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鸡骨常山属植物中阿朴菲类生物碱的心血管效应。

Cardiovascular effects of aspidofractinine-type alkaloids from Kopsia.

作者信息

Mok S L, Yoganathan K, Lim T M, Kam T S

机构信息

Department of Pharmacology, University of Malaya, Kuala Lumpur, Malaysia.

出版信息

J Nat Prod. 1998 Mar;61(3):328-32. doi: 10.1021/np9703712.

DOI:10.1021/np9703712
PMID:9544563
Abstract

Intravenous injection of the aspidofractinine alkaloid, kopsingine (1, 0.2-10.0 mg/kg) from Kopsia teoi, produced dose-related decreases in the mean arterial blood pressure and heart rate in anesthetized spontaneously hypertensive rats, which were similar to those seen in normotensive controls. Minor modifications in the molecular structure of kopsingine, as in kopsaporine (2, the 12-demethoxy derivative of kopsingine) and 14,15-dihydrokopsingine (4), did not significantly alter the hypotensive responses, whereas a more drastic change in the structure, as in the heptacyclic kopsidine A (3) and the 3-to-17 oxo-bridged compound 5, resulted in an increase in blood pressure. The antihypertensive effects of kopsingine (1) and its congeners (2 and 4) along with the pressor effects produced by the heptacyclic oxo-bridged compounds (5 and 3) could be ascribed to central as well as peripheral actions.

摘要

静脉注射从特奥氏蕊木中提取的阿朴菲类生物碱柯辛宁(1,0.2 - 10.0毫克/千克),可使麻醉的自发性高血压大鼠的平均动脉血压和心率呈剂量依赖性下降,这与正常血压对照大鼠的情况相似。柯辛宁分子结构的微小改变,如在柯萨波林(2,柯辛宁的12 - 去甲氧基衍生物)和14,15 - 二氢柯辛宁(4)中,并未显著改变其降压反应,而结构上更剧烈的变化,如在七环柯西定A(3)和3至17氧桥联化合物5中,则导致血压升高。柯辛宁(1)及其同系物(2和4)的降压作用以及七环氧桥联化合物(5和3)产生的升压作用可归因于中枢和外周作用。

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