Faculty of Pharmaceutical Sciences, Hoshi University, Shinagawa-ku, Tokyo, Japan.
Bioorg Med Chem. 2011 Jul 1;19(13):4075-9. doi: 10.1016/j.bmc.2011.05.014. Epub 2011 May 14.
Villocarines A-D (1-4), four new indole alkaloids have been isolated from the leaves of Uncaria villosa (Rubiaceae) and their structures were elucidated by 2D NMR methods and chemical correlations. Villocarine A (1) showed vasorelaxation activity against rat aortic ring and showed inhibition effect on vasocontraction of depolarized aorta with high concentration potassium, and also inhibition effect on phenylephrine (PE)-induced contraction in the presence of nicardipine in a Ca(2+) concentration-dependent manner. The vasorelaxant effect by 1 might be attributed mainly to inhibition of calcium influx from extracellular space through voltage-dependent calcium channels (VDC) and/or receptor-operated Ca(2+)-channels (ROC), and also partly mediated through the increased release of NO from endothelial cells and opening of voltage-gated K(+)-channels.
从钩藤（Rubiaceae）的叶子中分离得到了 4 种新的吲哚生物碱，分别为 Villocarines A-D（1-4）。通过二维 NMR 方法和化学相关确定了它们的结构。Villocarine A（1）对大鼠主动脉环具有血管舒张活性，并对高浓度钾引起的去极化主动脉血管收缩具有抑制作用，同时也对存在尼卡地平时由苯肾上腺素（PE）引起的收缩具有抑制作用，这种抑制作用呈钙离子浓度依赖性。1 的血管舒张作用主要归因于抑制电压依赖性钙通道（VDC）和/或受体操纵性钙通道（ROC）从细胞外空间流入钙离子，同时部分通过增加内皮细胞中一氧化氮的释放和开放电压门控钾通道来介导。
