acarbose / Generic mfg. - LARVOL DELTA

Novel C-4 sulfenylated pyrazoles as α-amylase inhibitors: Insights from in silico and in vitro studies. (PubMed, Bioorg Chem) - "Among all, compound 6b and 6i displayed highest inhibition of α-amylase with lower IC50 values than acarbose...The significant inhibition of the selected enzymes by chloro substituted analogues certainly shows relevance of "magic chloro effect" in biological system. The experimentally determined biological results strongly corroborated the in silico findings."

Journal • Preclinical • Diabetes • Metabolic Disorders

In-vitro, in-vivo and computational experiments for the antidiabetic potential of bioactive compound from Notholirion thomsonianum. (PubMed, Nat Prod Res) - "The IC50 values of the standard acarbose against α-glucosidase and α-amylase were 4.12 and 3.03 μg/ml, respectively...In-vivo analysis the Comp-1 displayed blood glucose level up to 117 at 28th day while the standard drug glibenclamide displayed 104...The study concludes that N. thomsonianum has a significant amount of bioactive chemicals with antidiabetic properties. These findings suggest the potential for conducting in-vivo tests in the future."

Journal • Preclinical • Diabetes • Metabolic Disorders

Impact of the Food Matrix on the Antioxidant and Hypoglycemic Effects of Betalains from Red Prickly Pear Juice After In Vitro Digestion. (PubMed, Foods) - "Notably, FJ showed the highest inhibition of α-amylase (72%) and α-glucosidase (68%), surpassing acarbose (50-60% inhibition). These findings highlight the critical role of the food matrix, particularly mucilage and pectin, in stabilizing betalains through non-covalent interactions and enhancing their hypoglycemic potential. Red prickly pear juice emerges as a promising functional food for managing postprandial glucose levels, offering valuable insights for developing betalain-rich foods to address type 2 diabetes."

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

Design, Synthesis and Alpha-glucosidase Inhibitory Effect of Pyrazole-1,2,3-Triazole Hybrids. (PubMed, Chem Biodivers) - "Compounds with 4-nitro and 4-chloro groups, respectively, proved the most significant, promising α-glucosidase inhibition activity with IC50 values of 3.35 and 6.58 µM, related to the cited inhibitor, acarbose (IC50 = 3.86 µM)...Structure-activity relationship analysis implied that the electron-leaving functions at the para position account for the variable enzyme inhibition. Therefore, developing novel therapeutic agents may assist as structural models in exploring diabetes mellitus."

Journal • Diabetes • Metabolic Disorders • Pompe Disease

Multi-omics investigation for the tumor immune microenvironment and spatial heterogeneity in hepatocellular carcinoma with PVTT: MyCAFs and NID1 in immune evasion. (ASCO 2025) - "When combined with tislelizumab, acarbose significantly enhanced T cell-mediated tumor cytotoxicity, inhibited tumor growth, and reduced NID1 expression, demonstrating superior efficacy compared to anti-PD-1 monotherapy, both in vitro and in vivo. Our findings demonstrate the critical role of myCAFs in shaping the tumor immune-suppressive environment that promotes PVTT formation. Targeting NID1, a key driver of this process, with acarbose effectively disrupts the myCAF-mediated immune barrier and synergistically enhances the efficacy of immunotherapy."

Heterogeneity • IO biomarker • Diabetes • Hepatocellular Cancer • Oncology • Solid Tumor • Thrombosis • CAFs • NID1

Design, Synthesis, Biological Evaluation, and Molecular Docking Studies of Novel 1,3,4-Thiadiazole Derivatives Targeting Both Aldose Reductase and α-Glucosidase for Diabetes Mellitus. (PubMed, ACS Omega) - "All of the members of the series showed a higher potential of aldose reductase inhibition (K I: 15.39 ± 1.61-176.50 ± 10.69 nM and IC50: 20.16 ± 1.07-175.40 ± 6.97 nM) compared to the reference inhibitor epalrestat (K I: 837.70 ± 53.87 nM, IC50: 265.00 ± 2.26 nM). Furthermore, compounds 6a, 6g, 6h, 6j, 6o, 6p, and 6q showed significantly higher inhibitory activity (K I: 4.48 ± 0.25 μM-15.86 ± 0.92 μM and IC50: 4.68 ± 0.23 μM-34.65 ± 1.78 μM) toward α-glucosidase compared to the reference acarbose (K I: 21.52 ± 2.72 μM, IC50: 132.51 ± 9.86 μM)...A cytotoxicity study was carried out with the L929 fibroblast cell line in vitro, revealing that all of the synthesized compounds were noncytotoxic. Furthermore, AMES test has been added to show the low mutagenic potential of the compounds 6h and 6o."

