4.4 Article

Quantitative Relationships Between the Cytotoxicity of Flavonoids on the Human Breast Cancer Stem-Like Cells MCF7-SC and Their Structural Properties

Journal

CHEMICAL BIOLOGY & DRUG DESIGN
Volume 86, Issue 4, Pages 496-508

Publisher

WILEY
DOI: 10.1111/cbdd.12512

Keywords

8-chloroflavanone; cyclin-dependent kinase 6; flavonoid; flow cytometry; immunofluorescence microscopy; in silico docking; QSAR

Funding

  1. Priority Research Centers Program (NRF) [2012-0006686]
  2. Next Generation Biogreen21 Program (RDA) [PJ009532]
  3. Konkuk University

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As some breast cancer-related deaths can be attributed to the metastasis of cancer stem cells, chemotherapeutic agents targeting breast cancer stem cells are of interest as a potential treatment. Flavonoids that exhibit cytotoxicity on breast cancer stem cells have rarely been observed. Thus, the objective of this study was to measure potential cytotoxic effects of 42 different flavonoids on the human breast cancer stem-like cell line, MCF7-SC. The relationship between flavonoid structural properties and cytotoxicity has not been reported previously; therefore, we determined quantitative structure-activity relationships using both comparative molecular field analysis and comparative molecular similarity analysis. Further biological experiments including Western blot analysis, flow cytometry, and immunofluorescence microscopy were also conducted on the most cytotoxic 8-chloroflavanone.

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