Studies were carried out on the in vitro covalent binding of the carcinogen trichloroethylene (TCE) to liver microsomal preparations and to exogenous DNA. The binding of TCE to liver microsomal proteins of male C57BL/6 x C3H/He F, (hereafter called B6C3F ) hybrid mice, a spe cies and strain susceptible to TCE-induced liver tumorigenesis, was 46% higher than that of [' 'C]TCE to micro somal prot...

Studies were carried out on the in vitro covalent binding of the carcinogen trichloroethylene (TCE) to liver microsomal preparations and to exogenous DNA. The binding of TCE to liver microsomal proteins of male C57BL/6 X C3H/He F1 (hereafter called B6C3F1) hybrid mice, a species and strain susceptible to TCE-induced liver tumorigenesis, was 46% higher than that of [14C]TCE to microsomal protein...

1. This study has examined ketoconazole (KT)-induced hepatotoxicity in vivo and in vitro, using male Sprague-Dawley rats with [(3)H]KT (1.5 micro Ci mg(-1)) at 40 and 90 mg KT kg(-1) doses. Blood and liver samples were collected from 0 to 24 h for alanine aminotransaminase (ALT), glutathione (GSH) and covalent binding analyses. 2. Covalent binding occurred as early as 0.5 h, peaked at 2 h (0.02...

Abstract Temperature and humidity (TH) post‐treatment is a relatively mild way to change the silk fibroin (SF) secondary structure. Here, urease immobilized in SF scaffold (SFS) by TH post‐treatment, effects of annealing on activity are examined. Fourier transform infrared indicates that SFS structure started when annealed at 35 °C with 100% relative for 20 min. The higher temperature, lower tr...

Phenylacetic acid (PAA) represents a substructure of a class of nonsteroidal anti-inflammatory carboxylic acid-containing drugs capable of undergoing metabolic activation in the liver to acylcoenzyme A (CoA)- and/or acyl glucuronide-linked metabolites that are proposed to be associated with the formation of immunogenic, and hence potentially hepatotoxic, drug-protein adducts. Herein, we investi...

Effect of Ascotbate on Covalent Binding of Benzene and Phenol Metabohtes to Isolated Tissue Preparations. SMART, R. C. and ZANNONI, V. G. (1985). Toxicol. Appl. Pharmacol. 77, 334-343. [‘4C]Phenol and [‘4C]benzene are metabolized in the presence of NADPH and hepatic microsomes isolated from phenobarbitalor benzene-pretreated or untreated guinea pigs to intermediates capable of covalently bindin...

This study investigates the inhibitory activities of gossypol, a natural polyphenolic compound from Gossypium spp., against Helicobacter pylori (HP) clinical strains and urease enzyme that plays key role in pathogenesis HP. Gossypol was detected to exhibit bacteriostatic action all HP tested with minimum concentration (MIC) values ranging 3.51 4.14 µg/mL. The activity (HPU) efficiently impeded ...

The hepatotoxicity of the analgesic acetaminophen is believed to be mediated by covalent binding to critical proteins. Radiolabeled 3'-hydroxyacetanilide, a regioisomer of acetaminophen, covalently binds to proteins at levels similar to those of acetaminophen, but without toxicity. Covalent binding has recently been detected by Western blot to a 50-kDa microsomal protein that comigrated with CY...

Covalent inhibition is a reemerging paradigm in kinase drug design, but the roles of inhibitor binding affinity and chemical reactivity in overall potency are not well-understood. To characterize the underlying molecular processes at a microscopic level and determine the appropriate kinetic constants, specialized experimental design and advanced numerical integration of differential equations a...

In this manuscript we report our attempts to determine if 14C-halothane or its metabolites interact with DNA. Three bioactivation systems were used: in vitro microsomal incubations, isolated hepatocytes, and in vivo administration. Even though we used optimal conditions for bioactivation, no significant covalent binding of 14C to DNA was observed. Slight 14C activity above background (6 dpm/0.1...