Antitumor action of a triazolyl aminoacyl penicillin derivative

BLANK VC; BELLIZZI YANINA; CORNIER P.G.; DELPICCOLO CM; BOGGIÁN D.B; MATA E.G.; ROGUIN, L. P

Buenos Aires

Congreso; International Congress of Translational Medicine. ?Cellular and Molecular Pathways as Therapeutic Targets; 2014

Facultad de Farmacia y Bioquímica y Facultad de Medicina, UBA

In the search of new antitumor agents, we have studied the effect of 18 penicillin derivatives (triazolyl aminoacyl penicillins) on the growth of two tumor cell lines (HeLa: human cervix carcinoma and B16: murine melanoma) and epithelial cells derived from normal murine mammary gland (NMuMG). These compounds are formed by a penicillin linked to a peptide through a triazole group. Particularly, one of these derivatives, which contains the dipeptide Phe-Leu (named TAP6) was 30 times more potent against tumor than non-tumor cells (IC50 3±1 µM, for HeLa and B16 cells vs IC50 102±8 µM, for NMuMG). B16 cell line was selected to study the mechanism of action of TAP6. When B16 cells were incubated in the presence of 20 µM of TAP6, there was an increment in the percentage of hipodiploid cells after 24h (62±8% TAP6 vs 7±3% control, p