acarbose / Generic mfg. - LARVOL DELTA

New α-glucosidase inhibitory isoflavone derivatives from the leaves of Placolobium vietnamense. (PubMed, J Asian Nat Prod Res) - "Among them, compound 1 exhibited the strongest α-glucosidase inhibition (IC50 21.6 ± 1.04 µM), which was markedly more potent than the positive control, acarbose (IC50 156.2 ± 5.43 µM). In addition, compound 1 showed the highest xanthine oxidase inhibitory activity (IC50 32.8 ± 0.08 µM), although it remained considerably less potent than the positive control, allopurinol (IC50 2.45 ± 0.01 µM)."

Journal

Cholecystectomy-Associated Postprandial Hypoglycemia. (PubMed, AACE Endocrinol Diabetes) - "The patient responded well to dietary modification and acarbose therapy. This case highlights the need to consider cholecystectomy in the differential diagnosis of postprandial hypoglycemia, especially when classic etiologies are excluded."

Journal • Diabetes • Hypoglycemia • Immunology • Metabolic Disorders • Solid Tumor

α-Glucosidase Inhibitory Potential of Citrus reticulata Peel-Derived Flavonoids-A Prelude for the Management of Type 2 Diabetes. (PubMed, Food Sci Nutr) - "Select citrus peel-derived flavonoids, quercetin (-9.2 kcal/mol) and rutin (-10.8 kcal/mol), and the commercial AGI, acarbose (-8.7 kcal/mol), showed strong binding affinities against α-glucosidase...The cytotoxicity profile of the selected compounds was also conducted on Caco-2 cells, with flavonoids showing no significant cytotoxic effects. Flavonoids could be used as AGIs with minimal gastrointestinal impacts, reducing residual starch entering the colon and decreasing glucose uptake."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Cyclitols and Aminocyclitols as Signals: Their Roles in Supporting Ecosystems and Promoting Human Health. (PubMed, J Nat Prod) - "Several C7-cyclitols and C7N-aminocyclitols, e.g., acarbose, validamycin, and kirkamide, have been associated with gut microbiota modulation, gene regulation in fungi and insects, and/or plant-bacteria endosymbiosis. While mycosporine-like amino acids (MAAs) are well known for their UV-protective activities, studies with human cells and animals have shown intriguing biological activities involving gene regulation and activation of signaling pathways. This article reviews the roles of this family of natural products as signaling molecules involved in various biological events, including bacterial colonization and gene regulation, with physiological and ecological implications that may affect human health and other organisms."

Journal • Review

Combining bioaffinity-ultrafiltration with in vivo and in vitro analyses to identify and characterize α-glucosidase inhibitors from Rosa roxburghii Tratt. Fruit. (PubMed, Food Chem X) - "in vivo studies showed that compared to the AUC of postprandial glucose in the model (2809.33 ± 64.84 mM·min) and in the acarbose group (2525.40 ± 54...Long-term administration of apigenin additionally improved lipid metabolic disorders. These results support the development of RRT fruit as a hypoglycemic functional food."

Journal • Preclinical • Metabolic Disorders • Type 2 Diabetes Mellitus

Phytoconstituents from the leaves of Viburnum cylindricum Buch. -Ham. ex D. Don and their enzyme inhibitory activities. (PubMed, Nat Prod Res) - "The bioactivity assessment revealed that compounds 3, 4, 8, 14, and 16 could potently inhibit α-glucosidase activity with IC50 values ranging from 20.83 to 28.52 μM compared to acarbose (IC50 = 29.71 μM) (p < 0.05). In addition, compounds 3 and 4 showed significant urease inhibition with IC50 values of 10.73 and 7.61 μM, respectively, comparable to thiourea (IC50 = 28.57 μM) (p < 0.05). Moreover, the molecular docking analysis elucidated the binding mechanisms between these bioactive compounds and the enzymes α-glucosidase and urease."

Journal • Diabetes • Inflammation • Metabolic Disorders

Strategic immobilization of α-amylase on a ZIF-8 nanoplatform for targeted bioactivity screening of Gynura medica extracts. (PubMed, Anal Methods) - "This immobilized system also demonstrated a high binding capacity of 189.5 mg g-1 for acarbose...Dose-response analyses demonstrated significant pancreatic amylase inhibition by identified compounds: ellagic acid-4-O-glucoside: 98.86 ± 2.3% (1.0 g L-1), quercetin-3-O-rhamnoside: 66.32 ± 1.9% (1.0 g L-1), and methyl gallate: 33.56 ± 1.2% (1.0 g L-1). Overall, ZIF-8@α-amylase is a promising solid-phase extraction platform for selectively enriching bioactive amylase inhibitors from complex botanical matrices, with potential in pharmaceutical discovery and diabetes management."

