5-HMF is widely presented in foods and produced through the degradation of
hexoses and Maillard reaction during heat treatment of foods containing reducing
sugars and
amino acids in an
acid environment. However, controversial conclusions on the
biological effects of 5-HMF have been drawn in previous studies. Therefore, the main aim of this study was to investigate the
antioxidant and antiproliferative activities of 5-HMF. The 2,2'-azinobis-3-ethylbenzothiazolin-6-sulfonic
acid (
ABTS) assay, the 1,1-diphenyl-2-picryhydrazyl (DPPH) assay, and the
hemolysis assay induced by
2,2'-azobis(2-amidinopropane) dihydrochloride (
AAPH) were performed to evaluate the
antioxidant capacity of 5-HMF. The results showed that 5-HMF exhibited novel
antioxidant activity by scavenging the
ABTS and DPPH
free radicals and inhibited the
AAPH-induced
hemolysis in a dose-dependent manner. In the
hemolysis assay, the reduction of ROS and MDA contents and the increase in
enzyme activities of SOD, CAT, and GPx were found in erythrocytes pretreated with 5-HMF, which demonstrated that 5-HMF could prevent the peroxidation from the source to protect the erythrocytes. The morphological changes of erythrocytes was also verified by observation using atomic force microscopy. The inhibitory effect of 5-HMF on human
cancer cell proliferation was investigated by MTT assay, flow cytometric analysis, and the TUNEL and
DAPI costaining assay. The results showed that 5-HMF displayed higher antiproliferative activity on human
melanoma A375 cells than other cell lines. Further investigation on the action mechanisms revealed that 5-HMF could induce A375 cell apoptosis and G0/G1 cell cycle arrest. The A375 cell apoptosis that 5-HMF induced was characterized by a TUNEL and
DAPI costaining assay. These findings suggest that 5-HMF could be developed as a novel natural
antioxidant with potential applications in
cancer chemoprevention.