Structurally modified Cyclovirobuxine-D Buxus alkaloids as effective analgesic agents through Cav3.2 T-Type calcium channel inhibition
文献类型：期刊论文
| 作者 | Munikishore,Rachakunta; Liu,Rui; Zhang,Shuqun; Zhao,Qin-Shi; Nian,Yin ; Zuo,Zhili
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| 刊名 | BIOORGANIC CHEMISTRY
 |
| 出版日期 | 2023 |
| 卷号 | 135页码:106493 |
| 关键词 | Buxus alkaloid Structural modification T -type calcium channel Analgesic activity Docking analysis Structure -activity relationship study BUXOZINE-C SEMPERVIRENS RING CONSTITUTION |
| ISSN号 | 1090-2120 |
| DOI | 10.1016/j.bioorg.2023.106493 |
| 英文摘要 | Cyclovirobuxine-D (CVB-D) is a Buxus alkaloid and a major active constituent in the Chinese medicinal herb Buxus microphylls. Traditionally, the natural alkaloid cyclovirobuxine-D has a long history of use as a traditional Chinese medicine for cardiovascular diseases as well as to treat a wide variety of medical conditions. As we found that CVB-D inhibited T-type calcium channels, we designed and synthesized a variety of fragments and analogues and evaluated them for the first time as new Cav3.2 inhibitors. Compounds 2-7 exhibited potency against Cav 3.2 channels, and two of them were more active than their parent molecules. As a result of the in vivo experiments, both compounds 3 and 4 showed significantly reduced writhes in the acetic acid-induced writhing test. Studies of molecular modeling have identified possible mechanism(s) of Cav3.2 binding. Moreover, the relationship be-tween structure and activity was studied in a preliminary manner. Our results indicated that compounds 3 and 4 could play an important role in the discovery and development of novel analgesics. |
| 学科主题 | Biochemistry & Molecular Biology ; Chemistry |
| WOS记录号 | WOS:000967346200001 |
| 源URL | [http://ir.kib.ac.cn/handle/151853/75478]  |
| 专题 | 中国科学院昆明植物研究所 |
| 推荐引用方式 GB/T 7714 | Munikishore,Rachakunta,Liu,Rui,Zhang,Shuqun,et al. Structurally modified Cyclovirobuxine-D Buxus alkaloids as effective analgesic agents through Cav3.2 T-Type calcium channel inhibition[J]. BIOORGANIC CHEMISTRY,2023,135:106493. |
| APA | Munikishore,Rachakunta,Liu,Rui,Zhang,Shuqun,Zhao,Qin-Shi,Nian,Yin,&Zuo,Zhili.(2023).Structurally modified Cyclovirobuxine-D Buxus alkaloids as effective analgesic agents through Cav3.2 T-Type calcium channel inhibition.BIOORGANIC CHEMISTRY,135,106493. |
| MLA | Munikishore,Rachakunta,et al."Structurally modified Cyclovirobuxine-D Buxus alkaloids as effective analgesic agents through Cav3.2 T-Type calcium channel inhibition".BIOORGANIC CHEMISTRY 135(2023):106493. |
入库方式： OAI收割
来源：昆明植物研究所
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