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Open AccessArticle

Structural Insight into the In Vitro Anti-Intravasative Properties of Flavonoids

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Department of Pathology, Medical University of Vienna, 1090 Vienna, Austria
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Department of Pharmacognosy, Faculty of Life Sciences, University of Vienna, 1090 Vienna, Austria
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Department of Medicine I, Medical University of Vienna, 1090 Vienna, Austria
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Department of Clinical Pharmacy and Diagnostics, Faculty of Life Sciences, University of Vienna, 1090 Vienna, Austria
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Department of Biology, Faculty of Science and Art, Adnan Menderes University, 90010 Aydin, Turkey
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Pharmacoinformatics Research Group, Department of Pharmaceutical Chemistry, Faculty of Life Sciences, University of Vienna, 1090 Vienna, Austria
*
Author to whom correspondence should be addressed.
Sci. Pharm. 2019, 87(3), 23; https://doi.org/10.3390/scipharm87030023
Received: 6 August 2019 / Revised: 27 August 2019 / Accepted: 30 August 2019 / Published: 3 September 2019
We investigated the effect of 21 flavonoids in a three-dimensional in vitro system for their ability to inhibit gap formation by MCF-7 breast cancer spheroids in monolayers of lymphendothelial cells. Different representatives of the classes of flavones, flavonols, and flavanones were tested in the circular chemorepellent-induced defects (CCID)-assay. Bay11-7082, a known inhibitor of CCID formation served as the positive control. This study provides the first comparison of the potential of flavonoids to suppress features influencing the intravasation of MCF-7 breast cancer cells aggregates through the lymph endothelial barrier. The most significant effects were seen after incubation with the flavones luteolin, chrysin, and apigenin. Additional hydroxylation or methoxylation in positions 6 or 8, as expected, resulted in decreased activity. The tested flavanones remained without or low efficacy. View Full-Text
Keywords: CCID assay; inhibition of gap formation; flavonoids; anti-invasive; breast cancer; structure-activity relationship CCID assay; inhibition of gap formation; flavonoids; anti-invasive; breast cancer; structure-activity relationship
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Eichsteininger, J.; Kirisits, K.; Smöch, C.; Stadlbauer, C.; Nguyen, C.H.; Jäger, W.; Özmen, A.; Ecker, G.; Krupitza, G.; Krenn, L. Structural Insight into the In Vitro Anti-Intravasative Properties of Flavonoids. Sci. Pharm. 2019, 87, 23.

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