascoside, and Study of Its Molecular Docking. [Journal Article]Chem Biodivers. 2023 Jan 24 [Online ahead of print]CB
- This study aimed to quantify verbascoside (VEB), perform molecular docking studies of VEB with the α-glucosidase (GL) of Bacillus stearothermophilus, and evaluate the inhibition of the enzyme by L. dulcis preparations. The substrate concentration and presence of reduced glutathione were evaluated for their effect on the in vitro inhibition of the GL enzyme. Assays were also performed in the prese…
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- Synthesis and evaluation of ent-Conduramine C-1 derivatives as α-glucosidase inhibitors via CSI-mediated amination reaction. [Journal Article]Carbohydr Res. 2023 Jan 18; 524:108746.CR
- Concise synthesis of ent-conduramine C-1 and its derivatives has been achieved by using commercially available d-ribose. The key steps in the synthesis are regioselective and diastereoselective amination of polybenzyl ethers by chlorosulfonyl isocyanate (CSI), chelation-controlled carbonyl addition, and intramolecular olefin metathesis. All of the synthesized compounds were evaluated for inhibito…
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- Fluorescence sensing and glycosidase inhibition effect of multivalent glycosidase inhibitors based on Naphthalimide-deoxynojirimycin conjugates. [Journal Article]Bioorg Chem. 2023 Jan 13; 132:106373.BC
- Synthetic glycoconjugates as chemical probes have been widely developed for the detection of glycosidase enzymes. However, the binding interactions between iminosugar derivatives and glycosidases were limited, especially for the binding interactions between multivalent glycosidase inhibitors and α-glycosidases. In this paper, three naphthalimide-DNJ conjugates were synthesized. Furthermore, the b…
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- Implication of solvent polarities on browntop millet (Urochloa ramosa) phenolic antioxidants and their ability to protect oxidative DNA damage and inhibit α-amylase and α-glucosidase enzymes. [Journal Article]Food Chem. 2023 Jan 12; 411:135474.FC
- Phenolics of browntop millet extracted in solvents with varying polarities [water, methanol, acetone (80%), ethanol (70%)] were comparatively assessed for their phenolic profiles, antioxidant activities, DNA damage protection and enzyme inhibitory properties. Results indicated that acetone (80%) and ethanol (70%) were most effective in extracting millet phenolics than other solvents. Gallic, caff…
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- Synthetic α-glucosidase inhibitors as promising anti-diabetic agents: Recent developments and future challenges. [Review]Eur J Med Chem. 2023 Jan 17; 249:115119.EJ
- Diabetes mellitus is one of the biggest challenges for the scientific community in the 21st century. It is a well-recognized multifactorial health problem contributes significantly to high mortality rates by causing serious health complications mainly related to cardiovascular diseases, kidney damage and neuropathy. The inhibition of α-glucosidase (enzyme that catalyses starch hydrolysis in the i…
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- Rhanteriol, a New Rhanterium suaveolens Desf. Lignan with Pharmacological Potential as an Inhibitor of Enzymes Involved in Neurodegeneration and Type 2 Diabetes. [Journal Article]
- Several specialized plant metabolites are reported to be enzyme inhibitors. In this investigation, the phytochemical composition and the biological activity of Rhanterium suaveolens Desf. were studied. One new lignan (rhanteriol 1) and seven known secondary metabolites were isolated from the aerial parts of R. suaveolens by using different chromatographic procedures. The biological properties of …
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- Synthesis, In Vitro α-Glucosidase Inhibitory Activity and Molecular Docking Study of New Benzotriazole-Based Bis-Schiff Base Derivatives. [Journal Article]
- This study was carried out to synthesize benzotriazole-based bis-Schiff base scaffolds (1-20) and assess them in vitro for α-glucosidase inhibitory potentials. All the synthetics analogs based on benzotriazole-based bis-Schiff base scaffolds were found to display an outstanding inhibition profile on screening against the α-glucosidase enzyme. The synthetic scaffolds showed a varied range of inhib…
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- α-Amylase and α-glucosidase inhibitors from the aerial parts of Chamaecrista pumila (Lam.) K. Larsen. [Journal Article]Nat Prod Res. 2023 Jan 20 [Online ahead of print]NP
- One new compound, 4,7-dihydroxy-2-hydroxymethyl-5,6-dimethoxyanthraquinone (1), along with eight known compounds (2-9) were isolated from the methanol extracts of the aerial parts of Chamaecrista pumila (Lam.) K. Larsen. Their chemical structure was determined based on spectroscopic data interpretation and comparison with the reported data. The inhibitory effects of them on α-amylase and α-glucos…
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- Thiazolidinedione use is associated with reduced risk of dementia in patients with type 2 diabetes mellitus: A retrospective cohort study. [Journal Article]J Diabetes. 2023 Jan 20 [Online ahead of print]JD
- CONCLUSIONS: Use of TZDs is associated with a decreased risk of dementia incidence in a mainland Chinese population with T2DM.
