In vitro antiproliferative and antiangiogenic effects of synthetic chalcone analogues

Martina Pilatova, Lenka Varinska, P. Perjési, Marek Sarissky, Ladislav Mirossay, Peter Solar, Alexander Ostro, Jan Mojzis

Research output: Contribution to journalArticle

52 Citations (Scopus)

Abstract

As flavonoids, chalcones possess a wide variety of biological activities including anticancer properties. In the present study we have investigated the in vitro antiproliferative and antiangiogenic effects of four synthetic chalcones.E-2-(4'-methoxybenzylidene)-1-benzosuberone (3) was the most active compound with IC50=10-7moll-1 in Jurkat cells. In both Jurkat and HeLa chalcone 3-treated cells we found a significant increase in the proportion of cancer cells in the G2/M phase of the cell cycle as well as an increase in cells having sub-G0/G1 DNA content which is considered to be a marker of apoptotic cell death. Apoptosis was also confirmed by annexin V staining and DNA fragmentation. These effects were associated with reduced expression of the anti-apoptotic gene, Bcl-2, and increased expression of the pro-apoptotic gene, Bax.Furthermore, chalcone 3 was selected to evaluate its effect on some angiogenic events. In non-toxic concentrations, chalcone 3 inhibited VEGF-induced migration of human umbilical vein endothelial cells. Moreover, it also decreased secretion of matrix metalloproteinase (mainly MMP-9) and vascular endothelial growth factor (VEGF).In conclusion, the present study has assessed the in vitro antiproliferative/antiangiogenic potential of chalcone 3. This results generate a. rationale for in vivo efficacy studies with this compound in preclinical cancer models.

Original languageEnglish
Pages (from-to)1347-1355
Number of pages9
JournalToxicology in Vitro
Volume24
Issue number5
DOIs
Publication statusPublished - Aug 2010

Fingerprint

Chalcone
Chalcones
Cells
Matrix Metalloproteinases
Vascular Endothelial Growth Factor A
Genes
bcl-2 Genes
Jurkat Cells
G2 Phase
Annexin A5
DNA
Endothelial cells
Human Umbilical Vein Endothelial Cells
DNA Fragmentation
Cell death
Bioactivity
Flavonoids
Cell Division
Inhibitory Concentration 50
Neoplasms

Keywords

  • Antiangiogenic
  • Antiproliferative
  • Chalcones

ASJC Scopus subject areas

  • Toxicology

Cite this

Pilatova, M., Varinska, L., Perjési, P., Sarissky, M., Mirossay, L., Solar, P., ... Mojzis, J. (2010). In vitro antiproliferative and antiangiogenic effects of synthetic chalcone analogues. Toxicology in Vitro, 24(5), 1347-1355. https://doi.org/10.1016/j.tiv.2010.04.013

In vitro antiproliferative and antiangiogenic effects of synthetic chalcone analogues. / Pilatova, Martina; Varinska, Lenka; Perjési, P.; Sarissky, Marek; Mirossay, Ladislav; Solar, Peter; Ostro, Alexander; Mojzis, Jan.

In: Toxicology in Vitro, Vol. 24, No. 5, 08.2010, p. 1347-1355.

Research output: Contribution to journalArticle

Pilatova, M, Varinska, L, Perjési, P, Sarissky, M, Mirossay, L, Solar, P, Ostro, A & Mojzis, J 2010, 'In vitro antiproliferative and antiangiogenic effects of synthetic chalcone analogues', Toxicology in Vitro, vol. 24, no. 5, pp. 1347-1355. https://doi.org/10.1016/j.tiv.2010.04.013
Pilatova, Martina ; Varinska, Lenka ; Perjési, P. ; Sarissky, Marek ; Mirossay, Ladislav ; Solar, Peter ; Ostro, Alexander ; Mojzis, Jan. / In vitro antiproliferative and antiangiogenic effects of synthetic chalcone analogues. In: Toxicology in Vitro. 2010 ; Vol. 24, No. 5. pp. 1347-1355.
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