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目的研究唐古特红景天舒张大鼠肺小动脉的活性部位及其作用机制。方法利用大孔吸附树脂制备唐古特红景天95%乙醇提取物的不同洗脱流份(去离子水,30%乙醇,70%乙醇,95%乙醇)。采用大鼠肺小动脉血管环离体灌流技术,筛选药物舒血管作用的活性部位。制备内皮完整及去内皮血管环,验证活性部位舒血管作用的靶点。利用去甲肾上腺素(NE)及氯化钾(KCl)预收缩血管环,明确活性部位的舒血管作用与钙通道的关系。利用左旋硝基精氨酸甲酯(L-NAME)、四乙基氯化铵(TEA)、氯化钡(Ba Cl2)预处理血管环,阐释活性部位影响血管张力的机制。结果大孔吸附树脂的70%乙醇洗脱流份是唐古特红景天95%乙醇提取物舒张肺小动脉的活性部位。活性部位可剂量依赖性地舒张肺小动脉,其对内皮完整血管环的作用强于对去内皮血管环的作用,两者比较,差异具有统计学意义(P<0.01)。活性部位舒血管的作用与其抑制细胞膜受体门控性钙通道有关。L-NAME、TEA、和Ba Cl2三种阻断剂能够不同程度地减弱活性部位对肺小动脉血管环的舒张作用。结论唐古特红景天舒血管作用的活性部位主要富集于大孔吸附树脂70%乙醇洗脱物里,其舒血管的效应主要作用于血管内皮,且呈现剂量依赖性。唐古特红景天舒张大鼠肺小动脉的可能作用机制:1、通过抑制细胞膜受体门控性钙通道,减少Ca2+流入血管平滑肌细胞引起血管舒张;2、作用于肺小动脉内皮,促进内皮细胞释放一氧化氮(NO)至平滑肌使平滑肌舒张;3、作用于肺小动脉平滑肌的钾离子通道,促进通道开放引起血管平滑肌舒张。
Objective To study the active site of pulmonary arterioles and its possible mechanism in Diabetic rats. Methods Different fractions (deionized water, 30% ethanol, 70% ethanol, 95% ethanol) of 95% ethanol extract of Rhodiola sachalinensis were prepared by macroporous adsorption resin. The rat pulmonary arteriolar vascular ring perfusion technique was used to screen the active site of drug vasodilatation. Preparation of endothelial integrity and endothelium-derived vascular rings to verify the active site of vasodilator target. The use of norepinephrine (NE) and potassium chloride (KCl) precontracted vascular rings, clear vasodilatation of the active site and the relationship between calcium channels. The vascular rings were pretreated with L-NAME, TEA and Ba Cl2, and the mechanism of the active site affecting the vascular tone was explained. Results The 70% ethanol elution fraction of macroporous resin was the active site of relaxation pulmonary arterioles of 95% ethanol extract of Rhodiola sachalinensis. The active site can relax the pulmonary arterioles in a dose-dependent manner, which has a stronger effect on the intact endothelium than on the endothelium. There is significant difference between the two groups (P <0.01). The vasodilator activity of the active site is related to its inhibition of cell-membrane receptor-gated calcium channels. L-NAME, TEA, and Ba Cl2 three kinds of blockers to varying degrees, weakened the active site of pulmonary arterial vascular relaxation. CONCLUSION: The active site of Rhodiola is mainly enriched in 70% ethanol eluate of macroporous adsorption resin, and its vasodilator effect mainly acts on the vascular endothelium in a dose-dependent manner. Tanggut Rhodiola lobe rat pulmonary arterioles possible mechanism: 1, by inhibiting cell membrane receptor-gated calcium channels, reducing the flow of Ca2 + into vascular smooth muscle cells to cause vasodilatation; 2, acting on the pulmonary arterioles endothelial, promote endothelial Cells release nitric oxide (NO) to the smooth muscle to relax the smooth muscle; 3, acting on the smooth muscle of pulmonary arterioles, potassium channels to promote the opening of the channel to cause vascular smooth muscle relaxation.