Wenjia Hou,1,2,* Lan Shen,1,* Yimin Zhu,1 Xuanjia Wang,1 Tianyu Du,1 Fang Yang,1 Yabin Zhu1 

1Health Science Center, Ningbo University, Ningbo, 315211, People’s Republic of China; 2State Key Laboratory of Molecular Engineering of Polymers, Fudan University, Shanghai, 200438, People’s Republic of China

*These authors contributed equally to this work

Correspondence: Wenjia Hou; Yabin Zhu, Email houwenjia@nbu.edu.cn; zhuyabin@nbu.edu.cn

Abstract: Fullerenes hold tremendous potential as alternatives to conventional chemotherapy or radiotherapy for tumor treatment due to their abilities to photodynamically kill tumor cells, destroy the tumor vasculature, inhibit tumor metastasis and activate anti-tumor immune responses, while protecting normal tissue through antioxidative effects. The symmetrical hollow molecular structures of fullerenes with abundant C=C bonds allow versatile chemical modification with diverse functional groups, metal clusters and biomacromolecules to synthesize a wide range of fullerene derivatives with increased water solubility, improved biocompatibility, enhanced photodynamic properties and stronger targeting abilities. This review introduces the anti-tumor mechanisms of fullerenes and summarizes the most recent works on the functionalization of fullerenes and the application of fullerene derivatives in tumor treatment. This review aims to serve as a valuable reference for further development and clinical application of anti-tumor fullerene derivatives.

Keywords: fullerene derivatives, tumor treatment, photodynamic treatment, metastasis inhibition, tumor vasculature, cellular immunity