Hydrocotyle bonariensis Comm ex Lamm (Araliaceae) leaves extract inhibits IKs not IKr potassium currents: Potential implications for anti-arrhythmic therapy

IF 4.3 3区 材料科学 Q1 ENGINEERING, ELECTRICAL & ELECTRONIC ACS Applied Electronic Materials Pub Date : 2022-07-01 DOI:10.1016/j.jtcme.2021.09.004
Komla Kaboua , Aklesso Mouzou , Tcha Pakoussi , Mindede Assih , Aurelien Chatelier , Aboudoulatifou Diallo , Patrick Bois , Jocelyn Bescond
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引用次数: 2

Abstract

Background and aim

Hydrocotyle bonariensis Comm ex Lamm (Araliaceae) is one of these plants sufficiently exploited in traditional African medicine for its hypotensive effect. However, the pharmacological effects of those plants on cardiac functions are not well known. The potassium currents IKs and IKr, responsible for the repolarization of cardiac cell action potential, strongly influence the human cardiac rhythm. Therefore, modulators of these currents have a beneficial or undesirable medical importance in relation to cardiac arrhythmias. In order to optimize the therapeutic use of this medicinal plant, we studied the effects of hydro-ethanolic leaf extract of Hydrocotyle bonariensis on both potassium currents.

Experimental procedure

The patch clamp experiments for IK currents recording were performed on the HEK 293 (Human Embryonic Kidney 293) cell line, stably transfected with either KCNQ1 and KCNE1 genes encoding the channel responsible for the "IKs" current (HEK293 IKs), or with hERG (human ether-a-go-go related gene) gene encoding "IKr" current (HEK293 IKr).

Results and conclusion

This study revealed that the hydro-ethanolic leaf extract of H. bonariensis significantly inhibits the slow potassium component (IKs) without altering the fast potassium component (IKr). The extract at 0.5 mg/ml decreases IKs conductance by 24 ± 4.1% (n = 6) without modifying its activation threshold suggesting a direct blockade of the slow potassium channel. This selective action of the extract on the IKs current reflects a class III anti-arrhythmic effect.

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水松叶提取物抑制IKs而非IKr钾电流:抗心律失常治疗的潜在意义
背景和目的天南星科(Araliaceae)是非洲传统医学中充分利用的降压植物之一。然而,这些植物对心脏功能的药理作用尚不清楚。负责心脏细胞动作电位复极的钾电流IKs和IKr强烈影响人类心律。因此,这些电流的调节剂在心律失常方面具有有益或不良的医学重要性。为了优化这种药用植物的治疗用途,我们研究了博纳水松的水乙醇叶提取物对两种钾电流的影响。实验程序记录IK电流的膜片钳实验在HEK 293(人胚胎肾293)细胞系上进行,该细胞系用编码负责“IKs”电流的通道(HEK293 IKs)的KCNQ1和KCNE1基因稳定转染,或与编码“IKr”电流的hERG基因(HEK293IKr)结合。0.5 mg/ml的提取物使IKs电导降低了24±4.1%(n=6),而没有改变其激活阈值,这表明直接阻断了慢钾通道。提取物对IKs电流的这种选择性作用反映了III类抗心律失常作用。
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4.30%
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567
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