Amylases Inhibitor

Docosapentaenoic acid (22n-3) is a component of phospholipids. Docosapentaenoic acid 22n-3 has inhibitory activity against α-amylase and α-glucosidase, with IC₅₀s value of 17 μg/mL and 22 μg/mL, respectively. Docosapentaenoic acid 22n-3 increases cell vitality. Docosapentaenoic acid 22n-3 has a weak anti-inflammatory effect.

Dehydrocholic acid (Dehydrocholate) is an orally active hydrocholeretic agent. Dehydrocholic acid modulates Autophagy, reduces serum amylase and lipase levels. Dehydrocholic acid has the effects of promoting choleretic function, protecting the liver, reducing pancreatic damage, and regulating cholesterol metabolism. Dehydrocholic acid can be used in the study of acute biliary pancreatitis and obstructive jaundice.

Rubusoside is a diterpene glycoside that is also a sweetener and solubilizer with anti-angiogenic, anti-cancer, anti-obesity, anti-allergic and anti-asthmatic effects. Rubusoside attenuates airway hyperresponsiveness and reduces inflammatory cells in bronchoalveolar lavage fluid (BALF), reducing OVA (HY-W250978)-induced airway inflammation. Rubusoside also prevents palmitic acid-induced lipotoxicity in pancreatic INS-1 cells, reduces the transport of human glucose transporters GLUT-1 and fructose GLUT-5, and inhibits NF-κB and α-amylase (α-amylase).

α-Amylase/α-Glucosidase-IN-25 is a α-Amylase inhibitor and a competitive α-Glucosidase inhibitor, with an IC₅₀ of 10.89 μM against α-glucosidase and an IC₅₀ of 20.62 μM against α-amylase. α-Amylase/α-Glucosidase-IN-25 limits carbohydrate digestion. α-Amylase/α-Glucosidase-IN-25 can be used in the research of type 2 diabetes.

α-Amylase/α-Glucosidase-IN-24 is a dual inhibitor of α-amylase and α-glucosidase, with IC₅₀ values of 40.18 μg/mL and 31.80 μg/mL, respectively. α-Amylase/α-Glucosidase-IN-24 exhibits weak anti-inflammatory and antioxidant activities, as well as moderate antibacterial activity. α-Amylase/α-Glucosidase-IN-24 can be used for the research of type 2 diabetes.

1-Hydroxyphenazine (Hemipyocyanine; 1-Phenazinol; Hemi-pyocyanin) is an inhibitor for α-Amylase with an IC₅₀ of 3.1 μg/mL. 1-Hydroxyphenazine exhibits anticancer and anti-inflammatory activity against cells A549, 1321N1 and RAW264.7, antifungal and antibacterial activity against strains Candida albicans, Aspergillus fumigatus, Escherichia coli and Xanthomonas campestris.

Quinoline-2-carboxylic acid exhibits antidiabetic activity. Quinoline-2-carboxylic acid can be used as drug intermediate for synthesis of various active compounds.

Dehydrocholic acid (Dehydrocholate) sodium is an orally active hydrocholeretic agent. Dehydrocholic acid sodium modulates Autophagy, reduces serum amylase and lipase levels. Dehydrocholic acid sodium has the effects of promoting choleretic function, protecting the liver, reducing pancreatic damage, and regulating cholesterol metabolism. Dehydrocholic acid sodium can be used in the study of acute biliary pancreatitis and obstructive jaundice.

Chrysin-7-O-glucuronide is a flavonoid found in Scutellaria baicalensis. Chrysin-7-O-glucuronide inhibits α-glucosidase and α-amylase with IC₅₀ values of 612.13 and 980.73 μg/mL. Chrysin-7-O-glucuronide suppresses NF-κB signaling activity. Chrysin-7-O-glucuronide scavenges free radicals, acts as a tight junction protector, and mitigates intestinal mucosal barrier injury. Chrysin-7-O-glucuronide can be used for the research of type 2 diabetes and severe acute pancreatitis-induced intestinal mucosal barrier injury.

2-Hydroxyquinoline is an inhibitor of α-glucosidase and α-amylase with IC₅₀ values of 64.4 µg/mL and 130.5 µg/mL, respectively. 2-Hydroxyquinoline can be used in the study of diabetes.

Gardenia yellow is a competitive inhibitor of α-Amylase (HY-B2193) and α-glucosidase. Gardenia yellow can bind to the catalytic sites of α-Amylase and α-glucosidase, inhibit starch digestion, and significantly increase the contents of resistant starch and slowly digestible starch in starch-based systems. Gardenia yellow reduces the glycemic index and hydrolysis index. Gardenia yellow can be used in diabetes-related research.

