利用靶向分离技术挖掘芒种花根部中PPAP类活性成分
文献类型：学位论文
| ; | |
| 作者 | 姜娜娜 |
| 答辩日期 | 2020-05 |
| 导师 | 许刚 |
| 英文摘要 | The chemical constituents of Hypericum genus in Guttiferae family mainly include phloroglucinol, terpenoid, dianthrone, xanthone and flavonoid. Among them, polycyclic polyprenylated acylphloroglucinols (PPAP) is a class of hybrid natural products with diverse structures and significant biological activity. Up to date, our group has carried out a series of systematic study on the chemical constituents of natural PPAP in more than 10 species of Hypericum. In the early stage, Hypericum henryi, as one of the most abundant Hypericum plants in Yunnan Province, has been carried out a systematic studies on PPAP of its aerial and fruit parts by our group, from which we isolated all the common PPAP types, such as bridged-cyclic, adamantane, spiro-cyclic and dicyclic PPAP. Notably, we also found that dicyclic PPAP have remarkable cytotoxic activities on a variety of tumor cell lines. Moreover, the pilot study demonstrated that the roots of H. henryi contained various types of PPAP, especially rich dicyclic PPAP. Therefore, in order to explore the active dicyclic PPAP and improve the systematic study on the whole plant of H. henryi, the roots of H. henryi was selected as the research objects. The isolation of the small polar chemical constituents from roots of H. henryi was carried out, guided by Targeted Isolated Method of HPLC-UV. A total of 50 compounds were characterized, including 14 new compounds. It is worthy to note that we found the first bridged-cyclic PPAP with diisoprenyl substitution at C-3; the first spiro-cyclic PPAP with 6/5/5 membered ring and twenty one active dicyclic PPAP. In the research of pharmacological activities, compounds 1, 7 and 8 were identified as the first PPAP type Cav3.1 T-type calcium channel (TTCC) inhibitors (IC50: 7.07, 6.19, 5.47 μM); compounds 18–21, 45 and 49 exhibited significant inhibitory activities agains five human tumor cell lines. Among them, compounds 18–21 have the most significant cytotoxic activities on HeLa (IC50: 0.069, 0.89, 0.88, 0.09 μM). In general, a lot of dicyclic PPAP were isolated from the roots of H. henryi, and some of them were studied at the cellular level and in vivo, moreover, the structures and types of PPAP isolated from roots are similar to those from aerial and fruit parts, but the trace constituents are different. |
| 源URL | [http://ir.kib.ac.cn/handle/151853/74138]  |
| 专题 | 昆明植物研究所_昆明植物所硕博研究生毕业学位论文 |
| 推荐引用方式 GB/T 7714 | 姜娜娜. 利用靶向分离技术挖掘芒种花根部中PPAP类活性成分, The Research of PPAP Type Active Constituents from the Roots of Hypericum henryi via Targeted Isolated Method[D]. 2020. |
入库方式： OAI收割
来源：昆明植物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。