posted on 2021-02-15, 06:14authored byHaijun Ma, Xiaoyan Zhang, Yang Yang, Shumu Li, Jiawei Huo, Yang Liu, Mirong Guan, Mingming Zhen, Chunying Shu, Jie Li, Chunru Wang
Hydrophilic fullerene derivatives
get notable performance in various
biological applications, especially in cancer therapy and antioxidation.
The biological behaviors of functional fullerenes are much dependent
on their surface physicochemical properties. The excellent reactive
oxygen species-scavenging capabilities of functional fullerenes promote
their outstanding performances in inhibiting pathological symptoms
associated with oxidative stress, including neurodegenerative diseases,
cardiovascular diseases, acute and chronic kidney disease, and diabetes.
Herein, fullerene derivatives with reversed surface charges in aqueous
solutions are prepared: cationic C60-EDA and anionic C60-(EDA-EA). Under the driving force of membrane potential
(negative inside) in the cell and mitochondria, C60-EDA
is much rapidly taken in by cells and transported into mitochondria
compared with C60-(EDA-EA) that is enriched in lysosomes.
With high cellular uptake and mitochondrial enrichment, C60-EDA exhibits stronger antioxidation capabilities in vitro than C60-(EDA-EA), indicating its better performance
in the therapy of oxidation-induced diseases. It is revealed that
the cellular uptake rate, subcellular location, and intracellular
antioxidation behavior of fullerene derivatives are primarily mediated
by their surface charges, providing new strategies for the design
of fullerene drugs and their biological applications.