acarbose / Generic mfg. - LARVOL DELTA

Total Synthesis and Biological Evaluation of Asterriquinol D Dimethyl Ether, Candidusin D, Kumbicins A-B, and Petromurins C-D as α-Glucosidase Inhibitors. (PubMed, J Org Chem) - "N-Boc-kumbicin A exhibited the most potent inhibitory activity (IC50 = 8.84 ± 3.38 μM) in comparison to the positive control acarbose (IC50 = 564.28 ± 4.68 μM). Kinetic studies indicated that N-Boc-kumbicin A was a reversible and mixed-type inhibitor of α-glucosidase. CD spectral analysis revealed that the interaction of N-Boc-kumbicin A with α-glucosidase caused significant conformational changes and modifications in the microenvironment of the enzyme's secondary structure, principally through the formation of hydrogen bonds and hydrophobic interactions as demonstrated by molecular docking studies."

Journal

In vitro and computational evaluation of the erectogenic and anti-diabetic potential of ethanol extract of Hymenodictyon pachyantha stem bark. (PubMed, In Silico Pharmacol) - "Our data revealed that EHP inhibited PDE-5 (IC50 = 0.58 mg/ml), arginase (IC50 = 0.57 mg/ml), and AchE (IC50 = 0.48 mg/ml), comparable with the reference drug, sildenafil (IC50 = 0.55 mg/ml). The results also showed that EHP inhibited α-amylase (IC50 = 0.81 mg/ml) and α-glucosidase (IC50 = 0.23 mg/ml) compared with the reference drug acarbose, which showed IC50 = 0.66 mg/ml and 0.25 mg/ml, respectively...Overall, our findings showed that EHP inhibited PDE-5, arginase, AchE, α-amylase, and α-glucosidase, with phytochemicals particularly rutin, naringin, catechin, and sapogenin showing the strongest docking affinities and favorable ADMET properties, indicating that EHP contains compounds with erectogenic and antidiabetic potentials; however, further research is required to confirm the safety and efficacy of EHP's phytocompounds using in vivo experiments. The online version contains supplementary material available at..."

Journal • Preclinical • Diabetes • Erectile Dysfunction • Metabolic Disorders • Pain

GB5, a synergistic phytotherapy for type 2 diabetes mellitus management: an integrated polyherbal approach from phytochemical profiling to network pharmacology. (PubMed, BMC Complement Med Ther) - "GB5's multi-targeted efficacy against hyperglycaemia, oxidative stress, and adipocyte dysfunction positions it as a promising complementary therapy for T2DM, meriting further in vivo evaluation."

Journal • Diabetes • Inflammation • Metabolic Disorders • Type 2 Diabetes Mellitus • PPARG • PTPN1

Multi-Target Screening of Anti-Diabetic and Antioxidant Potential Bioactive Constituents from Dandelion. (PubMed, Foods) - "Moreover, at least 5 of these compounds exhibited anti-diabetic activities comparable to the positive control drug acarbose, suggesting that they are principal bioactive constituents responsible for its hypoglycemic effects...In conclusion, these findings underscored the considerable potential of TMHM as a natural source of multifunctional bioactive compounds for nutraceutical, functional, and pharmaceutical applications. This study provided a critical foundation for elucidating the mechanisms underlying TMHM's anti-diabetic effects and its therapeutic potential in mitigating diabetes-related complications, thereby facilitating future development and utilization."

