Structure-Analgesic Activity Relationship Studies on the C-18- and C-19-Diterpenoid Alkaloids
文献类型：期刊论文
| 作者 | Wang, Jian-Li1; Shen, Xiang-Li2; Chen, Qiao-Hong1; Qi, Gong3; Wang, Wei3; Wang, Feng-Peng1 |
| 刊名 | CHEMICAL & PHARMACEUTICAL BULLETIN
 |
| 出版日期 | 2009-08 |
| 卷号 | 57期号:8页码:801-807 |
| 关键词 | diterpenoid alkaloid lappaconitine crassicauline A yunaconitine analgesic activity |
| ISSN号 | 0009-2363 |
| DOI | 10.1248/cpb.57.801 |
| 文献子类 | Article |
| 英文摘要 | For evaluation of C-18- and C-19-diterpenoid alkaloids as analgesics, three C-19-diterpenoid alkaloids were isolated from the roots of Aconitum hemsleyanum var. circinatum and A. transsecutum; and twenty-five semisynthetic C-18- or C-19-diterpenoid alkaloids were prepared from lappaconitine, crassicauline A or yunaconitine. In a mice acetic acid-induced abdominal constriction assay, four crassicauline A analogs and three yunaconitine analogs exhibited good analgesic activities with 77.8-94.1% inhibition range in 0.1-10 mg/kg subcutaneous (s.c.) dose range at the point of 20 min after drug administration. Among them, 8-O-deacetyl-8-O-ethylcrassicauline A (ED50=0.0972 mg/kg) and 8-O-ethylyunaconitine (ED50=0.0591 mg/kg) were the most potent analgesics relative to the reference drugs lappaconitine (ED50=3.50 mg/kg) and crassicauline A (ED50=0.0480 mg/kg). Analgesic activity data of these C-18- and C-19-diterpenoid alkaloids indicate that a tertiary amine in ring A, an acetoxyl or an ethoxyl group at C-8, an aromatic ester at C-14, and the saturation state of the ring D are important structural features necessary to the analgesic activity of the C-19-diterpenoid alkaloids. |
| WOS关键词 | NORDITERPENOID ALKALOIDS ; N-DEACETYLLAPPACONITINE ; LAPPACONITINE ; JESACONITINE ; DERIVATIVES |
| 资助项目 | National Natural Science Foundation of China[30672526] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000268547300003 |
| 出版者 | PHARMACEUTICAL SOC JAPAN |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279172]  |
| 专题 | 药理学第二研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Wang, Feng-Peng |
| 作者单位 | 1.Sichuan Univ, Dept Chem Med Nat Prod, Chengdu 610041, Peoples R China; 2.Sichuan Univ, W China Hosp 2, Chengdu 610041, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Jian-Li,Shen, Xiang-Li,Chen, Qiao-Hong,et al. Structure-Analgesic Activity Relationship Studies on the C-18- and C-19-Diterpenoid Alkaloids[J]. CHEMICAL & PHARMACEUTICAL BULLETIN,2009,57(8):801-807. |
| APA | Wang, Jian-Li,Shen, Xiang-Li,Chen, Qiao-Hong,Qi, Gong,Wang, Wei,&Wang, Feng-Peng.(2009).Structure-Analgesic Activity Relationship Studies on the C-18- and C-19-Diterpenoid Alkaloids.CHEMICAL & PHARMACEUTICAL BULLETIN,57(8),801-807. |
| MLA | Wang, Jian-Li,et al."Structure-Analgesic Activity Relationship Studies on the C-18- and C-19-Diterpenoid Alkaloids".CHEMICAL & PHARMACEUTICAL BULLETIN 57.8(2009):801-807. |
入库方式： OAI收割
来源：上海药物研究所
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