glucose oxidation

Glymidine sodium is a sulfonamide hypoglycemic agent which stimulates insulin secretion.

ZLY06 is a dual agonist of peroxisome proliferator-activated receptors (PPAR) δ and γ with oral activity (PPAR δ: EC50=341 nM; PPARγ: EC50=237 nM). It mediates the upregulation of CD36 and induces hepatic lipid accumulation by inhibiting the phosphorylation of AKT1. Moreover, ZLY06 significantly improves glucose and lipid metabolism without increasing body weight, primarily by enhancing the β-oxidation of fatty acids and reducing hepatic lipid synthesis, thereby alleviating fatty liver disease.

LY 377604 is an innovative compound functioning as a mixed β3-adrenergic receptor agonist and β1 β2-adrenergic receptor antagonist, showing potential for antidiabetic and anti-obesity effects. In rodent models, LY 377604 has been found to enhance energy expenditure and fat oxidation, reduce blood glucose levels, and induce weight loss while preserving lean body mass. A phase II clinical trial for obesity has been conducted in the United States.

UX4O is an allosteric inhibitor of UDP-glucose dehydrogenase (UGDH). The human UGDH (hUGDH) is a hexamer that catalyzes the oxidation of UDP-glucose to UDP-glucuronic acid. It exists in an active (E) state and an inactive (EΩ) state, which requires binding with the allosteric inhibitor UDP-xylose (UDP-Xyl) to stabilize the inactive form. UX4O may also serve as a physiologically relevant inhibitor of bacterial allosteric UGDH that does not produce UDP-Xyl.

Trimetazidine, an anti-ischemic (anti-anginal) metabolic agent, could improve myocardial glucose utilization through inhibition of long-chain 3-ketoacyl CoA thiolase activity and results in a reduction in fatty acid oxidation and a stimulation of glucose

SB 452533 is an antagonist of the vanilloid receptor 1(pKb: 7.8).

Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism. Pharmacologies of PPARδ receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys. CAY10592 is a full PPARδ agonist (EC50 = 30 nM) in a fatty acid oxidation assay of rat L6 muscle cells with desirable oral pharmacokinetic properties. In a transactivation assay using human PPAR receptors, CAY10592 acts as a selective partial PPARδ agonist (EC50 = 53 nM) with no effect on PPARα or PPARγ activity up to 30 μM. Chronic treatment of high fat fed ApoB100/CETP-transgenic mice with CAY10592 at a dose of 20 mg/kg increases HDL levels, decreases LDL and TG levels, and improves insulin sensitivity.

Dichloroacetate (DCA) is an inhibitor of all pyruvate dehydrogenase kinase (PDHK) isoforms, which are enzymes that phosphorylate and inhibit PDH in mitochondria. Inhibition of PDHK shifts cell metabolism from glycolysis to mitochondrial glucose oxidation, an effect that has relevance to cancer, type 2 diabetes, and other diseases. CAY10703 is a DCA trimer that is at least 10-fold more cytotoxic against leukemia cell lines than DCA. It is approximately 3-fold less cytotoxic than DCA against peripheral blood mononuclear cells from healthy blood donors. CAY10703 significantly reduces both basal and maximal respiration in leukemia cells. It is stable in vivo after subcutaneous inoculation, remaining in circulation for more than five hours after injection.

9,10-Dihydroxystearic acid, an oxidation derivative of oleic acid, exhibits beneficial effects on glucose tolerance and insulin sensitivity in KKAy mice.

1. Tiliroside (Tribuloside) shows anticarcinogenic activity. 2. Tiliroside shows hepatoprotective activity. 3. Tiliroside shows antioxidant and anti-inflammatory activity, can inhibit neuroinflammation in neurodegenerative disorders. 4. Tiliroside has anti-diabetic effect, are at least partially mediated through inhibitory effects on carbohydrate digestion and glucose uptake in the gastrointestinal tract. 5. Tiliroside and gnaphaliin are antioxidants against in vitro Cu(2+)-induced LDL oxidation in the same order of magnitude compared to that of the reference drug, probucol. 6. Tiliroside enhances fatty acid oxidation via the enhancement adiponectin signaling associated with the activation of both AMP-activated protein kinase and peroxisome proliferator-activated receptor α and ameliorates obesity-induced metabolic disorders.

