Potential antiarrhythmic effect of methyl 3,4,5-trimethoxycinnamate, a bioactive substance from roots of polygalae radix: suppression of triggered activities in rabbit myocytes.
Potential antiarrhythmic effect of methyl 3,4,5-trimethoxycinnamate, a bioactive substance from roots of polygalae radix: suppression of triggered activities in rabbit myocytes.
复制标题
远志根中的生物活性物质 3,4,5-三甲氧基肉桂酸甲酯的潜在抗心律失常作用：抑制兔肌细胞的触发活动。
DOI：
10.1248/bpb.b12-00654
复制
发表时间：
2013
影响因子：
2
通讯作者：
Lai
中科院分区：
文献类型：
--
作者：
Zhenghang Zhao;Minfeng Fang;D. Xiao;Mei Liu;N. Fefelova;Chen Huang;W. Zang;Lai
3，4，5-三甲氧基肉桂酸(TMCA)、3，4，5-三甲氧基肉桂酸甲酯(M-TMCA)和对甲氧基肉桂酸(PMCA)是口服远志的大鼠血清中的主要生物活性成分。远志是一种缓解失眠、焦虑和心悸的中药。本研究旨在研究其对兔分离的心肌细胞的直接电生理作用。采用膜片钳技术的全细胞构型，测定了酶法分离的成年兔心脏单个心肌细胞的动作电位(AP)和膜电流。用钙指示剂Fluo-4AM负载的心肌细胞中记录到了钙瞬变在远志代谢产物的三种活性物质中，只有M-TMCA(15-30 µM)以浓度依赖和可逆的方式显著缩短心肌细胞50%和90%复极时的动作电位时程(APD50和APD90)。M-TMCA对L钙电流(I(Ca，L))也有抑制作用，但对瞬时外向钾电流(I(TO))和稳态钾电流(I(K，SS))均无影响。此外，M-TMCA取消了异丙肾上腺素加BayK8644诱发的早期后除极(EADs)，抑制了延迟后除极(DAD)和触发活动(TA)。这种潜在的抗心律失常作用可能与抑制细胞内钙瞬变，从而抑制瞬时内向电流(I(Ti))有关。提示M-TMCA可能通过抑制钙通道发挥抗心律失常作用。
3,4,5-Trimethoxycinnamic acid (TMCA), methyl 3,4,5-trimethoxycinnamate (M-TMCA) and p-methoxycinnamic acid (PMCA) have been identified as the major bioactive components in the serum collected from rats treated with oral administration of Polygalae Radix ("YuanZhi," the roots of Polygala tenuifolia WILLD.), a traditional Chinese medicine used to relieve insomnia, anxiety and heart palpitation. The present study was designed to investigate its direct electrophysiological effects on isolated ventricular myocytes from rabbits. Whole-cell configuration of the patch-clamp technique was used to measure action potential (AP) and membrane currents in single ventricular myocytes enzymatically isolated from adult rabbit hearts. Ca(2+) transients were recorded in myocytes loaded with the Ca(2+) indicator Fluo-4AM. Among three bioactive substances of Polygala metabolites, only M-TMCA (15-30 µM) significantly shortened action potential duration at 50% and 90% repolarization (APD(50) and APD(90)) in cardiomyocytes in a concentration-dependent and a reversible manner. M-TMCA also inhibited L-type calcium current (I(Ca,L)), but showed effect on neither transient outward potassium current (I(to)) nor steady-state potassium current (I(K,SS)). Furthermore, M-TMCA abolished isoprenaline plus BayK8644-induced early afterdepolarizations (EADs) and suppressed delayed afterdepolarizations (DADs) and triggered activities (TAs). This potential anti-arrhythmic effects were likely attributed by the inhibition of I(Ca,L) and the suppression of intracellular Ca(2+) transients, which consequently suppress the generation of transient inward current (I(ti)). These findings suggest that M-TMCA may protect the heart from arrhythmias via its inhibitory effect on calcium channel.
登录
查看更多内容
影响因子：
5
作者：
Zhao Z;Fefelova N;Shanmugam M;Bishara P;Babu GJ;Xie LH
通讯作者：
Xie LH
DOI：
10.1152/ajpheart.00742.2011
发表时间：
2012-04-01
影响因子：
4.8
作者：
Zhao, Zhenghang;Wen, Hairuo;Xie, Lai-Hua
通讯作者：
Xie, Lai-Hua
DOI：
10.1152/ajpheart.00390.2009
发表时间：
2009-09-01
影响因子：
4.8
作者：
Xie, Lai-Hua;Weiss, James N.
通讯作者：
Weiss, James N.
胚胎鸡心脏中的 Ca2 瞬变：来自 Ca2 通道和肌浆网的贡献。
DOI：
10.1152/ajpheart.1996.270.2.h518
发表时间：
1996
期刊：
The American journal of physiology.
影响因子：
--
作者：
Brotto,MA;Creazzo,TL
通讯作者：
Creazzo,TL