主 办:北 京 中 医 药 大 学
ISSN 1006-2157 CN 11-3574/R

JOURNAL OF BEIJIGN UNIVERSITY OF TRADITIONAL CHINE ›› 2014, Vol. 37 ›› Issue (1): 58-62.doi: 10.3969/j.issn.1006-2157.2014.01.013

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Active constituents of inhibiting EGFR in ehtyl acetate extracts from Jixueteng (Caulis Spatholobi) analyzed by using UPLC-Q-TOF-MS

WANG Dong-mei1, LIN Sen-sen2, ZHENG Si-hao1, HUANG Lin-fang1   

  1. 1 Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences, Beijing 100193;
    2 Center for Drug Screening, China Pharmaceutical University
  • Received:2013-01-21 Online:2014-01-30 Published:2014-01-30

Abstract: Objective To screen the extracts with the inhibitive activity on epidermal growth factor receptor (EGFR) from Jixueteng (Caulis Spatholobi) by using the technique of homogeneous time-resolved fluorescence (HTRF), and to analyze and identify these active constituents by applying ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC/Q-TOF-MS). Methods The crude material of Jixueteng was percolated with petroleum ether, and then extracted with ethanol and ethyl acetate and boiled in water to obtain 4 extract fractions. The inhibitive effect of ethyl acetate extract on ERFR was detected by using HTRF and inhibitive rate was calculated. The UPLC/Q-TOF-MS procedure was performed on the chromatographic column of ACQUITY UPLC BEH C18, and the mobile phase was 0.1% formic acid solution (A)-acetonitrile (B) scanned in 200-400 nm. The data was collected by using ESI ion source in a positive ion mode. Results The ethyl acetate fractions of Jixueteng showed a strong inhibitive activity on EGFR and IC50 was 2.277 μg/mL. There were 15 chemicals identified from these active fractions, and their main constituents were flavonoids, among them 10 were as follows: (epi) catechin- (epi) catechin, myricetin -3' -O-β-D- xyloside, (epi) afzelechin- (epi) catechin, ononin, formononetin, afrormosin, epigallocatechin, vomifoliol -9-O-β-D- xylopyranosyl (1→6)-β-D- glucopyranside, luteolin-7-O-glucoside and (epi) gallocatechin-(epi) catechin. There were other 5 constituents unknown. The major active constituents are (epi) catechin-(epi) catechin, epigallocatechin and formononetin. Conclusion The flavonoids in ethyl acetate extracts from Jixueteng has a strong inhibitive activity on EGFR. The study hopes to provide theoretic bases for the anticancer application of Jixueteng and further tracking the separation of its active constituents.

Key words: epidermal growth factor receptor inhibitor, homogeneous time-resolved fluorescence, Jixueteng (Caulis Spatholobi), effective constituents, ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry

CLC Number: 

  • R284.2