| Ca(v)2.2 and Ca(v)3.1 calcium channel inhibitors from Valeriana jatamansi Jones | |
Jiang, He-Hai1,3; Dong, Wu2,4; Zhou, Jun2 ; Hu, Jiang-Miao2; Yang, Jian1; Nian, Yin1
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| 2017 | |
| 发表期刊 | RSC ADVANCES
 |
| ISSN | 2046-2069 |
| 卷号 | 7期号:72页码:45878-45884 |
| 摘要 | In China, the roots and rhizomes of Valeriana jatamansi Jones are traditionally used to treat gastrointestinal and rheumatic pain. Small molecule inhibitors of N-type (Ca(v)2.2) and T-type (Ca(v)3.1-3.3) calcium channels have become attractive resources in analgesic drug development. Therefore, in the present study, the isolated compounds (1-13) from V. jatamansi, including three new valepotriates (1-3), were initially evaluated on Ca(v)2.2 and Ca(v)3.1. As a result, compounds 1-12 showed weak to potent inhibition on Ca(v)2.2 peak currents at 30 mu M. Among them, compounds 1, 6, 7, 11 and 12 exhibited significant antagonistic effects, with EC50 values of 4.33, 2.18, 1.13, 2.70 and 7.8 mu M, respectively. Meanwhile, the aforementioned compounds exhibited 18.2 +/- 2.5% to 49.2 +/- 7.1% peak current inhibition on Ca(v)3.1 at 30 mu M. In addition, they also exhibited noticeable specificity against Ca(v)1.2, Ca(v)2.1, and KCNH2 (hERG) channels. |
| 关键词 | Iridoids Pain Antagonist Blocker Roots |
| 学科领域 | Chemistry, Multidisciplinary |
| DOI | 10.1039/c7ra07327e |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000412147000075 |
| 引用统计 | |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://ir.kib.ac.cn/handle/151853/54972 |
| 专题 | 植物化学与西部植物资源持续利用国家重点实验室 |
| 作者单位 | 1.Chinese Acad Sci, Key Lab Bioact Peptides Yunnan Prov, Key Lab Anim Models & Human Dis Mech, Ion Channel Res & Drug Dev Ctr,Kunming Inst Zool, Kunming 650223, Yunnan, Peoples R China 2.Chinese Acad Sci, State Key Lab Phytochem & Plant Resources West Ch, Kunming Inst Bot, Kunming 650201, Yunnan, Peoples R China 3.Kunming Univ Sci & Technol, Fac Life Sci & Technol, Kunming 650504, Yunnan, Peoples R China 4.Yunnan Univ Tradit Chinese Med, Fac Pharm, Kunming 650500, Yunnan, Peoples R China |
| 推荐引用方式 GB/T 7714 | Jiang, He-Hai,Dong, Wu,Zhou, Jun,et al. Ca(v)2.2 and Ca(v)3.1 calcium channel inhibitors from Valeriana jatamansi Jones[J]. RSC ADVANCES,2017,7(72):45878-45884. |
| APA | Jiang, He-Hai,Dong, Wu,Zhou, Jun,Hu, Jiang-Miao,Yang, Jian,&Nian, Yin.(2017).Ca(v)2.2 and Ca(v)3.1 calcium channel inhibitors from Valeriana jatamansi Jones.RSC ADVANCES,7(72),45878-45884. |
| MLA | Jiang, He-Hai,et al."Ca(v)2.2 and Ca(v)3.1 calcium channel inhibitors from Valeriana jatamansi Jones".RSC ADVANCES 7.72(2017):45878-45884. |
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| 10.1039@c7ra07327e.p（678KB） | 期刊论文 | 作者接受稿 | 开放获取 | CC BY-NC-SA | 浏览 下载 | |
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