Conjugation of tetracycline and penicillin with Sb(v) and Ag(i) against breast cancer cells

Abstract

Abstract Tetracycline (TecH 2 ) reacts with triphenylantimony (TPSb iii ) in the presence of hydrogen peroxide to form the [Ph3Sbv(Tec)] (TecAn). The sodium penicillin G (PenH) conjugates with Ag(i) towards [Ag(Pen)(MeCN)]2 (PenAcAg). TecAn and PenAcAg were characterized by melting point, X-ray fluorescence spectroscopy, attenuated total reflectance-Fourier transform infra-red, thermogravimetric-differential thermal analysis in solid state, ultraviolet-Vis spectroscopy, and nuclear magnetic resonance (1H and 13C-NMR), spectroscopies in solution. The molecular weight was determined with cryoscopy. The in vitro cytotoxic activity of TecAn and PenAcAg was evaluated against the human breast adenocarcinoma cell lines: MCF-7 (positive to hormones receptor (HR+)), MDA-MB-231 (negative to hormones receptor (HR−)), and their in vitro toxicity and genotoxicity were tested against normal human fetal lung fibroblast cells (MRC-5). The MCF-7 cells’ morphology and acridine orange/ethidium bromide staining suggest an apoptotic pathway for cell death. The binding affinity of TecAn and PenAcAg with DNA was, ex vivo, studied by UV-Vis and fluorescence spectroscopy and viscosity measurements of DNA solution. PenAcAg inhibits lipoxygenase (LOX) stronger than cisplatin, while no inhibitory activity has been detected for TecAn. The reduction of non-active Sb(v), of TecAn, to active Sb(iii) by glutathione (a tripeptide over expressed in tumor cells) was also investigated.