Next Article in Journal
Xanthones and Quinolones Derivatives Produced by the Deep-Sea-Derived Fungus Penicillium sp. SCSIO Ind16F01
Previous Article in Journal
The Use of Liposomes and Nanoparticles as Drug Delivery Systems to Improve Cancer Treatment in Dogs and Cats
Article Menu
Issue 12 (December) cover image

Export Article

Open AccessArticle
Molecules 2017, 22(12), 2169;

Relationship between Antioxidant and Anticancer Activity of Trihydroxyflavones

Department of Drug Chemistry, Faculty of Pharmacy, Lithuanian University of Health Sciences, LT-44307 Kaunas, Lithuania
Author to whom correspondence should be addressed.
Received: 14 November 2017 / Revised: 3 December 2017 / Accepted: 6 December 2017 / Published: 7 December 2017
Full-Text   |   PDF [1533 KB, uploaded 7 December 2017]   |  


Plant polyphenols have been highlighted not only as chemopreventive, but also as potential anticancer substances. Flavones are a subclass of natural flavonoids reported to have an antioxidant and anticancer activity. The aim of our study was to evaluate antioxidant and anticancer activity of seventeen trihydroxyflavone derivatives, including apigenin (API) and baicalein (BCL). Also, we wanted to find out if there is a correlation between those two effects. Cell growth inhibition testing was carried out using MTT assay in three different human cancer cell lines: lung (A549), breast (MCF-7) and brain epithelial (U87). Antioxidant activity was determined by the DPPH radical scavenging method. Thirteen trihydroxyflavones possessed anticancer activity against at least one tested cancer cell line. They were more active against the MCF-7 cell line, and the lowest activity was determined against the U87 cell line. The majority of compounds inhibited cancer cell growth at EC50 values between 10–50 µM. The most active compound was 3’,4’,5-trihydroxyflavone 7, especially against A549 and MCF-7 cell lines. The correlation between anti-proliferative and antioxidant activity was only moderate, and it was determined for A549 and U87 cancer cell lines. The most important fragment for those two effects is the ortho-dihydroxy group in ring B. Conclusions. Trihydroxyflavones demonstrated anticancer activity. Further and more detailed studies should to be carried out to estimate the structure–activity relationship of these compounds. View Full-Text
Keywords: trihydroxyflavone; flavonoid; antioxidant; anticancer; structure-activity relationship trihydroxyflavone; flavonoid; antioxidant; anticancer; structure-activity relationship

Graphical abstract

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

Share & Cite This Article

MDPI and ACS Style

Grigalius, I.; Petrikaite, V. Relationship between Antioxidant and Anticancer Activity of Trihydroxyflavones. Molecules 2017, 22, 2169.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top