李新天, 王幼林, 王金唏, 杨思军. 四氢原小檗碱类药物对培养大鼠单个心肌细胞内游离Ca2+的影响J. 药学学报, 1995, 30(8): 567-572.
引用本文: 李新天, 王幼林, 王金唏, 杨思军. 四氢原小檗碱类药物对培养大鼠单个心肌细胞内游离Ca2+的影响J. 药学学报, 1995, 30(8): 567-572.
XT Li, YL Wang, JX Wang , SJ Yang, . EFFECTS OF TETRAHYDROPROTOBERBERINES ON CYTOSOLIC FREE CALCIUM IN CULTURED RAT SINGLE MYOCARDIAL CELLSJ. Acta Pharmaceutica Sinica, 1995, 30(8): 567-572.
Citation: XT Li, YL Wang, JX Wang , SJ Yang, . EFFECTS OF TETRAHYDROPROTOBERBERINES ON CYTOSOLIC FREE CALCIUM IN CULTURED RAT SINGLE MYOCARDIAL CELLSJ. Acta Pharmaceutica Sinica, 1995, 30(8): 567-572.

四氢原小檗碱类药物对培养大鼠单个心肌细胞内游离Ca2+的影响

EFFECTS OF TETRAHYDROPROTOBERBERINES ON CYTOSOLIC FREE CALCIUM IN CULTURED RAT SINGLE MYOCARDIAL CELLS

  • 摘要: 用Fura-2/AM技术和AR-CM-MIC阳离子测定系统,直接测定了四氢小檗碱(tetrahy-droberberine,THB)、左旋四氢巴马汀(l-tetrahydropalmatine,THP)和左旋千金藤立定(l-stepholidine,SPO)对培养大鼠单个心室肌细胞内游离钙(Ca2+i)的影响,并与维拉帕米(Ver)做了比较。结果显示,THB,THP,SPD浓度为10~100μmol·L-1时,均可使静息Ca2+i轻度升高,河豚毒素不能抑制之;浓度为1~100μmol·L-1时,可明显抑制高K+引起的Ca2+i增高;30μmol·L-1对胞外高Ca2+和去甲肾上腺素引起的Ca2+i增高也有明显的抑制作用,但均较Ver的抑制作用为弱;THPB对哇巴因引起的ca2+i升高无明显抑制作用。结果提示,THB,THP,SPD在抑制电压依赖性钙通道从而影响细胞膜ca2+i内流方面与Ver相似,但比Ver弱。

     

    Abstract: Effect of tetrahydroberberine(THB),l-tetrahydropalmatine(THP) and l-stepholi-dine(SPD) were supposed to be related to the blocking of calcium influx. In this paper,using Fura-2/AM and AR- CM-MIC cation measurement system,the effects of THB,THP and SPD on cytosolicfree calcium(Ca2+i) in cultured rat single myocardial cells were examined and compared withverapamil(Ver). TH,THP and SPD(10~100μmol·L-1) were found to increase restingCa2+i gently,which was not depressed by tetrodotoxin. THB,THP and SPD(1~100μmol·L-1)were also shown to inhibit the KCl- inducedCa2+i elevation, the IC50 values of THBand SPD were 50.9(95%confidence limits: 18.5~140)μmol·L-1 and 23.5(95%confidencelimits 7.6~73.4)μmol·L-1, respectively. THB, THP and SPD 30μmol·L-1 were also shown toinhibit the elevation ofCa2+i induced by high extracellular calcium and norepinephrine; but theinhibitory effects of these drugs were weaker than those of Ver. The three compounds showed nosignificant effect on ouabain inducedCa2+i increas1e. These results suggest that the inhibitory effects of THB, THP and SPD on Ca2+i in myocite by blocking voltage- dependent calcium channels were similar but inferior to Ver.

     

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