23 Dysregulation of the protein kinase, glycogen synthase kinase–3 (GSK-3), has been 24 implicated in the development of Type 2 Diabetes Mellitus. GSK-3 protein expression 25 and kinase activity are elevated in diabetes, while selective GSK-3 inhibitors have shown 26 promise as modulators of glucose metabolism and insulin sensitivity. There are two 27 GSK-3 isoforms in mammals, GSK-3α and GSK-3...

During cholestasis, accumulation of conjugated bile acids may occur in the liver and lead to hepatocellular damage. Inspired by our recent development of N-11C-methyl-glycocholic acid—that is, 11C-cholylsarcosine—a tracer for PET of the endogenous glycine conjugate of cholic acid, we report here a radiosynthesis of N-11C-methyltaurine–conjugated bile acids and biodistribution studies in pigs by...

An improved synthesis route for obtaining known brassinosteroid analogues, i.e., methyl 2α,3α-dihydroxy-6-oxo-5α-cholan-24-oate (11), methyl 3α-hydroxy-6-oxo-7-oxa-5α-cholan-24-oate (15) and methyl 3α-hydroxy-6-oxa-7-oxo-5α-cholan-24-oate (16), from hyodeoxycholic acid (4) maintaining the native side chain is described. In the alternative procedure, the di-oxidized product 6, obtained in the ox...

A novel, fast, sensitive and robust method based on ultra-performance liquid chromatography coupled to atmospheric pressure electrospray ionization tandem mass spectrometry (UPLC-ESI-MS/MS) has been developed to separate two Tibolone stereoisomers i.e., 3α-Hydroxy Tibolone and 3β-Hydroxy Tibolone and to quantify 3α-Hydroxy Tibolone using p-toulenesulfonyl isocyanate (PTSI) as a derivatizing rea...

Although aberrant microRNA (miRNA) expression has frequently been observed in inflammatory bowel disease (IBD), its biological functions and targets remain largely unknown. Present study found that miR-19b was significantly downregulated in active Crohn's disease (CD). Using bioinformatics analysis, suppressor of cytokine signalling 3 (SOCS3), a physiological regulator of innate and adaptive im...

Dysregulation of the immune system contributes to the pathogenesis of neuropsychiatric disorders including schizophrenia. Here, we demonstrated that toll-like receptor (TLR)-2, a family of pattern-recognition receptors, is involved in the pathogenesis of schizophrenia-like symptoms. Psychotic symptoms such as hyperlocomotion, anxiolytic-like behaviors, prepulse inhibition deficits, social withd...

Alzheimer’s disease (AD) is a progressive neurodegenerative disorder that has no cure because its etiology still unknown, and main treatment the administration of acetylcholinesterase (AChE) inhibitors. The study mechanism action this family compounds critical for design new more potent specific In work, we molecular basis an uncompetitive inhibitor (compound 1, 2β, 3α-dihydroxy-5α-cholestan-6-...