acarbose / Generic mfg. - LARVOL DELTA

Canagliflozin or acarbose vs placebo to ameliorate post-bariatric hypoglycaemia: mechanistic insights from the HypoBar I randomised clinical trial (EASD 2025) - P2 | "While both pharmacological approaches failed to raise postprandial glycaemic nadir during the meal test, they altered postprandial glycaemic excursions and associated entero-pancreatic hormone dynamics and could, thus, prove relevant for PBH treatment through modulation of its pathophysiology."

Clinical • Diabetes • Hypoglycemia • Metabolic Disorders

Bidirectional Modulation of α-Glucosidase by Steroidal Saponins From Polygonatum kingianum var. grandifolium: Inhibitory and Activating Effects Align With the Yin-Yang Balance Theory. (PubMed, Chem Biodivers) - "Compound 4 exhibited stronger α-glucosidase inhibitory activity than the positive control acarbose, with a half-maximal inhibitory concentration of 213.9 µM, suggesting its potential as an inhibitor with hypoglycemic effects...These findings suggest that P. kingianum var. grandifolium exerts a dual regulatory effect on blood glucose levels through α-glucosidase inhibition and activation in diabetes management, aligning with the yin-yang balance theory in traditional Chinese medicine."

Journal • Diabetes • Metabolic Disorders

Thiazole-Thiadiazole Compounds for Enzymatic Modulation and Therapeutic Targeting in Diabetes Mellitus. (PubMed, Chem Biodivers) - "The compounds inhibitory potential against diabetes mellitus was contrasted with that of acarbose, the reference drug...Potent scaffold nontoxic nature was demonstrated by ADMET analysis, which supports their usage as a treatment in the future. Furthermore, DFT analyses provided the charge distribution of the compounds that drive chemical reactivity and enzyme interactions."

Journal • Diabetes • Metabolic Disorders

Synthesis and characterization of indole-3-butyric acid-based hydrazones: from multifunctional enzyme inhibition to therapeutic potential for drug development. (PubMed, Naunyn Schmiedebergs Arch Pharmacol) - "The thiophene-based compound exhibited potent acetylcholinesterase inhibition (IC50 1.95 ± 10.79 μM), surpassing the standard donepezil (IC50 4.53 ± 0.13 μM), and demonstrated effective α-amylase inhibition (IC50 0.99 ± 2.6 μM), comparable to acarbose (IC50 4.21 ± 0.27 μM). This compound also showed pronounced cytotoxicity against HeLa (96.31%, IC50 49.2 ± 0.02 μM) and PC-3 (97.42%, IC50 41.1 ± 0.11 μM) cell lines in comparison with standard doxorubicin (HeLa 98.7%, IC50 1.13 ± 0.18 μM and PC-3 80.8%, IC50 1.18 ± 0.21 μM)...Antibacterial assays revealed enhanced activity against Gram-positive (51.3 ± 3.5 mm) compared to cefixime (27 ± 0.31 mm) by aminodichlorophenyl derivative and Gram-negative (15.0 ± 0.12 mm) bacterial strains compared to cefixime (29 ± 0.17 mm) by thiophene-based compounds...The incorporation of sulfur and halogen along with amino..."

Journal • Infectious Disease • Oncology • Tyrosinase

Comparative cardiovascular outcomes and safety of hypoglycemic drug classes in patients with type 2 diabetes and hypertension: a multicenter cohort analysis. (PubMed, Cardiovasc Diabetol) - "This study highlights the differential cardiovascular effectiveness and safety profiles of hypoglycemic therapies in real-world settings, providing valuable insights for optimizing T2D management, particularly in patients with comorbid hypertension."

Clinical • Journal • Retrospective data • Atherosclerosis • Cardiovascular • Chronic Kidney Disease • CNS Disorders • Diabetes • Heart Failure • Hypertension • Immunology • Inflammatory Arthritis • Insomnia • Metabolic Disorders • Nephrology • Renal Disease • Sleep Disorder • Type 2 Diabetes Mellitus

In silico drug repurposing targeting fusion and nucleoprotein of human metapneumovirus: A step toward pandemic preparedness. (PubMed, Indian J Pharmacol) - "The study highlights mobocertinib, rutin, and levetiracetam as promising repurposed drugs against HMPV. While mobocertinib exhibited the strongest predicted binding affinity, levetiracetam demonstrated the best pharmacokinetic profile, making it a particularly viable candidate for further experimental validation. These results validate the usefulness of in silico drug repurposing in addressing unmet antiviral needs and warrant preclinical studies to evaluate therapeutic efficacy."

