Amide- and urea-based synthetic anticonvulsants, antihypoxics, and inducers of the hepatic monooxygenase system. IX. Synthesis and search for inducers of the liver cytochrome P-450-dependent monooxygenase system among carbamide-containing heterocyclic compounds

1993 ◽  
Vol 27 (6) ◽  
pp. 401-406 ◽  
Author(s):  
A. A. Bakibaev ◽  
R. R. Akhmedzhanov ◽  
A. Yu. Yagovkin ◽  
T. P. Novozheeva ◽  
V. D. Filimonov ◽  
...  
1988 ◽  
Vol 66 (7) ◽  
pp. 868-872
Author(s):  
Birgit M. Vockentanz ◽  
Bruce B. Virgo

The hepatic monooxygenase system was studied in hypophysectomized female rats infused for 5 days with ovine growth hormone (GH). At 7.5 μg∙h−1 GH decreased the total cytochrome P-450 by 16%; at 10 μg∙h−1 it reduced both cytochrome P-450 (31%) and the activity of ethylmorphine demethylase (31%). GH did not alter the activities of NADPH cytochrome c reductase or aniline hydroxylase. The lower GH dose decreased the amount of fast- and slow-turnover P-450 by 11 and 38%, respectively, while the higher dose decreased both by 49%. The loss of demethylase activity therefore correlates with the loss of fast-tumover P-450. This component is relatively more abundant in the female (fast: slow turnover of 4.3) than the male (fast: slow turnover of 2.5). GH did not affect the half-lives of the P-450 components, suggesting that it decreases their synthesis. The P-450 concentration in microsomes from GH-treated animals did not increase after incubation with hemin, suggesting that in vivo the hormone does not lower P-450 synthesis via depression of heme. Puromycin mimicked the effect of GH and when given with the hormone their effects on the P-450 levels were multiplicative (p < 0.05), suggesting different modes of action and that GH does not decrease P-450 by acting at translation.


Author(s):  
I. Shukurov ◽  
◽  
Ch. Khayrullayev ◽  
M. Gulomova ◽  
F. Umurov

The effect of vitamin E on rat liver cytochrome P-450 in experimental acute pancreatitis (AP) was studied. The animals were divided into 4 groups. The obtained data were compared with the indicators of the 1–st group (intact). During the experiment, the development of AP showed a decrease in the content of cytochrome P450 in the microsomal fraction. The administration of vitamin E to animals of the 4th group led to an increase in the content of cytochrome P-450, strengthening the protection of the liver, the abolition of inhibition of the monooxygenase system of the liver.


2011 ◽  
Vol 10 (5) ◽  
pp. 78-81 ◽  
Author(s):  
T. P. Novozheyeva ◽  
M. I. Smagina ◽  
N. A. Cherevko ◽  
S. N. Fateyeva

Benzobarbital and fluorbenzobarbital as monooxygenase system inductors increase the hepatic cytochrome P-450 level and the content of its isoenzymes 2B6, 2C9, 2Å1, accelerate aminopyrine, 7-ethoxyresorufine, 7-pentoxyresorufine, aniline and androstendione oxidation. Activity of benzobarbital and fluorbenzobarbital as inductors is to a large degree due to the action of their major metabolite — phenobarbital. Benzobarbital and fluorbenzobarbital unlike phenobarbital induce isoenzyme 3A4, responsible for androstendione 16b-OH-hydroxylation. PCN-type induction activity posses also native molecules of benzobarbital and fluorbenzobarbital.


1985 ◽  
Vol 34 (1) ◽  
pp. 85-91 ◽  
Author(s):  
Lothar Kling ◽  
Wolfgang Legrum ◽  
Karl J. Netter

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