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Empagliflozin reduces Ca/calmodulin-dependent kinase II activity in isolated ventricular cardiomyocytes
Article
Mustroph, Julian, Wagemann, Olivia, Lücht, Charlotte M., Trum, Maximilian, Hammer, Karin P., Sag, Can Martin, Lebek, Simon, Tarnowski, Daniel, Reinders, Jörg, Perbellini, Filippo, Terracciano, Cesare, Schmid, Christof, Schopka, Simon, Hilker, Michael, Zausig, York, Pabel, Steffen, Sossalla, Samuel T., Schweda, Frank, Maier, Lars S. and Wagner, Stefan (2018) Empagliflozin reduces Ca/calmodulin-dependent kinase II activity in isolated ventricular cardiomyocytes. ESC Heart Failure 5 (4), pp. 642-648.DOI to cite this document: 10.5283/epub.37761
Abstract
AimsThe EMPA-REG OUTCOME study showed reduced mortality and hospitalization due to heart failure (HF) in diabetic patients treated with empagliflozin. Overexpression and Ca2+-dependent activation of Ca2+/calmodulin-dependent kinase II (CaMKII) are hallmarks of HF, leading to contractile dysfunction and arrhythmias. We tested whether empagliflozin reduces CaMKII- activity and improves ...
AimsThe EMPA-REG OUTCOME study showed reduced mortality and hospitalization due to heart failure (HF) in diabetic patients treated with empagliflozin. Overexpression and Ca2+-dependent activation of Ca2+/calmodulin-dependent kinase II (CaMKII) are hallmarks of HF, leading to contractile dysfunction and arrhythmias. We tested whether empagliflozin reduces CaMKII- activity and improves Ca2+-handling in human and murine ventricular myocytes. Methods and resultsMyocytes from wild-type mice, mice with transverse aortic constriction (TAC) as a model of HF, and human failing ventricular myocytes were exposed to empagliflozin (1mol/L) or vehicle. CaMKII activity was assessed by CaMKII-histone deacetylase pulldown assay. Ca2+ spark frequency (CaSpF) as a measure of sarcoplasmic reticulum (SR) Ca2+ leak was investigated by confocal microscopy. [Na+](i) was measured using Na+/Ca2+-exchanger (NCX) currents (whole-cell patch clamp). Compared with vehicle, 24h empagliflozin exposure of murine myocytes reduced CaMKII activity (1.60.7 vs. 4.2 +/- 0.9, P<0.05, n=10 mice), and also CaMKII-dependent ryanodine receptor phosphorylation (0.8 +/- 0.1 vs. 1.0 +/- 0.1, P<0.05, n=11 mice), with similar results upon TAC. In murine myocytes, empagliflozin reduced CaSpF (TAC: 1.7 +/- 0.3 vs. 2.5 +/- 0.4 1/100m(-1)s(-1), P<0.05, n=4 mice) but increased SR Ca2+ load and Ca2+ transient amplitude. Importantly, empagliflozin also significantly reduced CaSpF in human failing ventricular myocytes (1 +/- 0.2 vs. 3.3 +/- 0.9, P<0.05, n=4 patients), while Ca2+ transient amplitude was increased (F/F-0: 0.53 +/- 0.05 vs. 0.36 +/- 0.02, P<0.05, n=3 patients). In contrast, 30min exposure with empagliflozin did not affect CaMKII activity nor Ca2+-handling but significantly reduced [Na+](i). ConclusionsWe show for the first time that empagliflozin reduces CaMKII activity and CaMKII-dependent SR Ca2+ leak. Reduced Ca2+ leak and improved Ca2+ transients may contribute to the beneficial effects of empagliflozin in HF.
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Details
| Item type | Article | ||||
| Journal or Publication Title | ESC Heart Failure | ||||
| Publisher | Wiley | ||||
| Open Access Type | Gold (with APC) | ||||
| Place of Publication | SAN FRANCISCO | ||||
| Volume | 5 | ||||
| Number of Issue or Book Chapter | 4 | ||||
| Page Range | pp. 642-648 | ||||
| Date | August 2018 | ||||
| Date of publication | 24 Sep 2018 15:02 | ||||
| Institutions | Medicine > Lehrstuhl für Innere Medizin II | ||||
| Identification Number |
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| Keywords | EXCHANGER; OUTCOMES; DISEASE; TRIAL; Empagliflozin; Heart failure; CaMKII; Calcium; Ca leak | ||||
| Dewey Decimal Classification | 600 Technology > 610 Medical sciences Medicine | ||||
| Status | Published | ||||
| Refereed | Yes, this version has been refereed | ||||
| Created at the University of Regensburg | Yes | ||||
| URN of the UB Regensburg | urn:nbn:de:bvb:355-epub-377616 | ||||
| Item ID | 37761 |
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