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

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 c...

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Main Authors: Julia Eichsteininger, Kerstin Kirisits, Claudia Smöch, Christa Stadlbauer, Chi Huu Nguyen, Walter Jäger, Ali Özmen, Gerhard Ecker, Georg Krupitza, Liselotte Krenn
Format: Article
Language:English
Published: MDPI AG 2019-09-01
Series:Scientia Pharmaceutica
Subjects:
Online Access:https://www.mdpi.com/2218-0532/87/3/23
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author Julia Eichsteininger
Kerstin Kirisits
Claudia Smöch
Christa Stadlbauer
Chi Huu Nguyen
Walter Jäger
Ali Özmen
Gerhard Ecker
Georg Krupitza
Liselotte Krenn
author_facet Julia Eichsteininger
Kerstin Kirisits
Claudia Smöch
Christa Stadlbauer
Chi Huu Nguyen
Walter Jäger
Ali Özmen
Gerhard Ecker
Georg Krupitza
Liselotte Krenn
author_sort Julia Eichsteininger
collection DOAJ
description 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.
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spelling doaj.art-9a52568d42d440f4882d85e1b7f9bca92022-12-22T04:09:50ZengMDPI AGScientia Pharmaceutica2218-05322019-09-018732310.3390/scipharm87030023scipharm87030023Structural Insight into the In Vitro Anti-Intravasative Properties of FlavonoidsJulia Eichsteininger0Kerstin Kirisits1Claudia Smöch2Christa Stadlbauer3Chi Huu Nguyen4Walter Jäger5Ali Özmen6Gerhard Ecker7Georg Krupitza8Liselotte Krenn9Department of Pathology, Medical University of Vienna, 1090 Vienna, AustriaDepartment of Pathology, Medical University of Vienna, 1090 Vienna, AustriaDepartment of Pathology, Medical University of Vienna, 1090 Vienna, AustriaDepartment of Pathology, Medical University of Vienna, 1090 Vienna, AustriaDepartment of Pathology, Medical University of Vienna, 1090 Vienna, AustriaDepartment of Clinical Pharmacy and Diagnostics, Faculty of Life Sciences, University of Vienna, 1090 Vienna, AustriaDepartment of Biology, Faculty of Science and Art, Adnan Menderes University, 90010 Aydin, TurkeyPharmacoinformatics Research Group, Department of Pharmaceutical Chemistry, Faculty of Life Sciences, University of Vienna, 1090 Vienna, AustriaDepartment of Pathology, Medical University of Vienna, 1090 Vienna, AustriaDepartment of Pharmacognosy, Faculty of Life Sciences, University of Vienna, 1090 Vienna, AustriaWe 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.https://www.mdpi.com/2218-0532/87/3/23CCID assayinhibition of gap formationflavonoidsanti-invasivebreast cancerstructure-activity relationship
spellingShingle Julia Eichsteininger
Kerstin Kirisits
Claudia Smöch
Christa Stadlbauer
Chi Huu Nguyen
Walter Jäger
Ali Özmen
Gerhard Ecker
Georg Krupitza
Liselotte Krenn
Structural Insight into the In Vitro Anti-Intravasative Properties of Flavonoids
Scientia Pharmaceutica
CCID assay
inhibition of gap formation
flavonoids
anti-invasive
breast cancer
structure-activity relationship
title Structural Insight into the In Vitro Anti-Intravasative Properties of Flavonoids
title_full Structural Insight into the In Vitro Anti-Intravasative Properties of Flavonoids
title_fullStr Structural Insight into the In Vitro Anti-Intravasative Properties of Flavonoids
title_full_unstemmed Structural Insight into the In Vitro Anti-Intravasative Properties of Flavonoids
title_short Structural Insight into the In Vitro Anti-Intravasative Properties of Flavonoids
title_sort structural insight into the in vitro anti intravasative properties of flavonoids
topic CCID assay
inhibition of gap formation
flavonoids
anti-invasive
breast cancer
structure-activity relationship
url https://www.mdpi.com/2218-0532/87/3/23
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