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小檗碱对豚鼠离体心房的变力性和变时性作用。

Inotropic and chronotropic activity of berberine on isolated guinea pig atria.

作者信息

Shaffer J E

出版信息

J Cardiovasc Pharmacol. 1985 Mar-Apr;7(2):307-15. doi: 10.1097/00005344-198503000-00016.

DOI:10.1097/00005344-198503000-00016
PMID:2581085
Abstract

The cardiac effects of berberine were studied in isolated right and left atrial preparations from guinea pigs. In spontaneously beating right atria, berberine (1 X 10(-5) -3 X 10(-4) M) caused bradycardia, which was not prevented by atropine (1 X 10(-7) M). Over the same concentration range, berberine increased developed force (dF) in left atria electrically driven at 1.5 Hz. This occurred in both untreated and reserpine-treated tissues as well as in the presence of 5 X 10(-7) M propranolol and 1 X 10(-5) M phentolamine. At a stimulation frequency of 1.5 Hz, left atrial responses to each concentration of berberine reached steady state in approximately 10 min. Concentrations of berberine greater than 3 X 10(-4) M depressed dF and increased resting tone until eventually the left atria failed to contract. Analysis of the effects of berberine on the contractile waveform of left atria showed a concentration-dependent increase in maximal positive dF/dt, maximal negative dF/dt, time to peak tension, and relaxation time. When maximal negative dF/dt was normalized for changes in dF (-dF/dt/dF), berberine showed inhibition of the relaxation process. Berberine had only slight effects on post-rest potentiation and paired pulse stimulation, but enhanced the response of left atria to increases in stimulation frequency. From these results, it appears that berberine has a unique profile of action in isolated guinea pig atrial tissue, showing both positive inotropic and negative chronotropic activity. Berberine produces its positive inotropic effect by enhancing both the force-velocity relationship and the duration of the active state.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

在豚鼠离体左右心房标本中研究了黄连素的心脏效应。在自主搏动的右心房中,黄连素(1×10⁻⁵ - 3×10⁻⁴ M)引起心动过缓,阿托品(1×10⁻⁷ M)不能阻止这种情况。在相同浓度范围内,黄连素增加了以1.5 Hz电驱动的左心房的收缩力(dF)。这在未处理和利血平处理的组织中均发生,并且在存在5×10⁻⁷ M普萘洛尔和1×10⁻⁵ M酚妥拉明的情况下也发生。在1.5 Hz的刺激频率下,左心房对每种浓度黄连素的反应在约10分钟内达到稳态。黄连素浓度大于3×10⁻⁴ M时会降低dF并增加静息张力,直到左心房最终停止收缩。对黄连素对左心房收缩波形的影响分析表明,最大正向dF/dt、最大负向dF/dt、达到峰值张力的时间和舒张时间呈浓度依赖性增加。当最大负向dF/dt针对dF的变化进行归一化(-dF/dt/dF)时,黄连素显示出对舒张过程的抑制作用。黄连素对静息后增强和成对脉冲刺激只有轻微影响,但增强了左心房对刺激频率增加的反应。从这些结果来看,黄连素在离体豚鼠心房组织中具有独特的作用特征,表现出正性肌力和负性变时活性。黄连素通过增强力-速度关系和活动状态的持续时间来产生其正性肌力作用。(摘要截断于250字)

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