Biochemical Basis of Anti-Cancer-Effects of Phloretin-A Natural Dihydrochalcone

Apple is a rich source of bioactive phytochemicals that help improve health by preventing and/or curing many disease processes, including cancer. One of the apple polyphenols is phloretin [2',4',6'-Trihydroxy-3-(4-hydroxyphenyl)-propiophenone], which has been widely investigated for i...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2019-01, Vol.24 (2), p.278
Main Author: Choi, Bu Young
Format: Article
Language:English
Subjects:
Antioxidants
Apoptosis
Cancer
Cancer therapies
Carcinogens
Cell death
cell proliferation
Chemotherapy
Colorectal cancer
Cyclins
DNA damage
Drug development
Enzymes
Epigenetics
Fruits
Glucose transporter
glucose uptake
Glycolysis
Inflammation
Inflammatory bowel disease
Kinases
Lifestyles
Lipid peroxidation
migration
Mitochondria
mRNA
phloretin
Phytochemicals
Polyphenols
Prevention
Radiation
Review
Skin
Tumor cells
Tumors
Xenografts
Xenotransplantation
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Summary:Apple is a rich source of bioactive phytochemicals that help improve health by preventing and/or curing many disease processes, including cancer. One of the apple polyphenols is phloretin [2',4',6'-Trihydroxy-3-(4-hydroxyphenyl)-propiophenone], which has been widely investigated for its antioxidant, anti-inflammatory and anti-cancer activities in a wide array of preclinical studies. The efficacy of phloretin in suppressing xenograft tumor growth in athymic nude mice implanted with a variety of human cancer cells, and the ability of the compound to interfere with cancer cells signaling, have made it a promising candidate for anti-cancer drug development. Mechanistically, phloretin has been reported to arrest the growth of tumor cells by blocking cyclins and cyclin-dependent kinases and induce apoptosis by activating mitochondria-mediated cell death. The blockade of the glycolytic pathway via downregulation of GLUT2 mRNA and proteins, and the inhibition of tumor cells migration, also corroborates the anti-cancer effects of phloretin. This review sheds light on the molecular targets of phloretin as a potential anti-cancer and anti-inflammatory natural agent.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules24020278