Liu S F, Cai Y N, Evans T W, McCormack D G, Barer G R, Barnes P J
Department of Thoracic Medicine, National Heart and Lung Institute, London, U.K.
Eur J Pharmacol. 1990 Dec 4;191(3):345-50. doi: 10.1016/0014-2999(90)94167-v.
We have investigated the dilator effect of ligustrazine, the semisynthetic principle of a traditional Chinese herbal remedy, on human pulmonary and bronchial arteries in vitro. Ligustrazine caused a concentration-dependent relaxation of human small pulmonary arteries, which was independent of endothelium. Although ligustrazine was equally potent in inducing dilatation of pulmonary and bronchial arteries, it was about 10 times more potent in relaxing small pulmonary arteries (300-500 microns i.d.) compared with lobar pulmonary arteries (7-8 mm i.d.). By contrast, the relaxant responses of small and lobar pulmonary arteries to sodium nitroprusside was not significantly different. Ligustrazine was equally potent in relaxing prostaglandin F2 alpha- or 5-hydroxytryptamine-precontracted pulmonary arteries, suggesting that it is not a prostaglandin F2 alpha or 5-hydroxytryptamine antagonist. Preincubating the vessels with propranolol (1 microM) or indomethacin (10 microM) had no significant effect on the ligustrazine-induced vasodilatation. However, ligustrazine caused concentration-dependent inhibition of calcium-evoked contraction when applied to rat aorta in calcium-free K(+)-depolarizing medium. We conclude that ligustrazine is a dilator of human pulmonary and bronchial arteries, which is endothelium-independent and that ligustrazine preferentially relaxes pulmonary resistance vessels rather than large conduit pulmonary arteries.
我们已经在体外研究了川芎嗪（一种传统中药的半合成成分）对人肺动脉和支气管动脉的舒张作用。川芎嗪可引起人小肺动脉浓度依赖性舒张，且该作用不依赖于内皮。尽管川芎嗪在诱导肺动脉和支气管动脉扩张方面效力相当，但与叶肺动脉（内径7 - 8毫米）相比，它在舒张小肺动脉（内径300 - 500微米）方面的效力约强10倍。相比之下，小肺动脉和叶肺动脉对硝普钠的舒张反应无显著差异。川芎嗪在舒张前列腺素F2α或5 - 羟色胺预收缩的肺动脉方面效力相当，这表明它不是前列腺素F2α或5 - 羟色胺拮抗剂。用普萘洛尔（1微摩尔）或吲哚美辛（10微摩尔）预孵育血管对川芎嗪诱导的血管舒张无显著影响。然而，在无钙的钾离子去极化培养基中应用于大鼠主动脉时，川芎嗪可引起钙诱发收缩的浓度依赖性抑制。我们得出结论，川芎嗪是一种人肺动脉和支气管动脉的舒张剂，其作用不依赖于内皮，且川芎嗪优先舒张肺阻力血管而非大的肺输送动脉。