Journal

Exploring the antidiabetic efficacy of 3-mercapto-1,2,4-triazoles as potential inhibitors of α-amylase and α-glucosidase: A comprehensive review. (PubMed, Int J Biol Macromol) - "The inhibitory potential of these scaffolds has been evaluated through various parameters, including IC50 values, percentage inhibition, molecular docking, SAR, and kinetic analyses, consistently showing promising results compared to standard drugs like acarbose. This supports the antidiabetic potential of 3-mercapto-1,2,4-triazole derivatives, focusing on the negative regulation of the enzymes α-amylase and α-glucosidase, highlighting their potential as effective agents for diabetes treatment and management."

Journal • Review • Diabetes • Metabolic Disorders

Green ultrasound‑assisted deep eutectic solvent extraction of flavonoid enzyme inhibitors from Blumea aromatica: process optimization, characterization, and mechanistic insights into α‑glucosidase and tyrosinase inhibition. (PubMed, J Enzyme Inhib Med Chem) - "The UAE-DES extract showed the strongest enzyme inhibition among all extracts tested (IC50 35.872 ± 0.294 µg/mL for α-glucosidase, 9.126 ± 0.285 μg/mL for tyrosinase), though the α-glucosidase inhibition was much weaker than acarbose, while tyrosinase inhibition was comparable to kojic acid...Molecular docking revealed strong binding affinities (≤ -5 kcal/mol), with corylin showing the highest binding to both enzymes through hydrogen bonds and van der Waals interactions. This approach supports sustainable discovery of natural enzyme inhibitors for antidiabetic and skin-whitening applications."

Journal • Tyrosinase

Development of 1,2,3-Triazoles as Dual Enzyme Inhibitors Targeting α-Amylase and α-Glucosidase for Type 2 Diabetes Intervention. (PubMed, Arch Pharm (Weinheim)) - "Among them, compound 6a exhibited the most potent α-glucosidase inhibition (IC50 = 22.15 ± 0.75 µM), comparable to the reference drug acarbose (IC50 = 21.07 ± 0.05 µM)...The DPPH assay revealed moderate to good activity for all compounds 6(a-o), with IC50 values ranging from 39.60 ± 0.15 to 99.45 ± 0.12 µM. These findings support the therapeutic potential of these compounds as antidiabetic agents."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Inhibition mechanism and behaviour of wedelolactone against α-glucosidase. (PubMed, J Enzyme Inhib Med Chem) - "Activity assay results discovered that wedelolactone functioned as a mixed-type inhibitor, with an IC50 of 39.12 ± 2.54 μM, surpassing the potency of the standard drug acarbose...Molecular docking studies provided insights into the specific interactions between wedelolactone and α-glucosidase. Collectively, these results laid the groundwork for the potential application of wedelolactone as a natural therapeutic agent in diabetes management."

Journal • Diabetes • Metabolic Disorders

Potential Therapeutic Benefits of Pepper Fruit Extract on Hyperglycemia and Dyslipidemia in Obese Type 2 Diabetic Mice. (PubMed, Cureus) - "Fifty mice were randomly assigned to five groups (n = 10 per group): a normal control group, a diabetic control group (db/db), a positive control group treated with acarbose (50 mg/kg), and two treatment groups receiving either 150 mg/kg or 300 mg/kg of "Meein" extract...Importantly, no significant effects on OGTT or lipid profiles were observed in this study. Further research is necessary to clarify the extract's effects on glucose metabolism and lipid regulation."

Journal • Preclinical • Diabetes • Dyslipidemia • Genetic Disorders • Metabolic Disorders • Obesity • Type 2 Diabetes Mellitus

Piperonal-derived Schiff base molecules as potential multi-target therapeutic agents against Alzheimer's and diabetes. (PubMed, Future Med Chem) - "Compounds 7 (IC50 = 5.73 ± 0.01; 3.52 ± 0.02 µM) and 17 (IC50 = 10.91 ± 0.02; 7.38 ± 0.02 µM) showed potent inhibitory effects against AG and AA enzymes, in comparison to acarbose (IC50 = 14.98 ± 0.02 µM; 14.64 ± 0.02 µM). However, analogs 7, 9, 10, 14, and 15, compounds 7 (IC50 = 2.92 ± 0.02; 3.34 ± 0.02 µM) and 9 (IC50 = 8.16 ± 0.03; 7.19 ± 0.03 µM) showed remarkable inhibitory results against AChE and BChE, respectively, compared to standard donepezil chloride (IC50 = 37.89 ± 0.02 µM; 41.56 ± 0.03 µM)...Synthesized derivatives were also checked for their antioxidant potential and demonstrated significant activity. These complementary studies highlight several hit candidates for further development as therapeutic agents against DM and AD."

