A Novel Toxin from Haplopelma lividum Selectively Inhibits the NaV1.8 Channel and Possesses Potent Analgesic Efficacy
文献类型：期刊论文
| 作者 | Meng P1,2,3; Huang HG4,5; Liu JZ[*]7; Lai R[*]1,2,3; Rong MQ[*]1,2,3; Wang G6; Yang SL1,2,3; Lu QM1,2,3 |
| 刊名 | Toxins
 |
| 出版日期 | 2017 |
| 卷号 | 9期号:X页码:e7 |
| 关键词 | NaV1.8 analgesia neurotoxin spider venom |
| 通讯作者 | jzliu21@heinfo.net ; rlai@mail.kiz.ac.cn ; rongmingqiang@mail.kiz.ac.cn |
| 英文摘要 | Spider venoms are a complex mixture of peptides with a large number of neurotoxins targeting ion channels. Although thousands of peptide toxins have been identified from venoms of numerous species of spiders, many unknown species urgently need to be investigated. In this study, a novel sodium channel inhibitor, µ-TRTX-Hl1a, was identified from the venom of Haplopelma lividum. It contained eight cysteines and formed a conserved cysteine pattern of ICK motif. µ-TRTX-Hl1a inhibited the TTX-resistant (TTX-r) sodium channel current rather than the TTX-sensitive (TTX-s) sodium channel current. Meanwhile, µ-TRTX-Hl1a selectively inhibited NaV1.8 with an IC50 value of 2.19 μM. Intraperitoneal injection of µ-TRTX-Hl1a dose-dependently reduced inflammatory and neuropathic pain in rodent models of formalin-induced paw licking, tail-flicking, acetic acid-induced writhing, and hot plate test. It showed a better analgesic effect than morphine in inflammatory pain and equipotent effect to morphine in neuropathic pain. These findings demonstrate that µ-TRTX-Hl1a might be a valuable tool for physiology studies on NaV1.8 and a promising lead molecule for pain therapeutics. |
| 收录类别 | SCI |
| 资助信息 | This work was supported by NSFC (31372208, U1302221, 81573320, 31600721), CAS (SAJC201308, SAJC201606) and Yunnan Province (2016FA008, 2015BC005, 2016FA006), the West light Doctoral program and Youth Innovation Promotion Association of China academic of science. Honggang Huang was supported by the postdoctoral fellowship from the Danish Diabetes Academy financed by the Novo Nordisk Foundation, Denmark. |
| 语种 | 英语 |
| 源URL | [http://159.226.149.26:8080/handle/152453/10795]  |
| 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.Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences & Yunnan Province, Kunming Institute of Zoology, Kunming 650223, Yunnan, China 2.United Laboratory of Natural Peptide of University of Science and Technology of China & Kunming Institute of Zoology, Chinese Academy of Science, Kunming 650223, Yunnan, China 3.Sino-African Joint Research Center, Chinese Academy of Science, Wuhan 430074, Hubei, China 4.Department of Biochemistry and Molecular Biology, University of Southern Denmark, Odense 5230, Denmark 5.The Danish Diabetes Academy, Odense 5230, Denmark 6.Life Sciences College, Nanjing Agricultural University, Nanjing 210095, Jiangsu, China 7.Key Laboratory of Animal Physiology, Biochemistry and Molecular Biology of Hebei Province, College of Life Sciences, Hebei Normal University, Shijiazhuang 050024, Hebei, China |
| 推荐引用方式 GB/T 7714 | Meng P,Huang HG,Liu JZ[*],et al. A Novel Toxin from Haplopelma lividum Selectively Inhibits the NaV1.8 Channel and Possesses Potent Analgesic Efficacy[J]. Toxins,2017,9(X):e7. |
| APA | Meng P.,Huang HG.,Liu JZ[*].,Lai R[*].,Rong MQ[*].,...&Lu QM.(2017).A Novel Toxin from Haplopelma lividum Selectively Inhibits the NaV1.8 Channel and Possesses Potent Analgesic Efficacy.Toxins,9(X),e7. |
| MLA | Meng P,et al."A Novel Toxin from Haplopelma lividum Selectively Inhibits the NaV1.8 Channel and Possesses Potent Analgesic Efficacy".Toxins 9.X(2017):e7. |
入库方式： OAI收割
来源：昆明动物研究所
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