glycoside hydrolase inhibitors


Summary: Compounds that inhibit or block the activity of GLYCOSIDE HYDROLASES such as ALPHA-AMYLASES and ALPHA-GLUCOSIDASES.

Top Publications

  1. Kassem S, Raz I. Is there evidence that oral hypoglycemic agents reduce cardiovascular morbidity or mortality? No. Diabetes Care. 2009;32 Suppl 2:S337-41 pubmed publisher
  2. Xiang P, Mei W, Chen H, Kong F, Wang H, Liao G, et al. Four new bi-phenylethylchromones from artificial agarwood. Fitoterapia. 2017;120:61-66 pubmed publisher
    ..Compounds 2-4 exhibited different levels of inhibitory activity against AChE with the inhibition ratios in the range of 10-45%. However, none of the compounds was active against the ?-glucosidase. ..
  3. Noreen T, Taha M, Imran S, Chigurupati S, Rahim F, Selvaraj M, et al. Synthesis of alpha amylase inhibitors based on privileged indole scaffold. Bioorg Chem. 2017;72:248-255 pubmed publisher
    ..78±0.16µM). All other analogs displayed good to moderate inhibitory potential. Structure-activity relationship was established through the interaction of the active compounds with enzyme active site with the help of docking studies. ..
  4. Tsujii E, Muroi M, Shiragami N, Takatsuki A. Nectrisine is a potent inhibitor of alpha-glucosidases, demonstrating activities similarly at enzyme and cellular levels. Biochem Biophys Res Commun. 1996;220:459-66 pubmed
    ..Nectrisine and castanospermine suppressed syncytium formation and hemolytic activity in Newcastle disease virus (NDV)-infected BHK cells, without blocking the synthesis and cell-surface expression of HANA glycoprotein of NDV. ..
  5. Xiao T, Guo Z, Sun B, Zhao Y. Identification of Anthocyanins from Four Kinds of Berries and Their Inhibition Activity to ?-Glycosidase and Protein Tyrosine Phosphatase 1B by HPLC-FT-ICR MS/MS. J Agric Food Chem. 2017;65:6211-6221 pubmed publisher
    ..06 ± 0.02 ?g/mL, followed by bilberry, mulberry, and cranberry. Molecular docking results showed that cyanidin aglycones had the highest inhibition activity to PTP1B. ..
  6. Winstone A, Stellitano L, Verity C. Niemann-Pick type C as a cause of progressive intellectual and neurological deterioration in childhood. Dev Med Child Neurol. 2017;59:965-972 pubmed publisher
    ..To describe the cases of Niemann-Pick type C (NP-C) disease in a United Kingdom epidemiological study of progressive intellectual and neurological deterioration in childhood...
  7. Zhou H, Li H, Du Y, Yan R, Ou S, Chen T, et al. C-geranylated flavanones from YingDe black tea and their antioxidant and ?-glucosidase inhibition activities. Food Chem. 2017;235:227-233 pubmed publisher
    ..Compound 1 exhibited higher ?-glucosidase inhibitory activity with a half-maximum inhibitory concentration value (IC50) of 10.2µM compared with acarbose (18.2µM). ..
  8. Tavani C, Bianchi L, De Palma A, Passeri G, Punzi G, Pierri C, et al. Nitro-substituted tetrahydroindolizines and homologs: Design, kinetics, and mechanism of ?-glucosidase inhibition. Bioorg Med Chem Lett. 2017;27:3980-3986 pubmed publisher
  9. Zhao Y, Chen M, Kongstad K, Jäger A, Staerk D. Potential of Polygonum cuspidatum Root as an Antidiabetic Food: Dual High-Resolution ?-Glucosidase and PTP1B Inhibition Profiling Combined with HPLC-HRMS and NMR for Identification of Antidiabetic Constituents. J Agric Food Chem. 2017;65:4421-4427 pubmed publisher
    ..77 ± 1.23 and 7.29 ± 2.32 ?M, respectively. These findings show that P. cuspidatum is a potential functional food for management of type 2 diabetes. ..

