6533b7d8fe1ef96bd126ae4d

RESEARCH PRODUCT

Polyphenolic Phytochemicals in Cancer Prevention and Therapy: Bioavailability versus Bioefficacy

Gloria CastellanoRyan W. DellingerRosario SalvadorMaría BenllochSalvador MenaElena ObradorJosé M. Estrela

subject

0301 basic medicinePhytochemicalsBiological AvailabilityPharmacology03 medical and health sciencesDrug Delivery Systems0302 clinical medicineIn vivoNeoplasmsDrug DiscoveryAnimalsAnticarcinogenic AgentsHumansAnticarcinogenic AgentsCancer preventionOrganic chemicalsChemistryPolyphenolsfood and beveragesAntineoplastic Agents PhytogenicBioavailability030104 developmental biologyPolyphenol030220 oncology & carcinogenesisMolecular MedicineBiological availability

description

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.

https://doi.org/10.1021/acs.jmedchem.6b01026