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- Evaluation and molecular modelling of bis-Schiff base derivatives as potential leads for management of diabetes mellitus. [Journal Article]
- Developing a medication to cure and manage diabetes mellitus complications is of interest in medicinal chemistry. Toward this end, six bis-biphenyl-salicylaldehyde Schiff base derivatives have been evaluated for their α-glucosidase inhibition, antiglycation and anti-inflammation potentials. Four compounds (compounds 2-5) showed an excellent α-glucosidase inhibitory effect superior to that produce…
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- Physicochemical properties and in vitro hypoglycemic activities of hsian-tsao polysaccharide fractions by gradient ethanol precipitation method. [Journal Article]Int J Biol Macromol. 2023 Jan 14; 231:123274.IJ
- Hsian-tsao polysaccharides fractions (HPs), including HP20, HP40, HP60, and HP80, were fractioned by gradient precipitation of 20 %, 40 %, 60 %, and 80 % (v/v) ethanol, respectively. Their physicochemical properties and in vitro hypoglycemic activities (inhibitory activities on α-amylase and α-glucosidase, glucose adsorption capacity, and glucose diffusion retardation) were determined. The result…
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- Design, synthesis and bio-evaluation of indolin-2-ones as potential antidiabetic agents. [Journal Article]Future Med Chem. 2023 Jan 16 [Online ahead of print]FM
- Background: Diabetes mellitus is a serious global health concern, and this is expected to impact more than 300 million people by 2025. The current study focuses on identifying substituted indolin-2-one-based inhibitors for two indispensable drug targets, α-amylase and α-glucosidase. Methods: The structures of synthetic compounds were confirmed by spectroscopic techniques and evaluated for enzyme …
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- Thioether-based novel transition metal complexes: Synthesis, DNA interaction, in vitro biological assay, DFT calculations, and molecular docking studies. [Journal Article]Bioorg Chem. 2023 Jan 05; 132:106343.BC
- A novel Schiff base ligand 2-(((2-(benzylthio)phenyl)imino)methyl)-4-chlorophenol and its cobalt, nickel, copper, and zinc metal complexes were prepared. Using B3LYP/6-31++G(d,p) method with LanL2DZ as basis set, the molecular structure of metal complexes has been optimized, and their parameters have been explored. The distorted octahedral geometries have been observed in cobalt, nickel, and copp…
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- Liver-related long-term outcomes of alpha-glucosidase inhibitors in patients with diabetes and liver cirrhosis. [Journal Article]
- Background: Adequate management of diabetes in patients with liver cirrhosis can be challenging. We conducted this study to investigate the liver-related long term outcomes of alpha-glucosidase inhibitors (AGIs) in patients with diabetes and cirrhosis. Methods: From National Health Insurance Research Database (NHIRD) in Taiwan, we recruited propensity-score matched alpha-glucosidase inhibitor use…
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- Prescribing pattern of anti-diabetic drugs and adherence to the American Diabetes Association's (ADA) 2021 treatment guidelines among patients of type 2 diabetes mellitus: A cross-sectional study. [Journal Article]
- CONCLUSIONS: Oral anti-diabetic agents predominate the prescribing pattern practices for type 2 DM but there was a shift in trend towards the use of fixed-dose combinations (FDC) in the management of type 2 DM, and majority of prescriptions were adherent to ADA treatment guidelines.