More Information


  1. Chen L, Li Z, Yao J, Peng Y, Huang R, Feng T, et al. Isoindolinone-containing meroterpenoids with ?-glucosidase inhibitory activity from mushroom Hericium caput-medusae. Fitoterapia. 2017;122:107-114 pubmed publisher
    ..Caputmedusins A-C (1-3) showed moderate inhibitory activity against ?-glucosidase with the IC50 values of 39.2, 36.2 and 40.8?M, respectively. ..
  2. Nguyen N, Dang P, Vu N, Le T, Nguyen M. Quinoliniumolate and 2H-1,2,3-Triazole Derivatives from the Stems of Paramignya trimera and Their ?-Glucosidase Inhibitory Activities: In Vitro and in Silico Studies. J Nat Prod. 2017;80:2151-2155 pubmed publisher
  3. Nguyen T, Nguyen D, Zhao B, Le D, Choi D, Kim Y, et al. A new lignan and a new alkaloid, and ?-glucosidase inhibitory compounds from the grains of Echinochloa utilis Ohwi & Yabuno. Bioorg Chem. 2017;74:221-227 pubmed publisher
    ..1±1.3, 58.9±3.7, and 40.9±1.1?M, respectively. The results indicate that the grains of E. utilis will be useful in the treatment of diabetes control agents. ..
  4. Chu W, Ho H, Huang K, Tsan Y, Liou Y, Wang Y, et al. The prescribing trend of oral antidiabetic agents for type 2 diabetes in Taiwan: An 8-year population-based study. Medicine (Baltimore). 2017;96:e8257 pubmed publisher
    ..This descriptive study presents the change in the prescription of OAD medication for different age groups during 2005 to 2012...
  5. Nguyen C, Trinh B, Tran T, Nguyen L, Jäger A, Nguyen L. Anti-diabetic xanthones from the bark of Garcinia xanthochymus. Bioorg Med Chem Lett. 2017;27:3301-3304 pubmed publisher
    ..1±0.3?M (compared with acarbose, IC50=900.0±3.0?M) whilst xanthochymusxanthone B (2) exhibited remarkable activity towards PTP1B with IC50 value of 8.0±0.6?M (compared with RK682, IC50=4.4±0.3?M). ..
  6. Kazmi M, Zaib S, Amjad S, Khan I, Ibrar A, Saeed A, et al. Exploration of aroyl/heteroaroyl iminothiazolines featuring 2,4,5-trichlorophenyl moiety as a new class of potent, selective, and in vitro efficacious glucosidase inhibitors. Bioorg Chem. 2017;74:134-144 pubmed publisher
    ..These results clearly identified a new class of structural leads which can be further investigated for the development of promising ?-glucosidase inhibitors for the prevention of diabetes mellitus. ..
  7. Zhang Y, Gao H, Liu R, Liu J, Chen L, Li X, et al. Quinazoline-1-deoxynojirimycin hybrids as high active dual inhibitors of EGFR and ?-glucosidase. Bioorg Med Chem Lett. 2017;27:4309-4313 pubmed publisher
    ..79nM), also to ?-glucosidase (IC50=0.39µM). The work could be very useful starting point for developing a new series of enzyme inhibitors targeting EGFR and/or ?-glucosidase. ..
  8. Kasturi S, Surarapu S, Uppalanchi S, Anireddy J, Dwivedi S, Anantaraju H, et al. Synthesis and ?-glucosidase inhibition activity of dihydroxy pyrrolidines. Bioorg Med Chem Lett. 2017;27:2818-2823 pubmed publisher
    ..The promising compounds 6i, 5o, 6o, 10a, 11a, 10f and 11f have been identified. Molecular docking simulations were done for compounds to identify important binding modes responsible for inhibition activity of ?-glucosidase. ..
  9. Liu Z, Ma S. Recent Advances in Synthetic ?-Glucosidase Inhibitors. ChemMedChem. 2017;12:819-829 pubmed publisher
    ..Beyond that, some enlightening strategies for the synthesis of relevant compounds are highlighted. ..