2,3,4-Trihydroxybenzoic acid is an α-amylase inhibitor with an IC₅₀ of 17.30 mM against porcine α-amylase. 2,3,4-Trihydroxybenzoic acid increases cellular p21 and p27 protein levels. 2,3,4-Trihydroxybenzoic acid inhibits cancer cell growth and delays starch digestion to suppress postprandial hyperglycemia. 2,3,4-Trihydroxybenzoic acid can be used in research related to colorectal cancer, breast cancer and type 2 diabetes.

Cichoriin is an orally active coumarin glycoside with broad biological activities. Cichoriin exhibits inhibitory activities against α-amylase, α-glucosidase, pancreatic lipase and DPP-IV, with IC₅₀ values of 5.76, 2.94, 16.83 and 9.16 μg/mL, respectively. Cichoriin significantly improves metabolic dysfunction-associated steatohepatitis (MASH) in mice by activating the AMPK signaling pathway. Cichoriin upregulates PPAR-γ in adipose tissue and alleviates obesity and associated cardiorenal injury in rats. Cichoriin blocks monosodium urate crystal-induced activation of the NLRP3 inflammasome and cell pyroptosis by inhibiting P2Y₁₄R (IC₅₀ = 8.47 nM). In silico virtual screening reveals that Cichoriin has a strong binding affinity for SARS-CoV-2.

Lotusine hydroxide is an orally active signaling pathway modulator and enzyme inhibitor, with an IC₅₀ of 30.60 μg/mL against α-amylase and an IC₅₀ of 36.15 μg/mL against α-glucosidase. Lotusine hydroxide inhibits the EGFR-Akt-ERK signaling pathway by reducing the levels of phosphorylated EGFR, Akt and ERK. Lotusine hydroxide induces apoptosis, triggers G₀/G₁ cell cycle arrest and inhibits cancer cell proliferation. Lotusine hydroxide reduces lipid peroxidation and increases the activities of SOD, CAT and GPx. Lotusine hydroxide is applicable to researches related to non-small cell lung cancer, type 2 diabetes and autism spectrum disorder.

Lotusine is an orally active signaling pathway modulator and enzyme inhibitor, with an IC₅₀ of 30.60 μg/mL against α-amylase and an IC₅₀ of 36.15 μg/mL against α-glucosidase. Lotusine inhibits the EGFR-Akt-ERK signaling pathway by reducing the levels of phosphorylated EGFR, Akt and ERK. Lotusine induces apoptosis, triggers G₀/G₁ cell cycle arrest and inhibits cancer cell proliferation. Lotusine reduces lipid peroxidation and increases the activities of SOD, CAT and GPx. Lotusine is applicable to researches related to non-small cell lung cancer, type 2 diabetes and autism spectrum disorder.

α-Amylase-IN-3 (Compound 4) is the inhibitor for α-Amylase, AChE and AChE with IC₅₀s of 18.04 μM, 21.04 μM and 22.2 μM, respectively. α-Amylase-IN-3 exhibits antioxidant activity. α-Amylase-IN-3 can be used in research of diabetes and oxidative stress associated disease.

2,4,6-Triphenylaniline has anti-diabetic activity and can be encapsulated in nano-emulsions (NE) to enhance stability and permeability. The NE loaded with 2,4,6-Triphenylaniline inhibits α-glucosidase and α-amylase.

Garcinoic acid is an orally active anti-inflammatory agent that crosses the blood-brain barrier. Garcinoic acid also enhances efferocytosis and enzyme/receptor regulation, and selectively inhibits human COX-2, porcine α-amylase, Saccharomyces cerevisiae α-glucosidase and human DNA polymerase β (IC₅₀=11 μM), as well as activates human PXR. Garcinoic acid enhances macrophage efferocytosis via receptors such as MerTK and LRP-1, and promotes the production of pro-resolving lipid mediators. Garcinoic acid inhibits NF-κB activation and pro-inflammatory cytokine secretion, interferes with Aβ aggregation, downregulates NLRP3 inflammasome activity, and binds to targets including CD44 and EGFR to inhibit leukemia cell proliferation. The pharmacological activities of Garcinoic acid, such as antioxidant, anti-inflammatory and lipid metabolism-regulating effects, are widely used in studies related to various diseases including atherosclerosis, Alzheimer's disease, type 2 diabetes, inflammatory bowel disease and viral pneumonia.

Quinoline-2-carboxylic acid exhibits antidiabetic activity. Quinoline-2-carboxylic acid can be used as drug intermediate for synthesis of various active compounds.

α-Amylase/α-Glucosidase-IN-10 (compound 5d) is an α-amylase and α-glucosidase inhibitor (IC₅₀: 30.39 μM and 65.1 μM) with potential diabetes inhibitory effects. α-Amylase/α-Glucosidase-IN-10 exhibits high gastrointestinal (GI) absorption in ADMET (Absorption, Distribution, Metabolism, Excretion and Toxicity) prediction. While α-Amylase/α-Glucosidase-IN-10 acts as a substrate for P-gp and does not cross the blood-brain barrier (BBB), there may be a risk of central nervous system side effects.