Journal • Diabetes • Metabolic Disorders • AKR1B1

Extraction, structural characterization, and bioactivity of laminarin and fucoidan from brown macroalgae Chorda filum. (PubMed, Carbohydr Res) - "It also exhibited strong α-glucosidase enzyme inhibition activity (IC50 0.125 ± 0.012 mg mL-1), equivalent to the model commercial compound acarbose...The molecular mass of CPF1 using gel permeation chromatography (GPC) was found to be approximately 64 kDa. In summary, CPF1, a bioactive, m-type laminarin, was successfully extracted and purified from the understudied filamentous macroalgae C. filum."

Journal

Synthesis, characterization, and in vitro and in silico α-glucosidase inhibitory evolution of novel N'-(2-cyclopentyl-2-phenylacetyl)cinnamohydrazide derivatives. (PubMed, RSC Adv) - "All the tested compounds displayed significant α-glucosidase inhibitory activity compared to the standard drug acarbose...The compounds 7b and 7d exhibit the highest docking energies, with same value of -10.1 kcal mol-1 with crucial hydrogen bonding interactions with HIS:280 and ASN:415, respectively. Furthermore, computational drug likeness/ADME/toxicity analysis was conducted on the compounds, which indicated that these compounds exhibit drug-like properties and possess favourable ADME and toxicity profiles."

Journal • Preclinical

Anti-Senescence Effect of Inhibiting Sodium-Glucose Cotransporter 2 and α-Glucosidase in a Type 2 Diabetes Mellitus Animal Model. (PubMed, Diabetes Metab J) - "As canagliflozin and acarbose have been shown to increase lifespan in mice, we investigated the effect of sodium-glucose cotransporter 2 (SGLT2) inhibitor, α-glucosidase inhibitor or both on the cellular senescence of β-cells in a T2DM mouse model. The combined administration of enavogliflozin and acarbose significantly reduced blood glucose, improved β-cell function, and reduced senescent β-cells in db/db mice. This combination therapy holds potential as a senotherapeutic strategy for managing T2DM."

Journal • Preclinical • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus • CDKN1A

Medically Refractory Nesidioblastosis as a Late Adverse Effect of Roux-en-Y Gastric Bypass. (PubMed, Cureus) - "He was trialed on numerous medications, which included octreotide, acarbose, diazoxide, and verapamil...Although evidence is lacking for use in this context, empagliflozin was then added to prevent the hyperglycemic spikes; however, this too proved ineffective at preventing hypoglycemic episodes...Endocrinologic surgery declined distal pancreatectomy due to high morbidity and mortality risk with questionable benefit. The patient opted to seek a second opinion at another medical center."

Adverse events • Journal • Cardiovascular • Chronic Kidney Disease • Congestive Heart Failure • Diabetes • Endocrine Disorders • Fibrosis • Gastroenterology • Genetic Disorders • Heart Failure • Hepatology • Hypoglycemia • Immunology • Liver Cirrhosis • Nephrology • Obesity • Pain • Pancreatitis • Renal Disease • Solid Tumor

Effect of acarbose and vildagliptin on plasma trimethylamine N-oxide levels in patients with type 2 diabetes mellitus: a 6-month, two-arm randomized controlled trial. (PubMed, Front Endocrinol (Lausanne)) - P4 | "Furthermore, the decline in TMAO levels correlated significantly with improvements in insulin resistance parameters. https://clinicaltrials.gov, identifier NCT02999841."

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

1-Phenyl-β-carboline-3-carboxamide-1,2,3-triazole-N-phenylacetamide hybrids as new α-glucosidase inhibitors. (PubMed, Sci Rep) - "In vitro anti-α-glucosidase assay demonstrated that all the new fourteen derivatives with IC50 values ranging from 64.0 to 661.4 µM were more potent than positive control acarbose with IC50 value of 750.0 and in vitro kinetic study revealed that the most potent compound among them, compound 14b, was an uncompetitive α-glucosidase inhibitor...Prediction of the pharmacokinetics and toxicity of the most potent compound 14b showed that our new compound had good toxicity profile as an oral drug candidate. Based on these findings, compound 14b can be considered as a promising candidate for the development of a new α-glucosidase inhibitor."