Journal • Diabetes • Metabolic Disorders

Properties of AgNPs stabilized with polyvinylpyrrolidone relevant to antidiabetic agents. (PubMed, Nanoscale) - "In vivo studies showed that AgNPs inhibited α-amylase, α-glucosidase, and dipeptidyl peptidase-4, up to 3.51, 3827.76, and 11 times more effective than acarbose and sitagliptin, respectively. Advanced glycation end products inhibition by AgNPs was up to 61.4 times higher than metformin. In vivo experiments revealed that AgNPs antihyperglycemic activities were close to acarbose, while the same hypoglycemic effect was achieved with AgNP doses up to 167 times lower than that of glibenclamide. The results show the possibility to decrease the glibenclamide dose by two orders, that indicates high AgNP perspective to reduce drug toxicity and side effects."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Hypoglycemic effects of lanostane triterpenoids from the fruiting bodies of Ganoderma lingzhi. (PubMed, Bioorg Chem) - "Moreover, compounds 7, 11, 14-17, and 22 exhibited promising inhibitory activity against α-glucosidase with IC50 values ranging from 32.72 to 146.10 μM, compared with that of acarbose. The dual-target inhibitory mechanisms of compound 7 against PTP1B and α-glucosidase were illuminated by the enzyme kinetic studies, molecular docking, and dynamic simulations. Consistently, compound 7 could significantly reduce postprandial blood glucose (PBG) levels in normal mice during glucose/sucrose/maltose tolerance test."

Journal • PTPN1

Hirata Syndrome Clinical Presentation and Management: A Single-Centre Experience. (PubMed, J ASEAN Fed Endocr Soc) - "Six IAS cases were identified, with most linked to α-lipoic acid in multivitamins and one to methimazole...Management included discontinuation of causative drugs, dietary changes with frequent complex carbohydrate meals, and pharmacotherapy (acarbose or prednisolone)...Early diagnosis using IAA measurement and appropriate management, including drug discontinuation, dietary adjustments, and pharmacotherapy, is essential. Further research is needed to refine treatment strategies and understand the pathogenesis of this rare syndrome."

Journal • Hypoglycemia • Immunology

Bioactive Potential of Tithonia diversifolia: Phytochemical Profiling and Multifunctional Activities. (PubMed, Chem Biodivers) - "Besides, substantial α-amylase and α-glucosidase enzyme inhibition was displayed by TDL (half-maximal inhibitory concentration values of 38.99 ± 1.10 and 49.62 ± 1.21 µg/mL), compared to TDF (45.26 ± 2.61 and 50.53 ± 1.82 µg/mL), respectively, and the acarbose standard. Antifungal evaluation demonstrated subtle potency differences, with TDF (800.0 µg/mL) displaying a lower minimum inhibitory concentration than TDL (900.0 µg/mL) at day 13. Collectively, these findings highlight T. diversifolia extracts as multifunctional agents with significant antioxidant, anticancer, antidiabetic, and antifungal potential, supporting their application in pharmaceutical drug development."

Journal • Breast Cancer • Lung Cancer • Oncology • Solid Tumor

Synthesis of new Pyridazinone derivatives and their dual inhibitory activity on aldose reductase and α-glucosidase. (PubMed, Bioorg Med Chem Lett) - "Among the tested molecules, compound 4, bearing a fluorinated thiadiazole moiety, exhibited the most potent activity with Ki values of 0.094 μM (ALR2) and 0.171 μM (α-Glu), surpassing standard inhibitors epalrestat and acarbose, respectively. These findings suggest that halogenated pyridazinone derivatives, especially fluorinated thiadiazole analogs, represent promising dual inhibitors for managing hyperglycemia and preventing diabetic complications. The dual-targeting approach demonstrated in this work offers a rational design framework for future antidiabetic drug development."

Journal • Diabetes • Metabolic Disorders • Pain • Renal Disease • Retinal Disorders • AKR1B1

Progress in Anti-ageing Drug Research for Age-related Diseases: A Review. (PubMed, Ageing Res Rev) - "This review explores the anti-ageing potential of nine repurposed drugs: aspirin, atorvastatin, enalapril, metformin, canagliflozin, liraglutide, acarbose, N-acetylcysteine and dasatinib (commonly combined with quercetin). Specifically, it focuses on their mechanisms through the mechanistic target of rapamycin, adenosine monophosphate-activated protein kinase, nuclear factor kappa B and senescence-associated secretory phenotype pathways...This review synthesises progress and obstacles in transitioning drug development from targeting individual age-related diseases to addressing ageing as a unified biological process. Ultimately, the goal is to support a paradigm shift where ageing is recognised as a modifiable condition, enabling longer healthy human lifespans."

