中国生化药物杂志
中國生化藥物雜誌
중국생화약물잡지
CHINESE JOURNAL OF BIOCHEMICAL PHARMACEUTICS
2015年
4期
70-73
,共4页
心宝丸%电生理学%HCN4 通道%瞬时电流%双电极电压钳%非洲爪蟾卵母细胞
心寶汍%電生理學%HCN4 通道%瞬時電流%雙電極電壓鉗%非洲爪蟾卵母細胞
심보환%전생이학%HCN4 통도%순시전류%쌍전겁전압겸%비주조섬란모세포
XinBao pill%electrophysiology%HCN4 channel%instantaneous current%double electrode voltage clamp%Xenopus Iaevis oocytes
目的：探讨心宝丸对人超极化激活环核苷酸门控阳离子通道4（hyperpolarization-activated cyclic nucleotide-gated channel 4，HCN4）电生理特性的影响，从基础医学上阐明心宝丸治疗心动过缓的机制。方法将人HCN4的mRNA 注射到非洲爪蟾卵母细胞，孵育2～3 d后，采用双电极电压钳技术观察40 mg／L心宝丸灌流液对HCN4通道电流的作用特点。结果测试电位－90 mV时40 mg／L心宝丸灌流液与对照组（无心宝丸的灌流液）相比，HCN4通道峰电流和尾电流有明显变化，半数最大激活电压（ V1／2）分别由（－103.61±3.57）mV、（－81.11±4.26）mV 变为（－106.42±5.33）mV、（－86.36±7.44）mV，斜率因子（k）分别由（15.15±2.23）mV、（11.78±0.85）mV变为（l7.33±3.58）mV、（12.39±1.51）mV （n＝10）。测试电位－90 mV时，40 mg／L 心宝丸灌流液使瞬时电流减少了（0.15±0.24）％，EC50为（30.8±4.8） mg／L （n＝8）。测试电位－140 mV到－100 mV 水平上，40 mg／L 心宝丸灌流液与对照组（无心宝丸的灌流液）相比延长HCN4通道激活时间常数：[（226.73±31.36）ms vs（143.67±21.44）ms；－140 mV，n＝10，P＜0.05]。40 mg／L心宝丸灌流液与对照组（无心宝丸的灌流液）相比延长HCN4通道去激活时间常数[（1293.53±95.02） ms vs （647.12±61.35）ms；－140 mV，n＝10，P＜0.05]。结论心宝丸呈浓度依赖性增强HCN4瞬时电流，延长通道激活和去激活过程。
目的：探討心寶汍對人超極化激活環覈苷痠門控暘離子通道4（hyperpolarization-activated cyclic nucleotide-gated channel 4，HCN4）電生理特性的影響，從基礎醫學上闡明心寶汍治療心動過緩的機製。方法將人HCN4的mRNA 註射到非洲爪蟾卵母細胞，孵育2～3 d後，採用雙電極電壓鉗技術觀察40 mg／L心寶汍灌流液對HCN4通道電流的作用特點。結果測試電位－90 mV時40 mg／L心寶汍灌流液與對照組（無心寶汍的灌流液）相比，HCN4通道峰電流和尾電流有明顯變化，半數最大激活電壓（ V1／2）分彆由（－103.61±3.57）mV、（－81.11±4.26）mV 變為（－106.42±5.33）mV、（－86.36±7.44）mV，斜率因子（k）分彆由（15.15±2.23）mV、（11.78±0.85）mV變為（l7.33±3.58）mV、（12.39±1.51）mV （n＝10）。測試電位－90 mV時，40 mg／L 心寶汍灌流液使瞬時電流減少瞭（0.15±0.24）％，EC50為（30.8±4.8） mg／L （n＝8）。測試電位－140 mV到－100 mV 水平上，40 mg／L 心寶汍灌流液與對照組（無心寶汍的灌流液）相比延長HCN4通道激活時間常數：[（226.73±31.36）ms vs（143.67±21.44）ms；－140 mV，n＝10，P＜0.05]。40 mg／L心寶汍灌流液與對照組（無心寶汍的灌流液）相比延長HCN4通道去激活時間常數[（1293.53±95.02） ms vs （647.12±61.35）ms；－140 mV，n＝10，P＜0.05]。結論心寶汍呈濃度依賴性增彊HCN4瞬時電流，延長通道激活和去激活過程。
