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球花夏枯草亚种黎巴嫩夏枯草中半日花烷二萜类化合物的解痉作用及构效关系

Antispasmodic effects and structure-activity relationships of labdane diterpenoids from Marrubium globosum ssp. libanoticum.

作者信息

Rigano Daniela, Aviello Gabriella, Bruno Maurizio, Formisano Carmen, Rosselli Sergio, Capasso Raffaele, Senatore Felice, Izzo Angelo A, Borrelli Francesca

机构信息

Department of Chemistry of Natural Products, University of Naples Federico II, Via D. Montesano 49, 80131 Naples, Italy.

出版信息

J Nat Prod. 2009 Aug;72(8):1477-81. doi: 10.1021/np9002756.

DOI:10.1021/np9002756
PMID:19650652
Abstract

Marrubium globosum ssp. libanoticum is a medicinal plant used in Lebanon to reduce pain and smooth muscle spasms. A chloroform extract obtained from M. globosum aerial parts reduced acetylcholine-induced contractions in the isolated mouse ileum. The purification of this extract identified, among 12 isolated labdane diterpenoids, four new compounds, named 13-epicyllenin A (4), 13,15-diepicyllenin A (5), marrulibacetal (9), and marrulactone (11). Their structures were determined by spectroscopic methods. Compound 9, which exerted antispasmodic activity, is likely the active ingredient of the extract. Preliminary structure-activity relationships for this class of compounds are suggested.

摘要

圆叶绵枣儿黎巴嫩亚种是黎巴嫩一种用于减轻疼痛和平滑肌痉挛的药用植物。从圆叶绵枣儿地上部分获得的氯仿提取物可降低离体小鼠回肠中乙酰胆碱诱导的收缩。对该提取物进行纯化后,在12种分离得到的半日花烷二萜类化合物中鉴定出4种新化合物,分别命名为13-表西列宁A(4)、13,15-二表西列宁A(5)、绵枣儿缩醛(9)和绵枣儿内酯(11)。通过光谱方法确定了它们的结构。具有抗痉挛活性的化合物9可能是该提取物的活性成分。本文还提出了这类化合物初步的构效关系。

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