scholarly journals Characterization of the Ontogeny of Hepatic UDP‐Glucuronosyltransferase Enzymes Based on Glucuronidation Activity Measured in Human Liver Microsomes

2019 ◽  
Vol 59 (S1) ◽  
Author(s):  
Justine Badée ◽  
Nahong Qiu ◽  
Abby C. Collier ◽  
Ryan H. Takahashi ◽  
William F. Forrest ◽  
...  
Keyword(s):  
Human Liver ◽  
Liver Microsomes ◽  
Human Liver Microsomes ◽  
Udp Glucuronosyltransferase

Characterization of paracetamol UDP-glucuronosyltransferase activity in human liver microsomes

1990 ◽  
Vol 40 (3) ◽  
pp. 595-600 ◽  
Author(s):  
J.O. Miners ◽  
K.J. Lillywhite ◽  
K. Yoovathaworn ◽  
M. Pongmarutai ◽  
D.J. Birkett
Keyword(s):  
Human Liver ◽  
Liver Microsomes ◽  
Human Liver Microsomes ◽  
Udp Glucuronosyltransferase

Imipramine N-Glucuronidation in Human Liver Microsomes: Biphasic Kinetics and Characterization of UDP-Glucuronosyltransferase Isoforms

2002 ◽  
Vol 30 (6) ◽  
pp. 636-642 ◽  
Author(s):  
Miki Nakajima ◽  
Eriko Tanaka ◽  
Tomo Kobayashi ◽  
Noriko Ohashi ◽  
Toshiyuki Kume ◽  
...  
Keyword(s):  
Human Liver ◽  
Liver Microsomes ◽  
Human Liver Microsomes ◽  
Biphasic Kinetics ◽  
Udp Glucuronosyltransferase

Characterization of the UDP Glucuronosyltransferase Activity of Human Liver Microsomes Genotyped for the UGT1A1*28 Polymorphism

2007 ◽  
Vol 35 (12) ◽  
pp. 2270-2280 ◽  
Author(s):  
Donglu Zhang ◽  
Duxi Zhang ◽  
Dan Cui ◽  
Janice Gambardella ◽  
Li Ma ◽  
...  
Keyword(s):  
Human Liver ◽  
Liver Microsomes ◽  
Human Liver Microsomes ◽  
Udp Glucuronosyltransferase

Characterization of 1′-Hydroxymidazolam Glucuronidation in Human Liver Microsomes

2007 ◽  
Vol 36 (2) ◽  
pp. 331-338 ◽  
Author(s):  
Bing Zhu ◽  
David Bush ◽  
George A. Doss ◽  
Stella Vincent ◽  
Ronald B. Franklin ◽  
...  
Keyword(s):  
Human Liver ◽  
Liver Microsomes ◽  
Human Liver Microsomes

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.

Sign in / Sign up

Export Citation Format

Share Document