Morita Hiroshi, Iizuka Toru, Choo Chee-Yan, Chan Kit-Lam, Takeya Koichi, Kobayashi Jun'ichi
Faculty of Pharmaceutical Sciences, Hoshi University, Shinagawa-ku, Tokyo, Japan.
Bioorg Med Chem Lett. 2006 Sep 1;16(17):4609-11. doi: 10.1016/j.bmcl.2006.06.008. Epub 2006 Jun 19.
A cyclic octapeptide, cyclosquamosin B (2), isolated from the seeds of Annona squamosa showed a vasorelaxant effect on rat aorta. It showed a slow relaxation activity against norepinephrine (NE)-induced contractions of rat aorta with/without endothelium. It showed inhibition effect on vasocontraction of depolarized aorta with high concentration potassium, but moderately inhibition effect on NE-induced contraction in the presence of nicardipine. These results showed that the vasorelaxant effect by 2 might be attributed mainly to inhibition of calcium influx from extracellular space through voltage-dependent calcium channels.
从番荔枝种子中分离得到的一种环状八肽环鳞木辛B(2)对大鼠主动脉具有血管舒张作用。它对去甲肾上腺素(NE)诱导的有/无内皮的大鼠主动脉收缩表现出缓慢的舒张活性。它对高浓度钾去极化主动脉的血管收缩有抑制作用,但在尼卡地平存在的情况下对NE诱导的收缩有中度抑制作用。这些结果表明,2的血管舒张作用可能主要归因于抑制细胞外空间通过电压依赖性钙通道的钙内流。