摘要
目的:研究前列地尔对离体兔主动脉内皮的作用及其可能机制。方法:记录累计浓度的前列地尔对去甲肾上腺素(NA)预收缩的离体兔主动脉环张力的影响,并观察N-硝基-L-精氨酸甲酯(L-NAME)、亚甲蓝(MB)、吲哚美辛(Indo)和2,5-双脱氧腺苷(DDAO)对前列地尔舒张NA预收缩内皮完整血管环的影响,进一步测定前列地尔对血管组织中NO含量及eNOS活性的影响。结果:前列地尔(0.02～10.00μg.L-1)对NA(10-6mol.L-1)预收缩的完整内皮和损伤内皮血管环均有浓度依赖性的舒张作用;但当内皮损伤时,这种舒张作用明显减弱。在内皮完整的血管环,L-NAME(10μmol.L-1)、MB(1μmol.L-1)和DDOA(10μmol.L-1)对前列地尔的舒血管作用存在显著抑制作用;Indo(10μmol.L-1)则无明显影响。前列地尔与血管共孵育后,血管组织中NO含量及eNOS活性均升高,与对照组相比,差异有显著性。结论:前列地尔通过活化eNOS,促进内皮细胞分泌NO,可以引起内皮依赖性舒张,为其临床应用提供了药理学依据。
OBJECTIVE To investigate the effect and mechanism of alprostadil on rabbit thoracic aorta endothelium. METH- ODS The isometric tension of the thoracic aorta rings in response to different concentrations of alprostadilwas measured. Then the aortic rings were divided into control group, L-NAME group, methylene blue （MB） group, 2＇, 5＇-dideoxyadenosine group （DDOA） ,indomethacin （Indo） group, and the aortic ring tension of different groups was measured. Level of NO and activity of eNOS in vascular tissue were also measured after the co-incubation of aorta rings with alprostadil. RESULTS Alprostadil could relax both intact-endothelium and damaged endothelium aorta rings, but the relaxation is lower in damaged endothelium aorta rings. Relaxations of thoracic aorta induced by alprostadil were inhibited by L-NAME, MB and DDOA, but not by Indo. Alpros tadil also markedly increased the levels of NO and eNOS activity in rat aorta tissue. CONCLUSION Alprostadil caused endothelium dependent relaxation through activation of eNOS and secretion of nitric oxide,which shed light on the pharmacological basis for the clinical application of alprostadil.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2010年第7期573-577,共5页
Chinese Journal of Hospital Pharmacy
关键词
前列地尔
主动脉环
血管舒张
内皮功能
一氧化氮
alprostadil
aorta rings
vasorelaxation
endothelial function
nitric oxide
