The Effect of Rivaroxaban on CYP4F2 and Transcription Factors’ Activity in HUVECs
Source abstract
Abstract
Interindividual variabilities between patients taking the anticoagulant rivaroxaban are a result of hepatic metabolism by CYP 450 enzymes. The objective of this study was to evaluate the impact of rivaroxaban on CYP4F2 and transcription factors’ activity in HUVECs. Rivaroxaban and its metabolites were detected by UPLC-ESI-MS and UPLC-QTOF-MS. CYP4F2, HNF4α, PXR and CAR expressions were determined in HUVECs by qPCR; CYP4F2 protein concentration was determined by ELISA. Rivaroxaban metabolites (M-1, M-2, M-5, M-8, M-10, M-11 and M-18) were detected in endothelial cells’ culture medium. Increasing concentrations of rivaroxaban determined lower 13-docosenamide concentrations. Rivaroxaban and dexamethasone reduced the expression of CYP4F2 when hsa-miR-24-3p—both CYP4F2 expression and CYP4F2 protein levels in HUVECs. The expression of the transcription factors HNF4α, PXR and CAR was not detected in HUVECs.
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Research context
OpenAlex topics: Atrial Fibrillation Management and Outcomes · Pharmacogenetics and Drug Metabolism · Antiplatelet Therapy and Cardiovascular Diseases
SciVX discovery tags are terminology-based. OpenAlex topics are source-provided classifications.
Affiliations
Institute of Cardiology, Lithuanian University of Health Sciences, Sukileliu 15, LT 50103 Kaunas, Lithuania
Institute of Microbiology and Virology, Lithuanian University of Health Sciences, Eiveniu 4, LT 50161 Kaunas, Lithuania
Institute of Pharmaceutical Technologies, Lithuanian University of Health Sciences, Sukileliu 13, LT 50166 Kaunas, Lithuania
Medical Academy, Lithuanian University of Health Sciences, A. Mickeviciaus 9, LT 44307 Kaunas, Lithuania
Faculty of Chemical Technology, Kaunas University of Technology, Radvilenu 19, LT 50254 Kaunas, Lithuania
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