α-glucosidase

α-Glucosidase (α-D-Glucosidase) is a carbohydrate hydrolyzing enzyme that catalyzes the release of α-glucose from the non-reducing end of the substrate, playing a vital role in glucose absorption by the small intestine. Inhibiting α-Glucosidase effectively manages non-insulin-dependent diabetes mellitus (NIDDM).

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).

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.

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 ).

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.

Acarbose (BAY g 5421) is a hypoglycemic agent that is an inhibitor of orally active alpha-glucosidase (IC50=11 nM). Acarbose enhances the hypoglycemic effect of sulfonylureas or insulin.

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

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

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.

(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.

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.

Ceftezole, an α-glucosidase inhibitor [IC50: 2.1 μM; Ki: 0.578 μM].

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.

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.

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.

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.

α-Amylase/α-Glucosidase-IN-1 (compound 33) is an effective inhibitor of α-amylase and α-glucosidase, with IC50 values of 2.01 and 2.09 μM, respectively. Kinetic studies predict that α-Amylase/α-Glucosidase-IN-1 has potential anti-hyperglycemia properties [1].

α-Glucosidase-IN-8 (Compound 4k) is a potent competitive inhibitor of α-glucosidase with an impressive IC50 value of 0.18 μg/mL [1].

α-Glucosidase-IN-9 (compound 7) is a highly potent α-glucosidase inhibitor with an IC50 of 55.6 μM, suitable for type II diabetes research [1].

α-Glucosidase-IN-16 is a highly effective and orally bioavailable inhibitor of α-glucosidase, displaying a remarkable IC50 value of 3.28 μM. This compound significantly decreases blood glucose levels in Streptozotocin-induced diabetic rats and exhibits noteworthy antidiabetic activity [1].

α-Glucosidase-IN-2 (compound 5d) is a potent α-glucosidase inhibitor with an inhibitory concentration (IC50) of 9.48 μM, functioning as an antidiabetic agent [1].

α-Glucosidase-IN-20 (Compound 3B) is a highly effective, orally active α-glucosidase inhibitor with potent anti-diabetic properties, evidenced by an IC50 value of 3.01 μM [1].