Robustadial A and B from Eucalyptus globulus Labill. and their anticancer activity as selective tyrosyl-DNA phosphodiesterase 2 inhibitors
文献类型：期刊论文
| 作者 | Zhang,Yu ; He,Xiao-Zhi; Yang,Hao; Liu,Hai-Yang; An,Lin-Kun
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| 刊名 | PHYTOTHERAPY RESEARCH
 |
| 出版日期 | 2021 |
| 卷号 | 35期号:9页码:5282-5289 |
| 关键词 | anticancer Eucalyptus globulus Labill inhibitors synergistic effect tyrosyl-DNA phosphodiesterase SMALL-MOLECULE INHIBITORS 1 TDP1 |
| ISSN号 | 0951-418X |
| DOI | 10.1002/ptr.7207 |
| 英文摘要 | Tyrosyl-DNA phosphodiesterase 2 (TDP2) is a recently discovered DNA repair enzyme that can repair topoisomerase 2-mediated DNA damage, resulting in cancer cell resistance. In this study, two compounds, robustadial A and B, were isolated from a fraction of the ethyl acetate extract of Eucalyptus globulus Labill. fruits based on TDP2 inhibition screening. The biological experiments indicated that robustadial A and B have TDP2 inhibitory activity with EC50 values of 17 and 42 mu M, respectively, but no tyrosyl-DNA phosphodiesterase 1 inhibition at 100 mu M. Robustadial A showed significant synergistic effects with the anticancer drug etoposide in four human cancer cell lines, non-small cell lung cancer cell line (A549), prostate cancer cell line (DU145), breast cancer cell line (MCF-7), colorectal adenocarcinoma cell line (HCT-116), and chicken lymphoma cell line (DT40), and chicken lymphoma cell line complementation with human TDP2 (DT40 hTDP2) with combination index values ranging from 0.21 to 0.74. This work will facilitate future efforts for the development of robustadial A-based TDP2 selective inhibitors. |
| WOS记录号 | WOS:000679055800001 |
| 源URL | [http://ir.kib.ac.cn/handle/151853/73791]  |
| 专题 | 中国科学院昆明植物研究所 |
| 作者单位 | 1.Chinese Acad Sci, State Key Lab Phytochem & Plant Resources West Ch, Kunming Inst Bot, Kunming, Yunnan, Peoples R China 2.Yang, Hao 3.[He, Xiao-Zhi 4.Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Peoples R China 5.[Zhang, Yu 6.Guangdong Prov Key Lab New Drug Design & Evaluat, Guangzhou, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang,Yu,He,Xiao-Zhi,Yang,Hao,et al. Robustadial A and B from Eucalyptus globulus Labill. and their anticancer activity as selective tyrosyl-DNA phosphodiesterase 2 inhibitors[J]. PHYTOTHERAPY RESEARCH,2021,35(9):5282-5289. |
| APA | Zhang,Yu,He,Xiao-Zhi,Yang,Hao,Liu,Hai-Yang,&An,Lin-Kun.(2021).Robustadial A and B from Eucalyptus globulus Labill. and their anticancer activity as selective tyrosyl-DNA phosphodiesterase 2 inhibitors.PHYTOTHERAPY RESEARCH,35(9),5282-5289. |
| MLA | Zhang,Yu,et al."Robustadial A and B from Eucalyptus globulus Labill. and their anticancer activity as selective tyrosyl-DNA phosphodiesterase 2 inhibitors".PHYTOTHERAPY RESEARCH 35.9(2021):5282-5289. |
入库方式： OAI收割
来源：昆明植物研究所
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