acarbose / Generic mfg. - LARVOL DELTA

Pseudoheterins A-J, cyclic peptides from Pseudostellaria heterophylla and their potential as antidiabetic agents targeting α-glucosidase. (PubMed, Phytochemistry) - "Compounds 2, 10, 12, 15, and 17 exhibited α-glucosidase inhibitory effects comparable to those of the positive control acarbose...In a zebrafish model, compound 2 effectively reduced glucose levels, regulated the expression of key metabolic genes (PEPCK, GCK, and SDHDB), and exhibited no obvious toxicity toward human cell lines or zebrafish at the tested concentrations. These results identify 2 as a potential lead compound for the development of new natural antidiabetic agents."

Journal • PCK2

A New Flavonoid Glycoside from the Stem Bark of Albizia saponaria: Isolation, Structural Elucidation, and In Silico Evaluation as a Potent α-Glucosidase Inhibitor. (PubMed, Pharmaceuticals (Basel)) - "To assess its inhibitory efficacy and pharmacokinetic profiles, an in silico comparative study was conducted against a database of related flavonoids (Quercitrin, Hyperoside, and Isoquercitrin) and the clinical drug Acarbose... These predictive findings establish Compound 1 as a highly promising, low-toxicity natural scaffold for anti-hyperglycemic drug development. Its superior binding affinity and minimized hepatotoxicity risk warrant subsequent in vitro and in vivo functional validation."

Journal • Diabetes • Gastrointestinal Disorder • Hepatology • Liver Failure • CYP3A4 • MGAM

Natural Product-Based Therapeutic Potential of Fagonia arabica: Phytochemical Characterization and Biological Activities of Leaf and Seed Extracts. (PubMed, Pharmaceuticals (Basel)) - "In addition, FASE exhibited potent α-amylase and α-glucosidase inhibitory activities (IC50 = 61.62 and 67.38 μg/mL, respectively), comparable to acarbose. These findings highlight F. arabica seed extract as a promising source of multifunctional bioactive compounds with potential pharmaceutical application."

Journal • Oncology • BCL2 • BCL2L1 • CASP3 • CASP8 • CASP9

Vincoside Lactam from Edible Uncaria rhynchophylla: A Food-Derived Indole Alkaloid for Dietary Postprandial Glycemic Regulation and Functional Food Development. (PubMed, Foods) - "In contrast to the gastrointestinal side effects commonly associated with synthetic α-glucosidase inhibitors such as acarbose, no gastrointestinal discomfort or other adverse effects were observed during the 12-day administration period. Collectively, our findings demonstrate that VCS-LT is a potent food-derived α-glucosidase inhibitor that effectively attenuates postprandial glucose excursion in diabetic mice, which supports its potential application as a functional food ingredient for daily dietary glycemic management. Nevertheless, our work remains at the proof-of-concept level, and future studies on processing stability, bioaccessibility, food-matrix interactions, sensory acceptability, and safety at food-use levels are essential before any commercial application can be envisioned."

Journal • Gastrointestinal Disorder • MGAM

Comparative evaluation of green-synthesized CeO2-rich and multi-rare-earth-containing oxide-rich nanoparticles prepared using Moringa oleifera seed extract: physicochemical characterization and preliminary cell-free screening. (PubMed, Nanoscale Adv) - "The estimated IC50 values were 129.1 µg mL-1 for α-amylase inhibition, compared with 79.57 µg mL-1 for acarbose, and 159.6 µg mL-1 for BSA thermal-denaturation inhibition, compared with 121.5 µg mL-1 for diclofenac sodium...Overall, the two compositionally distinct nanoparticle systems exhibited different physicochemical, colloidal, and assay-specific profiles, with multi-REO NPs generally showing greater cell-free responses. However, the findings do not establish rare-earth synergy, biological safety, or therapeutic efficacy, and require further mechanistic, interference-control, cytotoxicity, cellular, and in vivo evaluation."

Journal • Pain

Organ-Specific Phenolic Profiles, Antioxidant Capacity, and Enzyme-Inhibitory Activities of the Turkish Endemic Origanum bilgeri. (PubMed, Pharmaceuticals (Basel)) - "Under the present assay conditions, all organ extracts yielded lower α-glucosidase IC50 values (0.97-1.10 mg/mL) than acarbose (1.16 mg/mL). The root was particularly characterized by high verbascoside and chlorogenic acid contents, elevated total phenolic content, strong antioxidant performance across several assays, and α-glucosidase inhibitory activity. These findings support further investigation of O. bilgeri, particularly its root, using independent biological replicates and complementary phytochemical and biological approaches."

