Diseases triggered by an abnormally high level of cortisol (hypercortisolism), such as the Cushing's and metabolic syndromes, could be successfully tackled by inhibitors of CYP11B1, a steroidal cytochrome P450 enzyme that catalyzes the last hydroxylation step of the cortisol biosynthesis. S...
We investigated to compare species differences in amitriptyline (AMI) metabolism among mouse, rat, dog, and human liver microsomes. We developed a method for simultaneous determination of metabolic stability and metabolite profiling using predictive multiple reaction monitoring information-depen...
Cediranib (4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-[3-(1-pyrrolidinyl)propoxy]quinazoline; RECENTIN™), a vascular endothelial growth factor (VEGF) tyrosine kinase inhibitor (TKI) of all three VEGF receptors, is currently in Phase III clinical trials for the first-line treatment of c...
Nicotine is considered to be a specific substrate for UGT2B10, an isoform of human uridine diphosphate glucuronosyltransferase (UGT). In the present study, a sensitive and selective liquid chromatography/tandem mass spectrometry (LC–MS–MS) method for quantification of nicotine N-glucuronide in...
The dithiocarbamate analogs, N-benzyl-N-dithiocarboxy-D-glucamine (BDCG) and N-cyclohexyl-N-(2-hydroxy-3-sulfonatopropyl) dithiocarbamate (CAPSO-DTC), were evaluated as cadmium (Cd) antagonists in mice which had received repetitive injections of Cd to effect accumulation of substantial levels of...
Degradation of the acid red 97 dye using wet oxidation, by different oxidants, and electro-Fenton systems was investigated in this study. The oxidation effect of different oxidants such as molecular oxygen, periodate, persulfate, bromate, and hydrogen peroxide in wet oxidation system was compare...
Heat shock protein 90 (Hsp90) is an attractive chemotherapeutic target for antitumor drug development. Herein, we reported the design and synthesis of two series of novel N-(5-chloro-2,4-dihydroxybenzoyl)-1,2,3,4-tetrahydroisoquinoline-3- carboxamides as Hsp90 inhibitors using (S)-Tic (1,2,3,4-t...
A direct synthesis of enantiomerically pure (2S,4S,5R)-4,5,6-trihydroxynorleucine (1) from a carbohydrate precursor (D-glucosamine), is described. D-glucosamine was oxidized to 2-amino-2-deoxy-D-gluconic acid (2), which was converted into the 2-acylamido-hex-2-enono-1,4-(3, 4) and 1,5-lactone (5...
Osthol, [7-Methoxy-8-(3-metrhylbut-2-enyl)-2-chromenone], a simple Coumarin (Mol. Formula = C15H16O3), was isolated from petroleum ether extract of the root parts of the plant Prangos pabularia. The compound was characterized by MS, 1H NMR, 13C NMR, IR, X-ray diffraction (XRD), scanning electron...
BackgroundThe previous studies in a group of 4-arylpiperazinylalkyl derivatives of purine-2,6-dione and several other heterocyclic systems revealed their analgesic properties. In an effort to establish new analgesic agents we designed and synthesized a series of new 8-methoxy-1,3-dimethyl-2,6-di...
A series of laboratory experiments were conducted to study emissions of hexabromocyclododecane (HBCDD) into aqueous leaching fluid under simulated landfill conditions. Expanded (EPS) and extruded (XPS) polystyrene building insulation foam samples containing HBCDD were contacted with deionised Mi...
The concentrations of α-, β-, and γ-hexabromocyclododecane (HBCDD) diastereomers in atmospheric particle phase samples were determined at four United States Integrated Atmospheric Deposition Network (IADN) sites located in the North American Great Lakes basin collected between 1 January and 3...
The aim of the current study was to describe the fate of ingested α-hexabromocyclododecane (α-HBCDD) in fast-growing (FG) and slow-growing (SG) broilers, through an exposure to a dietary concentration of 50 ng α-HBCDD g−1 feed during 42 and 84 days, respectively. Depuration parameters were as...
A LC-ESI(−)-HRMS method dedicated to the analysis of 6 HBCDD enantiomers at trace levels in animal matrices was developed, using a cellulose based stationary phase with a particle size of 2.5 μm. This method was applied to a sample set derived from a kinetic study of α-HBCDD previously conduct...
Hexabromocyclododecanes (HBCDs) are flame retardants and emerging persistent organic pollutants. In the present study, α-, β-, and γ-HBCDs were measured in several fish species from rivers and an electronic waste (e-waste) recycling site in Pearl River Delta, South China. The concentrations o...
Human biomonitoring is a reliable method for evaluating human exposure to specific contaminants. Although blood is an ideal matrix for monitoring purposes, it is regarded as an invasive matrix. Therefore, current developments in the field of human biomonitoring are based on introducing new metho...
In vitro biotransformation of HBCDs by maize cytochrome P450 (CYP) enzymes, responses of CYPs to HBCDs at protein and transcription levels, and in silico simulation of interactions between CYPs and HBCDs were investigated in order to elucidate the roles of CYPs in the metabolism of HBCDs in maiz...
The new persistent organic pollutant (POP), 1,2,5,6,9,10-hexabromocyclododecane (HBCD), has been widely detected in various environmental media and proved to be biotoxic. However, the research on catalytic degradation of HBCD is in its infancy. Herein, we examined the degradation of α-HBCD, β-...
Hexabromocyclododecane (HBCD), a commonly used flame retardant, causes public concern due to its potential negative effects on organisms. Microplastics are suspected to contain certain amounts of HBCD. Wastewater treatment plants (WWTPs) are believed to be one of the largest sources of microplas...
Hexabromocyclododecanes (HBCDs) are the second-most widely used brominated flame retardants. They cause inappropriate antidiuretic hormone syndrome and can induce cancer. However, little information is available about bacterial degradation of HBCDs. In this study, HBCDs (α-, β- and γ-HBCD) de...
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