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Zingerone Nanotetramer Strengthened the Polypharmacological Efficacy of Zingerone on Human Hepatoma Cell Lines

Kung, Mei-Lang, Lin, Pei-Ying, Huang, Shih-Tsung, Tai, Ming-Hong, Hsieh, Shu-Ling, Wu, Chih-Chung, Yeh, Bi-Wen, Wu, Wen-Jeng, Hsieh, Shuchen
ACS applied materials & interfaces 2018 v.11 no.1 pp. 137-150
DNA damage, antineoplastic activity, apoptosis, caspases, cell cycle, drugs, hepatoma, human cell lines, nanoparticles, particle size, signal transduction, therapeutics, transcription factor NF-kappa B
We base this study on the concept of drug repositioning to reconstitute the natural product of zingerone as zingerone nanoparticles (zingerone NPs) through a one-pot synthesized process. The as-fabricated zingerone NPs were characterized; they possessed a particle size of 1.42 ± 0.67 nm and a reconstituted structure of zingerone nanotetramer. We further validate the effects of zingerone NPs on the antitumor activity and investigate the relative underlying mechanisms on the human hepatoma SK-Hep-1 and Huh7 cell lines. Our results demonstrated that zingerone NPs significantly inhibit Akt activity and NFκB expression as well as activate the caspases cascade signaling pathway which are involved in the antiproliferation, antitumorigenicity, disturbing cell cycle progression, and induction of DNA damage as well as cell apoptosis. These findings were promising to provide a “Nano-chemoprevention” strategy in future cancer therapeutics and medical and clinical applications.