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Keywords
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Ruthenium (II) Complexes, Tetrazole Ligand, Anticancer, Apoptosis, Autophagy
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Abstract
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Abstract
Background: The development of platinum-based metal complexes in oncology is limited due to vigorous toxicity and drug
resistance.
Objectives: This work aimed to study the cytotoxic activity and apoptosis induction of ruthenium complexes in a B16F10 cell line
therapy.
Methods: We prepared a series of innovative Ru(II) complexes [Ru(Tzphen)(bpy)(dcbpy)]+2 (S1), [Ru(dcbpy)2(Tzphen)]+2 (S2),
[Ru(Phen)2(Tzphen)]+2 (S3), [Ru(Tzphen)(bpy)2]+2 (S4), [Ru(dmbpy)2(Tzphen)]+2 (S5) based on 1,10-phenanthroline ligand containing
tetrazole and their anticancer properties investigated by cytotoxicity in vitro, reactive oxygen species, apoptosis with annexin V/PI
staining method, autophagy, and cell uptake.
Results: S1, S2, S3, S4, and S5 complexes showed comparable cytotoxicity activity relative to cisplatin against the B16F10 model.
Moreover, intracellular ROS levels increased due to the presence of the complexes. Among the investigated complexes, the
cells treated with the S5 complex indicated the highest apoptotic percentage (Q3) of 14.9% compared to the controls. The cell
adsorption of the complexes alsoshowedthat the S4andS5 complexeshadhigher cell adsorption, better internalization, andhigher
fluorescence light intensity.
Conclusions: The present work provides important guidance for designing and using Ru complexes in cancer therapy.
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