Improving the Efficacy of Plant Polyphenols

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

Download PDF Flyer

Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

This journal supports open access

Aims & ScopeAbstracted/Indexed in

Ranking and Category:
  • 27th of 59 in Chemistry, Medicinal

Submit Abstracts Online Submit Manuscripts Online

Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

View Full Editorial Board

Subscribe Purchase Articles Order Reprints

Current: 2.722
5 - Year: 2.849

Improving the Efficacy of Plant Polyphenols

Anti-Cancer Agents in Medicinal Chemistry, 14(10): 1332-1342.

Author(s): Lucia Biasutto, Andrea Mattarei, Nicola Sassi, Michele Azzolini, Matteo Romio, Cristina Paradisi and Mario Zoratti.

Affiliation: CNR Neuroscience Institute, Viale G. Colombo 3, 35121 Padova, Italy.


Plant polyphenols exhibit potentially useful effects in a wide variety of pathophysiological settings. They interact with proteins such as signalling kinases, transcription factors and ion channels, and modulate redox processes, such as those taking place in mitochondria. Biomedical applications of these natural compounds are however severely hindered by their low bioavailability, rapid metabolism, and often by unfavourable physico-chemical properties, e.g. a generally low water solubility. Derivatives are under development with the aim of improving their bioavailability and/or bioefficacy. Various strategies can be adopted. An increase in circulating blood levels of non-metabolized natural compound may be attainable through prodrugs. In the ideal prodrug, phenolic hydroxyls are protected by capping groups which a) help or at least do not hinder permeation of epithelia; b) prevent conjugative modifications during absorption and first-pass through the liver; c) are eliminated with opportune kinetics to regenerate the parent compound. Moreover, prodrugs may be designed with the goals of modulating physical properties of the parent compound, and/or changing its distribution in the body. A more specific action may be achieved by concentrating the compounds at specific sites of action. An example of the second approach is represented by mitochondria-targeted redox-active polyphenol derivatives, designed to intervene on radical processes in these organelles and as a tool either to protect cells from oxidative insults or to precipitate their death. Mitochondrial targeting can be achieved through conjugation with a triphenylphosphonium lipophilic cation. Quercetin and resveratrol were chosen as model polyphenols for these proof-of-concept studies. Data available at the moment show that both quercetin and resveratrol mitochondria-targeted derivatives are pro-oxidant and cytotoxic in vitro, selectively killing fast-growing and tumoural cells when supplied in the low μM range; the mechanism of ROS generation appears to differ between the two classes of compounds.

These approaches are emerging as promising strategies to obtain new efficient chemopreventive and/or chemotherapeutic drugs based on polyphenols derivatives.


Bioavailability, catechins, mitochondria, polyphenols, prodrugs, quercetin, resveratrol, triphenylphosphonium.

Purchase Online Order Reprints Order Eprints Rights and Permissions

Article Details

Volume: 14
Issue Number: 10
First Page: 1332
Last Page: 1342
Page Count: 11
DOI: 10.2174/1871520614666140627150054
Price: $58

Related Journals

Webmaster Contact: Copyright © 2016 Bentham Science