Corticosterone (CORT), the major glucocorticoid in rodents, is secreted from the adrenal gland, affects various organs in the body and regulates energy metabolism as a stress response. Although local steroidogenesis of androgens and estrogens in skeletal muscles has been previously reported, loc...

Individuals continuously confronted with various stresses in modern life generate high levels of cortisol (corticosterone in rodents), the major glucocorticoid secreted by adrenal gland when hypothalamic–pituitary–adrenal axis is activated. Chronic stress can induce constant release of glucoco...

All-cis-2,4,6,8-tetramethyl-2,4,6,8-tetrakis(triphenylsiloxy)cyclotetrasiloxane (4) and syn-1,3,9,11-tetramethyl-5,5,7,7,13,13,15,15-octaphenyltricyclo[9.5.1.13,9]octasiloxane (5) were synthesized by the reaction of cis,trans,cis-[MeSi(NCO)O]4 (1) with Ph3SiOH (2) and [Ph2Si(OH)]2O (3), respecti...

Meclizine (MEC), a histamine H1 antagonist, is used for the treatment of motion sickness and vertigo. In this study, we demonstrate that MEC dose-dependently induced apoptosis in human colon cancer cell lines (COLO 205 and HT 29 cells). Results of a DNA ladder assay revealed that DNA ladders app...

Meclizine is an agonist of human pregnane X receptor (PXR). It increases CYP3A4 mRNA expression, but decreases CYP3A-catalyzed testosterone 6β-hydroxylation in primary cultures of human hepatocytes, as assessed at 24 h after the last dose of meclizine. Therefore, the hypothesis to be tested is ...

To meet energy demands, dorsal root ganglion (DRG) neurons harbor high mitochondrial content, which renders them acutely vulnerable to disruptions of energy homeostasis. While neurons typically rely on mitochondrial energy production and have not been associated with metabolic plasticity, new st...

Dansyl amino acids having a free amino group and an asymmetric carbon atom were examined as a labeling reagent for chiral compounds containing carboxylic moieties to realize enantiomeric separation as well as fluorimetric determination. We tested dansyllysine by reacting it with (+)- and (−)-ibu...

The influence of tetrabutylammonium (TBA) as a hydrophobic charged additive of the mobile phase was investigated in a chromatographic system involving d,l-dansyl amino acids as the test solute enantiomers and immobilized human serum albumin as the chiral stationary phase. By varying the column t...

Protein-imprinted polymers, capable of specific transduction of protein binding events into fluorescent signal change, were designed and synthesized by using dansyl ethylenediamine-conjugated O-acryloyl l-hydroxyproline (Hyp-En-Dans). Human serum albumin (HSA) was used as a model target protein ...

In this paper, a chromatographic system using immobilized ristocetin as chiral stationary phase and vancomycin as chiral mobile phase additive (CMPA) was described in order to investigate the role of the glycopeptide heterodimerization on the retention and enantioselectivity of d,l-tryptophan an...

ABSTRACTProtein aggregation is a major instability that can occur during all stages of protein drug production and development. Protein aggregates may compromise the safety and efficacy of the final protein formulation. In this paper, various new excipients [phenylbutylamino-, benzyl-, and chole...

This work reports that Cu(II) complexes with l-prolinamide were used as chiral additives for the enantioseparations of dansyl amino acids by ligand exchange-capillary electrophoresis. Cu(II) complexes with l-prolinamides are present in the different forms with the change of pH, and responsible f...

The binding of chlorin p6, a model photosensitizer for photodynamic therapy (PDT), to the Sudlow’s site II of Human Serum Albumin (HSA) has been monitored by different spectroscopic methods. Displacement of Dansyl-l-Proline (DP) from its conjugate with HSA is manifested in the spectral shift an...

The studied 6-methylene-4-androsten-3-ones proved to be significantly inferior to 6-methylene-4-pregnene-3,20-dione and its 17-acetoxy derivative described in Part I as inhibitors of 4-ene-3-ketosteroid 5α-reductase[1] in vitro. Surprisingly, the 6-methylene derivative of testosterone was only ...

The effects of grinding on the crystallinity of cephalothin sodium, and on the chemical stability of the ground products were investigated by X-ray diffraction, infrared spectra and differential thermal analysis. The X-ray diffraction peaks of all samples decreased after grinding, but the diffra...

Four ester prodrugs derived from the bifunctional alkylating agent chlorambucil, and one of its nitro-derivatives, 3-nitrochlorambucil conjugated to prasterone and pregnenolone, were synthesized and tested for their cytotoxic activity against eight human cell lines, using the standard MTT assay....

The reaction of 4-alkylidene-5(4H)-oxazolones 2a-e with ethyl 3-oxo-4-triphenyphosphoranylidene-butyrate 1 affords dihydrobenzoxazoles 3a-c and the diastereoisomeric 1,3-cyclohexanedione ylides 4a-e and 5a-e. 3a is oxidized to the corresponding benzoxazoles 7a,b with iodine.

Reaction of methyl (triphenylphosphoranylidene)acetate in methanol with primary and secondary amines led to N-methylated derivatives. Similarly this mixture reacted with acids, phenol and phthalimide to afford methyl esters, anisole and N-methylphthalimide respectively. Treatment of ketolactam 2...

Tetronic and tetramic acids react with the cumulated ylide Ph3PCCO to afford 3-[(triphenylphosphoranylidene)acetyl] derivatives 4 and 5. These can be selectively methylated with Meerwein's salt, Me3O+BF4−, either at the 4-O atom of the heterocycle or, in the presence of 1,8-bis(dimethylamin...

Four new coordination polymers, namely, [Co(L)2]n (1) and [Co(L)(tp)0.5]n·nH2O (2), [Zn(L)2]n·0.5nH2O (3) and [Zn(L)(suc)0.5]n·nH2O (4) (HL = 4-(3-carboxyphenyl)-2,6-di(pyrazinyl)pyridine, H2tp = benzene-1,4-dicarboxylic acid, H2suc = succinic acid), were constructed by changing metal ion and...