Journal • Diabetes • Metabolic Disorders

Design, synthesis, in vitro, and in silico studies on promising α-glucosidase inhibitors based on a quinazolinone-thiophene scaffold. (PubMed, RSC Adv) - "These evaluations revealed that, in terms of druglikeness and pharmacokinetics, the new compounds were similar to acarbose, while they showed better toxicity profiles. Furthermore, the most potent compounds exhibited low cytotoxicity against normal NIH-3T3 cells."

Journal • Preclinical

Pharmacological effects and phenolic constituents of Rheum wittrockii. (PubMed, Pak J Pharm Sci) - "The present investigation concluded that the roots of Rheum wittrockii is a good source of phenolics. Its chloroform fraction showed potent antioxidant, anti-diabetic and antibacterial effects probably due to its three compounds isolated for the first time. The compounds are valuable pharmaceuticals with promising biological actions."

Journal • Infectious Disease

Clinical study on the treatment of type 2 diabetes mellitus complicated with CKD with Sangzhi alkaloids (ChiCTR) - P4 | N=60 | Not yet recruiting | Sponsor: Zhejiang Provincial People's Hospital; Zhejiang Provincial People's Hospital

New P4 trial • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Polyphenols from the aerial parts of Lespedeza cuneata and their inhibitory effects on PTP1B and α-glucosidase: insights from in vitro and in Silico analyses. (PubMed, J Nat Med) - "Notably, compounds 17 and 25 showed strong α-glucosidase inhibition (IC50 6.0 and 5.7 µM, respectively), outperforming the reference drug acarbose...Molecular docking and molecular dynamics studies indicated that compound 34 binds to an allosteric site of α-glucosidase, supporting its uncompetitive inhibition mechanism. These findings suggest that multiple constituents of L. cuneata contribute to its enzyme inhibitory activities and highlight the plant as a promising natural source of multifunctional enzyme inhibitors with potential applications in diabetes management."

Journal • Preclinical • Diabetes • Metabolic Disorders • PTPN1

Construction and biological evaluation of novel carbazole-5-phenyl-1,3,4-oxadiazole derivatives as multi-target hypoglycemic agents. (PubMed, Eur J Med Chem) - "All synthesized derivatives 5a-5u showed noticeable anti-α-glucosidase and anti-α-amylase activities (IC50: 9.79 ± 0.21-132.65 ± 1.52 μM, 6.15 ± 0.11-25.16 ± 0.75 μM, respectively) in comparison with the standard acarbose (IC50: 210.57 ± 0.91 μM, 26.17 ± 1.12 μM, respectively)...The derivative 5l could inhibit the activity of these enzyme proteins via binding to the enzyme or its substrate complex, quenching their intrinsic fluorescence, or affecting the conformation of enzyme proteins, and forming hydrophobic interactions and hydrogen bonds with them. In conjunction with the potential properties of compound 5l in inhibiting the postprandial blood glucose rise and low cytotoxicity, the title derivatives are expected to become lead molecules in developing new multi-target antidiabetes drugs."

Journal • Metabolic Disorders • Type 2 Diabetes Mellitus • PTPN1

Rational design and synthesis of new acetamide-indole-benzo[d]imidazole-carboxylic acid hybrids as dual PTP1B/α-glucosidase inhibitors. (PubMed, RSC Adv) - "The remaining compounds showed reduced efficacy relative to suramin. In contrast, only two compounds (8j and 8k) displayed marginally superior α-glucosidase inhibition compared to acarbose, while all other derivatives were less potent than the standard...Kinetic analysis of the most potent compound, 8l, confirmed a competitive inhibition mechanism against PTP1B. Molecular docking studies of the most active compounds yielded binding modes consistent with the in vitro activity, and molecular dynamics simulations further verified the stable binding of compound 8l within the PTP1B active site, supporting its potential as a lead PTP1B inhibitor."