  10. Taha M, Rahim F, Imran S, Ismail N, Ullah H, Selvaraj M, et al. Synthesis, ?-glucosidase inhibitory activity and in silico study of tris-indole hybrid scaffold with oxadiazole ring: As potential leads for the management of type-II diabetes mellitus. Bioorg Chem. 2017;74:30-40 pubmed publisher
  11. Nakamura K, Oe H, Kihara H, Shimada K, Fukuda S, Watanabe K, et al. DPP-4 inhibitor and alpha-glucosidase inhibitor equally improve endothelial function in patients with type 2 diabetes: EDGE study. Cardiovasc Diabetol. 2014;13:110 pubmed publisher
    ..Sitagliptin had protective effects on endothelial function without adverse events. registered at under UMIN000003951. ..
  12. Ovais M, Ayaz M, Khalil A, Shah S, Jan M, Raza A, et al. HPLC-DAD finger printing, antioxidant, cholinesterase, and α-glucosidase inhibitory potentials of a novel plant Olax nana. BMC Complement Altern Med. 2018;18:1 pubmed publisher
    ..ON-Cr may further be subjected to fractionation and polarity guided fractionation to narrow down the search for isolation of bioactive compounds. ..
  13. Rasouli H, Hosseini Ghazvini S, Adibi H, Khodarahmi R. Differential ?-amylase/?-glucosidase inhibitory activities of plant-derived phenolic compounds: a virtual screening perspective for the treatment of obesity and diabetes. Food Funct. 2017;8:1942-1954 pubmed publisher
    ..The findings of the current study may also shed light on a way of generating a new class of amylase/glucosidase inhibitors that will discriminately inhibit the on-target enzymes with negligible undesired off-target side effects. ..
  14. Jeong G, Kim T. Hydroxymethylation of Rutin Induced by Radiolysis as Novel ?-Glucosidase Inhibitors. Chem Pharm Bull (Tokyo). 2017;65:678-682 pubmed publisher
    ..The new unusual rutin derivatives 2 and 3 exhibited significantly enhanced inhibitory effects against ?-glucosidase with IC50 values of 23.1±1.2 and 11.2±0.7?µM, respectively, when compared to the parent rutin. ..
  15. Iqbal S, Khan M, Javaid K, Sadiq R, Fazal Ur Rehman S, Choudhary M, et al. New carbazole linked 1,2,3-triazoles as highly potent non-sugar ?-glucosidase inhibitors. Bioorg Chem. 2017;74:72-81 pubmed publisher
    ..0±0.057?M) and 25 (IC50=0.8±0.01?M) were found to be most active, and could serve as an attractive building block in the search of new non-sugar derivatives as anti-diabetic agents. ..
  16. Riaz T, Abbasi M, Rehman A, Siddiqui S, Shahid M, Fatima H, et al. Enzyme inhibitory, Antifungal, Antibacterial and hemolytic potential of various fractions of Colebrookia oppositifolia. Pak J Pharm Sci. 2017;30:105-112 pubmed
    ..coli. Chloroform fraction showed good activity against B. subtilis. Ethyl acetate fraction showed good activity against the P. multocida. All the studied fractions showed very less toxicity i.e. < 7%. ..
  17. Zhang L, Tu Z, Xie X, Wang H, Wang H, Wang Z, et al. Jackfruit (Artocarpus heterophyllus Lam.) peel: A better source of antioxidants and a-glucosidase inhibitors than pulp, flake and seed, and phytochemical profile by HPLC-QTOF-MS/MS. Food Chem. 2017;234:303-313 pubmed publisher
    ..Above results reveal promising potential of jackfruit peel as a new source of natural antioxidants and hypoglycemic agents. ..
  18. Macho González A, Garcimartín A, López Oliva M, Bertocco G, Naes F, Bastida S, et al. Fiber purified extracts of carob fruit decrease carbohydrate absorption. Food Funct. 2017;8:2258-2265 pubmed publisher
    ..w. reduced sodium-glucose-linked transporter-1 (SGLT1) levels in the duodenum. This study demonstrates the hypoglycemic properties of CFE, highlighting its potential role as a suitable nutritional strategy in diabetic patients. ..
