Research Progress in the Modification of Quercetin Leading to Anticancer Agents

  • Molecules. 2017 Jul 29;22(8):1270. doi: 10.3390/molecules22081270.
Alessandro Massi  1 ,  Olga Bortolini  2 ,  Daniele Ragno  3 ,  Tatiana Bernardi  4 ,  Gianni Sacchetti  5 ,  Massimo Tacchini  6 ,  Carmela De Risi  7
Affiliations
  • 1. Dipartimento di Scienze Chimiche e Farmaceutiche, Università di Ferrara, Via Luigi Borsari 46, I-44121 Ferrara, Italy. [email protected].
  • 2. Dipartimento di Scienze Chimiche e Farmaceutiche, Università di Ferrara, Via Luigi Borsari 46, I-44121 Ferrara, Italy. [email protected].
  • 3. Dipartimento di Scienze Chimiche e Farmaceutiche, Università di Ferrara, Via Luigi Borsari 46, I-44121 Ferrara, Italy. [email protected].
  • 4. Dipartimento di Scienze Chimiche e Farmaceutiche, Università di Ferrara, Via Luigi Borsari 46, I-44121 Ferrara, Italy. [email protected].
  • 5. Dipartimento di Scienze della Vita e Biotecnologie, Sezione di Botanica Applicata, Piazzale Luciano Chiappini 3, I-44123 Ferrara, Italy. [email protected].
  • 6. Dipartimento di Scienze della Vita e Biotecnologie, Sezione di Botanica Applicata, Piazzale Luciano Chiappini 3, I-44123 Ferrara, Italy. [email protected].
  • 7. Dipartimento di Scienze Chimiche e Farmaceutiche, Università di Ferrara, Via Luigi Borsari 46, I-44121 Ferrara, Italy. [email protected].
PMID: 28758919 DOI: 10.3390/molecules22081270
Abstract

The flavonoid quercetin (3,3',4',5,7-pentahydroxyflavone) is widely distributed in Plants, foods, and beverages. This polyphenol compound exhibits varied biological actions such as antioxidant, radical-scavenging, anti-inflammatory, Antibacterial, Antiviral, gastroprotective, immune-modulator, and finds also application in the treatment of obesity, cardiovascular diseases and diabetes. Besides, quercetin can prevent neurological disorders and exerts protection against mitochondrial damages. Various in vitro studies have assessed the Anticancer effects of quercetin, although there are no conclusive data regarding its mode of action. However, low bioavailability, poor aqueous solubility as well as rapid body clearance, fast metabolism and enzymatic degradation hamper the use of quercetin as therapeutic agent, so intense research efforts have been focused on the modification of the quercetin scaffold to obtain analogs with potentially improved properties for clinical applications. This review gives an overview of the developments in the synthesis and anticancer-related activities of quercetin derivatives reported from 2012 to 2016.

Keywords
anticancer; cell proliferation; cytotoxicity; methoxyflavones; multi-drug resistance (MDR); quercetin; quercetin derivatives.
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