Search results for "Pyrene"
showing 10 items of 260 documents
Stable Expression of Heterologous Microsomal Epoxide Hydrolase in BHK21 Cells: Influence on the Mutagenicity of Benzo[a]pyrene 4,5-Oxide
1992
Most environmental mutagens and carcinogens require metabolic activation to electro- philic intermediates capable of reacting with cellular target structures, such as DNA. These electrophilic intermediates are in addition subject to metabolic detoxification. This metabolism is mainly controlled by enzymes whose expression is very variable. Among other things, various enzymes are inducible by environmental chemicals. Understanding the toxicology of chemicals (for example, species differences, idiosyncrasias, organotropisms) therefore requires knowledge of critical host factors. One approach towards this goal involves the use of purified enzymes in metabolism and toxicological studies (Glatt …
Dihydrodiol Dehydrogenase: An Important Enzyme in Dihydrodiol-Epoxide Pathway — Mediated Benzo(A)Pyrene Mutagenicity
1978
Benzo(a)pyrene is metabolized to two major groups of mutagenically reactive metabolites: Monofunctional epoxides and dihydrodiol-epoxides. Various monooxygenase forms catalyze the various pathways at very different rates. In metabolic situations where the contribution by dihydrodiol-epoxides is small, epoxide hydratase represents a very efficient protective system. However, in situations where the mutagenic effect is predominately due to dihydrodiol-epoxide, the effect of epoxide hydratase is complicated and weak. We have now obtained evidence that a dihydrodiol dehydrogenase represents an efficient protective system in the latter situation. The enyzme was purified to homogeneity and the pu…
Enzymes as Regulators of Toxic Reactions by Electrophilic Metabolites
1979
Conversion of many compounds which are not electrophilically reactive as such to metabolites responsible for cytotoxic, mutagenic and/or carcinogenic effects is catalyzed by mammalian enzymes. Many reactive agents, whether metabolites or parent compounds, are also subject to inactivation by mammalian enzymes.
DRUG-DRUG INTERACTIONS VIA INHIBITION OF MICROSOMAL ENZYMES INVOLVED IN METABOLISM OF EPOXIDES PRODUCED BY MICROSOMAL MONOOXYGENASE
1977
SUMMARY Benzo(a)pyrene was activated by liver microsomes to mutagens detected by the reversion of histidine dependent Salmonella typhimurium TA 1537. Using pure epoxide hydratase or epoxide hydratase inhibitors, comparing animal species with high and low epoxide hydratase activity, or inducing monooxygenase activity, it was shown that epoxide hydratase was a critical enzyme for the inactivation of these mutagens. Many clinically used drugs are metabolized to epoxides. Epoxides are not necessarily mutagenic, but since epoxide hydratase has a very low substrate specificity, such epoxides may competitively inhibit the hydration of mutagenic epoxides, as demonstrated in the present study for th…
Individual Differences in DNA Repair Capacities in Man
1987
After metabolic activation of benzo[a]pyrene to the 7,8-dihydrodiol- 9,10-epoxide, this ultimate carcinogen preferentially binds to the exocyclic amino group of guanine. In order to investigate possible interindividual differenes in the capacity of repair of the DNA adducts formed from benzo[a]- pyrene 7,8-dihydrodiol 9,10-epoxide, their persistence in freshly isolated lymphocytes of several donors was studied. The results show a surprisingly large interindividual variation in DNA adduct formation and their persistence in freshly isolated lymphocytes. This range included several individuals with an apparent complete lack of repair capability for these adducts. Compared with controls, smoker…
Fluorescence Probe and Scanning Force Microscopic Studies of Water Soluble Comb-Shaped Copolymers Consisting of a Hydrophobic Poly(p-alkylstyrene) Ma…
2002
Fluorescence Probe and Scanning Force Microscopic Studies of Water Soluble Comb-Shaped Copolymers Consisting of a Hydrophobic Poly( p -alkylstyrene) Main Chainand Hydrophilic Poly(ethylene oxide) Grafted Chains
Effect of Monooxygenase Inducers on the Binding of Benzo-(A)Pyrene Metabolites to Cellular Macromolecules in Perfused Rat Lungs
1978
The irreversible binding of metabolically activated [3H]-benzo(a)pyrene (BP) to cellular macromolecules of isolated perfused rat lungs was studied. Lungs from differently pretreated animals were perfused in situ in a recirculating system without ventilation. BP with a specific activity of 10 mCi/μmol was added to 50 ml perfusion medium containing 40% washed bovine erythrocytes to a final concentration of 1 μM. DNA, RNA and protein fractions were isolated and assayed for irreversibly bound radioactivity.
Species Differences in Enzymes Controlling Reactive Epoxides
1987
Activities of enzymes involved in the metabolic formation and catabolism of epoxides were determined in liver subcellular preparations from 11 mammalian species and various strains of mice. The most conspicuous finding was that the activities of the microsomal epoxide hydrolase were clearly lower in the mouse than in the other species. This invited the working hypothesis that epoxides may be involved in mouse liver carcinogenesis. The carcinogens may be metabolised themselves to reactive epoxides or they may modify the metabolism of epoxides formed from endogenous or other foreign compounds. To examine the former point, phenobarbital, DDT (1,1-bis(p- chlorophenyl)-2,2,2-trichloroethane), li…
1,3-Di(hetero)aryl-7-substituted Pyrenes—An Undiscovered Area of Important Pyrene Derivatives
2019
Despite the pyrene derivatives have been covered extensively by scientists during the last years, many interesting properties and applications of pyrene derivatives have been presented, nowadays there are still areas of pyrenes’ chemistry that need to be fulfilled. Most of the described in literature pyrenes are 1,3,6,8-tetrasubstituted followed by 4,5,9,10-tetrasubstituted, 2,7-, and 1,6-, and 1,8-disubstituted pyrene derivatives. In the case of 1,3-di(hetero)aryl-7-substituted, there are only a few examples of derivatives containing at position 7 - tert-butyl group. In this work, the necessity of synthesis of 1,3-di(hetero)aryl-7-substituted pyrenes is presented based on the results of th…
Three independent channel nanohybrids as fluorescent probes
2015
A properly designed pyrene-capped CdSe/ZnS nanohybrid can act as a three-channel fluorescent sensor due to the independent emission of the pyrene monomer and excimer as well as that of the nanoparticle. As proof of principle, it was tested for a simple and rapid quantification of TNT in the presence of interferents of the same chemical family.