Selective Activation of Nociceptor TRPV1 Channel and Reversal of Inflammatory Pain in Mice by a Novel Coumarin Derivative Muralatin L from Murraya alata
文献类型：期刊论文
| 作者 | Wei NN1; Lv HN2; Wu Y3; Yang SL4; Sun XY5; Lai R4; Jiang Y[*]2; Wang KW[*]1,3,5 |
| 刊名 | JOURNAL OF BIOLOGICAL CHEMISTRY
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| 出版日期 | 2016 |
| 卷号 | 192期号:2页码:640-651 |
| 关键词 | calcium calcium imaging drug discovery drug screening ion channel neuron transient receptor potential channels (TRP channels) |
| 通讯作者 | yongjiang@bjmu.edu.cn |
| 合作状况 | 其它 |
| 英文摘要 | Coumarin and its derivatives are fragrant natural compounds isolated from the genus Murraya that are flowering plants widely distributed in East Asia, Australia, and the Pacific Islands. Murraya plants have been widely used as medicinal herbs for relief of pain, such as headache, rheumatic pain, toothache, and snake bites. However, little is known about their analgesic components and the molecular mechanism underlying pain relief. Here, we report the bioassay-guided fractionation and identification of a novel coumarin derivative, named muralatin L, that can specifically activate the nociceptor transient receptor potential vanilloid 1 (TRPV1) channel and reverse the inflammatory pain in mice through channel desensitization. Muralatin L was identified from the active extract of Murraya alata against TRPV1 transiently expressed in HEK-293T cells in fluorescent calcium FlexStation assay. Activation of TRPV1 current by muralatin L and its selectivity were further confirmed by whole-cell patch clamp recordings of TRPV1-expressing HEK-293T cells and dorsal root ganglion neurons isolated from mice. Furthermore, muralatin L could reverse inflammatory pain induced by formalin and acetic acid in mice but not in TRPV1 knock-out mice. Taken together, our findings show that muralatin L specifically activates TRPV1 and reverses inflammatory pain, thus highlighting the potential of coumarin derivatives from Murraya plants for pharmaceutical and medicinal applications such as pain therapy. |
| 资助信息 | This work was supported by Ministry of Science and Technology of China Research Grants 2013CB531302, 2013ZX09103001-015, and 2014 ZX09507003-006-004 (to K. W. W.), National Natural Sciences Foundation of China Grants 81222051 and 81473106, and National Key Tech- nology R&D Program “New Drug Innovation” of China Grants 2012ZX09301002-002-002 and 2012ZX09304-005 (to Y. J.). The authors declare that they have no conflicts of interest with the contents of this article. |
| 收录类别 | SCI |
| 语种 | 英语 |
| 源URL | [http://159.226.149.26:8080/handle/152453/9565]  |
| 专题 | 昆明动物研究所_动物毒素室 昆明动物研究所_动物模型与人类重大疾病机理重点实验室 |
| 作者单位 | 1.Department of Neurobiology and Neuroscience Research Institute, School of Basic Medical Sciences, Peking University Health Science Center. 2.State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191 3.Department of Molecular and Cellular Pharmacology, IDG/McGovern Institute for Brain Research, Peking University School of Pharmaceutical Sciences, Beijing 100191. 4.Key Laboratory of Animal Models and Human Disease Mechanisms, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, Yunnan 5.Department of Pharmacology, Qingdao University School of Pharmacy, Qingdao 266021, China. |
| 推荐引用方式 GB/T 7714 | Wei NN,Lv HN,Wu Y,et al. Selective Activation of Nociceptor TRPV1 Channel and Reversal of Inflammatory Pain in Mice by a Novel Coumarin Derivative Muralatin L from Murraya alata[J]. JOURNAL OF BIOLOGICAL CHEMISTRY,2016,192(2):640-651. |
| APA | Wei NN.,Lv HN.,Wu Y.,Yang SL.,Sun XY.,...&Wang KW[*].(2016).Selective Activation of Nociceptor TRPV1 Channel and Reversal of Inflammatory Pain in Mice by a Novel Coumarin Derivative Muralatin L from Murraya alata.JOURNAL OF BIOLOGICAL CHEMISTRY,192(2),640-651. |
| MLA | Wei NN,et al."Selective Activation of Nociceptor TRPV1 Channel and Reversal of Inflammatory Pain in Mice by a Novel Coumarin Derivative Muralatin L from Murraya alata".JOURNAL OF BIOLOGICAL CHEMISTRY 192.2(2016):640-651. |
入库方式： OAI收割
来源：昆明动物研究所
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