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- Pyrazole scaffold-based derivatives: A glimpse of α-glucosidase inhibitory activity, SAR, and route of synthesis. [Review]Arch Pharm (Weinheim). 2023 Jan 08 [Online ahead of print]AP
- The α-glucosidase is a validated target to develop drugs for treating type 2 diabetes mellitus. The existing α-glucosidase inhibitors have certain shortcomings related to side effects and route of synthesis. Accordingly, it is inevitable to develop new chemical templates as α-glucosidase inhibitors. Pyrazole derivatives have a special place in medicinal chemistry because of various biological act…
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- In Vitro Evaluation of Antidiabetic Potential of Cleistocalyx nervosum var. paniala Fruit Extract. [Journal Article]
- Diabetes mellitus is a complex global public health condition. Medicinal plants are significant resources in the research of alternative new drug active compounds. Cleistocalyx nervosum var. paniala (C. nervosum) is an indigenous berry fruit widely grown in Southeast Asia. The fruit of C. nervosum exhibit various medicinal properties and health benefits. This study aimed to investigate antidiabet…
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- In Vitro Evaluation of α-amylase and α-glucosidase Inhibition of 2,3-Epoxyprocyanidin C1 and Other Constituents from Pterocarpus erinaceus Poir. [Journal Article]
- Diabetes mellitus is a metabolic disorder which is one of the leading causes of mortality and morbidities in elderly humans. Chronic diabetes can lead to kidney failure, blindness, limb amputation, heart attack and stroke. Physical activity, healthy diets and medications can reduce the incidence of diabetes, so the search for more efficient antidiabetic therapies, most especially from natural pro…
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- Miglitol, an Oral Antidiabetic Drug, Downregulates Melanogenesis in B16F10 Melanoma Cells through the PKA, MAPK, and GSK3β/β-Catenin Signaling Pathways. [Journal Article]
- Hyperpigmentation is a common condition that causes darker spots or patches on the skin, which often look brown, black, gray, red, or pink. This results in unresolved psychological impact due to high anxiety, depression, and somatoform disorder. We aimed to repurpose an antidiabetic drug, miglitol, as an effective compound against hyperpigmentation when applied as a cosmeceutical agent. The prese…
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- Organ Weights in NPC1 Mutant Mice Partly Normalized by Various Pharmacological Treatment Approaches. [Journal Article]
- Niemann-Pick Type C1 (NPC1, MIM 257220) is a rare, progressive, lethal, inherited autosomal-recessive endolysosomal storage disease caused by mutations in the NPC1 leading to intracellular lipid storage. We analyzed mostly not jet known alterations of the weights of 14 different organs in the BALB/cNctr-Npc1m1N/-J Jackson Npc1 mice in female and male Npc1+/+ and Npc1-/- mice under various treatme…
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- Molecular profile and peripheral markers of neurodegeneration in patients with Niemann-Pick type C: Decrease in Plasminogen Activator Inhibitor type 1 and Platelet-Derived Growth Factor type AA. [Journal Article]Arch Biochem Biophys. 2023 Jan 04; 735:109510.AB
- Niemann-Pick type C1 (NPC1) is a fatal inherited disease, caused by pathogenic variants in NPC1 gene, which leads to intracellular accumulation of non-esterified cholesterol and glycosphingolipids. This accumulation leads to a wide range of clinical manifestations, including neurological and cognitive impairment as well as psychiatric disorders. The pathophysiology of cerebral damage involves los…
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- Nanomolar β-glucosidase and β-galactosidase inhibition by enantiomeric α-1-C-alkyl-1,4-dideoxy-1,4-imino-arabinitol derivatives. [Journal Article]Eur J Med Chem. 2023 Feb 05; 247:115056.EJ
