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苔藓中环二联苄类化合物的血管舒张作用。

Vasorelaxant effects of macrocyclic bis(bibenzyls) from liverworts.

机构信息

Faculty of Pharmaceutical Sciences, Hoshi University, Tokyo, Japan.

出版信息

Bioorg Med Chem. 2011 Jul 1;19(13):4051-6. doi: 10.1016/j.bmc.2011.05.019. Epub 2011 May 19.

Abstract

Vasorelaxant effects of a series of bis(bibenzyls) from liverworts such as Marchantia polymorpha and Marchantia paleacea on rat aorta demonstrated that they relaxed phenylephrine (PE)-induced contractions, which may be mediated through the increased release of NO from endothelial cells as well as opening of K(+) channels, and inhibition of Ca(2+) influx through voltage-dependent Ca(2+) channels (VDCs) and/or receptor-operated Ca(2+) channels (ROCs). Structure-activity relationship based on their structures was discussed. The presence of two aromatic rings which can be connected through two atoms bridge spacer may play an important role for vasorelaxant effect.

摘要

从地钱属植物如多形扁枝衣和苍白扁枝衣中分离得到的一系列双(联苄基)对大鼠主动脉具有血管舒张作用,表明它们可以通过增加内皮细胞中一氧化氮(NO)的释放以及开放钾(K+)通道来舒张去甲肾上腺素(PE)诱导的收缩,抑制通过电压依赖性钙(Ca2+)通道(VDCs)和/或受体操作的钙(Ca2+)通道(ROCs)的 Ca2+内流。还讨论了基于它们结构的构效关系。两个芳香环可以通过两个原子桥间隔物连接,这可能对血管舒张作用起着重要作用。

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