  19. Choby B. Diabetes Update: New Pharmacotherapy for Type 2 Diabetes. FP Essent. 2017;456:27-35 pubmed
    ..73 m2. Newer studies provide a better understanding of the mechanisms of and indications for use of sodium-dependent glucose cotransporter 2 inhibitors, glucagon-like peptide 1 receptor agonists, and inhaled insulin. ..
  20. Chen B, Tian J, Zhang J, Wang K, Liu L, Yang B, et al. Triterpenes and meroterpenes from Ganoderma lucidum with inhibitory activity against HMGs reductase, aldose reductase and ?-glucosidase. Fitoterapia. 2017;120:6-16 pubmed publisher
    ..8 to 21.5?M. This work provides chemical and biological evidence for the usage of extracts of G. lucidum as herbal medicine and food supplements for the control of hyperglycemic and hyperlipidemic symptoms. ..
  21. Zhen J, Dai Y, Villani T, Giurleo D, Simon J, Wu Q. Synthesis of novel flavonoid alkaloids as ?-glucosidase inhibitors. Bioorg Med Chem. 2017;25:5355-5364 pubmed publisher
    ..Addition of extra hydrogen bonding and hydrophobic groups on ring A would increase the inhibitory activity. ..
  22. Bljajić K, Petlevski R, Vujić L, Čačić A, Šoštarić N, Jablan J, et al. Chemical Composition, Antioxidant and α-Glucosidase-Inhibiting Activities of the Aqueous and Hydroethanolic Extracts of Vaccinium myrtillus Leaves. Molecules. 2017;22: pubmed publisher
    ..The study results indicate that V. myrtillus leaf may have promising properties as a supporting therapy for diabetes. ..
  23. Olaokun O, McGaw L, Eloff J, Naidoo V. Evaluation of the inhibition of carbohydrate hydrolysing enzymes, antioxidant activity and polyphenolic content of extracts of ten African Ficus species (Moraceae) used traditionally to treat diabetes. BMC Complement Altern Med. 2013;13:94 pubmed publisher
    ..Research is underway to isolate the active compound(s) responsible for the antidiabetic activity and to confirm the in vitro antidiabetic activity and to investigate in vitro toxicity. ..
  24. Liu S, Ai Z, Qu F, Chen Y, Ni D. Effect of steeping temperature on antioxidant and inhibitory activities of green tea extracts against ?-amylase, ?-glucosidase and intestinal glucose uptake. Food Chem. 2017;234:168-173 pubmed publisher
    ..Green tea steeped at 60°C had significantly stronger glucose uptake inhibitory activity (p<0.05). The integrated data suggested that steeping temperature should be considered when evaluating the biological activities of green tea. ..
  25. Ahmed A, Ahmed Q, Saxena A, Jamal P. Evaluation of in vitro antidiabetic and antioxidant characterizations of Elettaria cardamomum (L.) Maton (Zingiberaceae), Piper cubeba L. f. (Piperaceae), and Plumeria rubra L. (Apocynaceae). Pak J Pharm Sci. 2017;30:113-126 pubmed
    ..cardamomum. Our findings further justify the traditional claims of these plants as folk medicines to manage diabetes, however, through digestive enzymes inhibition effect. ..
  26. Mandrone M, Scognamiglio M, Fiorentino A, Sanna C, Cornioli L, Antognoni F, et al. Phytochemical profile and ?-glucosidase inhibitory activity of Sardinian Hypericum scruglii and Hypericum hircinum. Fitoterapia. 2017;120:184-193 pubmed publisher
  27. Kato E, Kushibiki N, Inagaki Y, Kurokawa M, Kawabata J. Astilbe thunbergii reduces postprandial hyperglycemia in a type 2 diabetes rat model via pancreatic alpha-amylase inhibition by highly condensed procyanidins. Biosci Biotechnol Biochem. 2017;81:1699-1705 pubmed publisher
    ..The abundant AT-P content and its comparable ?-amylase inhibition to acarbose, the anti-diabetic medicine, suggest that AT is a promising food supplement for diabetes prevention. ..
