The Effect of Rivaroxaban on CYP4F2 and Transcription Factors’ Activity in HUVECs
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 we...
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MDPI AG
2021
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oai:doaj.org-article:1a38647cd30e48b08d10a34b97e2881e2021-11-25T16:39:20ZThe Effect of Rivaroxaban on CYP4F2 and Transcription Factors’ Activity in HUVECs10.3390/app1122108512076-3417https://doaj.org/article/1a38647cd30e48b08d10a34b97e2881e2021-11-01T00:00:00Zhttps://www.mdpi.com/2076-3417/11/22/10851https://doaj.org/toc/2076-3417Interindividual 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. <i>CYP4F2, HNF4α, PXR</i> and <i>CAR</i> 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 <i>CYP4F2</i> when hsa-miR-24-3p—both <i>CYP4F2</i> expression and CYP4F2 protein levels in HUVECs. The expression of the transcription factors <i>HNF4α</i>, <i>PXR</i> and <i>CAR</i> was not detected in HUVECs.Ieva CiapieneVacis TatarunasAgne GiedraitieneVaidotas ZvikasValdas JakstasAudrone VeikutieneUgne MeskauskaiteUgne VenckyteAudrius PukalskasVaiva LesauskaiteMDPI AGarticleHUVECsrivaroxabaninflammationhsa-miR-24-3pCYP4F213-docosenamideTechnologyTEngineering (General). Civil engineering (General)TA1-2040Biology (General)QH301-705.5PhysicsQC1-999ChemistryQD1-999ENApplied Sciences, Vol 11, Iss 10851, p 10851 (2021) |
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DOAJ |
| collection |
DOAJ |
| language |
EN |
| topic |
HUVECs rivaroxaban inflammation hsa-miR-24-3p CYP4F2 13-docosenamide Technology T Engineering (General). Civil engineering (General) TA1-2040 Biology (General) QH301-705.5 Physics QC1-999 Chemistry QD1-999 |
| spellingShingle |
HUVECs rivaroxaban inflammation hsa-miR-24-3p CYP4F2 13-docosenamide Technology T Engineering (General). Civil engineering (General) TA1-2040 Biology (General) QH301-705.5 Physics QC1-999 Chemistry QD1-999 Ieva Ciapiene Vacis Tatarunas Agne Giedraitiene Vaidotas Zvikas Valdas Jakstas Audrone Veikutiene Ugne Meskauskaite Ugne Venckyte Audrius Pukalskas Vaiva Lesauskaite The Effect of Rivaroxaban on CYP4F2 and Transcription Factors’ Activity in HUVECs |
| description |
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. <i>CYP4F2, HNF4α, PXR</i> and <i>CAR</i> 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 <i>CYP4F2</i> when hsa-miR-24-3p—both <i>CYP4F2</i> expression and CYP4F2 protein levels in HUVECs. The expression of the transcription factors <i>HNF4α</i>, <i>PXR</i> and <i>CAR</i> was not detected in HUVECs. |
| format |
article |
| author |
Ieva Ciapiene Vacis Tatarunas Agne Giedraitiene Vaidotas Zvikas Valdas Jakstas Audrone Veikutiene Ugne Meskauskaite Ugne Venckyte Audrius Pukalskas Vaiva Lesauskaite |
| author_facet |
Ieva Ciapiene Vacis Tatarunas Agne Giedraitiene Vaidotas Zvikas Valdas Jakstas Audrone Veikutiene Ugne Meskauskaite Ugne Venckyte Audrius Pukalskas Vaiva Lesauskaite |
| author_sort |
Ieva Ciapiene |
| title |
The Effect of Rivaroxaban on CYP4F2 and Transcription Factors’ Activity in HUVECs |
| title_short |
The Effect of Rivaroxaban on CYP4F2 and Transcription Factors’ Activity in HUVECs |
| title_full |
The Effect of Rivaroxaban on CYP4F2 and Transcription Factors’ Activity in HUVECs |
| title_fullStr |
The Effect of Rivaroxaban on CYP4F2 and Transcription Factors’ Activity in HUVECs |
| title_full_unstemmed |
The Effect of Rivaroxaban on CYP4F2 and Transcription Factors’ Activity in HUVECs |
| title_sort |
effect of rivaroxaban on cyp4f2 and transcription factors’ activity in huvecs |
| publisher |
MDPI AG |
| publishDate |
2021 |
| url |
https://doaj.org/article/1a38647cd30e48b08d10a34b97e2881e |
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