Journal

Functional Characterization of Residues Affecting the Catalytic Activity of Glucosyltransferase from Streptococcus mutans. (PubMed, J Phys Chem B) - "Our findings revealed that mutations increased stability in the sucrose-bound system while decreasing stability in the acarbose-bound system, with consistent fluctuation patterns observed across different ligands. These dynamic changes in glucosyltransferase behavior could influence its catalytic efficiency."

Journal • Dental Disorders

Acarbose vs. Fast-Acting Insulin for the Treatment Postprandial Hyperglycemia in Gestational Diabetes Mellitus—The ACARB-GDM Study (ADA 2025) - "Available on Friday, June 13, 2025 at 08:00am CDT."

Diabetes • Gestational Diabetes • Metabolic Disorders

Variations of the chemical components and biological activities of Thymus capitatus essential oil from three regions in Palestine. (PubMed, Sci Rep) - "α-amylase inhibitory activity of the EOs samples was studied compared with the hypoglycemic drug, Acarbose...All samples showed anti-lipase activity higher than Orlistat at concentrations equal to or above 200 µg/ml...All samples showed promising cytotoxicity results against Hep-G2, with an average percent inhibition of 85% at a concentration of 62.5 µg/mL. The chemical composition of the EO of T. capitatus is related to the plant's origin, soil components, genetic variables, and climatic conditions, which in turn reflect the plant's biological activity."

Journal • Oncology

Enantiomeric diarylheptanoids from Ottelia acuminata var. acuminata and their α-glucosidase inhibitory activity. (PubMed, Nat Prod Bioprospect) - "Notably, compound 6 was the first diarylheptanoid glycoside isolated from this aquatic species, and its absolute configuration was unequivocally established through semi-synthesis. Biological evaluation demonstrated that compound 1 exhibited α-glucosidase inhibitory activity, with an inhibition ratio of 38.97% (acarbose as the positive control, inhibition ratio = 13.52%)."

Journal

Ultrasound-Assisted Extraction of Bioactive Compounds From Black Pine (Pinus nigra) Bark: Optimization and Evaluation of Their In Vitro Bioactivities. (PubMed, Food Sci Nutr) - "Accordingly, PBE showed stronger antidiabetic activity than acarbose, the reference antidiabetic drug, with half-maximal inhibitory concentration (IC50) values of 0.38 mg/mL and 0.46 mg/mL against α-glucosidase and α-amylase, respectively, compared to acarbose's IC50 values of 0.72 mg/mL and 0.66 mg/mL. At 2 mg/mL, PBE showed moderate anticholinesterase activity, inhibiting acetylcholinesterase (AChE) by 57.26% and butylcholinesterase (BChE) by 48.35%, compared to the stronger effects of galantamine hydrobromide, which inhibited AChE by 88.57% and BChE by 85.72%. These findings highlighted the potential of PBE as a natural source of bioactive compounds with diverse biological activities, including antioxidant, antidiabetic, anticancer, and anticholinesterase properties."

Journal • Preclinical • Oncology • Pain

Enhancement of Acarbose Production in Actinoplanes sp. QQ-12 via Multiple Engineering Strategies. (PubMed, J Agric Food Chem) - "Furthermore, following fed-batch fermentation optimization in shake flasks, the titer of acarbose in LGQ-17::3acb::stnYp-acbJ increased by 1.1-fold to reach 8.12 g/L. This genetic engineering toolkit with multiple Att/Int systems and high conjugation frequencies paves the way for future genetic engineering in Actinoplanes sp., and the engineered strain shows excellent potential for industrial application."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Novel Crown Ether-Functionalized Fusidic Acid Butyl Ester: Synthesis, Biological Evaluation, In Silico ADMET, and Molecular Docking Studies. (PubMed, Molecules) - "Synthesized crown ethers exhibited moderate α-glucosidase inhibition with (IC50 = 23.5 ± 0.2 to 76.5 ± 0.1 μM) when compared to acarbose as standard (IC50 = 5.2 ± 0.8 μM). The in silico ADMET predictions indicated that the prepared compounds obeyed (bRO5) and Veber's rule for the acceptance as orally administered drugs and indicated that all the prepared crown ethers exhibited calculated values of drug likeness parameters in acceptable ranges that showed good potential of these molecules for further drug development investigations."

