Xiao-Shan He, Qing Lin, Yun-Shu Ma, Ze-Pu Yu
Yunnan University of Traditional Chinese Medicine, Kunming 650500, China.
Chin J Nat Med. 2014 Jan;12(1):20-3. doi: 10.1016/S1875-5364(14)60004-2.
To study the effects of crebanine on voltage-gated Na(+) channels in cardiac tissues.
Single ventricular myocytes were enzymatically dissociated from adult guinea-pig heart. Voltage-dependent Na(+) current was recorded using the whole cell voltage-clamp technique.
Crebanine reversibly inhibited Na(+) current with an IC50 value of 0.283 mmol·L(-1) (95% confidence range: 0.248-0.318 mmol·L(-1)). Crebanine at 0.262 mmol·L(-1) caused a negative shift (about 12 mV) in the voltage-dependence of steady-state inactivation of Na(+) current, and retarded its recovery from inactivation, but did not affect its activation curve.
In addition to blocking other voltage-gated ion channels, crebanine blocked Na(+) channels in guinea-pig ventricular myocytes. Crebanine acted as an inactivation stabilizer of Na(+) channels in cardiac tissues.
研究克班宁对心脏组织电压门控性钠通道的作用。
采用酶解法从成年豚鼠心脏分离单个心室肌细胞。运用全细胞膜片钳技术记录电压依赖性钠电流。
克班宁可逆性抑制钠电流，IC50值为0.283 mmol·L⁻¹（95%可信区间：0.248 - 0.318 mmol·L⁻¹）。0.262 mmol·L⁻¹的克班宁使钠电流稳态失活的电压依赖性发生负向偏移（约12 mV），并延缓其从失活状态的恢复，但不影响其激活曲线。
除阻断其他电压门控性离子通道外，克班宁还可阻断豚鼠心室肌细胞的钠通道。克班宁在心脏组织中作为钠通道的失活稳定剂发挥作用。
