Screening for inhibitors of topoisomerase I from Lycoris radiata by combining ultrafiltration with liquid chromatography/mass spectrometry

doi:10.1002/rcm.7649

CORC > 武汉植物园 > 中国科学院武汉植物园

	Screening for inhibitors of topoisomerase I from Lycoris radiata by combining ultrafiltration with liquid chromatography/mass spectrometry
	Chen, Guilin 1,3; Guo, Mingquan 1,2; Tian, Yongqiang 1,3
刊名	RAPID COMMUNICATIONS IN MASS SPECTROMETRY
	2016-08-01
卷号	30 页码:95-99
ISSN号	0951-4198
DOI	10.1002/rcm.7649
英文摘要	RATIONALE: Although crude Amaryllidaceae alkaloids (AAs) extracted from Lycoris radiata are reported to exhibit significant anti-cancer activity, both the specific responsible alkaloid(s) and their targets remain elusive. Screening anticancer AAs targeted on topoisomerase I from crude AAs could be very helpful in tackling these two challenging questions. METHODS: An ultrafiltration method combined with liquid chromatography/electrospray ionization mass spectrometry (UF-LC/MS) was developed to screen for the inhibitors of topoisomerase I, which has been reported to mediate DNA unwinding during carcinoma proliferation. Enrichment factors (EFs) of different AAs were used to evaluate the binding affinity between AAs and topoisomerase I, and the AAs with higher EFs were further tested to validate the method. RESULTS: Eleven AAs from Lycoris radiata (ten of which were identified) were screened using UF-LC/MS, and a glaring discrepancy in EFs was revealed for the first time. One of the AAs, hippeastrine, with the highest EF at 49.3%, was further tested against topoisomerase I, and the IC50 value of hippeastrine was determined to be 23.0 mu mol/L, which is comparable with the well-known anti-cancer drug camptothecin at 19.3 mu mol/L. CONCLUSIONS: A simple, rapid and effective screening method using UF-LC/MS was developed and successfully applied to screen candidate inhibitors of topoisomerase I from crude AAs in Lycoris radiata, which may pave the way to further understand the potential anti-cancer constituents and mechanisms of Lycoris radiata. Copyright (C) 2016 John Wiley & Sons, Ltd.
WOS研究方向	Biochemistry & Molecular Biology ; Chemistry ; Spectroscopy
语种	英语
出版者	WILEY-BLACKWELL
WOS记录号	WOS:000382975400018
内容类型	期刊论文
源URL	[http://202.127.146.157/handle/2RYDP1HH/42]
专题	中国科学院武汉植物园
通讯作者	Guo, Mingquan
作者单位	1.Chinese Acad Sci, Wuhan Bot Garden, Key Lab Plant Germplasm Enhancement & Specialty A, Wuhan 430074, Peoples R China 2.Chinese Acad Sci, Sino Africa Joint Res Ctr, Wuhan 430074, Peoples R China 3.Chinese Acad Sci, Grad Univ, Beijing 100049, Peoples R China
推荐引用方式 GB/T 7714	Chen, Guilin,Guo, Mingquan,Tian, Yongqiang. Screening for inhibitors of topoisomerase I from Lycoris radiata by combining ultrafiltration with liquid chromatography/mass spectrometry[J]. RAPID COMMUNICATIONS IN MASS SPECTROMETRY,2016,30:95-99.
APA	Chen, Guilin,Guo, Mingquan,&Tian, Yongqiang.(2016).Screening for inhibitors of topoisomerase I from Lycoris radiata by combining ultrafiltration with liquid chromatography/mass spectrometry.RAPID COMMUNICATIONS IN MASS SPECTROMETRY,30,95-99.
MLA	Chen, Guilin,et al."Screening for inhibitors of topoisomerase I from Lycoris radiata by combining ultrafiltration with liquid chromatography/mass spectrometry".RAPID COMMUNICATIONS IN MASS SPECTROMETRY 30(2016):95-99.