Journal • Alzheimer's Disease • CNS Disorders • Diabetes • Metabolic Disorders • Pain

Synthesis, crystal structure, and in vitro evaluation of newer 2,4-thiazolidinedione hybrids as α-glucosidase inhibitors. (PubMed, Future Med Chem) - "Compared to Acarbose, VD-TZD hybrids displayed good AGI activity...The in silico ADMET profile of compound 6f indicates satisfactory oral drug-likeness and the absence of toxic effects. In conclusion, compound 6f could be considered a promising lead compound for further optimization in AGI development for the treatment of T2DM."

Journal • Preclinical • Type 2 Diabetes Mellitus

Introduction of new quinolone-2-thio-acetamide-propane hydrazide-benzimidazole derivatives as new α-glucosidase and α-amylase inhibitors. (PubMed, Sci Rep) - "This compound was 5 and 23.8 folds more potent than acarbose against α-glucosidase and α-amylase, respectively, and with excellent binding energies in comparison to acarbose attached to active sites of these enzymes. Molecular dynamics and pharmacokinetic studies of compound 12n was also performed."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

DES-Promoted Synthesis of 3,4-Dihydropyrimidinones and Their Antidiabetic and Antioxidant Evaluation Supported With Computational Studies. (PubMed, Chem Biodivers) - "Among the series, compound 3f exhibited superior inhibitory activity against α-glucosidase (IC50 = 35.25 µM) and α-amylase (IC50 = 38.61 µM), being ∼2.3- and ∼2.6-fold more potent, respectively, than the standard drug acarbose...Furthermore, density functional theory (DFT) studies revealed favorable electronic and reactivity profiles, whereas ADME/T predictions indicated good drug-likeness. Overall, compound 3f shows strong potential as a lead antidiabetic agent for managing postprandial hyperglycemia."

Journal • Diabetes

Pan-cancer analysis and oncogenic implications of MGAM and MGAM2: Toward precision oncology and drug repurposing in colorectal cancer. (PubMed, J Cell Commun Signal) - "In CRC patients, MGAM downregulation was confirmed in 64 samples, and WES revealed a novel MGAM mutation (rs2960746). These findings underscore MGAM and MGAM2 as promising biomarkers and therapeutic targets, supporting their relevance in advancing personalized oncology."

Journal • Pan tumor • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor • MGAM

Bioactive Potential of Nepenthes miranda Flower Extracts: Antidiabetic, Anti-Skin Aging, Cytotoxic, and Dihydroorotase-Inhibitory Activities. (PubMed, Plants (Basel)) - "For antidiabetic evaluation, the ethanol extract demonstrated potent α-glucosidase inhibition (IC50 = 24.53 μg/mL), outperforming standard inhibitors such as acarbose and quercetin...Furthermore, the ethanol extract strongly inhibited the activity of purified human dihydroorotase (IC50 = 25.11 μg/mL), indicating that disruption of pyrimidine biosynthesis may underlie its anticancer activity. Overall, this study provides the first characterization of N. miranda flower extracts, particularly the ethanol fraction, as a promising source of multifunctional bioactive compounds with possible applications in cosmetics, antidiabetic therapy, and cancer treatment."

Journal • Oncology • Squamous Cell Carcinoma • ELANE • Tyrosinase

Integrating data augmentation and BERT-based deep learning for predicting alpha-glucosidase inhibitors derived from Black Cohosh. (PubMed, Sci Rep) - "Further molecular docking and MD simulations presented this compound to interact stably with the enzyme and possess a high inhibition probability when compared to acarbose. The results of insilico drug discovery displayed that actaeaepoxide 3-O-xyloside is pointed out to be a potential candidate for diabetes therapy. In conclusion, the role of augmentation techniques and pre-trained models was also emphasized in the presented investigation to accelerate drug discovery toward more effective therapeutic solutions."

Journal • Cognitive Disorders • Diabetes • Genetic Disorders • Metabolic Disorders • Obesity

New 1E,1'E-hydrazine-bis(phenoxy-1,2,3-triazol-acetamide) derivatives as potent inhibitors against acetylcholinesterase, butyrylcholinesterase, and α-glucosidase. (PubMed, RSC Adv) - "In this regard, all the synthesized compounds were more potent than the standard inhibitors tacrine and donepezil against BChE, and most of these compounds were more potent than tacrine against AChE. Moreover, most of the target synthesized compounds were more potent than the standard inhibitor acarbose against α-glucosidase...Furthermore, docking studies demonstrated that compound 10k interacted with both the catalytic and peripheral anionic sites of AChE and BChE. This property led to the better efficacy of the compound in the treatment of AD."