Journal

A cascade nanoreactor based on metal azolate framework integrated natural enzyme for α-glucosidase activity assay and inhibitor screening. (PubMed, J Colloid Interface Sci) - "This platform was further applied for α-Glu inhibitor screening, with acarbose as a model inhibitor, and achieved precise quantification of inhibition efficiency (IC50 = 60.06 nM). This work not only establishes a versatile and efficient sensing platform for diabetes-related biomolecule detection but also pioneers a novel strategy for enzyme immobilization and multienzyme cascade construction, opening new avenues for multifunctional material design in biomedical research."

Journal • Diabetes • Metabolic Disorders

Comprehensive analysis of Syzygium cumini L. pomace extract as an α-amylase inhibitor: In vitro inhibition, kinetics, and computational studies. (PubMed, Bioorg Chem) - "Enzyme inhibition assays revealed an half-maximal inhibitory concentration (IC₅₀) value of 85.68 ± 5.22 μg/mL for the JP extract, comparable to acarbose (64.28 ± 7.15 μg/mL)...These findings suggest that R11 and JP extracts hold promise as anti-diabetic agents. Utilizing JP extract as a nutraceutical offers the dual benefit of diabetes management and sustainable waste valorization in jamun juice production."

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

Synthesis, structural insights and bio-evaluation of N-phenoxyethylisatin hydrazones as potent α-glucosidase inhibitors. (PubMed, RSC Adv) - "Interestingly, most of these compounds exhibited significant inhibitory activity against the α-glucosidase enzyme, with IC50 values ranging from 3.64 ± 0.13 to 94.89 ± 0.64 μM compared to the standard drug, acarbose (IC50 = 873.34 ± 1.67 μM)...ADMET profiling confirmed favourable pharmacokinetics for these compounds, including good oral bioavailability, balanced hydrophilicity, and minimal predicted toxicity. These findings highlight the potential of these compounds as promising candidates for the development of more effective treatments for hyperglycemia."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Nesidioblastosis post-bariatric surgery in an adult patient: a case report and review of literature. (PubMed, Ann Med Surg (Lond)) - "Her symptoms, including blurred vision, tremors, and altered consciousness, persisted despite medical therapy with octreotide, acarbose, and nifedipine. Nesidioblastosis is a rare condition but should be considered in the differential diagnosis of post-bariatric surgery hypoglycemia. This case highlights the importance of distinguishing nesidioblastosis from PBHS to ensure appropriate and effective management strategies."

Journal • Gastrointestinal Disorder • Hypoglycemia • Movement Disorders • Solid Tumor

Enzymatic synthesis of a new and bioactive dihydrochalcone: 3,4-dihydroxy-2',6'-dimethoxy dihydrochalcone. (PubMed, Nat Prod Res) - "Finally, both HDDC and DDDC displayed more than twice the anti-α-glucosidase activity of the clinic drug, acarbose. Moreover, DDDC was more stable in aqueous solution and with less cytotoxicity than HDDC. Overall, DDDC holds great promise as a component in pharmaceutical, cosmetic, and food products."

Journal • Inflammation • Tyrosinase

Psoriasiform Eruption Induced by Dapagliflozin (ESPE-ESE 2025) - "The patient had been on amlodipine and acarbose for 5 years, and no other medications were documented. In conclusion, dapagliflozin is now a cornerstone in the management of diabetes. Although cutaneous reactions are rare, they can sometimes be severe enough to warrant discontinuation of an agent that is otherwise beneficial for multiple systems."

Late-breaking abstract • Atopic Dermatitis • Cardiovascular • Congestive Heart Failure • Dermatology • Diabetes • Eosinophilia • Heart Failure • Hypertension • Hypoglycemia • Immunology • Infectious Disease • Metabolic Disorders • Nephrology • Pruritus • Psoriasis • Renal Disease • Type 2 Diabetes Mellitus • Urticaria