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埃塞俄比亚肉豆蔻和阿玛蒂姆比卡刺苞果的贝壳杉烯衍生物的心血管和利尿活性。

Cardiovascular and diuretic activity of kaurene derivatives of Xylopia aethiopica and Alepidea amatymbica.

作者信息

Somova L I, Shode F O, Moodley K, Govender Y

机构信息

Department of Human Physiology, University of Durban-Westville, Private Bag X54001, Durban, South Africa.

出版信息

J Ethnopharmacol. 2001 Oct;77(2-3):165-74. doi: 10.1016/s0378-8741(01)00285-9.

DOI:10.1016/s0378-8741(01)00285-9
PMID:11535360
Abstract

The extractives, crude and pure, of Alepidea amatymbica (AA) and Xylopia aethiopica (XA) were subjected to bioassay-directed phytochemical examination for potential cardiovascular and diuretic activity. All extractives and derivatives (XA/O, AA/1, xylopic acid, AA/3, AA/4, AA/5, AA/6, XA/1, XA/2, XA/3) displayed low toxicity, with LC(50) 0.5-5.0 ng/ml. For the first time, diterpene kaurenoids were reported to have significant systemic hypotensive and coronary vasodilatory effect accompanied with bradycardia. These effects were attributed to calcium antagonistic mechanism. The diuretic and natriuretic effects found were similar to the effects of chlorothiazide, suggesting inhibition of Na+ and K+ reabsorption in the early portion of the distal tubule. Further experiments are needed to elaborate the exact mechanisms of the hypotensive and diuretic effects of diterpene kaurenoids.

摘要

对阿非利加阿莱皮德草(AA)和埃塞俄比亚卡皮木(XA)的粗提取物和纯提取物进行了生物测定导向的植物化学检查,以检测其潜在的心血管和利尿活性。所有提取物和衍生物(XA/O、AA/1、木脂酸、AA/3、AA/4、AA/5、AA/6、XA/1、XA/2、XA/3)均显示低毒性,半数致死浓度(LC50)为0.5 - 5.0纳克/毫升。首次报道二萜贝壳杉烯类化合物具有显著的全身降压和冠状血管舒张作用,并伴有心动过缓。这些作用归因于钙拮抗机制。所发现的利尿和利钠作用与氯噻嗪的作用相似,表明其抑制了远曲小管起始段的Na+和K+重吸收。需要进一步的实验来阐明二萜贝壳杉烯类化合物降压和利尿作用的确切机制。

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