Journal • Review • Inflammation • mTOR

Chemical screening of Hibiscus rosa-sinensis for their phytochemicals and their in vitro/in silico evaluation as α-amylase inhibitors. (PubMed, Naunyn Schmiedebergs Arch Pharmacol) - "The MMGBSA calculations displayed the higher stability of the complex 3BAJ-HF3 than the complex of the target protein and standard drug acarbose. Thus, the natural compound β-stigmasterol glycoside (HF3) isolated from Hibiscus rosa-sinensis could play a promising role as a hypoglycemic agent for the development of safe and potential medicinal formulations targeting α-amylase."

Journal • Preclinical

From pulp to pomace: Distribution and bioactivity of free and bound phenolics in Rosa roxburghii. (PubMed, Food Chem X) - "Strong in vitro α-glucosidase inhibition was observed in RTP-EP and RTPS-FP, both of which demonstrated lower IC50 values than acarbose and exhibited mixed-type inhibition kinetics...Principal component analysis (PCA) and Pearson correlation analysis revealed strong associations between antioxidant activity and these specific flavonoids. These findings establish pomace as a rich source of bioactive phenolics and provide a mechanistic and compositional basis for the targeted recovery and application of R. roxburghii phenolics in functional food and nutraceutical formulations."

Journal

Mechanistic insight into the antidiabetic effects of Ficus hispida fruits: Inhibition of intestinal glucose absorption and pancreatic beta-cell apoptosis. (PubMed, PLoS One) - "In-vitro investigations demonstrated that, FhME exhibited notable α-glucosidase inhibitory activity compared to acarbose, as indicated by its low IC50 value of 850 µg/mL...Post-docking MM-GBSA study identified alpinumisoflavone and chlorogenic acid as exceptionally stable compounds. Molecular dynamics simulations conducted over 200 ns demonstrated that gallic acid and alpinumisoflavone produced the most stable complexes with caspase-3. These findings designate F. hispida fruits as a potential natural medicinal agent for Type 2 diabetes treatment, functioning through dual mechanisms of α-glucosidase inhibition and caspase-3 modulation of the apoptotic signaling pathway of the beta cells."

Journal • Atherosclerosis • Cardiovascular • Diabetes • Metabolic Disorders • Oncology • Type 2 Diabetes Mellitus • CASP3

Green microwave synthesis of pyrazole chalcone molecular hybrids efficient route to advanced diabetes therapeutics with DNA intercalative properties. (PubMed, RSC Adv) - "In vitro enzyme inhibition studies revealed promising dose dependent activity with compounds LIV (IC50 = 212.5 µM) and LII (IC50 = 215.2 µM) demonstrating superior α-glucosidase inhibition compared to acarbose (IC50 = 240.6 µM), while compound LI exhibited potent α-amylase inhibitory activity (IC50 = 501.9 µM)...The in silico drug-likeness and oral bioavailability profiles of pyrazole-chalcone fully comply with Lipinski's criteria and exhibit excellent ADMET properties. These comprehensive findings establish pyrazole chalcone hybrids as promising multifunctional molecular scaffolds with significant potential for next-generation antidiabetic therapeutics."

Journal • Diabetes • Metabolic Disorders

MetaMDA: explainable prediction of microbe-drug association utilizing random walks on a microbe-metabolite-drug heterogeneous network. (PubMed, Bioinformatics) - "Notably, we show MetaMDA's unique ability to predict MDAs involving microbes or drugs absent from labeled data, as illustrated by associations related to acarbose. Furthermore, mechanistic analysis of MetaMDA provides biological explanations for the associations between E. coli and escitalopram, highlighting its potential to reveal a deeper mechanistic understanding of microbe-drug associations. The code and datasets are available on Zenodo https://doi.org/10.5281/zenodo.17348446 and GitHub https://github.com/wqlyt17/MetaMDA. Supplementary data are available at Bioinformatics online."

