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Page 1
Metabolism of the aquatic pollutant diclofenac in the Lymnaea stagnalis freshwater gastropod.
Bouly L, Fenet H, Carayon JL, Gomez E, Géret F, Courant F. Bouly L, et al. Environ Sci Pollut Res Int. 2022 Dec;29(56):85081-85094. doi: 10.1007/s11356-022-21815-5. Epub 2022 Jul 6. Environ Sci Pollut Res Int. 2022. PMID: 35790636
Phase I metabolism involved hydroxylation, with detection of 3'-, 4'-, and 5-hydroxydiclofenac and three dihydroxylated metabolites, as well as cyclization, oxidative decarboxylation, and dehydrogenation, while phase II metabolism consisted of glucose and sulfate co …
Phase I metabolism involved hydroxylation, with detection of 3'-, 4'-, and 5-hydroxydiclofenac and three dihydroxylated metabo …
Discovery and Optimization of 5-Hydroxy-Diclofenac toward a New Class of Ligands with Nanomolar Affinity for the CaMKIIα Hub Domain.
Tian Y, Shehata MA, Gauger SJ, Ng CKL, Solbak S, Thiesen L, Bruus-Jensen J, Krall J, Bundgaard C, Gibson KM, Wellendorph P, Frølund B. Tian Y, et al. J Med Chem. 2022 May 12;65(9):6656-6676. doi: 10.1021/acs.jmedchem.1c02177. Epub 2022 May 2. J Med Chem. 2022. PMID: 35500061
We have recently pinpointed the CaMKIIalpha hub domain as the long-sought-after high-affinity target of gamma-hydroxybutyrate ligands substantiated with a high-resolution cocrystal of 5-hydroxydiclofenac (3). Herein, we employed in silico approaches to rationalize a …
We have recently pinpointed the CaMKIIalpha hub domain as the long-sought-after high-affinity target of gamma-hydroxybutyrate ligands substa …
Cytochrome P450 Expression and Chemical Metabolic Activity before Full Liver Development in Zebrafish.
Nawaji T, Yamashita N, Umeda H, Zhang S, Mizoguchi N, Seki M, Kitazawa T, Teraoka H. Nawaji T, et al. Pharmaceuticals (Basel). 2020 Dec 11;13(12):456. doi: 10.3390/ph13120456. Pharmaceuticals (Basel). 2020. PMID: 33322603 Free PMC article.
Whole-mount in situ hybridization revealed cyp2y3, 2r1, and 3a65 transcripts in larvae at 55 hpf after exposure to rifampicin, phenobarbital, or 2,3,7,8-tetrachlorodibenzo-p-dioxin from 30 hpf onward. Marked conversions of diclofenac to 4'-hydroxydiclofenac and 5-hydrox …
Whole-mount in situ hybridization revealed cyp2y3, 2r1, and 3a65 transcripts in larvae at 55 hpf after exposure to rifampicin, phenobarbital …
Different Roles of Human Cytochrome P450 2C9 and 3A Enzymes in Diclofenac 4'- and 5-Hydroxylations Mediated by Metabolically Inactivated Human Hepatocytes in Previously Transplanted Chimeric Mice.
Miura T, Uehara S, Shimizu M, Murayama N, Utoh M, Suemizu H, Yamazaki H. Miura T, et al. Chem Res Toxicol. 2020 Feb 17;33(2):634-639. doi: 10.1021/acs.chemrestox.9b00446. Epub 2019 Dec 31. Chem Res Toxicol. 2020. PMID: 31854189
After diclofenac administration, plasma levels of diclofenac, 5-hydroxydiclofenac, and diclofenac acylglucuronide were roughly similar in pretreated and untreated mice. ...
After diclofenac administration, plasma levels of diclofenac, 5-hydroxydiclofenac, and diclofenac acylglucuronide were roughly …
Degradation of diclofenac by H2O2 activated with pre-magnetization Fe0: Influencing factors and degradation pathways.