목적：탐토심보환대인초겁화격활배핵감산문공양리자통도4（hyperpolarization-activated cyclic nucleotide-gated channel 4，HCN4）전생리특성적영향，종기출의학상천명심보환치료심동과완적궤제。방법장인HCN4적mRNA 주사도비주조섬란모세포，부육2～3 d후，채용쌍전겁전압겸기술관찰40 mg／L심보환관류액대HCN4통도전류적작용특점。결과측시전위－90 mV시40 mg／L심보환관류액여대조조（무심보환적관류액）상비，HCN4통도봉전류화미전류유명현변화，반수최대격활전압（ V1／2）분별유（－103.61±3.57）mV、（－81.11±4.26）mV 변위（－106.42±5.33）mV、（－86.36±7.44）mV，사솔인자（k）분별유（15.15±2.23）mV、（11.78±0.85）mV변위（l7.33±3.58）mV、（12.39±1.51）mV （n＝10）。측시전위－90 mV시，40 mg／L 심보환관류액사순시전류감소료（0.15±0.24）％，EC50위（30.8±4.8） mg／L （n＝8）。측시전위－140 mV도－100 mV 수평상，40 mg／L 심보환관류액여대조조（무심보환적관류액）상비연장HCN4통도격활시간상수：[（226.73±31.36）ms vs（143.67±21.44）ms；－140 mV，n＝10，P＜0.05]。40 mg／L심보환관류액여대조조（무심보환적관류액）상비연장HCN4통도거격활시간상수[（1293.53±95.02） ms vs （647.12±61.35）ms；－140 mV，n＝10，P＜0.05]。결론심보환정농도의뢰성증강HCN4순시전류，연장통도격활화거격활과정。
Objective To explore the basic medical mechanism of XinBao pill on electrophysiological characteristics of hyperpolarization-activated cyclic nucleotide-gated channel 4 (HCN4), and illustrate the mechanism of its therapeutical effect on bradycardia.Methods Human HCN4 mRNA was injected into the Xenopus laevis oocytes, after incubated for 2 ~3 days, channel current properties of HCN4 perfused with 40 mg/L XinBao Pill were observed by double electrode voltage clamp technique.Results At-90mV test potential, compared with control group (no XinBao pill), HCN4 channel peak current and tail current in 40 mg/L XinBao pill group had obvious changes, and V1/2 from ( -103.61 ±3.57)mV to ( -106.42 ±5.33)mV in XinBao pill group, from( -81.11 ±4.26)mV to( -86.36 ±7.44)mV in control group.The values of k from (15.15 ±2.23)mV to (17.33 ±3.58) mV in XinBao pill group, from(11.78 ±0.85)mV to(12.39 ±1.51)mV in control group(n=10).At test potential -90 mV, 40 mg/L XinBao pill perfusion fluid decreased the instantaneous current of(0.15 ±0.24)%, the EC50 was (30.8 ±4.8)mg/L (n=8).At test potential-140 mV~-100 mV level, 40 mg/L XinBao pill group increased the channel activation time constant compared with control group[(226.73 ±31.36)ms vs(143.67 ± 21.44)ms;-140 mV,n=10,P<0.05].40 mg/L XinBao pill group increased the channel deactivation time constant compared with control group [(1293.53 ±95.02)ms vs (647.12 ±61.35)ms;-140 mV,n=10,P<0.05].Conclusion The XinBao pill enhances the instantaneous current of HCN4 in a concentration-dependent manner, and extents channel activation and deactivation processes.
