Bioactive compound D-Pinitol-loaded graphene oxide-chitosan-folic acid nanocomposite induced apoptosis in human hepatoma HepG-2 cells

Abstract

In the present study, we formulated a nanocomposite—comprising graphene oxide, chitosan, and folic acid—as a nanocarrier loaded with the phytochemical d-Pinitol and then subjected to spectroscopic and microscopic analyses to assess the shape, size, and structure of the nanocomposite. The nanocomposite was further subjected to cytotoxic analysis against hepatoma HepG-2 and non-malignant Vero cells using the MTT assay. The generation of ROS, disruption of mitochondrial membrane permeability, and induction of cell death were assessed with corresponding fluorescent staining. Finally, the apoptotic proteins Bax, Bcl2, and caspases were quantified using commercial kits. The characterization analysis confirmed the synthesis of the agglomerated spherical GO Chitosan D-Pinitol FA nanocomposites with an average particle size of 161.50 nm. The nanocomposite remarkably inhibited the HepG-2 cell viability with an IC50 concentration of 7.5 μg/mL but did not disturb the growth of non-malignant Vero cells. It effectively promoted the generation of ROS, disrupted MMP, and induced apoptosis in hepatoma HepG-2 cells, whereas it rendered minimal cytotoxicity even at high doses in mammalian Vero cells. It also promoted the caspase-3, -9, and Bax expressions but inhibited the Bcl-2 expression in the HepG-2 cells. Our findings suggest that the GO Chitosan D-Pinitol FA nanocomposite is a potent drug-loaded nanocarrier that can effectively induce an anticancer effect in hepatoma HepG-2 cells.