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从中药山豆根中分离得到的苦参碱的心血管效应。

Cardiovascular effects of matrine isolated from the Chinese herb Shan-dou-gen.

作者信息

Wei J W, Liao J F, Chuang C Y, Chen C F, Han P W

出版信息

Proc Natl Sci Counc Repub China B. 1985 Jul;9(3):215-9.

PMID:4070509
Abstract

Matrine, a pure compound isolated from the Chinese herb Shan-don-Gen (Sophora subprostrata), was studied for its effects on the cardiovascular system of the rat. Intravenous injections of matrine at doses from 5 mg to 20 mg/kg body weight exhibited dose-dependent hypotensive and bradycardiac effects. These effects lasted only 1 to 3 min. In the isolated atria and ventricle preparations, matrine at doses from 50 micrograms to 200 micrograms/ml increased the amplitudes of spontaneous contraction of the atria and electrically induced contraction of the ventricle, whereas the frequency of the spontaneous beating of the atria was reduced. The dose-dependent effects of matrine on the isolated preparations persisted as long as the compound was present. Tachyphylaxis was not observed with repeated applications of this compound to the isolated preparations. The positive inotropic effects on both atria and ventricle and the negative chronotropic effect on spontaneous beating of the atria by matrine were not blocked by diphenhydramine, atropine, phenoxybenzamine, propranolol, trifluoperazine, or methysergide. In contrast, verapamil significantly reduced the positive inotropic effect of matrine on the ventricle. In the isolated aortic strip preparation, matrine at a dose of 200 micrograms/ml led to a slight increase in muscle tone. The same dose of matrine induced a 35% increase of perfusion pressure in the hindleg perfusion model. These results suggest that the in vivo transient hypotensive effect of matrine is likely associated with a decrease in heart rate itself, since positive inotropic effects on both the atria and the ventricle, and vasoconstriction of some vascular beds could not be the cause of hypotension.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

苦参碱是从中药山豆根(苦参)中分离出的一种纯化合物,已对其对大鼠心血管系统的作用进行了研究。静脉注射剂量为5毫克至20毫克/千克体重的苦参碱呈现出剂量依赖性的降压和心动过缓作用。这些作用仅持续1至3分钟。在离体心房和心室标本中,剂量为50微克至200微克/毫升的苦参碱可增加心房自发收缩的幅度以及心室电诱导收缩的幅度,而心房自发搏动的频率则降低。只要该化合物存在,苦参碱对离体标本的剂量依赖性作用就会持续。对离体标本重复应用该化合物未观察到快速耐受性。苦参碱对心房和心室的正性肌力作用以及对心房自发搏动的负性变时作用不受苯海拉明、阿托品、酚苄明、普萘洛尔、三氟拉嗪或甲基麦角新碱的阻断。相比之下,维拉帕米显著降低了苦参碱对心室的正性肌力作用。在离体主动脉条标本中,剂量为200微克/毫升的苦参碱导致肌张力略有增加。相同剂量的苦参碱在后肢灌注模型中使灌注压升高了35%。这些结果表明,苦参碱在体内的短暂降压作用可能与心率本身的降低有关,因为对心房和心室的正性肌力作用以及某些血管床的血管收缩不可能是低血压的原因。(摘要截短至250字)

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Cardiovascular effects of matrine isolated from the Chinese herb Shan-dou-gen.从中药山豆根中分离得到的苦参碱的心血管效应。
Proc Natl Sci Counc Repub China B. 1985 Jul;9(3):215-9.
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Matrine inhibits vascular smooth muscle cell proliferation by modulating the expression of cell cycle regulatory genes.苦参碱通过调节细胞周期调控基因的表达抑制血管平滑肌细胞增殖。
Acta Pharmacol Sin. 2010 Oct;31(10):1329-35. doi: 10.1038/aps.2010.145. Epub 2010 Sep 13.