Amylases Inhibitor

Sekikaic acid is an α-glucosidase (Glucosidase) and α-amylase (Amylases) inhibitor with hypolipidemic, antioxidant and antidiabetic activities. Sekikaic acid significantly reduces LDL, total cholesterol, and total glyceride levels and causes pancreatic beta cell regeneration.

α-Amylase-IN-12 (Compound 5e) is an α-amylase inhibitor (IC₅₀: 0.15 mM) with a mixed inhibition. α-Amylase-IN-12 has an IC₅₀ of 9.40 mM against α-glucosidase. α-Amylase-IN-12 promotes glucose uptake in yeast cells and exhibits significant antiglycation activity at high concentrations. α-Amylase-IN-12 can be used for the research of diabetes.

Onjisaponin R is an α-amylase inhibitor. Onjisaponin R can be used in diabetes research.

α-Amylase/α-Glucosidase-IN-21 (Compound 4) is a dual-functional inhibitor of α-Glucosidase and α-Amylase with IC₅₀s of 0.27 and  0.19 µg/mL for α-Glucosidase and α-Amylase, respectively. α-Amylase/α-Glucosidase-IN-21 has an antidiabetic activity.α-Amylase/α-Glucosidase-IN-21 can be used for diabetes mellitus research.

2,7"-Phloroglucinol-6,6'-bieckol is an orally active dual α-amylase/α-glucosidase inhibitor with IC₅₀ values of 6.94 μM and 23.35 μM respectively. 2,7"-Phloroglucinol-6, 6'-bieckol alleviates postprandial hyperglycemia in diabetic mice. 2,7"-Phloroglucinol-6,6'-bieckol can be used in diabetes research.

α-Amylase/α-Glucosidase-IN-22 is an inhibitor of α-Amylase and α-Glucosidase with IC₅₀ values of 1.71 and 10.36 nM (5 and 23.8 folds more potent than Acarbose (HY-B0089)). α-Amylase/α-Glucosidase-IN-22 can be used for the researches of metabolic disease, such as diabetes.

α-glucosidase/PTP1B-IN-1 (compound 8a) is a potent α-glucosidase and PTP1B inhibitor with an IC₅₀ value of 66.3 μM and 47.0 μM, respectively. α-glucosidase/PTP1B-IN-1 exhibits excellent activities against α-amylase with an IC₅₀ of 30.62 μM. α-glucosidase/PTP1B-IN-1 can dock into the active pockets of α-glucosidase and PTP1B. α-glucosidase/PTP1B-IN-1 has potential to reduce the postprandial blood glucose and is used for Type 2 diabetes mellitus.

α-Amylase/α-Glucosidase-IN-7 (Compound 3f) is a competitive α-glucosidase and α-amylase enzyme inhibitor with IC₅₀ values of 18.52 and 20.25 µM, respectively. α-Amylase/α-Glucosidase-IN-7 can also effectively inhibit AChE and BChE, with IC₅₀ values of 9.25 and 10.06 µM respectively. α-Amylase/α-Glucosidase-IN-7 can be used in diabetes and Alzheimer’s research.

α-Amylase/α-Glucosidase-IN-8 (Compound 7p) is a potent dual inhibitor of α-amylase and α-glucosidase, with IC₅₀s of 10.19 and 10.33 μM, respectively. α-Amylase/α-Glucosidase-IN-8 has good anti-oxidant activity(IC₅₀ = 14.93 μM). α-Amylase/α-Glucosidase-IN-8 can be used for the research of diabetes.

HPA-IN-1 (Compound 1) is a potent and selective human pancreatic α-amylase (HPA) inhibitor with IC₅₀ values of 12.0 μM and 410.4 μM against HPA and α-glucosidase, respectively.

Quercetin 3-(6″-caffeoylsophoroside) is an orally active α-amylase inhibitor, with an IC₅₀ of 73.66 μg/mL. Quercetin 3-(6″-caffeoylsophoroside) presents in thehydro-methanolic extract of Cardamine hirsuta Linn. Quercetin 3-(6″-caffeoylsophoroside) shows the antidiabetic activities by oxidative stress reduction and α-amylase inhibition. Quercetin 3-(6″-caffeoylsophoroside) can be used for diabetes mellitus research.

