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Polyphenolic Phytochemicals in Cancer Prevention and Therapy: Bioavailability versus Bioefficacy

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† Department of Physiology, University of Valencia, 46010 Valencia, Spain
‡ Department of Health and Functional Valorization, San Vicente Martir Catholic University, 46008 Valencia, Spain
§ Elysium Health Inc., New York, New York 10012, United States
*Phone: 34-963864646. Fax: 34-963864642. E-mail: [email protected]
Cite this: J. Med. Chem. 2017, 60, 23, 9413–9436
Publication Date (Web):June 27, 2017
https://doi.org/10.1021/acs.jmedchem.6b01026
Copyright © 2017 American Chemical Society
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    Abstract

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    Natural polyphenols are organic chemicals which contain phenol units in their structures. They show antitumor properties. However, a key problem is their short half-life and low bioavailability under in vivo conditions. Still, definitively demonstrating the human benefits of isolated polyphenolic compounds (alone or in combination) using modern scientific methodology has proved challenging. The most common discrepancy between experimental and clinical observations is the use of nonphysiologically relevant concentrations of polyphenols in mechanistic studies. Thus, it remains highly controversial how applicable underlying mechanisms are with bioavailable concentrations and biological half-life. The present Perspective analyses proposed antitumor mechanisms, in vivo reported antitumor effects, and possible mechanisms that may explain discrepancies between bioavailability and bioefficacy. Polyphenol metabolism and possible toxic side effects are also considered. Our main conclusion emphasizes that these natural molecules (and their chemical derivatives) indeed can be very useful, not only as cancer chemopreventive agents but also in oncotherapy.

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