Antiproliferative activities of Amaryllidaceae alkaloids from Lycoris radiata targeting DNA topoisomerase I
文献类型：期刊论文
| 作者 | Chen, Gui-Lin2,3; Tian, Yong-Qiang2,3; Wu, Jian-Lin1; Li, Na1; Guo, Ming-Quan3,4 |
| 刊名 | SCIENTIFIC REPORTS
 |
| 出版日期 | 2016-12-06 |
| 卷号 | 6页码:10 |
| ISSN号 | 2045-2322 |
| DOI | 10.1038/srep38284 |
| 英文摘要 | Crude Amaryllidaceae alkaloids (AAs) extracted from Lycoris radiata are reported to exhibit significant anti-cancer activity. However, the specific alkaloids responsible for the pharmacodynamic activity and their targets still remain elusive. In this context, we strived to combine affinity ultrafiltration with topoisomerase I (Top I) as a target enzyme aiming to fish out specific bioactive AAs from Lycoris radiata. 11 AAs from Lycoris radiata were thus screened out, among which hippeastrine (peak 5) with the highest Enrichment factor (EF) against Top I exhibited good dose-dependent inhibition with IC50 at 7.25 +/- 0.20 mu g/mL comparable to camptothecin (positive control) at 6.72 +/- 0.23 mu g/mL. The molecular docking simulation further indicated the inhibitory mechanism between Top I and hippeastrine. The in vitro antiproliferation assays finally revealed that hippeastrine strongly inhibited the proliferation of HT-29 and Hep G2 cells in an intuitive dose-dependent manner with the IC50 values at 3.98 +/- 0.29 mu g/mL and 11.85 +/- 0.20 mu g/mL, respectively, and also induced significant cellular morphological changes, which further validated our screening method and the potent antineoplastic effects. Collectively, these results suggested that hippeastrine could be a very promising anticancer candidate for the therapy of cancer in the near future. |
| 资助项目 | Natural Science Foundation of China[81673580] ; the Hundred Talents Project from Chinese Academy of Sciences[29Y429291a0129] ; Sino-Africa joint research project[SAJC20160233] |
| WOS研究方向 | Science & Technology - Other Topics |
| 语种 | 英语 |
| 出版者 | NATURE PUBLISHING GROUP |
| WOS记录号 | WOS:000389370200001 |
| 源URL | [http://202.127.146.157/handle/2RYDP1HH/3597]  |
| 专题 | 中国科学院武汉植物园 |
| 通讯作者 | Guo, Ming-Quan |
| 作者单位 | 1.Macau Univ Sci & Technol, State Key Lab Qual Res Chinese Med, Taipa, Macau, Peoples R China 2.Chinese Acad Sci, Grad Univ, Beijing 100049, Peoples R China 3.Chinese Acad Sci, Wuhan Bot Garden, Key Lab Plant Germplasm Enhancement & Specialty A, Wuhan 430074, Peoples R China 4.Chinese Acad Sci, Sino Africa Joint Res Ctr, Wuhan 430074, Peoples R China |
| 推荐引用方式 GB/T 7714 | Chen, Gui-Lin,Tian, Yong-Qiang,Wu, Jian-Lin,et al. Antiproliferative activities of Amaryllidaceae alkaloids from Lycoris radiata targeting DNA topoisomerase I[J]. SCIENTIFIC REPORTS,2016,6:10. |
| APA | Chen, Gui-Lin,Tian, Yong-Qiang,Wu, Jian-Lin,Li, Na,&Guo, Ming-Quan.(2016).Antiproliferative activities of Amaryllidaceae alkaloids from Lycoris radiata targeting DNA topoisomerase I.SCIENTIFIC REPORTS,6,10. |
| MLA | Chen, Gui-Lin,et al."Antiproliferative activities of Amaryllidaceae alkaloids from Lycoris radiata targeting DNA topoisomerase I".SCIENTIFIC REPORTS 6(2016):10. |
入库方式： OAI收割
来源：武汉植物园
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