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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.
Molecules 2017, 22(12), 2169;
Received: 14 November 2017 / Revised: 3 December 2017 / Accepted: 6 December 2017 / Published: 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
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MDPI and ACS Style

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

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