Evaluation of biosafety/biocompatibility of calixpyridinium on different cell lines

Abstract

Biosafety of macromolecules is one of the potential obstacles to their further in vivo applications. In this study, the viability of cells treated with cationic macrocyclic calixpyridinium (CPY) was evaluated against six different types of cells (MDA-MB-231, A549, HepG2, L02, Hek293 and H9C2). CPY had slight cytotoxicity to non-tumor cell lines and higher cytotoxicity to tumor cell lines under the same conditions. To explore the nuclear and mitochondria alterations after administration of CPY, High Content Analysis (HCA) assay, a cell-based image analysis method was adopted by using fluorescence probes of Hoechst 33342 and Mitotracker Deep Red FM. CPY was found to cause slight swelling of cell nucleus and a drop of mitochondrial membrane potential (MMP), which were considered as important characteristics of cell necrosis/necroptosis. It’s indicated that CPY may be associated with cell necrosis/necroptosis at 1 mM especially on tumor cell-lines. The significant difference of cell viability on tumor/non-tumor cell lines exhibited a slight selectivity on tumor/non-tumor cell lines of CPY at 1 mM (high concentration). Therefore, it’s provided the potential for further application of drug delivery system for anticancer treatment in the future.