3,4,6-Tri-O-galloyl-D-glucose (3,4,6-Trigalloylglucose) is an α-amylase (porcine α-amylase IC₅₀ = 334.6 μM; K_i = 307.5 μM) and α-glucosidase (yeast α-glucosidase IC₅₀ = 46.5 μM; K_i = 39.9 μM) mixed type inhibitor. 3,4,6-Tri-O-galloyl-D-glucose exhibits free radical scavenging ability, ferric-reducing power, and antioxidant activity. 3,4,6-Tri-O-galloyl-D-glucose can be used for the research of diabetes.

α-Amylase/α-Glucosidase-IN-3 (Compound 17) is an α-Amylase/α-Glucosidase dual inhibitor, with IC₅₀s of 0.70 μM and 1.10 μM. α-Amylase/α-Glucosidase-IN-3 can be used for research of type-II diabetes mellitus.

Antidiabetic agent 5 (compound S1) is a antidiabetic agent. Antidiabetic agent 5 inhibits the activity of α-glucosidase and α-amylase with IC₅₀ values of 3.91，8.89 μM，respectively. Antidiabetic agent 5 decreases sugar levels. Antidiabetic agent 5 has the potential for the research of type-II diabetes.

Dendromoniliside D is a sesquiterpene glycoside. Dendromoniliside D can be isolated from D. nobile. Dendromoniliside D inhibits α-amylase. Dendromoniliside D can be used in the research of liver cancer, lung cancer, and breast cancer.

α-Amylase-IN-13 is an orally active, selective, brain-penetrant α-amylase inhibitor (IC₅₀ = 0.71 μM). α-Amylase-IN-13 inhibits α-amylase through a mixed type of inhibition mechanism. α-Amylase-IN-13 leads to a significant reduction in blood glucose level in diabetic rats. α-Amylase-IN-13 causes significant histopathological improvements in the kidney, liver, and pancreas. α-Amylase-IN-13 can be used for the study of diabetic complications.

4',5-Dihydroxy-3,3',7,8-tetramethoxyflavone is a 3-methoxyflavonoid compound. 4',5-Dihydroxy-3,3',7,8-tetramethoxyflavone inhibits α-Amylase.

Vulgarin is an orally active, naturally occurring eudesmane sesquiterpene with multiple biological activities including anti-inflammatory and antioxidant properties. Vulgarin targets and inhibits HMGB1, NF-κB and iNOS, while regulating key genes involved in hepatic gluconeogenesis; it also blocks inflammatory signaling pathways and inhibits the production and release of pro-inflammatory cytokines such as TNF-α and IL-1β. Vulgarin effectively alleviates pancreatic oxidative stress by reducing lipid peroxidation levels and restoring antioxidant enzyme activity. Vulgarin reverses abnormally elevated serum pancreatic enzyme levels, preserves the integrity of pancreatic acinar cells, and reduces pancreatic edema, hemorrhage and inflammatory infiltration. Vulgarin remodels the function of pancreatic endocrine cells, restores insulin content in β cells, and downregulates glucagon levels in α cells and somatostatin levels in δ cells. Vulgarin can be used in studies related to pancreatic injury and diabetes.

Ladyginoside A is a triterpenoid saponin found in the leaves of Polyscias fruticosa (L.) Harms. Ladyginoside A has inhibitory activities against α-amylase and α-glucosidase, and can regulate carbohydrate metabolism. Ladyginoside A also exhibits potential anti-inflammatory and mast cell stabilizing effects. Ladyginoside A can be used for the researches of inflammation and metabolic disease, such as diabetes.

α Amylase-IN-1 (Compound 11) is an α-Amylase inhibitor with an IC₅₀ value of 0.5509 μM. α Amylase-IN-1 has antioxidant activity with an IC₅₀ value of 53.49 μM for scavenging DPPH free radicals. IC₅₀ can be used in the study of diabetes and oxidative stress-related diseases.