In Vitro Inhibitory Effects of Synthetic Cannabinoid EAM-2201 on Cytochrome P450 and UDP-Glucuronosyltransferase Enzyme Activities in Human Liver Microsomes
Abstract
:1. Introduction
2. Results
3. Discussion
4. Materials and Methods
4.1. Chemicals and Reagents
4.2. Inhibitory Effects of EAM-2201 on Eight Major CYP Activities in Human Liver Microsomes
4.3. Inhibitory Effects of EAM-2201 on Six Major UGTs in Human Liver Microsomes
4.4. Time-Dependent Inhibition of CYP2C8, CYP2C9, CYP2C19 and CYP3A4 Activities by EAM-2201
4.5. Enzyme Kinetic Analysis
4.6. LC-MS/MS Analysis
4.7. Data Analysis
5. Conclusions
Acknowledgments
Author Contributions
Conflicts of Interest
References
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Sample Availability: Not available. |
Enzyme Activity | CYP | Ki (µM) | kinact (min−1) |
---|---|---|---|
Amodiaquine N-deethylase | 2C8 | 0.54 | 0.0633 |
Diclofenac 4′-hydroxylase | 2C9 | 3.0 | 0.0462 |
[S]-Mephenytoin 4′-hydroxylase | 2C19 | 3.8 | 0.0264 |
Midazolam 1′-hydroxylase | 3A4 | 4.1 | 0.0250 |
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Kong, T.Y.; Kwon, S.-S.; Cheong, J.C.; Kim, H.S.; Kim, J.Y.; Lee, H.S. In Vitro Inhibitory Effects of Synthetic Cannabinoid EAM-2201 on Cytochrome P450 and UDP-Glucuronosyltransferase Enzyme Activities in Human Liver Microsomes. Molecules 2018, 23, 920. https://doi.org/10.3390/molecules23040920
Kong TY, Kwon S-S, Cheong JC, Kim HS, Kim JY, Lee HS. In Vitro Inhibitory Effects of Synthetic Cannabinoid EAM-2201 on Cytochrome P450 and UDP-Glucuronosyltransferase Enzyme Activities in Human Liver Microsomes. Molecules. 2018; 23(4):920. https://doi.org/10.3390/molecules23040920
Chicago/Turabian StyleKong, Tae Yeon, Soon-Sang Kwon, Jae Chul Cheong, Hee Seung Kim, Jin Young Kim, and Hye Suk Lee. 2018. "In Vitro Inhibitory Effects of Synthetic Cannabinoid EAM-2201 on Cytochrome P450 and UDP-Glucuronosyltransferase Enzyme Activities in Human Liver Microsomes" Molecules 23, no. 4: 920. https://doi.org/10.3390/molecules23040920