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Biomedical subjects

A Minn

Publications and source records attributed to A Minn.

58 records · Page 4Linked to original sources

Inducibility of rat brain drug-metabolizing enzymes.

Cytochrome P450 from rat brain mitochondrial and microsomal fractions was found to be inducible by 3-methylcholanthrene, both in quantity of enzyme and in activity towards 7-ethoxyresorufin, which is a model substrate for the cytochrome P450 isoform specifically induced by 3-methylcholanthrene. Conversely, a phenobarbital treatment resulted in an induction of the microsomal cytochrome P450 only. On the other hand, the microsomal 1-naphthol-UDP-glucuronosyl transferase and epoxide hydrolase seemed to be non-inducible by 3-methylcholanthrene or by phenobarbital. The toxicological implications of these data are discussed.

Animals↗

Drug metabolizing enzymes in the brain and cerebral microvessels.

Several families of brain parenchyma and microvessel endothelial cell enzymes can metabolize substrates of exogenous origin. This xenobiotic metabolism includes functionalization and conjugation reactions and results in detoxication, but also possibly in the formation of pharmacologically active or neurotoxic products. The brain is partially protected from chemical insults by the physical barrier formed by the cerebral microvasculature of endothelial cells, which prevents the influx of hydrophilic molecules. These cells provide also, as a result of their drug-metabolizing enzyme activities, a metabolic barrier against penetrating lipophilic substances. The involvement of these enzymatic activities in neurotoxic events, probably responsible for neuronal dysfunctioning and/or death, neurodegenerative diseases and normal aging, is discussed.

Animals↗

[Drug conjugation in the brain].

Several drugs and environmental pollutants can cross the blood-brain barrier and reach the brain. This organ possesses an enzymatic equipment able to metabolize xenobiotics, therefore facilitating their elimination and maintaining brain homeostasis. This metabolism may result in the formation of toxic metabolites, which endanger neuronal integrity and may result in neurological disturbances. The main function of the conjugation enzymes present in the brain parenchyma and blood-brain or blood-cerebrospinal fluid interfaces is the detoxification of these reactive molecules, thus protecting the central nervous system. This review presents the main cerebral conjugating enzymes, and shows the interest for the design of new drugs of the knowledge of their activities.

Acetyltransferases↗