Potent anticancer activity of a new bismuth (III) complex against human lung cancer cells

The aim of this work is experimental study of an interesting bismuth(III) complex derived from pentadentate 2,6-pyridinedicarboxaldehyde bis(⁴N-methylthiosemicarbazone), [BiL(NO₃)₂]NO₃ {L=2,6-pyridinedicarboxaldehyde bis(⁴N-methylthiosemicarbazone)}. A series of in vitro biological studies indicate that the newly prepared [BiL(NO₃)₂]NO₃ greatly suppressed colony formation, migration and significantly induced apoptosis of human lung cancer cells A549 and H460, but did not obviously decrease the cell viability of non-cancerous human lung fibroblast (HLF) cell line, showing much higher anticancer activities than its parent ligands, especially with half maximum inhibitory concentration (IC₅₀) <3.5μM. Moreover, in vivo study provides enough evidence that the treatment with [BiL(NO₃)₂]NO₃ effectively inhibited A549 xenograft tumor growth on tumor-bearing mice (10mgkg^-1, tumor volume reduced by 97.92% and tumor weight lightened by 94.44% compared to control) and did not indicate harmful effect on mouse weight and liver. These results suggest that the coordination of free ligand with Bi(III) might be an interesting and potent strategy in the discovery of new anticancer drug candidates.