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芳樟烷类化合物在子宫松弛活性方面的构效关系。

Structure-activity relationships of aromadendranes in uterus-relaxant activity.

机构信息

Escuela de Medicina, Universidad Autónoma del Estado de Hidalgo, Eliseo Ramirez Ullua 400, Col. Doctores, Pachuca, Hidalgo, 42001, México.

出版信息

Z Naturforsch C J Biosci. 2009 Nov-Dec;64(11-12):840-6. doi: 10.1515/znc-2009-11-1214.

Abstract

Aromadendranes belong to a class of sesquiterpenes present in higher plant essential oils and marine animals. Although the biological activities include antifungal, antibacterial, antiviral, plant growth regulatory, antifeedant, repellent and cytotoxic, there is only one precedent for spasmolytic effects. In a previous report we have shown that the aromadendrene molecule known as spathulenol, isolated from Lepechinia caulescens, efficiently relaxes rat uterus rings and therefore in the present work we describe structure-activity relationships of thirteen aromadendranes, most of them having the trans-fused perhydroazulene skeleton, with spasmolytic activity.

摘要

阿罗玛二萜属于倍半萜类化合物,存在于高等植物精油和海洋动物中。虽然其生物活性包括抗真菌、抗菌、抗病毒、植物生长调节、拒食、驱避和细胞毒性,但仅有一个关于松弛平滑肌的先例。在之前的一份报告中,我们已经表明,从 Lepechinia caulescens 中分离出来的 known as spathulenol 的阿罗玛二萜分子能够有效地松弛大鼠子宫环,因此在本工作中,我们描述了十三种阿罗玛二萜的结构-活性关系,其中大多数具有顺式稠合的全氢薁骨架,具有松弛平滑肌的活性。

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