Glucosidase

Conduritol B epoxide is an irreversible inhibitor of β-glucosidase (GCase).

Gcase activator 1 (LTI-291) is a glucocerebrosidase (Gcase) activator.

Celgosivir (6 O-butanoyl castanospermine) is an inhibitor of α-glucosidase I. In vitro assay, it inhibits bovine viral diarrhoea virus (BVDV) ( IC50: 1.27 μM ).

Acarbose (BAY g 5421) is an inhibitor of α-Glucosidases with antihyperglycemic activity.

Bisabolone oxide A is a terpenoid isolated from Matricaria chamomilla L. It reduces neuronal excitability.Bisabolone oxide A inhibits α glucokinase and has been shown to inhibit α glucokinase in Helicoverpa armigera, Aedes vittatus, and Anopheles subpictus larvae and showed biotoxicity in Helicoverpa armigera, Aedes vittatus and Anopheles subpictus larvae experiments.

Mulberrofuran G, isolated from Morus alba L., has anti-hepatitis B virus activity and protects against ischemic injury-induced cell death. Mulberrofuran G is a dual inhibitor of PTP1B and alpha-glucosidase for use in the study of Alzheimer's disease.

Daucosterol (Sitogluside) has proliferation-enhancing activity, may be involved in the IGF1-AKT pathway. Daucosterol(β-Sitosterol β-D-glucoside) has efficient and inexpensive neuroprotectant effect, to contribute to IGF1-like activity, could be potentially developed as a medicine for ischemic stroke treatment.

Jionoside B1 is isolated from the roots of Jionoside (Gaertn.) and inhibits α-glucosidase.

1. Pinoresinol diglucoside (Pinoresinol Diglucopyranoside) is a putative α-glucosidase inhibiting compound. 2. Pinoresinol diglucoside is a important antihypertensive compound.

1-Deoxynojirimycin (Moranoline) is a potent α-glucosidase inhibitor, suppressing postprandial blood glucose, thereby possibly preventing diabetes mellitus.

Licochalcone C (LICOCHALCONEC) has potent antioxidant properties and inhibition of bacterial growth and cellular respiration. It has cardioprotection effect, via antioxidant, anti-inflammatory, and anti-apoptotic activities. Licochalcone C exhibit inhibitory activity with cytotoxicity in a rat basophilic leukaemia cell line, RBL-2H3. Licochalcone C induces apoptosis via B-cell lymphoma 2 family proteins in T24 cells, it may be a potential adjuvant therapeutic agent for bladder cancer.

1. 3-Butylidenephthalide (Butylidene phthalide) has antihyperglycemic effect is due to inhibition of α-glucosidase at the intestinal level, inhibited the activity of yeast-α-glucosidase (IC(5) 2.35 mM) in a noncompetitive fashion with a K(i) of 4.86 mM.

Manghaslin (Quercetin 3-O-rutinoside-(1->2)-O-rhamnoside) has considerable α-glucosidase inhibitory activity, illustrating the anti-diabetic potential of phenolic-rich litchi pulp extracts. Manghaslin also shows inhibitory activity against AChE

Kaempferol-3,7-di-O-β-glucoside (Kaempferol 3,7-diglucoside) is a flavonol from Morettia philaena that inhibits α-amylase, α-glucosidase, and acetylcholinesterase. It exhibits neuroprotective activity, slowing amyloid β peptide-induced damage in differentiated neuronal cells SH-SY5Y, and can be used in the study of neurological disorders such as Alzheimer's disease.

Castanospermine (1,6,7,8-Tetrahydroxyoctahydroindolizine) is a natural compound that inhibits α- and β-glucosidases, especially glucosidase l.

1. Isovitexin (Apigenin-6-C-Glucoside) exhibits a potential antioxidant activity. 2. Isovitexin shows a strong antihyperglycemic action, inhibits α-glucosidase in vivo.

