Determination of metabolic profile of anti-malarial trioxane CDRI 99/411 in rat liver microsomes using HPLC

2011 ◽  
Vol 26 (1) ◽  
pp. 115-122 ◽  
Author(s):  
Smriti Mishra ◽  
Lakshmi Manickavasagam ◽  
Girish Kumar Jain
Keyword(s):  
Rat Liver ◽  
Metabolic Profile ◽  
Liver Microsomes ◽  
Rat Liver Microsomes

A Direct, Highly Sensitive Fluorometric Assay for a Microsomal Cytochrome P450-Mediated O-Demethylation Using a Novel Coumarin Analog as Substrate

2000 ◽  
Vol 55 (11-12) ◽  
pp. 915-922 ◽  
Author(s):  
René Roser ◽  
Helmut Thomas
Keyword(s):  
Rat Liver ◽  
Liver Microsomes ◽  
Fluorometric Assay ◽  
Excitation Wavelength ◽  
Monooxygenase System ◽  
Rat Liver Microsomes ◽  
Monooxygenase Activity ◽  
Continuous Increase ◽  
Highly Sensitive

A highly sensitive fluorometric assay for the determination of monooxygenase activity in liver microsomes is described. The assay is based on the use of 3-chloro-7-methoxy-4-methylcoumarin which is demethylated to 3-chloro-7-hydroxy-4-methylcoumarin. The rate of formation of 3-chloro-7-hydroxy-4-methylcoumarin was recorded as an increase of fluorescence (λA = 380 nm, λF = 480 nm ) with time. When 3-chloro-7-methoxy-4-methylcoumarin was incubated in the presence of MgCl2and NADPH with rat liver microsomes, a continuous increase of the fluorescence could be measured. The reaction proceeded linearly for about 10 min and at least up to a concentration of 0.1 mg/ml of microsomal protein. Besides 3-chloro-7-hydroxy-4-methylcoumarin a hydroxylated derivative of the substrate was formed as a second metabolite during the incubation. Using an excitation wavelength of 480 nm and a fluorescence/em ission w avelength of 480 nm, the fluorescence of this substance (λA = 338 nm, λF = 422 nm ) amounted only to about 1% of the fluorescence of the main product. The use of 3-chloro-7-methoxy-4-methylcoumarin as substrate enables the fluorometric determination of the O-dealkylation activity of a cytochrom e P450-dependent monooxygenase system in rat liver which is inducible by phenobarbital but not by 3-methylcholanthrene.

Influence of monooxygenase inducers on the metabolic profile of phenanthrene in rat liver microsomes

Toxicology ◽  
1982 ◽  
Vol 25 (4) ◽  
pp. 333-343 ◽  
Author(s):  
Jürgen Jacob ◽  
Achim Schmoldt ◽  
Gernot Grimmer
Keyword(s):  
Rat Liver ◽  
Metabolic Profile ◽  
Liver Microsomes ◽  
Rat Liver Microsomes

Simple method for determination of the active metabolite of the inotropic drug pimobendan in rat liver microsomes

2000 ◽  
Vol 744 (1) ◽  
pp. 189-193 ◽  
Author(s):  
Shin-ichiro Kuriya ◽  
Shigeru Ohmori ◽  
Mayuko Hino ◽  
Chiaki Senda ◽  
Kenji Sakai ◽  
...  
Keyword(s):  
Rat Liver ◽  
Active Metabolite ◽  
Liver Microsomes ◽  
Rat Liver Microsomes ◽  
Simple Method ◽  
Inotropic Drug
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