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Rapid screening of bioactive compounds from natural products by integrating 5-channel parallel chromatography coupled with on-line mass spectrometry and microplate based assays.

Abstract
A high throughput method was developed for rapid screening and identification of bioactive compounds from traditional Chinese medicine, marine products and other natural products. The system, integrated with five-channel chromatographic separation and dual UV-MS detection, is compatible with in vitro 96-well microplate based bioassays. The stability and applicability of the proposed method was validated by testing radical scavenging capability of a mixture of seven known compounds (rutin, dihydroquercetin, salvianolic acid A, salvianolic acid B, glycyrrhizic acid, rubescensin A and tangeretin). Moreover, the proposed method was successfully applied to the crude extracts of traditional Chinese medicine and a marine sponge from which 12 bioactive compounds were screened and characterized based on their anti-oxidative or anti-tumor activities. In particular, two diterpenoid derivatives, agelasine B and (-)-agelasine D, were identified for the first time as anti-tumor compounds from the sponge Agelas mauritiana, showing a considerable activity toward MCF-7 cells (IC50 values of 7.84±0.65 and 10.48±0.84 μM, respectively). Our findings suggested that the integrated system of 5-channel parallel chromatography coupled with on-line mass spectrometry and microplate based assays can be a versatile and high efficient approach for the discovery of active compounds from natural products.
AuthorsYufeng Zhang, Shun Xiao, Lijuan Sun, Zhiwei Ge, Fengkai Fang, Wen Zhang, Yi Wang, Yiyu Cheng
JournalAnalytica chimica acta (Anal Chim Acta) Vol. 777 Pg. 49-56 (May 13 2013) ISSN: 1873-4324 [Electronic] Netherlands
PMID23622964 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Validation Study)
CopyrightCopyright © 2013 Elsevier B.V. All rights reserved.
Chemical References
  • Antineoplastic Agents
  • Antioxidants
  • Biological Products
Topics
  • Animals
  • Antineoplastic Agents (chemistry, pharmacology)
  • Antioxidants (chemistry, pharmacology)
  • Biological Assay (methods)
  • Biological Products (chemistry, pharmacology)
  • Cell Line, Tumor
  • Chromatography, Liquid
  • Drug Screening Assays, Antitumor
  • Drug Stability
  • HL-60 Cells
  • Humans
  • Mass Spectrometry
  • Porifera (chemistry)
  • Reproducibility of Results
  • Time Factors

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