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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. ; Wagner, Stefan

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 typeArticle
Journal or Publication TitleESC Heart Failure
PublisherWiley
Open Access TypeGold (with APC)
Place of PublicationSAN FRANCISCO
Volume5
Number of Issue or Book Chapter4
Page Rangepp. 642-648
DateAugust 2018
Date of publication24 Sep 2018 15:02
InstitutionsMedicine > Lehrstuhl für Innere Medizin II
Identification Number
ValueType
10.1002/ehf2.12336DOI
KeywordsEXCHANGER; OUTCOMES; DISEASE; TRIAL; Empagliflozin; Heart failure; CaMKII; Calcium; Ca leak
Dewey Decimal Classification600 Technology > 610 Medical sciences Medicine
StatusPublished
RefereedYes, this version has been refereed
Created at the University of RegensburgYes
URN of the UB Regensburgurn:nbn:de:bvb:355-epub-377616
Item ID37761

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