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Future Med Chem. 2017 Nov;9(17):2011-2028. doi: 10.4155/fmc-2017-0118. Epub 2017 Oct 27.

New insights for the use of quercetin analogs in cancer treatment.

Author information

1
Department of Pharmacy, Health & Nutritional Sciences, University of Calabria, 87036, Arcavacata di Rende, Italy.
2
The Department of ChiBioFarAm, Institute for the Study of Nanostructured Materials, ISMN-CNR, O.U. Palermo, University of Messina, 98166, Messina, Italy.
3
Department of Science, University of Basilicata, 85100, Potenza, Italy.
4
Ospedale Policlinico San Martino, 16132, Genoa, Italy.

Abstract

AIM:

Quercetin (Q1) is a flavonoid widely present in plants and endowed with several pharmacological properties mostly due to its antioxidant potential. Q1 shows anticancer activity and could be useful in cancer prevention. On the other hand, Q1 is poorly soluble in water and unstable in physiological systems, and its bioavailability is very low.

METHODS:

A small set of Q1 derivatives (Q2-Q9) has been synthesized following opportunely modified chemical procedures previously reported. Anticancer activity has been evaluated by MTT assay. Human Topoisomerases inhibition has been performed by direct enzymatic assays. Apoptosis has been evaluated by TUNEL assay. ROS production and scavenging activity have been determined by immunofluorescence.

RESULTS:

The anticancer profile of a small library of Q1 analogues, in which the OH groups were all or partially replaced with hydrophobic functional groups, has been evaluated. Two of the studied compounds demonstrated an interesting cytotoxic profile in two breast cancer models showing the capability to inhibit human Topoisomerases.

CONCLUSION:

The studied compounds represent suitable leads for the development of innovative anticancer drugs. [Formula: see text].

KEYWORDS:

ROS scavengers; human Topoisomerases I and II; quercetin analogs

PMID:
29076772
DOI:
10.4155/fmc-2017-0118
[Indexed for MEDLINE]

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