Acta Pharmaceutica, Vol. 70 No. 2, 2020.
Short communication, Note
https://doi.org/10.2478/acph-2020-0003
Curcumin-loaded nanostructured lipid carrier induced apoptosis in human HepG2 cells through activation of DR5/caspases-mediated extrinsic apoptosis pathway
FENGLING WANG
; Department of Pharmacy, The Second People’s Hospital of Hefei, Hefei 230011, Anhui, China; Institute of Drug Metabolism, School of Pharmaceutical Sciences, Anhui University of Chinese Medicine, Hefei 230012, Anhui, China
XI YE
; Department of Pharmacy, The Second People’s Hospital of Hefei, Hefei 230011, Anhui, China
DANDAN ZHAI
; Department of Pharmacy, The Second People’s Hospital of Hefei, Hefei 230011, Anhui, China
WENTING DAI
; Department of Pharmacy, The Second People’s Hospital of Hefei, Hefei 230011, Anhui, China
YIFAN WU
; Institute of Drug Metabolism, School of Pharmaceutical Sciences, Anhui University of Chinese Medicine, Hefei 230012, Anhui, China
JIN CHEN
; Department of Pharmacy, The Second People’s Hospital of Hefei, Hefei 230011, Anhui, China
WEIDONG CHEN
; Institute of Drug Metabolism, School of Pharmaceutical Sciences, Anhui University of Chinese Medicine, Hefei 230012, Anhui, China
Abstract
Curcumin is a lipophilic anti-cancer compound extracted from turmeric. Our previous study demonstrated that the curcumin-loaded nanostructured lipid carrier (Cur-NLC) exhibits superior anti-cancer activity in inhibiting proliferation as well as inducing apoptosis of human HepG2 cells compared to native curcumin. This study aims to unveil the mechanisms underlying the pro-apoptotic effect of Cur-NLC on HepG2 cells. Evidence indicates that low expression of death receptors (DRs) on cancer cell membranes leads to attenuated apoptosis signaling. This study showed that Cur-NLC significantly increased total expression of DR5 protein while simultaneously upregulated cell membrane expression of DR5. Cur-NLC significantly increased caspase-8 and caspase-3 activities, accompanied by increased apoptosis. Furthermore, enhanced apoptosis was inhibited in the presence of a pan-caspase inhibitor, Z-VAD-FMK. Therefore, Cur-NLC induced activation of the extrinsic apoptosis pathway via modulating the DR5/caspase-8/-3 mediated apoptosis pathway in HepG2 cells, suggesting that Cur-NLC is a promising therapeutic agent or supplement for the treatment of hepatocellular carcinoma.
Keywords
curcumin-loaded nanostructured lipid carrier; apoptosis; death receptor 5; caspase-8; caspase-3; HepG2 cells
Hrčak ID:
220890
URI
Publication date:
30.6.2020.
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