(-)-Naringenin 4’,7-Dimethyl Ether Isolated from Nardostachys jatamansi Relieves Pain Through Inhibition of Multiple Channels | |
Department | 中科院西北特色植物资源化学重点实验室/甘肃省天然药物重点实验室 |
Ru-Rong Gu1,2; Xian-Hua Meng3; Yin Zhang2; Hai-Yan Xu2; Li Zhan2; Zhao-Bing Gao1,2,4,5; Jun-Li Yang3; Yue-Ming Zheng2 | |
The second department | 药物化学与新药分子研究团队 |
2022 | |
Source Publication | Molecules |
Volume | 5Issue:27Pages:1735 |
Abstract | (-)-Naringenin 40,7-dimethyl ether ((-)-NRG-DM) was isolated for the first time by our lab from Nardostachys jatamansi DC, a traditional medicinal plant frequently used to attenuate pain in Asia. As a natural derivative of analgesic, the current study was designed to test the potential analgesic activity of (-)-NRG-DM and its implicated mechanism. The analgesic activity of (-)-NRG-DM was assessed in a formalin-induced mouse inflammatory pain model and mustard oilinduced mouse colorectal pain model, in which the mice were intraperitoneally administrated with vehicle or (-)-NRG-DM (30 or 50 mg/kg) (n = 10 for each group). Our data showed that (-)-NRGDM can dose dependently (30~50 mg/kg) relieve the pain behaviors. Notably, (-)-NRG-DM did not affect motor coordination in mice evaluated by the rotarod test, in which the animals were intraperitoneally injected with vehicle or (-)-NRG-DM (100, 200, or 400 mg/kg) (n = 10 for each group). In acutely isolated mouse dorsal root ganglion neurons, (-)-NRG-DM (1~30 _M) potently dampened the stimulated firing, reduced the action potential threshold and amplitude. In addition, the neuronal delayed rectifier potassium currents (IK) and voltage-gated sodium currents (INa) were significantly suppressed. Consistently, (-)-NRG-DM dramatically inhibited heterologously expressed Kv2.1 and Nav1.8 channels which represent the major components of the endogenous IK and INa. A pharmacokinetic study revealed the plasma concentration of (-)-NRG-DM is around 7 _M, which was higher than the effective concentrations for the IK and INa. Taken together, our study showed that (-)-NRG-DM is a potential analgesic candidate with inhibition of multiple neuronal channels (mediating IK and INa). |
Keyword | (-)-Naringenin 40,7-dimethyl ether analgesic candidate mechanism study delayed rectifier potassium currents ion channels |
DOI | 10.3390/molecules27051735 |
If | 4.927 |
Language | 英语 |
compositor | 第三作者单位 |
Citation statistics | |
Document Type | 期刊论文 |
Identifier | http://ir.licp.cn/handle/362003/29299 |
Collection | 中科院西北特色植物资源化学重点实验室/甘肃省天然药物重点实验室 |
Corresponding Author | Zhao-Bing Gao; Jun-Li Yang; Yue-Ming Zheng |
Affiliation | 1.School of Chinese Materia Medica, Nanjing University of Chinese Medicine 2.Center for Neurological and Psychiatric Research and Drug Discovery, Shanghai Institute of Materia Medica, Chinese Academy of Sciences 3.CAS Key Laboratory of Chemistry of Northwestern Plant Resources and Key Laboratory for Natural Medicine of Gansu Province, Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences (CAS) 4.Zhongshan Institute of Drug Discovery, Institution for Drug Discovery Innovation, Chinese Academy of Sciences 5.University of Chinese Academy of Sciences |
Recommended Citation GB/T 7714 | Ru-Rong Gu,Xian-Hua Meng,Yin Zhang,等. (-)-Naringenin 4’,7-Dimethyl Ether Isolated from Nardostachys jatamansi Relieves Pain Through Inhibition of Multiple Channels[J]. Molecules,2022,5(27):1735. |
APA | Ru-Rong Gu.,Xian-Hua Meng.,Yin Zhang.,Hai-Yan Xu.,Li Zhan.,...&Yue-Ming Zheng.(2022).(-)-Naringenin 4’,7-Dimethyl Ether Isolated from Nardostachys jatamansi Relieves Pain Through Inhibition of Multiple Channels.Molecules,5(27),1735. |
MLA | Ru-Rong Gu,et al."(-)-Naringenin 4’,7-Dimethyl Ether Isolated from Nardostachys jatamansi Relieves Pain Through Inhibition of Multiple Channels".Molecules 5.27(2022):1735. |
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