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
2017
发表期刊RSC ADVANCES
ISSN2046-2069
卷号7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
收录类别SCI
语种英语
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.
条目包含的文件 下载所有文件
文件名称/大小 文献类型 版本类型 开放类型 使用许可
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
个性服务
推荐该条目
保存到收藏夹
查看访问统计
导出为Endnote文件
谷歌学术
谷歌学术中相似的文章
[Jiang, He-Hai]的文章
[Dong, Wu]的文章
[Zhou, Jun]的文章
百度学术
百度学术中相似的文章
[Jiang, He-Hai]的文章
[Dong, Wu]的文章
[Zhou, Jun]的文章
必应学术
必应学术中相似的文章
[Jiang, He-Hai]的文章
[Dong, Wu]的文章
[Zhou, Jun]的文章
相关权益政策
暂无数据
收藏/分享
文件名: 10.1039@c7ra07327e.pdf
格式: Adobe PDF
所有评论 (0)
暂无评论
 

除非特别说明,本系统中所有内容都受版权保护,并保留所有权利。