S-蜂斗菜素和蜂斗菜内酯通过阻断电压门控钙通道来扩张血管，并阻断DNA合成。
S-petasin and butterbur lactones dilate vessels through blockage of voltage gated calcium channels and block DNA synthesis.
作者信息
Sheykhzade Majid, Smajilovic Sanela, Issa Ali, Haunso Stig, Christensen Søren Brøgger, Tfelt-Hansen Jacob
机构信息
Department of Pharmacology and Pharmacotherapy, Faculty of Pharmaceutical Sciences, University of Copenhagen, Copenhagen, Denmark.
出版信息
Eur J Pharmacol. 2008 Sep 28;593(1-3):79-86. doi: 10.1016/j.ejphar.2008.07.004. Epub 2008 Jul 10.
Eremophilanlactones isolated from roots of Petasites hybridus (L.) G.M. et Sch. (Asteraceae) and S-petasin have vasodilatory effects with pD(2) -log (EC(50)) values of 6.01+/-0.08, 5.24+/-0.10, 4.74+/-0.13, and 5.43+/-0.06 for S-petasin, the (Z)-3-methylthioacrylic ester of 2beta-hydroxy-8betaH-7(11)-eremophilene-12,8-olide, the angelic ester of 2beta-hydroxy-8alphaH-7(11)-eremophilene-12,8-olide, and the angelic ester of 2beta-hydroxy-8betaH-7(11)-eremophilene-12,8-olide, respectively, in the mesenteric arteries. The pD(2) values were somewhat lower for all compounds in aortic segments. The vasodilation was caused by a blockage of the voltage gated calcium channels. S-petasin, (Z)-3-methylthioacrylic ester of 2beta-hydroxy-8betaH-7(11)-eremophilene-12,8-olide, and the angelic ester of 2beta-hydroxy-8alphaH-7(11)-eremophilene-12,8-olide displayed similar potencies in inhibiting DNA synthesis in cardiomyocytes and vascular smooth muscle cells.
从蜂斗菜（Petasites hybridus (L.) G.M. et Sch.，菊科）根部分离得到的雅槛蓝内酯和S-蜂斗菜素具有血管舒张作用，在肠系膜动脉中，S-蜂斗菜素、2β-羟基-8βH-7(11)-雅槛蓝烯-12,8-内酯的(Z)-3-甲硫基丙烯酸酯、2β-羟基-8αH-7(11)-雅槛蓝烯-12,8-内酯的当归酸酯以及2β-羟基-8βH-7(11)-雅槛蓝烯-12,8-内酯的当归酸酯的pD(2) -log (EC(50))值分别为6.01±0.08、5.24±0.10、4.74±0.13和5.43±0.06。在主动脉段中，所有化合物的pD(2)值均略低。血管舒张是由电压门控钙通道的阻断引起的。S-蜂斗菜素、2β-羟基-8βH-7(11)-雅槛蓝烯-12,8-内酯的(Z)-3-甲硫基丙烯酸酯以及2β-羟基-8αH-7(11)-雅槛蓝烯-12,8-内酯的当归酸酯在抑制心肌细胞和血管平滑肌细胞DNA合成方面表现出相似的效力。
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