Journal • PTPN1

Impact of Different Extraction Methods on the Physicochemical Characteristics and Bioactivity of Polysaccharides from Baobab (Adansonia suarezensis) Fruit Pulp. (PubMed, Foods) - "Bioactivity assessments revealed that ASP-AL and ASP-ALU possessed superior antioxidant capacities, demonstrating the lowest IC50 values for DPPH radical scavenging (113.67-116.67 μg/mL) and ABTS radical scavenging (79.33-79.67 μg/mL), as well as potent α-glucosidase inhibitory activity (IC50: 0.146-0.206 mg/mL), outperforming other extracts and the positive control acarbose. Correlation analysis indicated that enhanced bioactivity was associated with lower molecular weight and reduced uronic acid content. These findings underscore that alkaline extraction is an efficient strategy for obtaining highly bioactive polysaccharides from Adansonia suarezensis fruit pulp, providing a valuable theoretical foundation for their utilization in developing nutraceuticals and functional foods."

Journal

Computational-experimental integration identifies potent carbohydrate-hydrolyzing enzyme inhibitors from Nardostachys jatamansi: molecular docking, dynamics and pharmacokinetic predictions. (PubMed, Front Pharmacol) - "N. jatamansi extract demonstrated experimentally superior enzyme inhibition compared to acarbose, while computational analysis identified Virolin and Nardostachysin as promising drug candidates, establishing a validated integrative approach for accelerating natural product antidiabetic lead discovery."

Journal • PK/PD data • Pain

Tailored pyrrole-based imidazothiazole scaffolds: Synthetic elaboration, enzyme kinetic profiling and DFT-guided molecular docking toward Antidiabetic therapeutics. (PubMed, Comput Biol Chem) - "These compounds exhibited promising anti-diabetic activity, notably compound 8 emerged as a leading candidate (3.50 ± 0.20, and 4.10 ± 0.10 µM) which outperformed the potential of acarbose (6.20 ± 0.10 and 6.70 ± 0.20 µM), a reference drug...All the experimental results and in silico validations demonstrate that potent compounds possess significant anti-diabetic activity profile. Their ability to outperform an existing diabetes mellitus inhibitor and maintaining a favorable safety profile suggest that these compounds have potential to be further used in drug development and optimization against Diabetes Mellitus."

Journal • Diabetes • Metabolic Disorders

Nitric oxide and α-glucosidase inhibitors from Ludwigia adscendens: An integrated in vitro and in silico study. (PubMed, Bioorg Med Chem Lett) - "Among the tested compounds, sulfuretin (8) exhibited the most potent NO inhibitory activity (IC50 = 12.3 ± 0.56 μM), while uvaol (3) and ursolic aldehyde (4) showed strong α-glucosidase inhibition (IC50 = 5.6 ± 0.7 and 4.2 ± 0.3 μM, respectively), surpassing acarbose...In silico ADMET (absorption, distribution, metabolism, excretion, and toxicity) analysis predicted acceptable drug-likeness and low acute toxicity for the active compounds. Collectively, these results identify sulfuretin as a promising dual anti-inflammatory and antidiabetic scaffold, while triterpenoid derivatives emerge as potent and selective α-glucosidase inhibitors, providing a rational basis for further medicinal chemistry optimization."

Journal • Preclinical • Diabetes • Inflammation • Metabolic Disorders • CXCL8

New multitarget antidiabetic potential agents based on sulfaguanidine: design, synthesis, and biological evaluation. (PubMed, RSC Adv) - "Interestingly, all the synthesized sulfaguanidine derivatives exhibited significant α-glucosidase and α-amylase inhibitory potentials that were more potent than acarbose. The prominent interactions with the α-amylase and α-glucosidase active sites can be used to computationally rationalize the significant in vitro inhibitory activity of the synthesized sulfaguanidine derivatives against both enzymes. This study reveals that sulfaguanidine-conjugated pyrazole or oxazole derivatives are prospective multitarget therapeutic candidates that can be employed for the treatment of T2DM, which is characterized by complicated etiologies."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Thiazolidinedione-based dual inhibitors of α-amylase and aldose reductase: Design, in vitro evaluation, and in vivo hypoglycemic activity. (PubMed, Bioorg Med Chem) - "Compound 9a, containing an N-acetamide linker and a 4-fluorobenzylidene group, inhibited AR (IC₅₀ = 117.6 nM) and α-AMY (IC₅₀ = 2.2 μM), with lower IC₅₀ values than epalrestat (127 nM) and acarbose (15 μM), respectively. In a streptozotocin-induced diabetic mouse model, 9a reduced blood glucose levels by 68.4% at a dose of 50 mg/kg. These results suggest that 9a could serve as a starting point for further development of multi-target antidiabetic agents."

