Structure-activity relationship of Baifuzi-cerebrosides on BKCa channel activation

被引：7

作者：

Zhou, Li ^{[1
]}

Zhang, Yu-Jiao ^{[1
]}

Gao, Li-Juan ^{[2
]}

Ye, Ying ^{[2
]}

Qi, Jian-Hua ^{[2
]}

Qi, Zhi ^{[1
]}

机构：

[1] Xiamen Univ, Dept Basic Med Sci, Coll Med, Xiamen 361102, Peoples R China

[2] Zhejiang Univ, Coll Pharmaceut Sci, Hangzhou 310058, Zhejiang, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 75卷

基金：

中国国家自然科学基金;

关键词：

Baifuzi-cerebroside; Ischemic stroke; BKCa channel; RECEPTOR POTENTIAL CHANNELS; CA2+-ACTIVATED K+ CHANNELS; FATTY-ACIDS; POTASSIUM CHANNELS; ISCHEMIC STROKE; ION CHANNELS; CONDUCTANCE; MODULATION; BETA; REPOLARIZATION;

D O I：

10.1016/j.ejmech.2014.01.007

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Our previous study reported that a mixture of cerebrosides from traditional Chinese medicine Baifuzi could activate BKCa channel. It is curious to know the effect of each single cerebroside on the channel. Here we isolated 5 pure cerebrosides from the mixture and determined their chemical structures. The most potent one increased the single channel open probability 6 folds with EC50 value of 1.0 mu M. The structure activity relationship revealed that acyl chain length of cerebrosides has potent effect, while configuration of double bond at C8-C9 on their long chain base has weak effect on the channel activity. Thus, this research provides a guide for design and synthesis of a lead cerebroside with more potent effect on the BKCa channel. (C) 2014 Elsevier Masson SAS. All rights reserved.

引用

页码：301 / 307

页数：7

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