IHVR-17028 is a potent broad-spectrum ERα-glucosidase I (α-glucosidase? I) inhibitor with IC50 of 0.24 μM and antiviral activity. IHVR-17028 inhibited BVDV, TCRV and DENV, and EC50 values were 0.4 μM, 0.26 μM and 0.3 μM, respectively. IHVR-17028 can be used to study infectious diseases.

Brevifolincarboxylic acid is a natural product isolated from Polygonum capitatum, it has inhibitory effect on the aryl hydrocarbon receptor (AhR). Brevifolincarboxylic acid is an α-glucosidase inhibitor with an IC50 of 323.46 μM.

Terphenyllin has α-glucosidase inhibitory activity, and is a natural product isolated from the coral derived fungus Aspergillus candidus.

ethyl rosmarinate inhibit the activity of tyrosinase, α-glucosidase, and matrix metalloproteinase-1 (MMP-1).

Gigantol is a novel inhibitor of the Wnt β-catenin pathway. It inhibits Wnt β-catenin signaling through downregulation of phosphorylated LRP6 and cytosolic β-catenin in breast cancer cells. Gigantol may be developed as a promising neuroprotective agent for successful MSC transplantation in ischemic diseases, it shows the protective effect against hydrogen peroxide-induced apoptosis in rat bone marrow mesenchymal stem cells through the PI3K Akt pathway.Gigantol inhibits aldose reductase gene to exert its anti-cataract activity. Gigantol induces growth inhibition and apoptosis of HepG2 cells via the PI3K Akt NF-κB signaling pathway.Gigantol also shows α-glucosidase inhibitory activity.

Voglibose (Glustat), an N-substituted derivative of valiolamine, exhibits excellent inhibitory activity against α-glucosidases and action against hyperglycemia and various disorders caused by hyperglycemia.

4',5-Dihydroxyflavone is a soybean LOX-1 inhibitor (Ki: 102.6 μM) and a yeast α-Glucosidase inhibitor (IC50: 66 μM).

N-Caffeoyl O-methyltyramine is isolated from Cuscuta reflexa with strong inhibitory activity against α-glucosidase with IC50 of 103.58 μM.

1. Kuwanon G (Moracenin B) as dual inhibitors of PTP1B and α-glucosidase enzymes, as well as insulin sensitizers, it may potentially be utilized as an effective treatment for Type II diabetes mellitus. 2. Kuwanon G has anti-inflammatory activity, it can attenuate atherosclerosis through inhibiting foam cell formation and inflammatory response. 3. Kuwanon G is a potent inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase B. 4. Kuwanon G shows acetylcholinesterase (AChE) and butyrylcholinesterase(BChE) inhibitory activities, it may be a promising candidate for preventive and therapeutic agents for Alzheimer's disease. 5. Kuwanon G prevents the pathological progression of allergic asthma through the inhibition of lung destruction by inflammation and immune stimulation. 6. Kuwanon G has antibacterial activity against oral pathogens. 7. Kuwanon G is a specific antagonist for the GRP-preferring receptor and can be useful for studying the physiological and pathological role of GRP.

Rebaudioside A (Reb A) is a novel agent of glycoside clathration of pharmacons, acts as α-glucosidase inhibitor.

AMP-Deoxynojirimycin (AMP-DNM) is a potent inhibitor of ceramide glucosyltransferase and GCase 2, as well as GlcCer biosynthesis, and is utilized in the study of Parkinson's disease and diabetes.

Butyl isobutyl phthalate (ButylIsobutylPhthalate) is a non-competitive α-glucosidase inhibitor(IC50 :38 μM),it shows a hypoglycemic effect

Ginkgolic Acid (C13:0) (6-Tridecylsalicylic acid): 0exhibits the highest α-glucosidase inhibitory activity.

Viscidulin III (Ganhuangenin) is present in Scutellaria baicalensis and acts as an α-glucosidase inhibitor.

Ceftezole sodium (Falomesin) is a broad-spectrum cephalosporin antibiotic active gram-negative and gram-positive bacteria except for Proteus vulgaris, Pseudomonas aeruginosa, and Serratia marcescens. It has the inhibition of cell wall synthesis via affinity for penicillin-binding proteins. It also inhibits alpha-glucosidase.

