Antinociceptive activities and mechanism of action of Cepharanthine
文献类型：期刊论文
| 作者 | Wei, Xiang-Yan1,2; Long, Jian-Dong1; Chai, Jing-Rui1; Chen, Jing1 ; Gao, Jian-Ping2; Wang, Yu-Jun1; Liu, Jing-Gen1
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| 刊名 | BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
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| 出版日期 | 2022-07-23 |
| 卷号 | 614页码:219-224 |
| 关键词 | Cepharanthine Antinociception mu opioid receptors Constipation |
| ISSN号 | 0006-291X |
| DOI | 10.1016/j.bbrc.2022.04.083 |
| 通讯作者 | Gao, Jian-Ping(zydgjp@aliyun.com) ; Wang, Yu-Jun(yjwang@simm.ac.cn) |
| 英文摘要 | Cepharanthine is an alkaloid that isolated from Stephania cepharantha Hayata, however , its analgesic properties are unclear and the molecular targets that mediating Cepharanthine-induced analgesia are not explored yet. In the current study, mice pain models including hot plate, acetic acid-induced writhing and formalin tests were conducted to evaluate the antinociceptive actions of Cepharanthine. [H-3]-ligand competitive binding assay was applied to determine the binding affinity and selectivity of Cepharanthine at kappa, mu and delta opioid receptors. Cepharanthine-induced constipation was investigated using the small intestinal transit test. The results showed that intraperitoneal injection of Cepharanthine produced potent antinociception with an ED50 value of 24.5 mg/kg in the acetic acid-induced writhing test. In the formalin test, Cepharanthine produced moderate antinociception with the maximum analgesic activity of 42.6 +/- 11.3% in phase I and 60.1 +/- 7.7% in phase II, respectively. Cepharanthine had no effects in the hot plate test. In vitro radioligand binding assay, Cepharanthine exhibited a high affinity for mu opioid receptors with a Ki value of 80 nM, without binding to kappa and delta opioid receptors. Correspondingly, Cepharanthine-mediated antinociceptive effects were antagonized by pretreatment with opioid receptor antagonist naloxone. Cepharanthine also decreased the small intestine propulsion rates in the small intestinal transit test. Together, this study firstly demonstrates that Cepharanthine produces potent antinociception in acetic acid-induced visceral pain and moderate antinociception in formalin-induced inflammatory pain, and its mechanism of action may be through activation of mu opioid receptors. (C) 2022 Published by Elsevier Inc. |
| WOS关键词 | OPIOID RECEPTOR AGONIST ; ALKALOID CEPHARANTHINE ; CELLS |
| 资助项目 | Science and Technology Commission of Shanghai Municipality[20ZR1468200] ; National Natural Science Foundation of China[82030112] ; National Natural Science Foundation of China[81773710] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Biophysics |
| 语种 | 英语 |
| WOS记录号 | WOS:000809809500012 |
| 出版者 | ACADEMIC PRESS INC ELSEVIER SCIENCE |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/301567]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Gao, Jian-Ping; Wang, Yu-Jun |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Key Lab Receptor Res, Shanghai 201203, Peoples R China 2.Shanghai Univ Tradit Chinese Med, Dept Pharmacol, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wei, Xiang-Yan,Long, Jian-Dong,Chai, Jing-Rui,et al. Antinociceptive activities and mechanism of action of Cepharanthine[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,2022,614:219-224. |
| APA | Wei, Xiang-Yan.,Long, Jian-Dong.,Chai, Jing-Rui.,Chen, Jing.,Gao, Jian-Ping.,...&Liu, Jing-Gen.(2022).Antinociceptive activities and mechanism of action of Cepharanthine.BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,614,219-224. |
| MLA | Wei, Xiang-Yan,et al."Antinociceptive activities and mechanism of action of Cepharanthine".BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS 614(2022):219-224. |
入库方式： OAI收割
来源：上海药物研究所
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