Mechanism of biochemical action of substituted 4-methylbenzopyran-2-ones. Part 7: assay and characterization of 7,8-diacetoxy-4-methylcoumarin:protein transacetylase from rat liver microsomes based on the irreversible inhibition of cytosolic glutathione S-Transferase

2000 ◽  
Vol 8 (7) ◽  
pp. 1707-1712 ◽  
Author(s):  
Hanumantharao G Raj ◽  
Virinder S Parmar ◽  
Subhash C Jain ◽  
Ekta Kohli ◽  
Nizamuddin Ahmad ◽  
...  
2000 ◽  
Vol 19 (11) ◽  
pp. 623-631 ◽  
Author(s):  
M A Gyamfi ◽  
N Hokama ◽  
K Oppong-Boachie ◽  
Y Aniya

In this study we examined the effect of the aqueous extract of Thonningia sanguinea (T.S.) on 7-ethoxyresorufin 0- deethylase (EROD, CYPlAl), 7-pentoxyresorufin-dealkylase (PROD, CYP2B1/2), 7-methoxyresorufin 0- demethylase (MROD, CYP1A2), aniline hydroxylase (aniline, CYP2E1), p-nitrophenol hydroxylase (PNPH, CYP2E1) and erythromycin N-demethylase (ERDM, CYP3A1) in rat liver in vitro and in vivo. Although T.S. extract increased ERDM activity in induced rat liver microsomes, it showed a dose-dependent inhibitory effectin vitro on other P450 monooxygenase activities particularly EROD and PROD, which are mediated primarily by CYPlAl and CYP2B1/2, respectively. PROD, EROD and MROD activities were also decreased by 18%, 19% and 40%, respectively, in hepatic microsomes prepared from rats treated with T.S. extract for 3 days. Kinetic analysis of CYP activity of 3-methylchloranthrene-induced microsomes demonstrated that T.S. inhibited EROD and MROD activities by a noncompetitive and competitive mechanism, respectively. The analysis of alterations produced by T.S. on PROD kinetic parameters in phenobarbital-induced microsomes suggested that the inhibition is noncompetitive. Pretreatment of rats with T.S. prolonged pentobarbital and phenobarbital sleeping time; however, plasma phenobarbital concentration determined on awakening showed no significant difference between control and T.S.-treated rats. T.S. was also found to be a potent inhibitor of the liver cytosolic glutathione S-transferase. These data suggest that selective modulation of CYP isoenzymes by T.S. might con-tribute to protection of the liver from xenobiotic-induced intoxication or to alteration of the action of drug (s) conco-mitantly administered besides its antioxidative properties.


2008 ◽  
Vol 46 (5) ◽  
pp. 419-423 ◽  
Author(s):  
R. Zhang ◽  
C.-h. Liu ◽  
T.-l. Huang ◽  
N.-s. Wang ◽  
S.-q. Mi

1986 ◽  
Vol 154 (2) ◽  
pp. 281-287 ◽  
Author(s):  
Rudiger KOCH ◽  
Arno DEGER ◽  
Hans-Martin JACK ◽  
Karl-Norbert KLOTZ ◽  
Dieter SCHENZLE ◽  
...  

Steroids ◽  
1998 ◽  
Vol 63 (4) ◽  
pp. 186-192 ◽  
Author(s):  
Junichi Goto ◽  
Naoaki Murao ◽  
Chifumi Nakada ◽  
Takashi Motoyama ◽  
Junji Oohashi ◽  
...  

2006 ◽  
Vol 1758 (1) ◽  
pp. 124-131 ◽  
Author(s):  
Annamaria Tonazzi ◽  
Michele Galluccio ◽  
Francesca Oppedisano ◽  
Cesare Indiveri

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