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(-)-Naringenin 4 ',7-dimethyl Ether Isolated from Nardostachys jatamansi Relieves Pain through Inhibition of Multiple Channels

文献类型：期刊论文

作者Gu, Ru-Rong2,3; Meng, Xian-Hua4,5; Zhang, Yin3; Xu, Hai-Yan3; Zhan, Li3; Gao, Zhao-Bing1,2,3,6; Yang, Jun-Li4,5; Zheng, Yue-Ming3
刊名MOLECULES
出版日期2022-03-01
卷号27期号:5页码:17
关键词(-)-Naringenin 4 ',7-dimethyl ether analgesic candidate mechanism study delayed rectifier potassium currents ion channels
DOI10.3390/molecules27051735
通讯作者Gao, Zhao-Bing(zbgao@simm.ac.cn) ; Yang, Jun-Li(yangjl@licp.cas.cn) ; Zheng, Yue-Ming(zhengyueming@simm.ac.cn)
英文摘要(-)-Naringenin 4',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 (-)-NRG-DM can dose dependently (30 similar to 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 similar to 30 mu M) potently dampened the stimulated firing, reduced the action potential threshold and amplitude. In addition, the neuronal delayed rectifier potassium currents (I-K) and voltage-gated sodium currents (I-Na) were significantly suppressed. Consistently, (-)-NRG-DM dramatically inhibited heterologously expressed Kv2.1 and Nav1.8 channels which represent the major components of the endogenous I K and I Na . A pharmacokinetic study revealed the plasma concentration of (-)-NRG-DM is around 7 mu M, which was higher than the effective concentrations for the I-K and I-Na . Taken together, our study showed that (-)-NRG-DM is a potential analgesic candidate with inhibition of multiple neuronal channels (mediating I-K and I-Na).
WOS关键词DORSAL-ROOT GANGLION ; GATED POTASSIUM CHANNELS ; K+ CURRENT ; COMPONENT ; NEURONS ; TARGET
资助项目National Science Fund for Distinguished Young Scholars[81825021] ; National Natural Science Foundation of China[81773707] ; National Natural Science Foundation of China[32161143019] ; Youth Innovation Promotion Association of the Chinese Academy of Sciences[2020284] ; Fund of Science and Technology Commission of Shanghai Municipality[19431906000] ; Natural Science Foundation of Gansu Province[20JR5RA570] ; CAS Pioneer Hundred Talents Program
WOS研究方向Biochemistry & Molecular Biology ; Chemistry
语种英语
WOS记录号WOS:000775635800001
出版者MDPI
源URL[http://119.78.100.183/handle/2S10ELR8/299967]  
专题中国科学院上海药物研究所
通讯作者Gao, Zhao-Bing; Yang, Jun-Li; Zheng, Yue-Ming
作者单位1.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
2.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China
3.Chinese Acad Sci, Ctr Neurol & Psychiat Res & Drug Discovery, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
4.Chinese Acad Sci, Lanzhou Inst Chem Phys, CAS Key Lab Chem Northwestern Plant Resources, Lanzhou 730000, Peoples R China
5.Chinese Acad Sci, Lanzhou Inst Chem Phys, Key Lab Nat Med Gansu Prov, Lanzhou 730000, Peoples R China
6.Chinese Acad Sci, Zhongshan Inst Drug Discovery, Inst Drug Discovery Innovat, Zhongshan 528400, Peoples R China
推荐引用方式
GB/T 7714		 Gu, Ru-Rong,Meng, Xian-Hua,Zhang, Yin,et al. (-)-Naringenin 4 ',7-dimethyl Ether Isolated from Nardostachys jatamansi Relieves Pain through Inhibition of Multiple Channels[J]. MOLECULES,2022,27(5):17.
APA Gu, Ru-Rong.,Meng, Xian-Hua.,Zhang, Yin.,Xu, Hai-Yan.,Zhan, Li.,...&Zheng, Yue-Ming.(2022).(-)-Naringenin 4 ',7-dimethyl Ether Isolated from Nardostachys jatamansi Relieves Pain through Inhibition of Multiple Channels.MOLECULES,27(5),17.
MLA Gu, Ru-Rong,et al."(-)-Naringenin 4 ',7-dimethyl Ether Isolated from Nardostachys jatamansi Relieves Pain through Inhibition of Multiple Channels".MOLECULES 27.5(2022):17.

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来源：上海药物研究所

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