Robustadial A and B from Eucalyptus globulus Labill. and their anticancer activity as selective tyrosyl-DNA phosphodiesterase 2 inhibitors

doi:10.1002/ptr.7207

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	Robustadial A and B from Eucalyptus globulus Labill. and their anticancer activity as selective tyrosyl-DNA phosphodiesterase 2 inhibitors
	Zhang,Yu; He,Xiao-Zhi ; Yang,Hao ; Liu,Hai-Yang; An,Lin-Kun
	2021
发表期刊	PHYTOTHERAPY RESEARCH
ISSN	0951-418X
卷号	35 期号:9 页码:5282-5289
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.
关键词	anticancer Eucalyptus globulus Labill inhibitors synergistic effect tyrosyl-DNA phosphodiesterase SMALL-MOLECULE INHIBITORS 1 TDP1
DOI	10.1002/ptr.7207
WOS记录号	WOS:000679055800001
引用统计	被引频次：9[WOS] [WOS记录] [WOS相关记录]
文献类型	期刊论文
条目标识符	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.[Zhang, Yu 2.Yang, Hao 3.Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Peoples R China 4.[He, Xiao-Zhi 5.Chinese Acad Sci, State Key Lab Phytochem & Plant Resources West Ch, Kunming Inst Bot, Kunming, Yunnan, Peoples R China 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.