<abstract xmlns="http://www.w3.org/1999/xhtml"><p>Pyrazolone-based derivative metal complexes were reported to have cytotoxicity in some tumor cells. In this study, the antitumor effect of [Cu(PMPP-SAL)(EtOH)] (PMPP-SAL = <italic>N</italic>-(1-phenyl-3-methyl-4-propenylidene-5-pyrazolone)- salicylidene hydrazide anion) in murine melanoma B16 cells <italic>in vitro</italic> and <italic>in vivo</italic> was investigated. The results showed that [Cu(PMPP-SAL)(EtOH)] inhibited the survival of B16 cells <italic>in vitro</italic>, and the <italic>IC</italic><sub>50</sub> value was superior to cisplatin (DDP) (<italic>p</italic> &lt; 0.001). B16 cell apoptosis was significantly higher in comparison to the control group (DMSO) (<italic>p</italic> &lt; 0.01), and cell cycle arrest occurred at the G0/G1 phase. When challenged C57 BL/6J mice were treated with [Cu(PMPPSAL)(EtOH)], a smaller volume of B16 solid tumors were reported than the control group (<italic>p</italic> &lt; 0.01), with lower positive expression indices of CD 34, vascular endothelial growth factor (VEGF) and basic fibroblast growth factor (bFGF) (<italic>p</italic> &lt; 0.01). Moreover, the tumor growth was suppressed in mice due to the induction of apoptosis, as detected by the TUNEL assay (<italic>p</italic> &lt; 0.001). In summary, [Cu(PMPP-SAL)(EtOH)] effectively inhibited the growth of B16 cells <italic>in vitro</italic> and <italic>in vivo</italic> due to the induction of apoptosis and the inhibition of intra-tumoral angiogenesis, demonstrating its therapeutic potential in melanoma treatment.</p></abstract>

Pyrazolone-based derivative metal complexes were reported to have cytotoxicity in some tumor cells. In this study, the antitumor effect of [Cu(PMPP-SAL)(EtOH)] (PMPP-SAL = N-(1-phenyl-3-methyl-4-propenylidene-5-pyrazolone)- salicylidene hydrazide anion) in murine melanoma B16 cells in vitro and in vivo was investigated. The results showed that [Cu(PMPP-SAL)(EtOH)] inhibited the survival of B16 cells in vitro, and the IC50 value was superior to cisplatin (DDP) (p < 0.001). B16 cell apoptosis was significantly higher in comparison to the control group (DMSO) (p < 0.01), and cell cycle arrest occurred at the G0/G1 phase. When challenged C57 BL/6J mice were treated with [Cu(PMPPSAL)(EtOH)], a smaller volume of B16 solid tumors were reported than the control group (p < 0.01), with lower positive expression indices of CD 34, vascular endothelial growth factor (VEGF) and basic fibroblast growth factor (bFGF) (p < 0.01). Moreover, the tumor growth was suppressed in mice due to the induction of apoptosis, as detected by the TUNEL assay (p < 0.001). In summary, [Cu(PMPP-SAL)(EtOH)] effectively inhibited the growth of B16 cells in vitro and in vivo due to the induction of apoptosis and the inhibition of intra-tumoral angiogenesis, demonstrating its therapeutic potential in melanoma treatment.

Antitumor effect of a pyrazolone-based-complex [Cu(PMPP-SAL)(EtOH)] against murine melanoma B16 cell <italic>in vitro</italic> and <italic>in vivo</italic>

Xinjiang Key Laboratory of Biological Resources and Genetic Engineering

College of Life Science and Technology Xinjiang University

Acta Pharmaceutica

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Antitumor effect of a pyrazolone-based-complex [Cu(PMPP-SAL)(EtOH)] against murine melanoma B16 cell  and 

Pyrazolone-based derivative metal complexes were reported to have cytotoxicity in some tumor cells. In this study, the antitumor effect of [Cu(PMPP-SAL)(EtOH)]...

Antitumor effect of a pyrazolone-based-complex [Cu(PMPP-SAL)(EtOH)] against murine melanoma B16 cell in vitro and in vivo

Published Online: May 13, 2020

Page range: 561 - 575

Accepted: Feb 10, 2020

DOI: https://doi.org/10.2478/acph-2020-0040

Keywords
malignant melanoma, [Cu(PMPP-SAL)(EtOH)], apoptosis, tumor microangiogenesis

© 2020 Ayipairi Abula et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Antitumor effect of a pyrazolone-based-complex [Cu(PMPP-SAL)(EtOH)] against murine melanoma B16 cell in vitro and in vivo

Published Online: May 13, 2020

Page range: 561 - 575

Accepted: Feb 10, 2020

DOI: https://doi.org/10.2478/acph-2020-0040

Keywordsmalignant melanoma, [Cu(PMPP-SAL)(EtOH)], apoptosis, tumor microangiogenesis

© 2020 Ayipairi Abula et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Keywords
malignant melanoma, [Cu(PMPP-SAL)(EtOH)], apoptosis, tumor microangiogenesis