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目的:研究川芎嗪代谢产物川芎嗪甲酸(CTPZ)对大鼠阴茎海绵体平滑肌细胞(PCSMC)胞质内游离钙离子浓度的影响。方法:用新型Ca~(2+)荧光染色剂Fluo-3/AM负载大鼠PCSMC,细胞分为氯化钾(KCl)和去甲肾上腺素(NE)作用组,应用激光扫描共聚焦显微镜(LSCM)实时测定胞质内[Ca~(2+)]的变化,分别观察不同浓度的CTPZ对高钾和NE诱导胞质内钙浓度升高的影响,并与母药川芎嗪作用相比。结果:静息状态下,CTPZ对大鼠PCSMC胞质内[Ca~(2+)]无明显影响。1,10,100μmol·L~(-1)CTPZ能显著抑制高钾诱发的细胞内的钙浓度升高的影响,抑制率分别为(39.8±4.3)%,(49.2±3.6)%,(58.2±3.9)%。也能抑制1μmol·L~(-1)NE诱发钙库释放的细胞内[Ca~(2+)]升高,抑制率分别为(20.8±3.9)%,(32.3±2.5)%,(43.7±3.2)%。结论:CTPZ对大鼠PCSMC电压依赖性钙通道和细胞内钙库释放的抑制作用,能降低PCSMC胞质内[Ca~(2+)]水平,其作用效果比母药川芎嗪佳。
OBJECTIVE: To study the effect of ligustrazine metabolite Chuanxiongzine formate (CTPZ) on cytosolic intracellular calcium concentration in smooth muscle cells of rat penis corpus cavernosum (PCSMC). METHODS: Rat PCSMCs were loaded with a novel Ca~(2+) fluorescent stain Fluo-3/AM. The cells were divided into potassium chloride (KCl) and norepinephrine (NE) groups. Laser scanning confocal microscopy was used. LSCM was used to measure the changes of [Ca 2+ ] in cytoplasm in real time. The effects of different concentrations of CTPZ on the increase of intracellular calcium concentration induced by high potassium and NE were observed and compared with that of parent drug Chuanxiongzine. RESULTS: At rest, CTPZ had no significant effect on [Ca 2+ ] in the cytoplasm of rat PCSMCs. 1,10,100 μmol·L -1 CTPZ could significantly inhibit the effect of hyperkalemia-induced increase in intracellular calcium concentration. The inhibition rates were (39.8±4.3)%, (49.2±3.6)%, and (58.2±) respectively. 3.9)%. It also inhibited the intracellular [Ca 2+ ] elevation induced by calcium release from 1 μmol·L -1 NE, and the inhibition rates were (20.8±3.9)% and (32.3±2.5)%, respectively (43.7 ±3.2)%. CONCLUSION: CTPZ inhibits the release of voltage-dependent calcium channels and intracellular calcium stores in rat PCSMCs, which can reduce [Ca 2+ ] levels in the cytoplasm of PCSMCs. The effect of CTPZ is better than that of parent drug ligustrazine.