Journal • Alzheimer's Disease • CNS Disorders • Diabetes • Metabolic Disorders • Neuroblastoma • Oncology • Pain • Solid Tumor

Synthesis and radiolabelled evaluation of novel pyrimidine derivatives as dual α-amylase inhibitors and GIT-targeted molecular imaging probe. (PubMed, RSC Adv) - "Compound 1 showed the strongest inhibitory in vitro amylase effect, in comparison to the reference drug acarbose...A gradual increase in muscle uptake was observed, raising possible insights into side effects reported with similar drugs. These results suggest that compound 1 not only possesses potent amylase-blocking and related effective antidiabetic activity but also holds promise as a molecular probe for molecular dynamic imaging for the GIT system."

Journal • Gastrointestinal Disorder

Molecular insights of acarbose metabolization catalyzed by acarbose-preferred glucosidase. (PubMed, Nat Commun) - "Additionally, further investigation of the acarbose analogs acarstatins A and B that are resistant to Apg is conducted by computational analysis. Overall, our studies provide perspectives into the intricacies of Apg's catalytic mechanism, contributing to the design of next-generation hypoglycemic pharmaceuticals."

Journal

Proximate Composition, Phytochemicals, Phenolic Compounds, and Bioactive Characterization of Mauritia flexuosa L.f. Seeds. (PubMed, Plants (Basel)) - "Notably, MFS ethanolic extracts exhibited significant in vitro antihyperglycemic activity via inhibiting α-amylase and α-glucosidase enzymes, demonstrating comparable inhibition to acarbose at higher concentrations. High-performance liquid chromatography-mass spectrometry (UHPLC-ESI-HRMS) analysis of the seed extract identified phenolic compounds including ellagic, p-coumaric, and chlorogenic acids, as well as flavonoids such as quercetin, myricetin, and epicatechin. This study provides the first evidence of the hypoglycemic activity of MFSs, offering valuable insights into their phytochemistry and potential therapeutic applications."

Journal • Diabetes • Metabolic Disorders

Design and Synthesis of Sulfonium and Selenonium Derivatives Bearing 3',5'-O-Benzylidene Acetal Side Chains as Potent α-Glucosidase Inhibitors. (PubMed, ChemMedChem) - "In vivo, 20b (15.0 mg kg-1) reduced postprandial blood glucose levels in sucrose-loaded mice by 40.6% (15 min), 49.5% (30 min), and 43.6% (60 min), surpassing acarbose (20.0 mg kg- 1)...Cytotoxicity assessments confirmed the favorable safety profile of selected compounds in normal cell lines. Enzyme kinetic studies demonstrated fully competitive inhibition of α-glucosidase by these sulfonium salts."

Journal • MGAM

Novel Biphenyls From Garcinia multiflora: Isolation and α-Amylase Inhibitory Properties. (PubMed, Chem Biodivers) - "The results showed that all seven compounds exhibited strong binding to α-amylase. Additionally, further enzyme inhibition assays using a multifunctional microplate reader revealed that, compared with the positive control acarbose (half-maximal inhibitory concentration [IC50] = 17.23 ± 2.43 µM), only compounds 5 (IC50 = 2190 ± 180 µM) and 6 (IC50 = 4420 ± 1480 µM) exhibited relatively weak α-amylase inhibitory activity."

Journal

Molecular Docking and In Vitro Assessment of Gymnema sylvestre R. Br. and Trigonella foenum-graecum L. Phytochemicals as Dual α-Amylase and α-Glucosidase Inhibitors. (PubMed, Chem Biodivers) - "The α-amylase and α-glucosidase inhibitory potentials were screened in vitro using 50% EtOH extracts of G. sylvestre leaves and T. foenum-graecum seeds with acarbose as the reference compound...In vitro assays further revealed that T. foenum-graecum seed extract showed the highest α-amylase inhibition (IC50 = 12.09 ± 2.13 mg/mL) and α-glucosidase inhibition (IC50 = 5.23 ± 0.33 mg/mL). Trigoneoside XIIa, trigofoenoside G, and gymnemasaponin V were identified as promising drug candidates for the development of antidiabetic drug leads, further validating the in vitro α-amylase and α-glucosidase inhibitory potentials."

Journal • Preclinical