Journal • Tyrosinase

Synthesis, Characterization, Biological Evaluation and In Silico Studies of Some New Thiazole Derivatives. (PubMed, Pharmaceuticals (Basel)) - "Enzyme inhibition studies showed that electron-withdrawing substituents such as 4-SO2CH3 (compound 3) and 3,4-diCl (compound 5) enhanced both AChE/BChE and α-amylase/α-glucosidase inhibition, surpassing the activity of acarbose in antidiabetic assays, while electron-donating groups reduced potency...In addition, in silico ADMET predictions for the compounds have been performed. These results indicate that the thiazole-benzodioxole scaffold is a promising framework for developing multifunctional agents with combined neuroprotective, antidiabetic, and antioxidant activities."

Journal • Pain

Integrated network pharmacology, molecular docking, ADMET profiling and In vitro α-amylase inhibitory evaluation of Cardiospermum halicacabum Linn. Against diabetes mellitus. (PubMed, In Silico Pharmacol) - "The extract exhibited concentration-dependent α-amylase inhibition, reaching 71.27 ± 1.31% inhibition at 1000 μg/mL, with an IC50 of 218.40 μg/mL, whereas acarbose showed 97.10 ± 0.60% inhibition at 1000 μg/mL, with an IC50 of 62.43 μg/mL...These findings provide computational evidence supported by preliminary experimental validation; however, further target-specific in vitro, in vivo, and clinical studies are required to confirm the proposed mechanisms. The online version contains supplementary material available at https://doi.org/10.1007/s40203-026-00756-8."

Journal • Preclinical • Diabetes • Metabolic Disorders • AKT1 • MAPK8 • PIK3CA • PTPN1

In silico pathway-based subtractive proteomics for identifying novel drug targets in Candida albicans with structure-guided drug repurposing of aspartate-semialdehyde dehydrogenase inhibitors. (PubMed, J Mol Model) - "The structure-guided virtual screening identified five potent hits: Acarbose, Iotrolan, Iodixanol, Nystatin, and Ferric derisomaltose, which exhibit better affinity, ranging from -12.25 to -11.90 kcal/mol with CaASADH and exhibits stable binding during 500 ns MD simulations, highlighting their potential as lead compounds for anti-C. Subtractive proteomics pipeline was performed in a standalone Linux environment, and the three-stage Schrödinger's Glide docking algorithm was used for molecular docking studies. All MD simulations were conducted using GROMACS for 500 ns, and the conformational dynamic stability was examined using RMSD, RMSF, Rg, SASA, PCA, CD-HIT, BLASTp, DrugBank, BlastKOALA, screening, SiteMap, LigPrep, SwissParam, MMPBSA, and CHARMM36 force field."

Journal • Infectious Disease

Icaritin and its N-Boc-amino acid ester derivatives: Chemistry, structure-activity relationships, and preliminary mechanistic insights. (PubMed, Eur J Med Chem) - "The N-Boc-l-proline ester M1 was the most potent α-glucosidase inhibitor (IC50 = 5.5 ± 0.5 nM), 1.5-fold and 2.0-fold more active than its parent ICT (8.3 ± 0.5 nM) and acarbose (11.0 ± 0.6 nM), and remained intact in simulated gastric and intestinal fluids...In palmitate-induced insulin-resistant HepG2 cells, M1 (20 μM) increased glucose consumption by 58.1% over the model group, lowered intracellular ROS to approximately 2.6-fold of control, and reduced lipid accumulation to a level comparable to metformin. These effects were accompanied by downregulation of glucose-6-phosphatase and upregulation of catalase, without significantly altering basal glucose consumption in normal HepG2 cells. Together, these findings establish a scalable route to ICT and demonstrate that esterification of its phenolic hydroxyl groups can modify α-glucosidase inhibition and cellular metabolic phenotypes, identifying M1 as a lead compound meriting in vivo validation."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus • CAT

Adult-Onset Nesidioblastosis Following Roux-en-Y Gastric Bypass: A Diagnostic Challenge in Post-Bariatric Hypoglycemia (ACG 2026) - "Dietary modifications and acarbose failed to alleviate symptoms...A robust, greater than twofold rise from baseline insulin levels is localized exclusively to the proximal splenic artery distribution, peaking at 77.4 μU/mL at 30 seconds. This positive finding successfully localized the endogenous insulin hypersecretion to the body of the pancreas, consistent with intraoperative ultrasound, guiding the targeted surgical intervention."

