摘要
目的:研究对氯苄基四氢小檗碱(CPU-86017)及其光学异构体对内钙释放及外钙内流引起的血管平滑肌收缩的抑制作用。方法:以有钙、无钙液中加高钾(KCl)100mmol·L-1或苯肾上腺素1μmol·L-1并在无钙液中复钙引起的大鼠胸主动脉环的收缩,比较CPU-86017及其光学异构体对内钙释放及外钙内流引起的血管平滑肌收缩的抑制作用。结果:CPU-86017及其4种光学异构体均能抑制KCl引起的内钙释放,外钙内流,其中,Zh003、Zh004作用强于CPU-86017;Zh001、Zh002作用弱于CPU-86017。对于苯肾上腺素引起的内钙释放与外钙内流,Zh004有明显的抑制作用,而Zh001、Zh002与Zh003作用不明显,均能抑制KCl引起的内钙释放与外钙内流。结论:与CPU-86017相比,Zh001、Zh002和Zh003对α受体阻断作用明显降低,Zh003与受体调控钙通道几乎没有作用,对电压依赖钙通道的阻断作用,Zh003和Zh004活性增强。
AIM：To compare the effect of p-Chlorobenzyletrahydroberberine（CPU-86017） and its four kinds of optical isomers Zh001, Zh002, Zh003 and Zh004 on intracellular calcium mobilization and calcium entry by suppression on isolated vascular smooth contraction. METHODS： CPU-86017 and four kinds of optical isomers （ 10, 30,100 μmol·L^-1） were applied to suppress 6 kinds of contractions performed as below. Group 1 ： KCl （ 100 mmol·L^-1 ） induced contractions in normal K-H solution; Group 2： KCl caused contractions in Ca^2＋ -free K-H solution; Group 3： contractions induced by adding 3.0 mmol·L^-1 CaCI2 to the Ca^2＋-free K-H solution after using KCl caused contractions in Ca^2＋ -free K-H solution： Performing the same procedure as the former except for using phenylephrine instead of KCl. RESULTS： All the compounds inhibited the contraction induced by intracellular calcium release and extra-cellular calcium entry induced by KCl. The potencies of Zh003 and Zh004 were higher than that of CPU-86107 while Zh001 and Zh002 were lower. Zh004 had significant inhibitory effect on phenylephrine intracellular calcium release and extracellular calcium entry, and the effects of Zh001, Zh002 and Zh003 were faint. CONCLUSION： For the blocking effect on α-adrenergic receptor, Zh001, Zh002 and Zh003 decreased evidently when compared with CPU-86017. Zh003 almost had no blocking effect on receptor-operated channel. The inhibitory effects on vohage-depencled channel of Zh003 and Zh004 were increased.
出处
《中国天然药物》
SCIE
CAS
CSCD
2006年第6期456-459,共4页
基金
国家自然科学基金资助项目(No.30230170)~~
