Evaluation of the in vitro/in vivo drug interaction potential of BST204, a purified dry extract of ginseng, and its four bioactive ginsenosides through cytochrome P450 inhibition/induction and UDP-glucuronosyltransferase inhibition

2014 ◽  
Vol 68 ◽  
pp. 117-127 ◽  
Author(s):  
Yu Fen Zheng ◽  
Soo Hyeon Bae ◽  
Eu Jin Choi ◽  
Jung Bae Park ◽  
Sun Ok Kim ◽  
...  
2012 ◽  
Vol 2012 ◽  
pp. 1-7 ◽  
Author(s):  
Hye Young Ji ◽  
Kwang Hyeon Liu ◽  
Ji Hyeon Jeong ◽  
Dae-Young Lee ◽  
Hyun Joo Shim ◽  
...  

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.


2013 ◽  
Vol 136 (2) ◽  
pp. 450-457 ◽  
Author(s):  
Sang Yoon Lee ◽  
Ji-Yoon Lee ◽  
Wonku Kang ◽  
Kwang-il Kwon ◽  
Soo Jin Oh ◽  
...  

2018 ◽  
Vol 40 (8) ◽  
pp. 1322-1337 ◽  
Author(s):  
Sook Jin Seong ◽  
Woo Youl Kang ◽  
Jae-Kyung Heo ◽  
Jungjae Jo ◽  
Won Gu Choi ◽  
...  

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Sarvesh Sabarathinam ◽  
Satish Kumar Rajappan Chandra ◽  
Vijayakumar Thangavel Mahalingam

AbstractMaha yogaraja guggulu (MYG) is a classical herbomineral polyherbal formulation being widely used since centuries. The aim of this study was to investigate the effect of MYG formulation and its major constituents E & Z guggulsterone on CYP3A4 mediated metabolism. In vitro inhibition of MYG and Guggulsterone isomers on CYP3A4 was evaluated by high throughput fluorometric assay. Eighteen Adult male Sprague–Dawley rats (200 ± 25 g body weight) were randomly divided into three groups. Group A, Group B and Group C were treated with placebo, MYG and Standard E & Z guggulsterone for 14 days respectively by oral route. On 15th day, midazolam (5 mg/kg) was administered orally to all rats in each group. Blood samples (0.3 mL) were collected from the retro orbital vein at 0.25, 0.5, 0.75, 1, 2, 4, 6, 12 and 24 h of each rat were collected. The findings from the in vitro & in vivo study proposed that the MYG tablets and its guggulsterone isomers have drug interaction potential when consumed along with conventional drugs which are CYP3A4 substrates. In vivo pharmacokinetic drug interaction study of midazolam pointed out that the MYG tablets and guggulsterone isomers showed an inhibitory activity towards CYP3A4 which may have leads to clinically significant interactions.


2014 ◽  
Vol 55 (2) ◽  
pp. 168-178 ◽  
Author(s):  
Claudia Kasserra ◽  
Mahmoud Assaf ◽  
Matthew Hoffmann ◽  
Yan Li ◽  
Liangang Liu ◽  
...  

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