Bariatric surgery • Clinical • Diabetes • Hypoglycemia • Metabolic Disorders • Solid Tumor • Type 2 Diabetes Mellitus

Chemical Profiling and In Vitro Bioactivities of Extracts from the Red Alga Jania rubens Collected from the Lebanese Coast. (PubMed, Mar Drugs) - "Significant α-amylase inhibition was observed with dichloromethane/methanol and lipid extracts, comparable to acarbose...These results highlight J. rubens as a potential reservoir of bioactive compounds with promising in vitro activities related to diabetes, thrombotic disorders, inflammation, and oxidative stress. Further research is needed to isolate the active compounds, validate their efficacy in vivo, assess safety, and elucidate the underlying mechanisms."

Journal • Preclinical • Diabetes • Inflammation • Metabolic Disorders • Thrombosis

Plasma as Proxy for Tissue Metabolism When Extending Lifespan in Mice. (PubMed, Metabolites) - " We used untargeted metabolomic data from plasma, liver, gastrocnemius muscle, kidney, inguinal fat, and gonadal fat tissues from mice treated with lifespan-extending interventions: caloric restriction, rapamycin, canagliflozin, 17-α estradiol, and acarbose. Overall, plasma can only serve as limited proxy for tissue metabolism. Yet, several potential blood biomarkers were discovered as concordant in plasma and tissues in lifespan-extending interventions."

Journal • Preclinical

Preliminary structural characterization and potential glucose metabolism-regulating effects of Armillaria mellea mycelial polysaccharide in insulin-resistant HepG2 cells. (PubMed, Int J Biol Macromol) - "AMMP exhibited moderate competitive and reversible inhibition of α-amylase and α-glucosidase, with weaker inhibitory potency than acarbose, and fluorescence quenching analysis suggested that the interactions were mainly mediated by van der Waals forces and hydrogen bonds...KEGG analysis showed several exploratory pathway-level signals, although none remained significant after FDR correction. These findings provide preliminary in vitro evidence that AMMP may regulate glucose metabolism, oxidative stress, and insulin resistance-related molecular responses in insulin-resistant HepG2 cells, supporting further evaluation in suitable in vivo models."

Journal • CXCL8 • IL6

Variations and implications of Irisin, FGF-23, and N-MID osteocalcin in diabetic osteoporosis patients undergoing acarbose plus sitagliptin therapy: A prospective cohort analysis. (PubMed, J Med Biochem) - "Fracture prediction efficacy was markedly enhanced (AU C= 0.822) by combining the three indices, with statistical superiority over single-index analysis (P< 0.05). The combined detection of Irisin, FGF-23, and N-MID enables early detection of DOP while allowing for dynamic assessment of treatment outcomes and fracture risk."

Journal • Diabetes • Metabolic Disorders • Musculoskeletal Diseases • Orthopedics • Osteoporosis • Rheumatology • FGF23

Stilbenoids from the bark of Hopea odorata: antioxidant and antidiabetic activities. (PubMed, Fitoterapia) - "The newly isolated compounds 1 and 2 showed low DPPH radical scavenging activity but displayed considerable α-glucosidase inhibition relative to acarbose (IC50 = 109.7 ± 0.8 and 174.0 ± 8.1 μM, respectively, vs. 913.7 ± 19.6 μM). Notably, 15 emerged as the most potent compound, demonstrating stronger radical scavenging capacity than ascorbic acid (IC50 = 36.3 ± 1.3 μM vs. 86.5 ± 1.2 μM) and remarkable α-glucosidase inhibition (IC50 = 27.9 ± 1.8 μM)."

Journal

Eco-Friendly Zinc Oxide Nanoparticles from Trachystemon orientalis L.: Examination of Their Antibacterial, Anti-Alzheimer, and Antidiabetic Potentials. (PubMed, Curr Med Chem) - "This study successfully synthesized rod-shaped zinc oxide nanoparticles with significant antimicrobial and enzyme-inhibitory properties. These findings highlight the potential of biogenically synthesized ZnONPs as multifunctional agents in the development of new therapeutic strategies for managing bacterial infections and metabolic disorders."

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

Fatty Acid Composition of Fixed Oil of Linum strictum and Its Antibiofilm, Anticoagulant, and α-Amylase Inhibitory Effects-In Vitro and In Silico Study. (PubMed, Chem Biodivers) - "α-Amylase inhibition reached 85.98% (IC50 = 0.0134 mg/mL), comparable to acarbose. Molecular docking revealed favorable binding of α-oleic acid to BEL-1 β-lactamase and α-linolenic acid to DNA gyrase B."

