Glucosidase

(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. (E)-3-(4-Methoxyphenyl)acrylic acid has hepatoprotective activity, antiamnesic activity, enhances cognitive effects, and can be used to lower blood pressure sugar.

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.

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 ).

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

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.

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

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

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

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

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

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.

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

α-Glucosidase-IN-42 (Compound 26), a 9-O-berberrubine carboxylate derivative, exhibits potent α-glucosidase inhibitory activity with an IC50 value of 1.61 μM and has potential for use in antidiabetic research [1].

Oroxin A (Baicalin-7-glucoside) is a partial PPARγ agonist that can activate PPARγ transcriptional activation in vitro and in vivo. Oroxin A also exhibited inhibitory activity against α-glucosidase and antioxidant capacity.

α-Glucosidase-IN-40 (compound 5) serves as a noncompetitive inhibitor of the α-glucosidase enzyme, exhibiting an inhibitory concentration (IC50) of 24.62 μM [1].

Kaempferol-3,7-di-O-β-glucoside (Kaempferol 3,7-diglucoside) is a flavonol from Morettia philaena, It can inhibit α-amylase, α-glucosidase and Acetylcholinesterase. Kaempferol-3, 7-di-o-β-Glucoside has neuroprotective activity and can slow down differentiated neuronal cells SH-SY5Y from Amyloid β peptide-induced damage. Kaempferol-3, 7-di-o-β-Glucoside can be used to study neurological disorders like Alzheimer's disease.

α-Glucosidase-IN-38 (Compound 11j) is a potent α-glucosidase inhibitor, demonstrating an IC50 of 12.44±0.38 μM, and is significant in the context of Diabetes mellitus (DM) management [1].

α-Glucosidase-IN-41 (compound 5o), a potent inhibitor of α-glucosidase, induces alterations in the secondary structure of the enzyme, thereby impeding its catalytic function. This compound is utilized in the study of diabetes mellitus [1].

α-Glucosidase-IN-39 is a potent α-glucosidase enzyme inhibitor, exhibiting an IC50 value of 869.06 ppm. It is applicable for use in antidiabetic studies [1].

GCase Modulator-1 (Compound 9g), a quinazoline derivative, functions as a glucosidase modulator with an AC50 value of 2.23 µM [1].

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

α-Glucosidase-IN-27 (compound 8l), an α-glucosidase inhibitor with an IC50 value of 25.78 μM, demonstrates potential for research into type 2 diabetes (D2M) [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. This compound 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].

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

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

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

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.

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

Mortatarin F (Compound 1), a renyleted flavonoid derived from mulberry leaves, functions as an α-glucosidase inhibitor with an IC50 value of 8.7 μM, making it pertinent for hypoglycemic research [1].

Mortatarin G (compound 3), a prenylated flavonoid derived from mulberry leaves, demonstrates potent α-glucosidase inhibition, evidenced by an IC50 value of 20.4±1.4 μM [1].

α-Glucosidase-IN-28 (Compound 18) is an α-glucosidase inhibitor with an IC50 of 0.62 μM and Ki value of 3.93 μM. It interacts with the enzyme's original binding site (OBS) and establishes multiple hydrophobic interactions with adjacent amino acids. This compound is utilized in diabetes and related diseases research [1].

Glucocerebrosidase-IN-1 (compound 11a) hydrochloride is a potent, selective GCase (glucocerebrosidase) inhibitor with IC50 and Ki values of 29.3 μM and 18.5 μM, respectively. It is utilized in the research of Gaucher disease (GD) and Parkinson’s disease (PD) [1].

α-Glucosidase-IN-30 (compound 8c) is a potent, orally active competitive inhibitor of α-glucosidase, exhibiting a K i of 40.0 µM and an IC50 of 49.0 µM. It is non-cytotoxic to both cancerous MCF-7 and normal HDF cell lines, rendering it suitable for Type 2 diabetes research [1].

α-Amylase/α-Glucosidase-IN-5 (compound 4l) functions as a dual inhibitor, effectively inhibiting both α-glucosidase (Glucosidase) and α-amylase (Amylases) with IC50 values of 5.96 μM and 1.62 μM, respectively, exhibiting potential for antidiabetic activity [1].

α-Glucosidase-IN-31 (compound R1) is a potent oral α-Glucosidase inhibitor with an IC50 of 10.1 μM, demonstrating significant blood glucose reduction and antidiabetic activity [1].

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.

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

Kaempferol 3-O-gentiobioside is a flavonoid isolated from C. alata leaves with antidiabetic activity. It possesses activity against α-glucosidase and displays a carbohydrate enzyme inhibitory effect (IC50: 50 μM).

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

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.

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.

α-Glucosidase-IN-33 (compound 7c), with an IC50 of 2.39 μM, is a potent inhibitor of α-glucosidase and is relevant in research on type 2 diabetes and hyperglycemia [1].

α-Glucosidase-IN-34 (compound 7f) is a potent inhibitor of α-glucosidase, exhibiting an IC50 of 2.90 μM, and is applicable in research related to type 2 diabetes and hyperglycemia [1].

Casuarictin, a potent competitive inhibitor of α-glucosidase, exhibits an IC50 of 0.21 μg/mL and functions as a presenilin stabilization factor-like (PSFL) protein inhibitor, making it relevant in Alzheimer's disease research [1].

Flaccidoside III, a flavonoid and triterpenoid compound extracted from the aerial parts of N. sativa (Ranunculaceae), demonstrates inhibition of α-Glucosidase (IC50: 256.7 μM) and exhibits potential antioxidant and antidiabetic properties [1].

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.

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