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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Cytotoxicity of trans-chalcone and licochalcone A against breast cancer cells is due to apoptosis induction and cell cycle arrest

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Buso Bortolotto, Luis Felipe ; Barbosa, Flavia Regina ; Silva, Gabriel ; Bitencourt, Tamires Aparecida ; Beleboni, Rene Oliveira ; Baek, Seung Joon ; Marins, Mozart ; Fachin, Ana Lucia
Total Authors: 8
Document type: Journal article
Source: BIOMEDICINE & PHARMACOTHERAPY; v. 85, p. 425-433, JAN 2017.
Web of Science Citations: 20

Chalcones are precursors of flavonoids that exhibit structural heterogeneity and potential antitumor activity. The objective of this study was to characterize the cytotoxicity of trans-chalcone and licochalcone A (LicoA(1)) against a breast cancer cell line (MCF-7) and normal murine fibroblasts (3T3). Also the mechanisms of the anti-cancer activity of these two compounds were studied. The alkaline comet assay revealed dose-dependent genotoxicity, which was more responsive against the tumor cell line, compared to the 3T3 mouse fibroblast cell line. Flow cytometry showed that the two chalcones caused the cell cycle arrest in the G1 phase and induced apoptosis in MCF-7 cells. Using PCR Array, we found that trans-chalcone and LicoA trigger apoptosis mediated by the intrinsic pathway as demonstrated by the inhibition of Bcl-2 and induction of Bax. In western blot assay, the two chalcones reduced the expression of cell death-related proteins such as Bcl-2 and cyclin D1 and promoted the cleavage of PARP. However, only trans-chalcone induced the expression of the CIDEA gene and protein in these two experiments. Furthermore, transient transfections of MCF-7 using a construction of a promoter-luciferase vector showed that trans-chalcone induced the expression of the CIDEA promoter activity in 24 and 48 h. In conclusion, the results showed that trans-chalcone promoted high induction of the CIDEA promoter gene and protein, which is related to DNA fragmentation during apoptosis. (C) 2016 Published by Elsevier Masson SAS. (AU)

FAPESP's process: 12/06889-7 - Genetic diversity of Solanum lycocarpum and phytochemical study to evaluate the antimicrobial activity, cytotoxic and genotoxic of alkaloids
Grantee:Ana Lucia Fachin Saltoratto
Support Opportunities: Regular Research Grants
FAPESP's process: 12/02920-7 - Transcriptome of the dermatophyte Trichophyton rubrum in response to antifungal transchalcona in culture conditions that simulate infection
Grantee:Tamires Aparecida Bitencourt
Support Opportunities: Scholarships in Brazil - Doctorate
Grantee:Luis Felipe Buso Bortolotto
Support Opportunities: Scholarships in Brazil - Master