Journal • Preclinical • Infectious Disease

Design, synthesis, and computational assessment of bis‑oxadiazole ligands targeting α-amylase and α-glucosidase: DFT, docking, and ADME studies. (PubMed, Future Med Chem) - "Among the synthesized derivatives, compound 10 exhibited the most potent activity, showing IC50 values of 1.80 and 2.10 μM against α-amylase and α-glucosidase, respectively, in comparison with the positive control acarbose (IC50 = 5.50 and 5.60 μM, respectively)...ADMET analysis indicated favorable pharmacokinetic and toxicity profiles for the most active derivatives. The combined experimental and computational results demonstrate significant structure-activity relationships within the bis-oxadiazole scaffold, identifying compound 10 as a promising lead candidate for further optimization as a dual enzyme inhibitor for diabetes management."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Orange Peel-Mediated Co-formation of a ZnO-Calcite Mixed-Phase Nanostructured Material: Physicochemical Characterization and Preliminary In vitro Antioxidant, α-Glucosidase Inhibitory, and Differential Cytotoxicity Assessment. (PubMed, Cell Biochem Biophys) - "α-Glucosidase inhibition yielded an IC₅₀ of 0.2537 µg/mL (95% CI: 0.2251-0.2867), compared with 0.2067 µg/mL for acarbose. In MTT assays, the material showed IC₅₀ values of 100.0 µg/mL in HepG2 cells and 365.7 µg/mL in HDFn cells, corresponding to an SI of 3.66. These findings indicate preliminary differential cellular sensitivity together with measurable radical-scavenging and enzyme-inhibitory activities, while phase-specific mechanisms and biological safety require further investigation."

Journal • Preclinical

Crystal structure, intermolecular interactions, Hirshfeld surface analysis, theoretical studies and biological evaluation of (E)-5-(benzyloxy)-2-{[(2,5-dimethoxyphenyl)imino]methyl}phenol, a new Schiff base. (PubMed, Acta Crystallogr C Struct Chem) - "Compared with the corresponding reference inhibitors, BDIMPh showed a slightly higher IC50 value than donepezil for AChE, a slightly lower IC50 value than ethacrynic acid for GST and a higher IC50 value than acarbose for α-glucosidase. These results indicate an enzyme-dependent inhibitory profile rather than uniformly superior activity relative to the reference inhibitors."

Journal • Pain • Tyrosinase

Dumping Syndrome Following Endoscopic Sleeve Gastroplasty. (PubMed, ACG Case Rep J) - "Dietary modification and acarbose provided meaningful relief. This case raises the possibility that ESG-related changes in gastric physiology may predispose to dumping syndrome, particularly after subsequent abdominal surgery."

Journal • Gastroenterology • Genetic Disorders

In silico modeling and in vitro evaluation of antidiabetic potential of exopolysaccharides from Brassicaceae root endophytic bacteria. (PubMed, J Genet Eng Biotechnol) - "Docking produced stable poses (RMSD <2 Å) and predicted stronger binding for acarbose than for individual monosaccharides; among the latter, D-mannose showed the most favorable energy against α-glucosidase. Brassicaceae root bacterial endophytes produced crude EPS with potential α-glucosidase inhibitory activity, supporting further purification and structure-activity analysis to define active fractions and inhibitory mechanisms."

Journal • Preclinical

TRIM28 SUMOylates IRF3 in astrocytes to drive neutrophils infiltration and ischemic cerebral injury. (PubMed, Cell Death Differ) - "Importantly, virtual screening of the FDA-approved drug library identified Acarbose as a pharmacological inhibitor of TRIM28-IRF3 axis, and Acarbose administration relieved neutrophils brain infiltration and cerebral injury after IS. Our findings highlight the critical role of TRIM28 in regulating crosstalk between astrocytes and neutrophils and nominate TRIM28 as a tractable therapeutic target for ischemic cerebral injury."

Journal • Cardiovascular • Inflammation • Ischemic stroke • Targeted Protein Degradation • CXCL1 • CXCR2 • TRIM28

Oxadiazole-based Inhibitors Targeting Carbohydrate-Hydrolyzing Enzymes in Type 2 Diabetes Mellitus: Synthetic Strategies, Structure- Activity Relationships, and Translational Perspectives. (PubMed, Mini Rev Med Chem) - "However, clinically used inhibitors such as acarbose, miglitol, and voglibose are associated with gastrointestinal intolerance, limited selectivity, and variable efficacy, highlighting the need for improved therapeutic agents...Despite encouraging preclinical findings, clinical translation remains constrained by insufficient pharmacokinetic, toxicological, and long-term efficacy data. Future research should prioritize systematic ADMET evaluation, standardized biological validation, and mechanistic expansion beyond carbohydrase inhibition to enable the development of clinically viable oxadiazole-based antidiabetic agents."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus • AKR1B1 • NLRP3 • PTPN1