Direct comparison of UDP-glucuronosyltransferase and cytochrome P450 activities in human liver microsomes, plated and suspended primary human hepatocytes from five liver donors

2017 ◽  
Vol 109 ◽  
pp. 96-110 ◽  
Author(s):  
Shalenie P. den Braver-Sewradj ◽  
Michiel W. den Braver ◽  
Audrey Baze ◽  
Joachim Decorde ◽  
Massimiliano Fonsi ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Human Liver ◽  
Liver Microsomes ◽  
Human Hepatocytes ◽  
Human Liver Microsomes ◽  
Primary Human Hepatocytes ◽  
Udp Glucuronosyltransferase ◽  
Liver Donors

scholarly journals Effect of a New Prokinetic Agent DA-9701 Formulated with Corydalis Tuber and Pharbitidis Semen on Cytochrome P450 and UDP-Glucuronosyltransferase Enzyme Activities in Human Liver Microsomes

2012 ◽  
Vol 2012 ◽  
pp. 1-7 ◽  
Author(s):  
Hye Young Ji ◽  
Kwang Hyeon Liu ◽  
Ji Hyeon Jeong ◽  
Dae-Young Lee ◽  
Hyun Joo Shim ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Human Liver ◽  
Liver Microsomes ◽  
Human Liver Microsomes ◽  
Udp Glucuronosyltransferase ◽  
Index Value ◽  
Tuber Extract ◽  
Corydalis Tuber

DA-9701 is a new botanical drug composed of the extracts of Corydalis tuber and Pharbitidis semen, and it is used as an oral therapy for the treatment of functional dyspepsia in Korea. The inhibitory potentials of DA-9701 and its component herbs, Corydalis tuber and Pharbitidis semen, on the activities of seven major human cytochrome P450 (CYP) enzymes and four UDP-glucuronosyltransferase (UGT) enzymes in human liver microsomes were investigated using liquid chromatography-tandem mass spectrometry. DA-9701 and Corydalis tuber extract slightly inhibited UGT1A1-mediated etoposide glucuronidation, with 50% inhibitory concentration (IC50) values of 188 and 290 μg/mL, respectively. DA-9701 inhibited CYP2D6-catalyzed bufuralol1′-hydroxylation with an inhibition constant (Ki) value of 6.3 μg/mL in a noncompetitive manner. Corydalis tuber extract competitively inhibited CYP2D6-mediated bufuralol1′-hydroxylation, with aKivalue of 3.7 μg/mL, whereas Pharbitidis semen extract showed no inhibition. The volume in which the dose could be diluted to generate an IC50equivalent concentration (volume per dose index) value of DA-9701 for inhibition of CYP2D6 activity was 1.16 L/dose, indicating that DA-9701 may not be a potent CYP2D6 inhibitor. Further clinical studies are warranted to evaluate thein vivoextent of the observedin vitrointeractions.

Evaluation of P450 Inhibition and Induction by Artemisinin Antimalarials in Human Liver Microsomes and Primary Human Hepatocytes

2012 ◽  
Vol 40 (9) ◽  
pp. 1757-1764 ◽  
Author(s):  
Jie Xing ◽  
Brian J. Kirby ◽  
Dale Whittington ◽  
Yakun Wan ◽  
David R. Goodlett
Keyword(s):  
Human Liver ◽  
Liver Microsomes ◽  
Human Hepatocytes ◽  
Human Liver Microsomes ◽  
Primary Human Hepatocytes

SEQUENTIAL METABOLISM OF 2,3,7-TRICHLORODIBENZO-P-DIOXIN (2,3,7-triCDD) BY CYTOCHROME P450 AND UDP-GLUCURONOSYLTRANSFERASE IN HUMAN LIVER MICROSOMES

2004 ◽  
Vol 32 (8) ◽  
pp. 870-875 ◽  
Author(s):  
Noriyuki Kasai ◽  
Toshiyuki Sakaki ◽  
Raku Shinkyo ◽  
Shin-ichi Ikushiro ◽  
Takashi Iyanagi ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Human Liver ◽  
Liver Microsomes ◽  
Human Liver Microsomes ◽  
Sequential Metabolism ◽  
Udp Glucuronosyltransferase

scholarly journals Corydaline Inhibits Multiple Cytochrome P450 and UDP-Glucuronosyltransferase Enzyme Activities in Human Liver Microsomes

Molecules ◽  
2011 ◽  
Vol 16 (8) ◽  
pp. 6591-6602 ◽  
Author(s):  
Hye Young Ji ◽  
Kwang Hyeon Liu ◽  
Hyeri Lee ◽  
Sae Rom Im ◽  
Hyun Joo Shim ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Enzyme Activities ◽  
Human Liver ◽  
Liver Microsomes ◽  
Human Liver Microsomes ◽  
Udp Glucuronosyltransferase
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