- A series of α-1-C-alkyl DAB (1,4-dideoxy-1,4-imino-d-arabinitol) and LAB (1,4-dideoxy-1,4-imino-l-arabinitol) derivatives with aryl substituents have been designed as analogues of broussonetine W (12), and assayed as glycosidase inhibitors. While the inhibition spectrum of α-1-C-alkyl DAB derivative 16 showed a good correlation to that of broussonetine W (12), introduction of substituents on the …
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- Production of enzymatic hydrolysates with in vitro antioxidant, antihypertensive, and antidiabetic properties from proteins derived from Arthrospira platensis. [Journal Article]Food Res Int. 2023 Jan; 163:112270.FR
- The microalga Arthrospira platensis BEA 005B was produced using 80 m2 (9 m3) raceway photobioreactors achieving a biomass productivity of 28.2 g·m-2·day-1 when operating the reactors in semi-continuous mode (0.33 day-1). The produced biomass was rich in proteins (58.1 g·100 g-1) and carbohydrates (25.6 g·100 g-1); the content of phycocyanins and allophycocyanins was 115.4 and 36.9 mg·g-1, respect…
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- Inconsistency between polyphenol-enzyme binding interactions and enzyme inhibition: Galloyl moiety decreases amyloglucosidase inhibition of catechins. [Journal Article]Food Res Int. 2023 Jan; 163:112155.FR
- Inhibiting carbohydrate-hydrolyzing enzymes has been considered as an effective approach for controlling starch digestion and postprandial blood glucose level. α-Amylase and amyloglucosidase (AMG) are commonly applied in analysis of starch digestion behaviour. Catechins have been shown with the inhibiting effects on α-amylase. However, the inhibitory activity of catechins against AMG needs to be …
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- Miglustat, a glucosylceramide synthase inhibitor, mitigates liver fibrosis through TGF-β/Smad pathway suppression in hepatic stellate cells. [Journal Article]Biochem Biophys Res Commun. 2023 Jan 29; 642:192-200.BB
- Transforming growth factor (TGF)-β/Smad pathway is implicated in the pathogenesis of liver fibrosis, a condition characterized by excessive deposition of extracellular matrix (ECM) proteins such as collagen in response to chronic inflammation. It has been reported that ceramide regulates collagen production through TGF-β/Smad pathway activation. In this study, we examined whether miglustat, an in…
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- Mechanistic Insight of Synthesized 1,4-Dihydropyridines as an Antidiabetic Sword against Reactive Oxygen Species. [Journal Article]J Med Chem. 2023 Jan 12; 66(1):991-1010.JM
- The pharmacologically privileged DHP derivatives were synthesized using the pragmatic multicomponent Hantzsch synthesis to screen the antidiabetic activity. Initially, the candidates were screened using an in vivo blood glucose test, where compound 8b showed the most prominent antidiabetic effect (% potency = 218%) compared to glimepiride. Then, a propositioned structure-activity relationship stu…
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- Antioxidant Activity and Inhibition of Carbohydrate Digestive Enzymes Activities of Artemisia campestris L. [Journal Article]Front Biosci (Schol Ed). 2022 09 21; 14(4):25.FB
- CONCLUSIONS: These results showed that the Artemisia campestris L. has highest phenolic content, antioxidant activity and demonstrated a postprandial anti-hyperglycemic effect via the inhibiting of the carbohydrate digestive enzyme (α -amylase and α -glucosidase) and the intestinal glucose absorption.
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- Synthesis and Biological Evaluation of Substituted Pyrazole-Fused Oleanolic Acid Derivatives as Novel Selective α-Glucosidase Inhibitors. [Journal Article]Chem Biodivers. 2022 Dec 27 [Online ahead of print]CB
- A series of novel substituted pyrazole-fused oleanolic acid derivative were synthesized and evaluated as selective α-glucosidase inhibitors. Among these analogs, compounds 4a-4f exhibited more potent inhibitory activities compared with their methyl ester derivatives, and standard drugs acarbose and miglitol as well. Besides, all these analogs exhibited good selectivity towards α-glucosidase over …
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