School of Pharmacy, Hebei University of Chinese Medicine.
Hebei Key Laboratory of Chinese Medicine Research on Cardio-Cerebrovascular Disease.
Biol Pharm Bull. 2020;43(9):1367-1374. doi: 10.1248/bpb.b20-00298.
Crocetin is a major bioactive ingredient in saffron (Crocus sativus L.) and has favorable cardiovascular effects. Here, the effects of crocetin on L-type Ca current (I), contractility, and the Ca transients of rat cardiomyocytes, were investigated via patch-clamp technique and the Ion Optix system. A 600 µg/mL dose of crocetin decreased I 31.50 ± 2.53% in normal myocytes and 35.56 ± 2.42% in ischemic myocytes, respectively. The current voltage nexus of the calcium current, the reversal of the calcium current, and the activation/deactivation of the calcium current was not changed. At 600 µg/mL, crocetin abated cell shortening by 28.6 ± 2.31%, with a decrease in the time to 50% of the peak and a decrease in the time to 50% of the baseline. At 600 µg/mL, crocetin abated the crest value of the ephemeral Ca by 31.87 ± 2.57%. The time to half maximal of Ca peak and the time constant of decay of Ca transient were both reduced. Our results suggest that crocetin inhibits L-type Ca channels, causing decreased intracellular Ca concentration and contractility in adult rat ventricular myocytes. These findings reveal crocetin's potential use as a calcium channel antagonist for the treatment of cardiovascular disease.
西红花中的主要生物活性成分西红花酸可对心血管系统产生有益影响。本研究采用膜片钳技术和 Ion Optix 系统,研究了西红花酸对大鼠心肌细胞 L 型钙电流(I)、收缩力和钙瞬变的影响。600μg/mL 剂量的西红花酸可使正常心肌细胞中的 I 降低 31.50±2.53%,缺血心肌细胞中的 I 降低 35.56±2.42%。钙电流的电流电压关系、钙电流的反转以及钙电流的激活/失活均未发生改变。在 600μg/mL 时,西红花酸使细胞缩短减少 28.6±2.31%,峰值至 50%的时间和基线至 50%的时间均缩短。在 600μg/mL 时,西红花酸使瞬间 Ca 峰值的峰值降低 31.87±2.57%。钙峰的半最大值时间和钙瞬变的衰减时间常数均缩短。结果表明,西红花酸抑制 L 型钙通道,导致成年大鼠心室心肌细胞内 Ca 浓度和收缩力降低。这些发现表明西红花酸可能作为钙通道拮抗剂用于心血管疾病的治疗。