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

• Published in: Chemical biology & drug design 2015-10, Vol.86 (4), p.496-508
• Main Authors: Jung, Hyeryoung, Shin, Soon Young, Jung, Yearam, Tran, Thao Anh, Lee, Hye Ok, Jung, Kang-Yeoun, Koh, Dongsoo, Cho, Somi Kim, Lim, Yoongho
• Format: Article
• Language: English
• Subjects: 8-chloroflavanone; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Breast Neoplasms - drug therapy; Breast Neoplasms - metabolism; Breast Neoplasms - pathology; cyclin-dependent kinase 6; Cytotoxins - chemistry; Cytotoxins - pharmacology; Drug Screening Assays, Antitumor; Female; flavonoid; Flavonoids - chemistry; Flavonoids - pharmacology; flow cytometry; Humans; immunofluorescence microscopy; in silico docking; MCF-7 Cells; Neoplastic Stem Cells; QSAR
• ISSN: 1747-0277; 1747-0285
• DOI: 10.1111/cbdd.12512

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. Chemotherapeutic agents targeting breast cancer stem cells are of interest as a potential treatment. The objective of this study was to measure cytotoxic effects of flavonoids on the human breast cancer stem‐like cell line. 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.