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[8]-姜辣素对豚鼠心房肌的强心作用,[8]-姜辣素是肌浆网Ca++-泵三磷酸腺苷酶的激活剂

Cardiotonic action of [8]-gingerol, an activator of the Ca++-pumping adenosine triphosphatase of sarcoplasmic reticulum, in guinea pig atrial muscle.

作者信息

Kobayashi M, Ishida Y, Shoji N, Ohizumi Y

机构信息

Mitsubishi-Kasei Institute of Life Sciences, Tokyo, Japan.

出版信息

J Pharmacol Exp Ther. 1988 Aug;246(2):667-73.

PMID:2457078
Abstract

[8]-Gingerol (gingerol), a component of ginger, produced a concentration-dependent positive inotropic effect on guinea pig isolated left atria at concentrations of 1 X 10(-6) to 3 X 10(-5) M. Gingerol also exhibited positive inotropic and chronotropic effects on guinea pig right atria. The gingerol-induced inotropic effect was abolished by ryanodine, but was little affected by propranolol, chlorpheniramine, cimetidine, tetrodotoxin, diltiazem or reserpine. The time to peak tension and relaxation time within a single contraction were shortened by gingerol (1 X 10(-5) M) as well as isoproterenol, whereas they were prolonged by BAY K 8644. In guinea pig isolated atrial cells, gingerol (3 X 10(-6) M) caused an increase in the degree and the rate of longitudinal contractions. In guinea pig left atria, gingerol (1 X 10(-6) to 3 X 10(-5) M) gave little influence on the action potential, although it increased the contractile force of the atria. The whole-cell patch-clamp experiments showed that the slow inward current was little affected by gingerol (1 X 10(-6) to 3 X 10(-5) M) in voltage-clamped guinea pig cardiac myocytes. The measurement of extravesicular Ca++ concentration using a Ca++ electrode indicated that gingerol (3 X 10(-6) to 3 X 10(-5) M) accelerated the Ca++ uptake of fragmented sarcoplasmic reticulum (SR) prepared from canine cardiac muscle in a concentration-dependent manner.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

[8]-姜辣素(姜酚)是生姜的一种成分,在浓度为1×10⁻⁶至3×10⁻⁵M时,对豚鼠离体左心房产生浓度依赖性正性肌力作用。姜辣素对豚鼠右心房也表现出正性肌力和变时作用。姜辣素诱导的肌力作用被ryanodine消除,但普萘洛尔、氯苯那敏、西咪替丁、河豚毒素、地尔硫䓬或利血平对其影响较小。姜辣素(1×10⁻⁵M)和异丙肾上腺素均可缩短单次收缩的张力峰值时间和舒张时间,而BAY K 8644则使其延长。在豚鼠离体心房细胞中,姜辣素(3×10⁻⁶M)可导致纵向收缩的程度和速率增加。在豚鼠左心房中,姜辣素(1×10⁻⁶至3×10⁻⁵M)对动作电位影响较小,尽管它增加了心房的收缩力。全细胞膜片钳实验表明,在电压钳制的豚鼠心肌细胞中,姜辣素(1×10⁻⁶至3×10⁻⁵M)对慢内向电流影响较小。使用Ca⁺⁺电极测量细胞外Ca⁺⁺浓度表明,姜辣素(3×10⁻⁶至3×10⁻⁵M)以浓度依赖性方式加速了从犬心肌制备的破碎肌浆网(SR)对Ca⁺⁺的摄取。(摘要截断于250字)

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