Mitochondrion targeting peptide-modified magnetic graphene oxide delivering mitoxantrone for impairment of tumor mitochondrial functions

In this study, we prepared mitochondrion targeting peptide-grafted magnetic graphene oxide (GO) nanocarriers for efficient impairment of the tumor mitochondria. The two-dimensional GOMNP-MitP nanosheets were synthesized by grafting magnetic gamma-Fe2O3 to the surface of GO, followed by covalent modification of mitochondrion targeting peptide (MitP). GOMNP-MitP exhibited the high capacity of loading the anticancer drug mitoxantrone (MTX), and preferentially targeted the tumor mitochondria. With the aid of alternating magnetic field (AMF), the MTX-loading GOMNP-MitP released MTX to the mitochondria, severely impairing mitochondrial functions, including attenuation of ATP production, decrease in mitochondrial membrane potential (MMP), and further leading to activation of apoptosis. This study realized high-efficient mitochondrion-targeting drug delivery for anticancer therapy by twodimensional nanoplatforms. (C) 2020 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.

Automated summary

This study achieved efficient impairment of tumor mitochondria by preparing mitochondrion targeting peptide-grafted magnetic graphene oxide nanocarriers. The nanocarriers exhibited high drug-loading capacity for anticancer drug delivery and preferential targeting of tumor mitochondria, leading to severe impairment of mitochondrial functions and activation of apoptosis. The study demonstrates the potential of two-dimensional nanoplatforms for mitochondrion-targeting drug delivery in cancer therapy.