α-amylase-in-4

α-Amylase-IN-4 (Compd 10y) exhibits the highest amylase inhibition with an IC50 value of 17.83 ± 0.14 μg mL [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].

1. Ethyl trans-caffeate (Caffeic Acid Ethyl Ester) has anti-inflammatory activity. 2. Ethyl trans-caffeate may as a promising natural compound for future application in chronic liver disease. 3. Ethyl trans-caffeate is a potent chemopreventive compound against skin carcinogenesis caused by solar UV exposure. 4. Ethyl trans-caffeate is the high-resolution structures of representative inhibitors in complex with human pancreatic α-amylase. 5. Ethyl trans-caffeate strongly inhibits neoplastic transformation of JB6 Cl41 cells without toxicity. PI3K, ERK1 2, and p38 kinase activities were suppressed by direct binding with HOEC in vitro.

4 -C18 EGCG is an effective inhibitor of α-amylase and α-glucosidase, with IC50 values of 3.74 μM and 0.81 μM respectively. It inhibits carbohydrate-hydrolyzing enzymes, reducing oxidative stress and inflammation, and demonstrates anti-diabetic activity. Additionally, 4 -C18 EGCG downregulates pro-inflammatory cytokines and exhibits cytotoxicity at 50 μM in primary human peripheral blood mononuclear cells (PBMC), and non-cancerous cell lines 3T3-L1 and HEK 293.

ABCB1-IN-4 (Compound C6z) is an orally active inhibitor of α-amylase and α-glucosidase, with IC50 values of 1.63 μM and 0.14 μM, respectively. It holds potential for diabetes research.

7,4'-Di-O-methylapigenin (4',7-DIMETHOXY-5-HYDROXYFLAVONE) can inhibit α-glucosidase and α-amylase enzymes and enhance 2-NBDG uptake in L6 cells, it has hypolipidemic effect on mouse pre-adipocyte (3T3L1) cell lines.

α-Amylase-IN-3 (Compound 4) is a non-competitive inhibitor of α-Amylase with an IC50 value of 18.04 μM. It exhibits radical scavenging activities with IC50 values of 16.04 μM for DPPH and 16.99 μM for ABTS. α-Amylase-IN-3 demonstrates good protein–ligand interaction characteristics for α-Amylase, and may possess pharmacological activities, such as anti-oxidative and anti-inflammatory properties, contributing to the research of diabetes and oxidative stress-associated diseases[1].

DPP-4-IN-11 (compound 10) is an orally active DPP-4 inhibitor (IC50=2.75 μM) with anti-type 2 diabetes activity. This compound exerts its hypoglycemic effects by inhibiting the activity of α-glucosidase (IC50=3.02 μM) and α-amylase (IC50=3.3 μM).

2-Chloro-4-nitrophenyl-β-D-maltotrioside is a chromogenic substrate employed in bioluminescence and fluorescence assays for the detection of alpha-amylase.