Ca(v)2.2 and Ca(v)3.1 calcium channel inhibitors from Valeriana jatamansi Jones
文献类型：期刊论文
| 作者 | Jiang, He-Hai1,3; Dong, Wu2,4; Zhou, Jun2 ; Hu, Jiang-Miao2; Yang, Jian1; Nian, Yin1
|
| 刊名 | RSC ADVANCES
 |
| 出版日期 | 2017 |
| 卷号 | 7期号:72页码:45878-45884 |
| ISSN号 | 2046-2069 |
| 关键词 | Iridoids Pain Antagonist Blocker Roots |
| DOI | 10.1039/c7ra07327e |
| 英文摘要 | 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. |
| 学科主题 | Chemistry, Multidisciplinary |
| 语种 | 英语 |
| WOS记录号 | WOS:000412147000075 |
| 源URL | [http://ir.kib.ac.cn/handle/151853/54972]  |
| 专题 | 昆明植物研究所_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. |
入库方式： OAI收割
来源：昆明植物研究所
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