  28. Ali F, Khan K, Salar U, Taha M, Ismail N, Wadood A, et al. Hydrazinyl arylthiazole based pyridine scaffolds: Synthesis, structural characterization, in vitro ?-glucosidase inhibitory activity, and in silico studies. Eur J Med Chem. 2017;138:255-272 pubmed publisher
    ..In silico study was confirmed that substituents like halogens (Cl) and nitro (NO2) which have negative inductive effect were found to make important interactions with active site residues. ..
  29. Mosbah H, Chahdoura H, Kammoun J, Hlila M, Louati H, Hammami S, et al. Rhaponticum acaule (L) DC essential oil: chemical composition, in vitro antioxidant and enzyme inhibition properties. BMC Complement Altern Med. 2018;18:79 pubmed publisher
    ..The results revealed that the RaEO is a new promising potential source of antioxidant compounds, endowed with good practical applications for human health. ..
  30. Tsunosue M, Mashiko N, Ohta Y, Matsuo Y, Ueda K, Ninomiya M, et al. An alpha-glucosidase inhibitor, acarbose treatment decreases serum levels of glyceraldehyde-derived advanced glycation end products (AGEs) in patients with type 2 diabetes. Clin Exp Med. 2010;10:139-41 pubmed publisher
  31. Bianchi C, Miccoli R, Daniele G, Penno G, Del Prato S. Is there evidence that oral hypoglycemic agents reduce cardiovascular morbidity/mortality? Yes. Diabetes Care. 2009;32 Suppl 2:S342-8 pubmed publisher
  32. Flores Bocanegra L, González Andrade M, Bye R, Linares E, Mata R. ?-Glucosidase Inhibitors from Salvia circinata. J Nat Prod. 2017;80:1584-1593 pubmed publisher
    ..Molecular docking and dynamic studies revealed that compounds 6 and 7 might bind to ?-glucosidases at the catalytic center of the enzyme. ..
  33. Sun H, Ding W, Song X, Wang D, Chen M, Wang K, et al. Synthesis of 6-hydroxyaurone analogues and evaluation of their ?-glucosidase inhibitory and glucose consumption-promoting activity: Development of highly active 5,6-disubstituted derivatives. Bioorg Med Chem Lett. 2017;27:3226-3230 pubmed publisher
    ..In addition, compounds 7f and 10c exhibited significant glucose consumption promoting activity at 1?M. ..
  34. Proença C, Freitas M, Ribeiro D, Oliveira E, Sousa J, Tomé S, et al. ?-Glucosidase inhibition by flavonoids: an in vitro and in silico structure-activity relationship study. J Enzyme Inhib Med Chem. 2017;32:1216-1228 pubmed publisher
    ..The present work suggests that several of the studied flavonoids have the potential to be used as alternatives for the regulation of PPHG...
  35. Xie Z, Wang G, Wang J, Chen M, Peng Y, Li L, et al. Synthesis, Biological Evaluation, and Molecular Docking Studies of Novel Isatin-Thiazole Derivatives as α-Glucosidase Inhibitors. Molecules. 2017;22: pubmed publisher
    ..36 ± 0.13 μm. Molecular docking studies revealed the existence of hydrophobic interaction, CH-π interaction, arene-anion interaction, arene-cation interaction, and hydrogen bond between these compounds and α-glucosidase enzyme. ..
  36. Wang G, Wang J, Xie Z, Chen M, Li L, Peng Y, et al. Discovery of 3,3-di(indolyl)indolin-2-one as a novel scaffold for ?-glucosidase inhibitors: In silico studies and SAR predictions. Bioorg Chem. 2017;72:228-233 pubmed publisher
    ..This study showed these 3,3-di(indolyl)indolin-2-ones as a new class of ?-glucosidase inhibitors. ..
  37. Gao E, Ren F, Zou J, Yu Y, Fan H, Zhou Z, et al. Chiral resolution, absolute configuration, and bioactivity of a new racemic asarone derivative from the rhizome of Acorus tatarinowii. Fitoterapia. 2017;122:7-10 pubmed publisher
    ..The ?-glucosidase inhibitory and acetylcholinesterase (AChE) inhibitory activities of 1 were evaluated, and it exhibited ?-glucosidase inhibitory activity with potency close to that of the positive control (acarbose). ..
