scholarly journals In vitro screening of reversible and time-dependent inhibition on CYP3A by TM208 and TM209 in rat liver microsomes

2012 ◽  
Vol 2 (2) ◽  
pp. 181-187 ◽  
Author(s):  
Miaoran Ning ◽  
Liang Li ◽  
Jian Li ◽  
Zaiquan Li ◽  
Runtao Li ◽  
...  
Keyword(s):  
Rat Liver ◽  
Liver Microsomes ◽  
Time Dependent ◽  
Rat Liver Microsomes ◽  
In Vitro Screening ◽  
Dependent Inhibition ◽  
Time Dependent Inhibition

In vitro metabolism in Sprague–Dawley rat liver microsomes of forsythoside A in different compositions of Shuang–Huang–Lian

Fitoterapia ◽  
2011 ◽  
Vol 82 (8) ◽  
pp. 1222-1230 ◽  
Author(s):  
Wei Zhou ◽  
Liu-qing Di ◽  
Jin-jun Shan ◽  
Xiao-lin Bi ◽  
Le-tian Chen ◽  
...  
Keyword(s):  
Rat Liver ◽  
Liver Microsomes ◽  
In Vitro Metabolism ◽  
Rat Liver Microsomes ◽  
Sprague Dawley ◽  
Sprague Dawley Rat

scholarly journals In Vitro Characterization of Borneol Metabolites by GC--MS Upon Incubation with Rat Liver Microsomes

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

In Vitro Metabolism of E2, G2: Novel Bile Acid-Coupling Camptothecin Analogues, in Rat Liver Microsomes

2021 ◽  
Vol 16 ◽  
Author(s):  
Xiangli Zhang ◽  
Qin Shen ◽  
Yi Wang ◽  
Leilei Zhou ◽  
Qi Weng ◽  
...  
Keyword(s):  
Bile Acid ◽  
Phase I ◽  
Rat Liver ◽  
Deoxycholic Acid ◽  
Liver Microsomes ◽  
Intrinsic Clearance ◽  
Rat Liver Microsomes ◽  
Camptothecin Analogues

Background: E2 (Camptothecin - 20 (S) - O- glycine - deoxycholic acid), and G2 (Camptothecin - 20 (S) - O - acetate - deoxycholic acid) are two novel bile acid-derived camptothecin analogues by introducing deoxycholic acid in 20-position of CPT(camptothecin) with greater anticancer activity and lower systematic toxicity in vivo. Objective: We aimed to investigate the metabolism of E2 and G2 by Rat Liver Microsomes (RLM). Methods: Phase Ⅰ and Phase Ⅱ metabolism of E2 and G2 in rat liver microsomes were performed respectively, and the mixed incubation of phase I and phase Ⅱ metabolism of E2 and G2 was also processed. Metabolites were identified by liquid chromatographic/mass spectrometry. Results: The results showed that phase I metabolism was the major biotransformation route for both E2 and G2. The isoenzyme involved in their metabolism had some difference. The intrinsic clearance of G2 was 174.7mL/min. mg protein, more than three times of that of E2 (51.3 mL/min . mg protein), indicating a greater metabolism stability of E2. 10 metabolites of E2 and 14 metabolites of G2 were detected, including phase I metabolites (mainly via hydroxylations and hydrolysis) and their further glucuronidation products. Conclusion: These findings suggested that E2 and G2 have similar biotransformation pathways except some difference in the hydrolysis ability of the ester bond and amino bond from the parent compounds, which may result in the diversity of their metabolism stability and responsible CYPs(Cytochrome P450 proteins).

Sex Difference in Inhibition of In Vitro Mexazolam Metabolism by Various 3-Hydroxy-3-Methylglutaryl-Coenzyme A Reductase Inhibitors in Rat Liver Microsomes

2002 ◽  
Vol 30 (8) ◽  
pp. 904-910 ◽  
Author(s):  
Michi Ishigami ◽  
Wataru Takasaki ◽  
Toshihiko Ikeda ◽  
Toru Komai ◽  
Kiyomi Ito ◽  
...  
Keyword(s):  
Sex Difference ◽  
Rat Liver ◽  
Coenzyme A ◽  
Liver Microsomes ◽  
Rat Liver Microsomes ◽  
Reductase Inhibitors ◽  
Coenzyme A Reductase

Effect of Solvents on the Time-Dependent Inhibition of CYP3A4 and the Biotransformation of AZD3839 in Human Liver Microsomes and Hepatocytes

2012 ◽  
Vol 41 (1) ◽  
pp. 159-169 ◽  
Author(s):  
Jenny Aasa ◽  
Yin Hu ◽  
Göran Eklund ◽  
Anders Lindgren ◽  
Pawel Baranczewski ◽  
...  
Keyword(s):  
Human Liver ◽  
Liver Microsomes ◽  
Human Liver Microsomes ◽  
Time Dependent ◽  
Effect Of Solvents ◽  
Dependent Inhibition ◽  
Time Dependent Inhibition
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