Dual effect of cicletanine on the Na+-H+ exchanger in chick embryonic cardiomyocytes
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Published on: February 24, 2017
E Samain1, G Dagher, H Bouillier
1INSERM Unité 337, Faculté de Médicine Broussais-Hôtel Dieu, Paris, France.
Insights
Cicletanine, an antihypertensive drug, shows a dual effect on the sodium-hydrogen exchanger (Na+-H+) in cardiac cells. Low concentrations inhibit Na+-H+ activity, while higher concentrations stimulate it, impacting intracellular pH recovery.
Area of Science:
- Cardiology
- Cell Physiology
- Pharmacology
Background:
- The sodium-hydrogen exchanger (Na+-H+) is crucial for regulating intracellular pH (pHi) in cardiac cells.
- Na+-H+ exchanger activity is implicated in cardiac cell injury during ischemia and reperfusion.
- Cicletanine is an antihypertensive agent with reported cardioprotective effects.
Purpose of the Study:
- To investigate the effect of cicletanine on Na+-H+ exchanger activity in isolated chick embryo ventricular cardiomyocytes.
- To determine how cicletanine influences intracellular pH (pHi) recovery following an acid load.
Main Methods:
- Ventricular cardiomyocytes were isolated from chick embryos.
- Na+-H+ exchanger activity was measured by assessing the rate of pHi recovery after an induced acid load.
- Cardiomyocytes were exposed to varying concentrations of cicletanine (10(-7) M to 10(-5) M).
Main Results:
- Cicletanine exhibited a concentration-dependent, dual effect on Na+-H+ exchanger activity.
- Low cicletanine concentration (10(-7) M) significantly decreased Na+-H+ exchanger activity.
- Higher cicletanine concentrations (10(-6) M to 10(-5) M) significantly stimulated Na+-H+ exchanger activity.
Conclusions:
- Cicletanine modulates intracellular pH (pHi) recovery in cardiac cells after an acid load.
- The dual effect of cicletanine on the Na+-H+ exchanger suggests complex regulatory mechanisms in cardiac physiology.
- Findings contribute to understanding cicletanine's potential cardioprotective mechanisms during ischemia-reperfusion.
Abstract:
Na+-H+ exchanger is thought to play an important role in the regulation of the intracellular pH (pHi) and in the cardiac cell injury induced by ischemia and reperfusion. The aim of this study was to assess the effect of cicletanine, an antihypertensive compound in humans, which has been reported to have cardioprotective effect under an ischemia-reperfusion process, on Na+-H+ exchanger activity in ventricular cardiomyocytes isolated from chick embryo. Na+-H+ exchanger activity was assessed by the rate of pHi recovery after an acid load. A dual effect was observed: at low concentration of cicletanine (10(-7) M), Na+-H+ exchanger activity was significantly decreased, whereas at higher concentrations (10(-6)-10(-5) M), a significant stimulation of the exchanger was observed. These results suggest that cicletanine modulates pHi recovery in cardiac cells after cellular acid load.

