Search results for "inducer"
showing 8 items of 178 documents
Fermentbestimmungen in Erythrocyten von Kranken mit Porphyria cutanea tarda
1969
In Erythrocyten von 12 Kranken mit Porphyria cutanea tarda konnte eine Aktivitatssteigerung der Enzyme G-6-PDH, 6-PGDH sowie der NADH- und der NADPH-abhangigen Glutathionreduktion festgestellt werden, deren Ursache diskutiert wird.
Dihydrodiol Dehydrogenase: Substrate Specificity, Inducibility and Tissue Distribution
1982
The present study shows that: Dihydrodiol dehydrogenase activity is present in the 100,000 g supernatant fraction of extrahepatic tissues. Dihydrodiol dehydrogenase is able to oxidize the hydroxy group and to reduce the keto group of a number of xenobiotics including quinones derived from polycyclic aromatic hydrocarbons. Dihydrodiol dehydrogenase was not inducible by various substances including hormones, polycyclic aromatic hydrocarbons, substrates of the enzyme and potent inducers of monooxygenases, epoxide hydrolase and glutathione S-transferases. Only in the case of thyroxine was a weak induction with a high dose of the hormone observed.
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.
Retinoid acid and analogs as potent inducers of differentiation and apoptosis. New promising chemopreventive and chemotherapeutic agents in oncology
2001
Abstract In this report we will describe the preparation and the biological activity of a novel class of heterocyclic arotinoids endowed with potent cytotoxic and apoptotic acitivity. Structureactivity relationship studies revealed that the different stereochemistry at the C9 double bond of retinoids seems associated with a different biological activity: potent apoptotic activity for the cis-isomers, whereas differentiating activity for the trans structures. An interesting modified Wittig procedure that allows easily to arotinoids will also be described. The substitution of the alkenyl portion with a more flexible oxymethyl or aminomethyl moiety gave compounds with poor activity, whereas i…
INDUCTION OF CYTOCHROME P-448 BY 3-METHYLCHOLANTHRENE IN THE RAT DURING INHIBITION OF PROTEIN SYNTHESIS IN VIVO
1977
Administration of cycloheximide in vivo during induction of rats with 3-methylcholanthrene prevents the increase in total cytochrome P-450 content usually seen under the influence of the inducer. The population of cytochromes P-450 in the livers of these animals is, however, similar to that in the completely induced animals. Microsomal aryl hydrocarbon hydroxylase activity and biphenyl-2-hydroxylation are enhanced severalfold and biphenyl-4-hydroxylation is enhanced twofold. Monooxygenase activity shows the same pattern of preferential inhibition as in microsomes from animals which had received the inducer only. The affinity of the reduced cytochromes for the ligand metyrapone is considerab…
Cytochrome-P450 phosphorylation as a functional switch
2002
Xenobiotic metabolizing cytochromes P450 (CYP) were shown to be phosphorylated in vitro (using purified protein kinases together with purified CYPs), in intact cells (in V79 cells after transfection of cDNAs coding for individual CYPs, in diagnostic mutants, in hepatocytes), and in whole organisms (rats). CYP phosphorylation is highly isoenzyme selective in that only some CYPs are phosphorylated. Protein kinase A (PKA) was identified as a major catalyst for the phosphorylation of CYPs. The PKA recognition motif Arg-Arg-X-Ser is present in several members of the CYP2 family, but is used by only some of them, most notably by CYP2B1/2B2 and CYP2E1. For CYP2B1 it was shown that a substantial po…
Evidence of autoinduction heterogeneity via expression of the agr system of listeria monocytogenes at the single-cell level
2011
ABSTRACT To investigate if the primary function of the Agr system of Listeria monocytogenes is to monitor cell density, we followed Agr expression in batch cultures, in which the autoinducer concentration was uniform, and in biofilms. Expression was heterogeneous, suggesting that the primary function of Agr is not to monitor population density.
The induction of hepatic microsomal metabolism in rats following acute administration of a mixture of polybrominated biphenyls.
1976
Abstract Firemaster BP6, a mixture of polybrominated biphenyls (PBBs), was administered to female Sprague-Dawley rats (170–180 g) as a single ip injection at 25 and 150 mg/kg. Other animals received phenobarbital (PB), 3-methylcholanthrene (3MC), or PB and 3MC together. Animals were killed at intervals of 12, 24, 48, 192, and 336 hr after treatment with PBBs, or 24 hr after PB, MC, or PB-MC, and various hepatic microsomal parameters were measured. After 150 mg/kg of PBBs, cytochrome P450 concentrations reached a maximum by 48 hr (225% of control), then remained elevated through 336 hr. A similar pattern of induction was observed for epoxide hydratase and aniline hydroxylase activities. In c…