Tryptophan, N-indol-3-ylacetyl- (6CI) (Indole-3-acetyl-L-tryptophan) is involved in regulatory mechanisms for the control of auxin activity during physiological and pathophysiological responses. It may also be used in the synthesis of β-D-galactosidase and β-D-glucosidase inhibitors.

β-Glucosidase is a glucoside bond hydrolase widely found in organisms and is involved in glucose metabolism, which can be used to study diseases caused by abnormal glucose metabolism.

Kaempferol 3-O-gentiobioside, a flavonoid isolated from C. alata leaves, exhibits antidiabetic activity and α-glucosidase inhibition, demonstrating a carbohydrate enzyme inhibitory effect (IC50: 50 μM).

NCGC00092410 (ML008) is a glucocerebrosidase (GC) inhibitor with IC50 value of 31 nM. It can be used for the study of Gaucher disease caused by mutation of glucocerebrase gene.

1-Deoxynojirimycin hydrochloride (Moranoline) is a potent and selective inhibitor of alpha-glucosidase, most commonly found in mulberry leaves. Duvoglustat is used to suppress the elevation of postprandial hyperglycemia.

α-Glucosidase-IN-23 is an orally active inhibitor of α-glucosidase that can decrease blood glucose levels by inhibiting α-glucosidase (IC50 = 4.48 μM).

(Z)-Butylidenephthalide ((Z)-3-Butylidenephthalide) has antitumor and hypoglycemic effects, and can effectively inhibit the tumor growth of glioma and inhibit R-glucosidase activity.

Magnoloside B, a phenylethanol glycoside from the fruit of Magnolia officinalis, is an α-glucosidase inhibitor with protective effects against free radical-induced oxidative damage and can be used in cancer research.

α-Glucosidase-IN-4 is a potent α-glucosidase inhibitor exhibiting antihypertensive and hypoglycemic activity.

α-Glucosidase-IN-22 is a selective inhibitor of α-glucosidase (IC50=0.64 μM). α-Glucosidase-IN-22 has antidiabetic activity and has potential in type 2 diabetes (T2DM) studies.

(E)-3-(4-Methoxyphenyl)acrylic acid is a small molecule compound isolated from the rhizome of Etlingera pavieana (Pierre ex Gagnep.) R. M. Sm. It is a novel α-glucosidase inhibitor with hepatoprotective, antiamnesic, and cognitive enhancement activities, and it can be used to lower blood pressure sugar.

N1,N10-Bis(p-coumaroyl)spermidine, which can be extracted from the herb of alfalfa, exhibits inhibitory effects on alpha-glucosidase.

Naringinase is a hydrolytic enzymatic complex that exhibits α-L-rhamnosidase and β-D-glucosidase activities. It is widely found in nature and is primarily utilized for the biotransformation of steroids, antibiotics, and glycosides.

Erythro-Guaiacylglycerol beta-coniferyl ether is a compound that can be extracted from the stems and leaves of mung beans and has inhibitory effects on alpha-glucosidase with an EC50 value of 18.71 μM.

α-Glucosidase-IN-26 (Compound 7i), with an IC50 value of 4.63 µM, functions as an α-glucosidase inhibitor and is utilized in type 2 diabetes mellitus (T2DM) research [1].

α-Amylase α-Glucosidase-IN-4 (compound 5), a dual inhibitor targeting α-amylase (Amylases) and α-glucosidase (Glucosidase), exhibits potent inhibition with IC50 values of 1.10 μM and 0.15 μM respectively, and is noted for its potential antidiabetic activity [1].

Compound 56 (Antidiabetic agent 2) is a glucose-uptake promoter that inhibits DPP-4, PTP-1B, α-amylase, and α-glucosidase, with IC50 values of 0.036, 0.042, 0.241, and 0.185 μM, respectively. This agent effectively decreases blood glucose levels [1].