In Vitro inhibitory effects of non-steroidal antiinflammatory drugs on UDP-glucuronosyltransferase 1A1-catalysed estradiol 3?-glucuronidation in human liver microsomes

2005 ◽  
Vol 26 (1) ◽  
pp. 35-39 ◽  
Author(s):  
Yuji Mano ◽  
Takashi Usui ◽  
Hidetaka Kamimura
Keyword(s):  
Human Liver ◽  
Liver Microsomes ◽  
Human Liver Microsomes ◽  
Inhibitory Effects ◽  
Antiinflammatory Drugs ◽  
Udp Glucuronosyltransferase ◽  
Non Steroidal Antiinflammatory Drugs

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.

scholarly journals Erratum: In Vitro Metabolism and Inhibitory Effects of Pranlukast in Human Liver Microsomes [Biol. Pharm. Bull. 32(4): 688-693 (2009)]

2009 ◽  
Vol 32 (7) ◽  
pp. 1311
Author(s):  
Kazuhiro Yoneda ◽  
Ichiro Matsumoto ◽  
Fumitaka Sutoh ◽  
Ryunosuke Higashi ◽  
Ken-ichi Nunoya ◽  
...  
Keyword(s):  
Human Liver ◽  
Liver Microsomes ◽  
Human Liver Microsomes ◽  
In Vitro Metabolism ◽  
Inhibitory Effects

scholarly journals In Vitro Metabolism and Inhibitory Effects of Pranlukast in Human Liver Microsomes

2009 ◽  
Vol 32 (4) ◽  
pp. 688-693 ◽  
Author(s):  
Kazuhiro Yoneda ◽  
Ichiro Matsumoto ◽  
Fumitaka Sutoh ◽  
Ryunosuke Higashi ◽  
Ken-ichi Nunoya ◽  
...  
Keyword(s):  
Human Liver ◽  
Liver Microsomes ◽  
Human Liver Microsomes ◽  
In Vitro Metabolism ◽  
Inhibitory Effects
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