Structure-activity relationship of Baifuzi-cerebrosides on BKCa channel activation
Zhou, L; Zhang, YJ; Gao, LJ; Ye, Y; Qi, JH; Qi, Z
| HERO ID | 2902754 |
|---|---|
| In Press | No |
| Year | 2014 |
| Title | Structure-activity relationship of Baifuzi-cerebrosides on BKCa channel activation |
| Authors | Zhou, L; Zhang, YJ; Gao, LJ; Ye, Y; Qi, JH; Qi, Z |
| Journal | European Journal of Medicinal Chemistry |
| Volume | 75 |
| Page Numbers | 301-307 |
| Abstract | 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 μM. 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. |
| Doi | 10.1016/j.ejmech.2014.01.007 |
| Pmid | 24556145 |
| Wosid | WOS:000333775600031 |
| Is Certified Translation | No |
| Dupe Override | No |
| Is Public | Yes |
| Language Text | English |