【摘要】 目的研究血根碱（San）对小鼠肠系膜血管及血管平滑肌细胞（VSMCs）收缩的抑制作用;并观察其对RhoA相关蛋白激酶（ROCK1）表达的影响,探讨引起该抑制作用的作用机制。方法利用微血管张力测定仪（DMT）,测定San对血管收缩工具药氯化钾（KCl）预收缩后微血管的张力影响,并计算血管平滑肌松弛作用的IC50值;进一步利用成像分析技术观测San对KCl预收缩VSMCs后的影响,最后通过蛋白免疫印迹以及细胞免疫荧光法测定San对VSMCs中ROCK1蛋白的表达水平的影响。结果与ROCK1抑制剂法舒地尔（Fas）比较(IC₅₀为14.34μmol·L^-1),San对KCl预收缩的肠系膜动脉的松弛作用较强,其IC50为1.098μmol·L^-1,且呈现不（弱）可逆的趋势。进一步在细胞水平上验证,与模型组（KCl）VSMCs的长度（40.03±4.91）μm比较,药物组（KCl+San）VSMCs的长度（46.12±6.37）μm显著延长（P<0.01）。蛋白免疫印迹与免疫荧光结果发现San可显著抑制ROCK1蛋白表达（P<0.01）。结论 San对KCl诱导的肠系膜血管平滑肌收缩具有明显的抑制作用,其作用机制可能与调控ROCK1蛋白表达相关。更多还原

【Abstract】 Objective To study the inhibitory effect of sanguinarine（San） on the contraction of mouse mesentericvessel and vascular smooth muscle cells（VSMCs）;and to observe its effect on the expression of RhoA-associatedprotein kinase（ROCK1） and to explore the mechanism of the inhibition. Methods The microvasculature tension ofVSMCs was determined using a microvessel tension meter（DMT） after being precontracted by vasocontractorpotassium chloride（KCl）. The IC₅₀ value of relaxing vascular smooth muscle was calculated and KCl-precontractedVSMCs was further observed using imaging analysis technique. Finally,the expression of ROCK1 protein in VSMCswas detected by Western Blot and immunofluorescence. Results Compared with ROCK1 inhibitor fasudil（Fas）(IC50was 14.34 μmol·L^-1),San had a stronger relaxation effect on mesenteric artery preconstricted by KCl with IC50 of 1.098 μmol·L^-1and showed no（weak） reversibility. Compared with the length of VSMCs（40.03±4.91 μm） in model group（KCl）,the length of VSMCs（46.12±6.37） μm of drug group（KCl+San） was significantly prolonged（P < 0.01）. Western Blot and immunofluorescence detection showed that San could significantly inhibit theexpression of ROCK1 protein（P < 0.01）. Conclusion San has a significant inhibitory effect on KCl-inducedmesenteric vascular smooth muscle contraction,and its mechanism may be related to the down-regulation of ROCK1 protein.更多还原