Heterogeneity • Journal • Oncology

Effect of Simulated Gastrointestinal Digestion on the Phenolic Composition and Bioactivity of Cymbopogon flexuosus Extracts. (PubMed, Foods) - "Extracts mildly inhibited α-amylase but more strongly inhibited α-glucosidase as shown with applied enzyme inhibition assays, especially EtD (76.93% at a concentration of 10 mg/mL), which showed stronger activity than controls but remained below acarbose (87.74% at 1 mg/mL). All extracts promoted HaCaT keratinocyte growth and reduced HCT-116 colon cancer cell viability at 250 µg/mL, with the strongest effects in AqC and AqD. Overall, GID decreased antioxidant activity but enhanced antidiabetic potential, confirming the safety and selective anticancer effects of C. flexuosus extracts."

Journal • Colon Cancer • Colorectal Cancer • Oncology • Solid Tumor

Searching for Hypoglycemic Compounds from Brazilian Medicinal Plants Through UPLC-HRMS and Molecular Docking. (PubMed, Plants (Basel)) - "In vitro testing confirmed that isoquercitrin effectively inhibited α-glucosidase (IC50 = 0.09 mg mL-1), showing stronger activity than acarbose...Acute toxicity in zebrafish showed low toxicity for L. origanoides and A. cearensis and moderate levels for J. pectoralis, supporting their overall safety. These findings highlight these species as promising sources of bioactive compounds for developing safe, plant-based antidiabetic agents."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

From Bench to Bioactivity: An Integrated Medicinal Development Based on Kinetic and Simulation Assessment of Pyrazolone-Oxadiazole Coupled Benzamide as Promising Inhibitors of Diabetes Mellitus. (PubMed, Pharmaceuticals (Basel)) - "The potential of all derivatives was tested by screening them against alpha-amylase and alpha-glucosidase in comparison with reference anti-diabetic drug acarbose (4.50 ± 0.20 µM and 4.90 ± 0.30 µM)...The results of docking were further confirmed via molecular dynamics analysis, whereas the pharmacophore model of analog 3 supports the formation of a stable hydrogen bond network of derivatives with the receptor site of the enzyme. Collectively in silico and in vitro results underscore the therapeutic potential of these derivatives for the effective treatment of diabetes in the future."

Journal • Diabetes • Metabolic Disorders

Peptides from 'Vaina Morada' Black Bean Inhibit α-Amylase and α-Glucosidase: A Combined In Silico-In Vitro Study. (PubMed, Foods) - "Molecular docking indicated that several peptide sequences showed equal or stronger binding affinities compared to acarbose...Also, the dialyzed hydrolysate demonstrated the highest enzyme inhibition, with IC50 values of 0.78 mg/mL for α-amylase and 0.60 mg/mL for α-glucosidase. "Vaina morada" black bean protein hydrolysates are a rich source of multifunctional peptides, supporting their potential application in functional food formulations aimed at preventing or managing type 2 diabetes."

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

Synthetic α-glucosidase inhibitory peptides designed by molecular docking: In vitro screening and anti-hyperglycemic efficacy in diabetic mice. (PubMed, Eur J Med Chem) - "Both peptides exhibited concentration-dependent inhibition of α-glucosidase, with GIP1 showing the strongest activity (IC50 = 37.85 μg/mL) and maintaining 1.05 % higher inhibition than acarbose at equivalent doses...Moreover, GIP1 and GIP2 showed good digestive stability and excellent systemic safety, with no signs of hepatic, renal, or hematological toxicity after 14 days of administration. Overall, this work highlights GIP1 as a promising, safe, and biocompatible peptide-based α-glucosidase inhibitor with therapeutic potential for diabetes management."