  38. Dang P, Nguyen H, Nguyen H, Vo T, Le T, Phan T, et al. Lignans from the Roots of Taxus wallichiana and Their ?-Glucosidase Inhibitory Activities. J Nat Prod. 2017;80:1876-1882 pubmed publisher
    ..All tested compounds were found to possess ?-glucosidase inhibitory activity, with formosanol (9) showing the most potent effect with an IC50 value of 35.3 ?M. ..
  39. Wang G, Chen M, Wang J, Peng Y, Li L, Xie Z, et al. Synthesis, biological evaluation and molecular docking studies of chromone hydrazone derivatives as ?-glucosidase inhibitors. Bioorg Med Chem Lett. 2017;27:2957-2961 pubmed publisher
    ..In summary, our studies shown that these chromone hydrazone derivatives are a new class of ?-glucosidase inhibitors. ..
  40. Nakamura S, Tanabe K, Yoshinaga K, Shimura F, Oku T. Effects of 1,5-anhydroglucitol on postprandial blood glucose and insulin levels and hydrogen excretion in rats and healthy humans. Br J Nutr. 2017;118:81-91 pubmed publisher
    ..Furthermore, 1,5-AG might suppress the blood glucose elevation through the inhibition of sucrase, as well as intestinal glucose absorption. ..
  41. Alam M, Zaidul I, Ghafoor K, Sahena F, Hakim M, Rafii M, et al. In vitro antioxidant and, ?-glucosidase inhibitory activities and comprehensive metabolite profiling of methanol extract and its fractions from Clinacanthus nutans. BMC Complement Altern Med. 2017;17:181 pubmed publisher
    ..The phytochemical investigation showed the existence of active constituents in Clinacanthus nutans extract and fractions. ..
  42. Xie Y, Yang Y, Li S, Xu Y, Lu W, Chen Z, et al. Phenylsulfonylfuroxan NO-donor phenols: Synthesis and multifunctional activities evaluation. Bioorg Med Chem. 2017;25:4407-4413 pubmed publisher
    ..These hybrid phenylsulfonyfuroxan-based NO-donor phenols offer a multifunctional prodrug design concept for the development of therapeutic or preventive agents for metabolic syndrome. ..
  43. Alam F, Saqib Q, Ashraf M. Zanthoxylum armatum DC extracts from fruit, bark and leaf induce hypolipidemic and hypoglycemic effects in mice- in vivo and in vitro study. BMC Complement Altern Med. 2018;18:68 pubmed publisher
    ..It can be concluded that Z. armatum extracts showed excellent antidiabetic potential in vivo and in vitro and could be considered for further appraisal in clinical assessment and drug development. ..
  44. Wei J, Huo X, Yu Z, Tian X, Deng S, Sun C, et al. Phenolic acids from Balanophora involucrata and their bioactivities. Fitoterapia. 2017;121:129-135 pubmed publisher
    ..New compound 8 also could inhibit the acetyl transfer activity of GlmU moderately with the IC50 value of 18.21?M, which was a new antibacterial target. ..
  45. Chaudhry F, Choudhry S, Huma R, Ashraf M, Al Rashida M, Munir R, et al. Hetarylcoumarins: Synthesis and biological evaluation as potent ?-glucosidase inhibitors. Bioorg Chem. 2017;73:1-9 pubmed publisher
    ..53±0.002µM. Molecular docking has predicted the plausible binding interactions of compounds 3f, 3g and 3j with ?-glucosidase. ..
  46. Sabiu S, Ajani E, Sunmonu T, Ashafa A. KINETICS OF MODULATORY ROLE OF Cyperus esculentus L. ON THE SPECIFIC ACTIVITY OF KEY CARBOHYDRATE METABOLIZING ENZYMES. Afr J Tradit Complement Altern Med. 2017;14:46-53 pubmed publisher
    ..i>Cyperus esculentus L. is one of the therapeutically implicated botanicals against several degenerative diseases including diabetes mellitus...
  47. Podsedek A, Majewska I, Kucharska A. Inhibitory Potential of Red Cabbage against Digestive Enzymes Linked to Obesity and Type 2 Diabetes. J Agric Food Chem. 2017;65:7192-7199 pubmed publisher