α-glucosidase i

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.

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.

1. Vitexin has antinociceptive and antispasmodic activities. 2. Vitexin exhibits a prominent first-pass effect. 3. Vitexin has antioxidant, antimyeloperoxidase, and α-glucosidase inhibitory activities. 4. Vitexin can either inhibit or induce activities of

Celgosivir hydrochloride (MBI 3253 hydrochloride) is an α-glucosidase I inhibitor and inhibits bovine viral diarrhoea virus (BVDV) (IC50: 1.27 μM).

Isotanshinone I with IC50s of 1.13 μM and 0.432 μM for α-glucosidase and AGE, respectively. Isotanshinone I has inhibitory activity against α-glucosidase and formation of AGE,

IHVR-19029 is an effective endoplasmic reticulum (ER) α-glucosidases I and II inhibitor (IC50: 0.48 μM for ER a-glucosidase I). IHVR-19029 efficiently blocks the replication of several hemorrhagic fever viruses, such as Ebola virus, Dengue virus, and Rift

α-Glucosidase-IN-83 (compound I-1) is a potent inhibitor of α-glucosidase, demonstrating an IC50 of 1.49 μg mL. This compound effectively reduces blood glucose levels in vivo.

Australine is a pyrrolizidine alkaloid originally isolated fromC. australethat has enzyme inhibitory activities.1,2,3It is an inhibitor of glucoamylase (IC50= 5.8 μM) that also inhibits glucosidase I, sucrase, maltase, andA. nigerα-glucosidase (IC50s = 20, 28, 35, and 28 μM, respectively).2,3Australine is selective for these enzymes over glucosidase II, α- and β-mannosidase, and α- and β-galactosidase up to 500 μM, β-glucosidase, with only 5% inhibition at 66 μM, as well as isomaltase and trehalase (IC50= 97 and 160 μM, respectively). Australine (500 μg/ml) inhibits glycoprotein processing of viral glycoproteins in influenza virus-infected MDCK cells and induces the accumulation of glycoproteins.2 1.Molyneux, R.J., Benson, M., Wong, R.Y., et al.Australine, a novel pyrrolizidine alkaloid glucosidase inhibitor from Castanospermum australJ. Nat. Prod.51(6)1198-1206(1988) 2.Tropea, J.E., Molyneux, R.J., Kaushal, G.P., et al.Australine, a pyrrolizidine alkaloid that inhibits amyloglucosidase and glycoprotein processingBiochemistry28(5)2027-2034(1989) 3.Kato, A., Kano, E., Adachi, I., et al.Australine and related alkaloids: easy structural confirmation by 13C NMR spectral data and biological activitiesTetrahedron Asymmetry14(3)325-331(2003)

Deoxynojirimycin (dNM) tetrabenzyl ether is an intermediate for the synthesis of glucosylceramide synthase inhibitors such as 1-dNM, a glucose analog that potently inhibits α-glucosidase I and II.

EB-0150 is a potent inhibitor of ER α-glucosidase (α-Glu) I (IC50: 0.73 μM) and (α-Glu) II (IC50: 0.0337 μM), and is an N-substituted valerian derivative with broad-spectrum antiviral effects, holding potential for broad-spectrum drug discovery against existing and emerging viruses and for research.

EB-0156, an N-substituted valerian derivative, is a potent inhibitor of ER α-glucosidase (α-Glu) I and II with IC50 values of 0.0479 and <0.001 μM, respectively, exhibiting broad-spectrum antiviral activity and potential for drug discovery against existing and emerging viruses.

EB-0176 is an N-substituted valerian derivative that exhibits broad-spectrum antiviral activity and is a potent ER α-glucosidase (α-Glu) I and II inhibitor with IC50s of 0.6439 and 0.0011 μM, respectively.EB-0176 exhibits investigational potential as a broad-spectrum drug against existing and emerging viruses.

PBI-6DNJ, an orally active and potent multivalent glycosidase inhibitor, demonstrates significant inhibition activity against α-glucosidase from mice, featuring a K i value of 0.14 μM. It also exhibits notable hypoglycemic activity, making it suitable for type 2 diabetes research [1].

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

1-Deoxynojirimycin, a potent glucose analog, inhibits α-glucosidase I and II effectively. Its derivative, N-5-Carboxypentyl-1-deoxynojirimycin, serves as a ligand for glucosidase I and II purification, utilizing carboxypentyl groups for affinity chromatography resin linkage. Furthermore, N-5-Carboxypentyl-1-deoxynojirimycin demonstrates comparable or superior inhibition of glucosidase compared to 1-deoxynojirimycin, with inhibition constants (Ki) of 0.45 µM and 2.1 µM, respectively, for pig liver glucosidase I.

α-Glucosidase-IN-63 (Compound 4d) serves as an α-Glucosidase inhibitor with an IC 50 value of 0.44 μM. Additionally, it exhibits inhibitory activity against hCA II, demonstrating a K i of 7.0 nM. The compound is also effective when administered orally. [1]

Tangshenoside I is a natural product isolated from Codonopsis pilosula, which may be related to the its hematopoietic and immune functions and has a weak α-glucosidase inhibitory activity.