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Ethacrynic Acid (ethacrynic + acid)

Distribution by Scientific Domains
Chemistry50%

Selected Abstracts

Rat Liver Microsomal Lipid Peroxidation Produced during the Oxidative Metabolism of Ethacrynic Acid

BASIC AND CLINICAL PHARMACOLOGY & TOXICOLOGY, Issue 4 2001
Kyoko Yamamoto
Two oxidative metabolites of ethacrynic acid with dicarboxylic acid and hydroxylated ethyl group, respectively, were formed in the reaction mixture. The oxidative metabolism of ethacrynic acid was inhibited by cytochrome P450 inhibitors. The formation of TBARS was remarkably depressed by inhibitors like diethyldithiocarbamate and disulfiram. These results indicate that lipid peroxidation occurred in rat liver microsomes through the oxidative metabolism of ethacrynic acid. [source]

Purification and characterization of a glutathione S -transferase from the fungus Cunninghamella elegans

FEMS MICROBIOLOGY LETTERS, Issue 2 2001
Chang-Jun Cha
Abstract Cunninghamella elegans grown on Sabouraud dextrose broth had glutathione S -transferase (GST) activity. The enzyme was purified 172-fold from the cytosolic fraction (120,000×g) of the extract from a culture of C. elegans, using Q-Sepharose ion exchange chromatography and glutathione affinity chromatography. The GST showed activity against 1-chloro-2,4-dinitrobenzene, 1,2-dichloro-4-nitrobenzene, 4-nitrobenzyl chloride, and ethacrynic acid. Sodium dodecyl sulfate,polyacrylamide gel electrophoresis gel filtration chromatography revealed that the native enzyme was homodimeric with a subunit of Mr 27,000. Comparison by Western blot analysis implied that this fungal GST had no relationship with mammalian ,-, ,-, and ,-class GSTs, although it showed a small degree of cross-reactivity with a ,-class GST. The N-terminal amino acid sequence of the purified enzyme showed no significant homology with other known GSTs. [source]

Indirect laser-induced fluorescence detection of diuretics separated by capillary electrophoresis

JOURNAL OF SEPARATION SCIENCE, JSS, Issue 5 2006
Xiuhan Yang
Abstract Indirect LIF detection was applied to the detection of four acidic diuretics separated by CZE. Semiconductor laser was employed to provide the stable excitation of 473 nm. With an optimized electrophoretic buffer system which contained 5 mM of triethylamine, 0.1 ,M of fluorescein, and 5% of n -butanol, fast separation of four diuretics (ethacrynic acid, chlorthalidone, bendroflumethiazide, and bumetanide) can be performed within 3 min with the detection limits of 0.2,2 ,g/mL. The impacts of buffer components including the concentrations of the electrolytes, fluorescence probe, and the organic additives were demonstrated. The method was applied for the detection of diuretics in urine. As an alternative way for the fast analysis of diuretics, this indirect detection method provided the technical support for future microchip performances, in which diuretics may be detected in the microchip by the common LIF detector without derivatization. [source]

Purification and partial characterization of glutathione S -transferase from insecticide-resistant field populations of Liposcelis paeta Pearman (Psocoptera: Liposcelididae)

ARCHIVES OF INSECT BIOCHEMISTRY AND PHYSIOLOGY (ELECTRONIC), Issue 2 2009
Shuang Wu
Abstract Enzymes that possess glutathione S-transferase (GST) activity were purified to homogeneity by glutathione-agarose affinity chromatography from three field populations of Liposcelis paeta (Pearman). These populations were collected from Nanyang city of Henan Province (NY), Wuzhou (WZ) and Hezhou (HZ) cities of Guangxi Province, China, and had different susceptibilities to dichlorvos [LC50s of the NY (281.48,mg/m2), the WZ (285.07,mg/m2), and the HZ (243.52,mg/m2), respectively]. The specific activities of purified enzymes from these three populations increased 32.24-, 99.81-, and 42.52-fold, respectively. Kinetic analyses showed that the catalytic activity of purified GST from NY population towards GSH was much higher than the others, while WZ population reached the highest in V. SDS,polyacrylamide electrophoresis revealed that the purified GST had two subunits with a molecular mass of 23.31 and 20.43,kDa for NY, 53.14 and 20.13,kDa for WZ, and 50.79 and 19.42,kDa for HZ, respectively. The in vitro inhibition studies of GSTs indicated that three kinds of insecticides (chlorpyrifos, carbosulfan, and cypermethrin) and five metallic ions (Zn2+, Ba2+, Ca2+, Hg2+, Mn2+, and Mg2+) all possessed inhibitory effects on purified GST, and ethacrynic acid (EA, a specific inhibitor of GST) expressed inhibitory effects. In the bioassay, three populations of L. paeta had different susceptibilities to different insecticides, even after they were reared on diets consisting of 25% EA. The GST activities of L. paeta from different areas also showed different temperature and pH stabilities. The differences in GST among the three populations may be attributed partially to the differences in control practices for psocids between Henan and Guangxi Provinces. © 2009 Wiley Periodicals, Inc. [source]

Rat Liver Microsomal Lipid Peroxidation Produced during the Oxidative Metabolism of Ethacrynic Acid

BASIC AND CLINICAL PHARMACOLOGY & TOXICOLOGY, Issue 4 2001
Kyoko Yamamoto
Two oxidative metabolites of ethacrynic acid with dicarboxylic acid and hydroxylated ethyl group, respectively, were formed in the reaction mixture. The oxidative metabolism of ethacrynic acid was inhibited by cytochrome P450 inhibitors. The formation of TBARS was remarkably depressed by inhibitors like diethyldithiocarbamate and disulfiram. These results indicate that lipid peroxidation occurred in rat liver microsomes through the oxidative metabolism of ethacrynic acid. [source]

Organometallic Ruthenium Inhibitors of Glutathione- S -Transferase P1-1 as Anticancer Drugs

CHEMMEDCHEM, Issue 12 2007
Han Ang Dr.
Abstract Ruthenium,arene complexes conjugated to ethacrynic acid were prepared as part of a strategy to develop novel glutathione- S -transferase (GST) inhibitors with alternate modes of activity through the organometallic fragment, ultimately to provide targeted ruthenium-based anticancer drugs. Enzyme kinetics and electrospray mass spectrometry experiments using GST P1-1 and its cysteine-modified mutant forms revealed that the complexes are effective enzyme inhibitors, but they also rapidly inactivate the enzyme by covalent binding at Cys,47 and, to a lesser extent, Cys,101. They are highly effective against the GST Pi-positive A2780 and A2780cisR ovarian carcinoma cell lines, are among the most effective ruthenium complexes reported so far, and target ubiquitous GST Pi overexpressed in many cancers. [source]