Journal • Preclinical • Diabetes • Hematological Disorders • Metabolic Disorders

Abietane diterpenoids and their biological activities from Premna herbacea Roxb. (PubMed, Phytochemistry) - "Salvilenone (10) exhibited α-glucosidase inhibition with an IC50 value of 34.6 μM, significantly outperforming the positive control, acarbose (IC50 = 190.4 μM)...Bharangin (2) demonstrated notable cytotoxicity against A549 human lung adenocarcinoma cell lines with an IC50 value of 19.4 μM. A plausible biosynthetic pathway for the isolated diterpenoids is also proposed."

Journal • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Triazole-containing xanthone-furanose/pyranose hybrids: synthesis of potential α-glucosidase inhibitors. (PubMed, Eur J Med Chem) - "Furthermore, an oral sucrose tolerance test (OSTT) in both healthy and diabetic mice demonstrated that benzoxanthone derivatives 17f and 18f prevent the hyperglycemic peak that occurs after sucrose administration. Although α-glucosidase inhibition is a key mechanism of action for xanthone 17f, it also improved plasma glucose levels after 60 min of sucrose administration in diabetic mice, resulting in a decrease of 42 % compared to initial glucose levels and showing better reduction than acarbose (reduction of 22 %), suggesting a complementary antidiabetic effect."

Journal • Diabetes • Type 2 Diabetes Mellitus

In silico and in vitro evaluation of flavonoid derivatives for diabetes management: molecular dynamics, and enzyme kinetics for pancreatic alpha-amylase and alpha-glucosidase. (PubMed, In Silico Pharmacol) - "Acarbose showed a Ki' of 25 ± 0.4 µM for amylase and a Ki of 73 ± 0.5 µM for glucosidase, while several flavonoids, including 7-hydroxyflavanone, 2'-hydroxyflavanone, 4'-hydroxyflavanone, liquiritigenin, naringenin, eriodictyol, and ampelopsin displayed lower Ki' values between 9 and 21 µM for amylase and between 6 and 19 µM for glucosidase, indicating stronger affinity for the enzyme-substrate complex...The combined in silico and in vitro workflow provides a validated strategy for systematically evaluating flavonoid derivatives as potential enzyme-targeted therapeutics for diabetes management. The online version contains supplementary material available at 10.1007/s40203-025-00493-4."

Journal • Preclinical • Diabetes • Metabolic Disorders

Drug repurposing for type 2 diabetes: computational studies of potential alpha-glucosidase inhibitors from DrugBank. (PubMed, In Silico Pharmacol) - "We selected 10 compounds with top docking performance, and rescoring these compounds with MMGBSA calculations produced arbekacin, neamine, and sisomicin with a binding free energy of - 72.13, - 55.14, and - 69.07 kcal/mol, respectively, as the top three compounds. These compounds were subsequently analysed and compared with the standard drug, acarbose for their protein-binding stability using molecular dynamics simulation (MDS) approach. The MDS analysis suggests that sisomicin exhibited the most stable interactions and stronger post-MDS binding free energy with alpha-glucosidase. These findings suggest that sisomicin is a potential inhibitor of alpha-glucosidase, and a novel candidate for drug repurposing in antidiabetic therapy."

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

Network pharmacology reveals Artemetin from Artemisia annua as a multitarget agent against hepatocellular carcinoma with α-amylase-inhibitory potential. (PubMed, In Silico Pharmacol) - "UHPLC‒MS analysis of the methanol-based extract revealed multiple anticancer and antidiabetic compounds, predominantly flavonoids. In vitro validation demonstrated significant dose-dependent inhibition of HepG2 cell viability (up to 96.25% ± 0.5 reduction at 200 μM) and notable α-amylase inhibitory activity (30.22% at 1 µg/mL), albeit less potent than that of acarbose...These findings warrant further validation through in vitro and in vivo studies to advance its clinical application. The online version contains supplementary material available at 10.1007/s40203-025-00462-x."

Journal • Hepatocellular Cancer • Oncology • Solid Tumor • CDC37 • EGFR • ER • HSP90AA1