Abstract:
:A series of new ionic Pt(II) complexes of general formula [Pt(II)(A)n(Cl)(AO)]X (A=en, NH3; n=1, 2; X-=BF4-, NO3-, PF6-, CF3SO3-), 1-5, containing Acridine Orange (AO) bound to the metal atom through the endocyclic N atom, have been tested in human melanoma cells (M14, JR8 and PLF2), human neuroblastoma cell line SH-SY5Y and its cis-platin resistant subline SH-SY5Yres. The Pt(II) compounds, and in particular complexes 1 and 4, exhibit higher cytotoxic activity at lower concentration compared to cis-DDP in melanoma cells, affecting cell growth behavior and causing cell cycle perturbation. Moreover, M14 and JR8 cell lines were not able to rescue the impairment due to the new Pt(II) complexes since perturbation of cell cycle phases and cell proliferation inhibition were found after 72 h of recovery time. In order to evaluate whether GSTP1 may play a role in chemo-resistance of our melanoma model, we investigated the effect of the treatment with these Pt(II) compounds on GSTP1 gene expression. Up-regulation of GSTP1, evaluated by Qreal-time PCR was observed after treatment with complexes 1 and 4, showing that the effect of these Pt(II) compounds is GSTP1 indipendent. The lack of resistance of the new Pt(II)-AO complexes and their cytotoxicity, cell growth and cell cycle recovery in melanoma cells provide the basis for the development of new platinum anticancer compounds, directed to those tumors that over express GSTs enzymes.
journal_name
Chem Biol Interactjournal_title
Chemico-biological interactionsauthors
Valentini A,Pucci D,Crispini A,Federici G,Bernardini Sdoi
10.1016/j.cbi.2006.03.011subject
Has Abstractpub_date
2006-07-10 00:00:00pages
241-50issue
3eissn
0009-2797issn
1872-7786pii
S0009-2797(06)00077-9journal_volume
161pub_type
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