Journal • Preclinical • Diabetes • Metabolic Disorders • AKR1B1

In vitro regeneration of Kroenleinia grusonii (Hildm.) Lodé and characterisation of metabolomic profiling, and its antidiabetic potential via in vitro and computational testing. (PubMed, Nat Prod Res) - "HPLC revealed significantly higher chlorogenic acid, catechin, and methyl gallate levels in A3 plantlets (p ≤ 0.05) compared with controls. Methanolic extracts showed strong α-glucosidase inhibition (IC50 25.20 ± 0.6 µg/mL) and α-amylase inhibition (IC50 17.8 ± 0.6 µg/mL), comparable to acarbose. Docking against α-glucosidase (PDB ID: 8YIE) confirmed strong binding affinities, supporting antidiabetic potential overall."

Journal • Preclinical

Design, synthesis, and combined computational and experimental evaluation of novel 1,2,4-triazole Schiff base hybrids as potent dual inhibitors of urease and α-glucosidase. (PubMed, Future Med Chem) - "Against α-glucosidase, 5b showed strong activity (IC50 = 13.78 ± 0.89 μg/mL), comparable to acarbose (11.08 ± 0.85 μg/mL), whereas 5a was moderate (19.66 ± 2.08 μg/mL)...Interaction analyses revealed hydrogen-bond networks, π-π stacking, π-cation/anion contacts, and hydrophobic stabilization; phenolic substituents in 5b reinforced active-site complementarity. By integrating spectroscopy, quantum-chemical characterization, enzyme assays, and docking, this work identifies 5a and especially 5b as multifunctional scaffolds for dual urease and α-glucosidase inhibition with potential utility against Helicobacter pylori-associated gastric disease and type 2 diabetes."

Journal • Diabetes • Infectious Disease • Metabolic Disorders • Type 2 Diabetes Mellitus

A HILIC-PDA(-MS) profiling approach for the analysis of (methyl esterified) unsaturated galacturonic acid oligosaccharides released from pectins and food by-products. (PubMed, Carbohydr Res) - "Determination of molar relative response factors (RRF) of de-esterified uGalA-OS (degree of polymerization (DP) = 2-13) in relation to acarbose (internal standard) at 235 nm allows for (semi-)quantitative estimation of (methyl esterified) uGalA-OS and for application in other laboratories...The developed profiling approach can be useful to analyze the specificity of a pectin lyase by analysis of uGalA-OS released from commercial pectin: The pectin lyase applied here appears to prefer a methyl group at cleavage subsite -1, but probably does not require a methyl group at subsite +1. In another application, various methyl esterified uGalA-OS (DP ≤ 12) were identified in enzymatically treated carrot pomace, a pectin-rich food by-product that can potentially be used to enhance nutritional properties of food products."

Journal

The gerotherapeutic drugs rapamycin, acarbose, and phenylbutyrate extend lifespan and enhance healthy aging in house crickets. (PubMed, Res Sq) - "Post-treatment lifespan was prolonged by rapamycin (HR = 0.42, P < 0.001) and reduced by acarbose in females (HR's = 2.92 to 3.03, P's < 0.05). Intermittent rapamycin preserved survival, cognition, and locomotion, while acarbose and phenylbutyrate produced selective benefits, supporting A. domesticus as a scalable model for geroprotective drug discovery."

Journal

Alleviation of adverse effects associated with α-glucosidase inhibitors by Ocimum basilicum L., Matricaria chamomilla L., and Salvia officinalis L. reveals novel selective inhibition of Bacillus α-glucosidase by acarbose. (PubMed, J Ethnopharmacol) - "The novel finding was related to acarbose inhibition and specifically its potent selectivity of Bacillus α-glucosidase which discredits and disproves the theory that excess bacterial fermentation is the cause behind acarbose's reported adverse effects. Thus, this research study rather proves that acarbose negatively affects gut bacterial enzymes, promoting microbiome dysbiosis and therefore future research should at the forefront focus on the rehabilitation of diabetic patients' gut microbiome and intestinal health."

Adverse events • Journal • Diabetes • Gastrointestinal Disorder • Hepatocellular Cancer • Hepatology • Metabolic Disorders • Metabolic Dysfunction-Associated Steatotic Liver Disease • Oncology • Solid Tumor • Type 2 Diabetes Mellitus

Porcine serum maltase-glucoamylase: structure, kinetics, and inhibition. (PubMed, J Enzyme Inhib Med Chem) - "The apparent mixed-type inhibition can be more accurately attributed to dual competitive inhibition mechanisms. These findings contribute to the advancement of functional foods and therapeutic interventions for postprandial hyperglycaemia and type 2 diabetes."

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