Li X, Zhou M, Pan Y. Li X, et al. Chemosphere. 2018 Dec;212:853-862. doi: 10.1016/j.chemosphere.2018.08.144. Epub 2018 Aug 29. Chemosphere. 2018. PMID: 30193234
In addition, preliminary degradation mechanism was elucidated by major products identification using UPLC-MS, through which the degradation intermediates, such as 4-hydroxy-diclofenac or 5-hydroxydiclofenac, 2,6-dichloroaniline, phenylacetic acid, 1,3-dichlorobenzen …
In addition, preliminary degradation mechanism was elucidated by major products identification using UPLC-MS, through which the degradation …
In vivo and in vitro diclofenac 5-hydroxylation mediated primarily by cytochrome P450 3A enzymes in common marmoset livers genotyped for P450 2C19 variants.
Nakanishi K, Uehara S, Kusama T, Inoue T, Shimura K, Kamiya Y, Murayama N, Shimizu M, Uno Y, Sasaki E, Yamazaki H. Nakanishi K, et al. Biochem Pharmacol. 2018 Jun;152:272-278. doi: 10.1016/j.bcp.2018.04.002. Epub 2018 Apr 5. Biochem Pharmacol. 2018. PMID: 29626440
An anti-inflammatory drug, diclofenac is reportedly metabolized mainly by human cytochrome P450 (P450) 2C9 to 4'-hydroxydiclofenac and minorly by P450 3A4 to 5-hydroxydiclofenac that leads to reactive intermediates. In this study, in vivo pharmacokinetics in six mar …
An anti-inflammatory drug, diclofenac is reportedly metabolized mainly by human cytochrome P450 (P450) 2C9 to 4'-hydroxydiclofenac and minor …
Reduction and Scavenging of Chemically Reactive Drug Metabolites by NAD(P)H:Quinone Oxidoreductase 1 and NRH:Quinone Oxidoreductase 2 and Variability in Hepatic Concentrations.
den Braver-Sewradj SP, den Braver MW, Toorneman RM, van Leeuwen S, Zhang Y, Dekker SJ, Vermeulen NPE, Commandeur JNM, Vos JC. den Braver-Sewradj SP, et al. Chem Res Toxicol. 2018 Feb 19;31(2):116-126. doi: 10.1021/acs.chemrestox.7b00289. Epub 2018 Jan 11. Chem Res Toxicol. 2018. PMID: 29281794 Free PMC article.
The reduction of the clozapine nitrenium ion supports association studies showing that NQO2 is a genetic risk factor for clozapine-induced agranulocytosis. The 5-hydroxydiclofenac quinone imine, which was previously shown to be reduced by NQO1, was not reduced by NQ …
The reduction of the clozapine nitrenium ion supports association studies showing that NQO2 is a genetic risk factor for clozapine-induced a …
An evaluation of myeloperoxidase-mediated bio-activation of NSAIDs in promyelocytic leukemia (HL-60) cells for potential cytotoxic selectivity.
Morgan AGM, Babu D, Michail K, Siraki AG. Morgan AGM, et al. Toxicol Lett. 2017 Oct 5;280:48-56. doi: 10.1016/j.toxlet.2017.07.894. Epub 2017 Jul 25. Toxicol Lett. 2017. PMID: 28754375
We tested the enzymatic peroxidation of three NSAIDs, namely diclofenac, indomethacin, and naproxen in comparison with their hepatic metabolites, 4'- hydroxydiclofenac (4'-OHD), 5-hydroxydiclofenac (5-OHD), O-desmethyl-N-deschlorobenzoylindomethacin (DMBI), O-desmet …
We tested the enzymatic peroxidation of three NSAIDs, namely diclofenac, indomethacin, and naproxen in comparison with their hepatic metabol …
The self-sufficient P450 RhF expressed in a whole cell system selectively catalyses the 5-hydroxylation of diclofenac.
Klenk JM, Nebel BA, Porter JL, Kulig JK, Hussain SA, Richter SM, Tavanti M, Turner NJ, Hayes MA, Hauer B, Flitsch SL. Klenk JM, et al. Biotechnol J. 2017 Mar;12(3). doi: 10.1002/biot.201600520. Epub 2017 Feb 8. Biotechnol J. 2017. PMID: 28098428
Here we have used the self-sufficient P450 RhF (CYP116B2) from Rhodococcus sp. in a whole cell system to reproducibly catalyze the highly regioselective oxidation of diclofenac to 5-hydroxydiclofenac. The product is a human metabolite and as such is an important sta …
Here we have used the self-sufficient P450 RhF (CYP116B2) from Rhodococcus sp. in a whole cell system to reproducibly catalyze the highly re …
42 results