Inhibition of xenobiotic-degrading hydrolases by organophosphinates. Annual progress report No. 1 Jul 82-1 Jul 83
Technical Report
·
OSTI ID:6884377
Organophosphinate pretreatment agents for chemical warfare defense inhibited carboxylester hydrolase from porcine liver and from rabbit liver. Recovery of rabbit liver monomeric carboxylester hydrolase to at least 30% of its initial activity was observed 48 hr. after inhibition by certain 4-nitrophenyl alkyl(phenyl)phosphinates and analogues. When ranked according to the initial rates at which their phosphinylated enzymes recovered, they were methyl(phenyl)>methyl(2-thienyl)>methyl(2-furyl)>ethyl(phenyl)>di-2-thienyl>diphenyl. Recovery was less than 20% in 96 hr. following inhibition by methyl(naphthyl),di-2-furyl, isopropyl(phenyl), dichloromethyl(phenyl), and bis chloromethyl substituted analogues. High performance liquid chromatography on silica using 10% to 20% 2-propanol in hexane as mobile phase resulted in satisfactory chromatograms for all except the most polar phosphinates. This method was useful in determining purity and decomposition of the compounds. Arylester hydrolase was purified 30-fold from rabbit serum by a sequence of polyethylene glycol fractionation, ion exchange chromatography, ammonium sulfate fractionation, molecular exclusion chromatography and pseudo-affinity chromatography. The partially purified enzyme was activated by 2.5 mM divalent calcium.
- Research Organization:
- Clemson Univ., SC (USA). Dept. of Entomology, Fisheries and Wildlife
- OSTI ID:
- 6884377
- Report Number(s):
- AD-A-139650/6
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
550200 -- Biochemistry
560305* -- Chemicals Metabolism & Toxicology-- Vertebrates-- (-1987)
59 BASIC BIOLOGICAL SCIENCES
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
ANIMALS
BIOCHEMICAL REACTION KINETICS
CARBON-OXYGEN LYASES
CARBOXYLESTERASES
CHOLINESTERASE
CHROMATOGRAPHY
DOMESTIC ANIMALS
ENZYME ACTIVITY
ENZYME INHIBITORS
ENZYMES
ESTERASES
HYDRO-LYASES
HYDROLASES
KINETICS
LIQUID COLUMN CHROMATOGRAPHY
LYASES
MAMMALS
METABOLISM
ORGANIC COMPOUNDS
ORGANIC PHOSPHORUS COMPOUNDS
RABBITS
REACTION KINETICS
SEPARATION PROCESSES
STRUCTURE-ACTIVITY RELATIONSHIPS
SWINE
TOXICITY
VERTEBRATES
560305* -- Chemicals Metabolism & Toxicology-- Vertebrates-- (-1987)
59 BASIC BIOLOGICAL SCIENCES
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
ANIMALS
BIOCHEMICAL REACTION KINETICS
CARBON-OXYGEN LYASES
CARBOXYLESTERASES
CHOLINESTERASE
CHROMATOGRAPHY
DOMESTIC ANIMALS
ENZYME ACTIVITY
ENZYME INHIBITORS
ENZYMES
ESTERASES
HYDRO-LYASES
HYDROLASES
KINETICS
LIQUID COLUMN CHROMATOGRAPHY
LYASES
MAMMALS
METABOLISM
ORGANIC COMPOUNDS
ORGANIC PHOSPHORUS COMPOUNDS
RABBITS
REACTION KINETICS
SEPARATION PROCESSES
STRUCTURE-ACTIVITY RELATIONSHIPS
SWINE
TOXICITY
VERTEBRATES