Gliclazide-d4 is intended for use as an internal standard for the quantification of gliclazide by GC- or LC-MS. Gliclazide is a sulfonylurea and an inhibitor of pancreatic β-cell ATP-sensitive potassium (KATP) channels. It is selective for pancreatic β-cell over cardiac and arterial smooth muscle cell KATP channels. Gliclazide (5 μM) increases insulin-induced glucose uptake and glucose transporter 4 (GLUT4) translocation to the plasma membrane in a differentiated 3T3L1 adipocyte model of insulin resistance induced by hydrogen peroxide. Gliclazide (5 and 10 μg ml) reduces LDL oxidation by human aortic smooth muscle cells (HASMCs), decreasing TBARS content and 8-isoprostane levels. It also decreases oxidized LDL-induced HASMC proliferation and monocyte adhesion when used at concentrations ranging from 1 to 10 μg ml. Gliclazide (5 mg kg) reduces serum glucose levels and increases glucose uptake by isolated rat hindquarters in a model of diabetes induced by streptozotocin (STZ).

Glucose dehydrogenase (GDH) is an oxidoreductase enzyme that facilitates the oxidation of β-D-glucose into β-D-glucono-1,5-lactone, while concurrently reducing cofactor NADP+ to NADPH, and to a lesser degree, NAD+ to NADH. It can utilize both NAD+ and NADP+ as cofactors and serves in the regeneration of NADH and NADPH [1] [2].

Dityrosine, an oxidation product of protein formed through the intermolecular cross-linking of tyrosyl radicals from the reactive oxygen species (ROS) and tyrosine interaction, is associated with decreased hippocampal expression of NMDA receptor subunits Nr1, Nr2a, and Nr2b when administered intragastrically at 320 µg kg per day, leading to memory impairments in mice as evidenced by their performance in a novel object recognition test. Additionally, it raises fasting blood glucose levels while reducing plasma insulin levels and the pancreatic expression of insulin synthesis-related genes Ins2, Pdx1, and MafA. Increased dityrosine levels have been positively linked to a range of diseases, including autism spectrum disorder, cataracts, Alzheimer's disease, Parkinson's disease, atherosclerosis, and cystic fibrosis.

3-Aminoisobutyric acid, a non-protein amino acid resultant from thymine catabolism, plays a significant role in metabolic activities. At a 5 µM concentration, it triggers browning in primary adipocytes, notably elevating uncoupling protein 1 (UCP-1) and CIDEA expression. Additionally, it boosts PPARα expression in both primary adipocytes and mouse inguinal white adipose tissue (WAT) in vivo, alongside enhancing β-oxidation in hepatocytes. Its plasma levels surge post-exercise in mice, and its administration at 100 mg/kg daily curtails weight gain and body fat without diminishing food consumption or hiking energy output, whilst ameliorating glucose tolerance. Notably, 3-aminoisobutyric acid concentrations are heightened in individuals with β-ureidopropionase deficiency, a genetic flaw impairing pyrimidine degradation, affecting plasma, urine, and cerebrospinal fluid.

Ninerafaxstat hifts cellular metabolism from fatty acid oxidation to glucose oxidation.Ninerafaxstat decreases fatty acid oxidation and improve overall mitochondrial respiration.Ninerafaxstat inhibit the growth and proliferation of cancer cells [1].

Ninerafaxstat trihydrochloride shifts cellular metabolism to glucose oxidation from fatty acid oxidation. Ninerafaxstat trihydrochloride improves overall mitochondrial respiration and reduces fatty acid oxidation, thereby inhibiting the proliferation and growth of cancer cells.

4-Oxododecanedioic acid is an organic acid containing a ketone group that can be used in studies related to organic synthesis and fatty acid metabolism. Studies related to its structural analog dodecanedioic acid have found that intake of long-chain dicarboxylic acid increases beta-oxidation of fatty acids, decreases body fat accumulation, and improves glucose tolerance.

2-Amino-3-carboxy-1,4-naphthoquinone is an electron transfer mediator that can alter glucose metabolism in homofermentative lactic acid bacteria. It also serves as a novel growth stimulator for bifidobacteria, influencing their end-product profile through the mediated oxidation of NAD(P)H.

Selaginellin has a neuroprotective effect against L-glutamate-induced neurotoxicity through mechanisms related to anti-oxidation and anti-apoptosis via scavenging reactive oxygen species and up-regulating the expression of klotho gene. Selaginellin shows