Antiproliferative and Enzyme Docking Analysis of Engleromycin from Engleromyces goetzei

doi:10.3390/molecules24010166

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	Antiproliferative and Enzyme Docking Analysis of Engleromycin from Engleromyces goetzei
	Guo, Mingquan 2,3; Ma, Hong 1,3; Chen, Guilin 2,3; Zhang, Yongli 2,3
刊名	MOLECULES
	2019
卷号	24 期号:1 页码:9
关键词	Engleromyces goetzei engleromycin antiproliferative activities molecular docking
ISSN号	1420-3049
DOI	10.3390/molecules24010166
英文摘要	Engleromyces goetzei P. Henn. (E. goetzei) has been widely used as a traditional herb for many years in Kenya due to its diverse biological effects. Although engleromycin was first isolated from E. goetzei in 1980, its pharmacological activity is still unknown. In this study, engleromycin from E. goetzei was identified by spectroscopic analyses, and subsequently examined for its antiproliferative activity using human cancer cell lines of SGC-7901, HT-29, HeLa and A549. As a result, it was revealed that engleromycin strongly inhibited the growth of SGC-7901, HT-29, HeLa and A549 cells with IC50 values at 26.77 +/- 1.69 mu M, 7.73 +/- 0.18 mu M, 7.00 +/- 0.12 mu M and 3.14 +/- 0.03 mu M, respectively. The results of topoisomerase II (Top II) inhibition assay in vitro implied that engleromycin might be a Top II inhibitor. Further insights into the potential mechanism of antiproliferative activity displayed that engleromycin could dock into the binding pockets of Top II, like the clinical inhibitor doxorubicin, and then inhibit the biological activity of Top II. Taken together, our findings suggest that engleromycin has an anticancer potential, and may serve as a leading compound for the development of antitumor agents.
资助项目	Natural Science Foundation of China[81673580] ; Major Project for Special Technology Innovation of Hubei Province-Sino-foreign Cooperation Project[2017AHB054]
WOS研究方向	Biochemistry & Molecular Biology ; Chemistry
语种	英语
出版者	MDPI
WOS记录号	WOS:000457150200166
内容类型	期刊论文
源URL	[http://202.127.146.157/handle/2RYDP1HH/6456]
专题	中国科学院武汉植物园
通讯作者	Guo, Mingquan
作者单位	1.Childrens Hosp Los Angeles, Haematol & Oncol Div, Los Angeles, CA 90027 USA 2.Chinese Acad Sci, Sinoafrica Joint Res Ctr, Wuhan 430074, Hubei, Peoples R China 3.Chinese Acad Sci, Wuhan Bot Garden, Key Lab Plant Germplasm Enhancement & Specialty A, Wuhan 430074, Hubei, Peoples R China
推荐引用方式 GB/T 7714	Guo, Mingquan,Ma, Hong,Chen, Guilin,et al. Antiproliferative and Enzyme Docking Analysis of Engleromycin from Engleromyces goetzei[J]. MOLECULES,2019,24(1):9.
APA	Guo, Mingquan,Ma, Hong,Chen, Guilin,&Zhang, Yongli.(2019).Antiproliferative and Enzyme Docking Analysis of Engleromycin from Engleromyces goetzei.MOLECULES,24(1),9.
MLA	Guo, Mingquan,et al."Antiproliferative and Enzyme Docking Analysis of Engleromycin from Engleromyces goetzei".MOLECULES 24.1(2019):9.