In vitro and in vivo effects of inhibitors on actin and myosin
Autor: | Sabine Richter, René Martin, Hans-Joachim Knölker, Herwig O. Gutzeit |
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Rok vydání: | 2020 |
Předmět: |
Cell Survival
Oryzias Clinical Biochemistry Pharmaceutical Science Myosins 01 natural sciences Biochemistry chemistry.chemical_compound Structure-Activity Relationship In vivo Cell Movement Drug Discovery Myosin Tumor Cells Cultured Humans Kaempferols Molecular Biology Actin biology Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry Chemistry Organic Chemistry Cell migration biology.organism_classification Enzyme assay In vitro Actins 0104 chemical sciences 010404 medicinal & biomolecular chemistry biology.protein Molecular Medicine Quercetin Kaempferol |
Zdroj: | Bioorganicmedicinal chemistry. 30 |
ISSN: | 1464-3391 |
Popis: | The interaction of actin and myosin is essential for cell migration. We have identified kaempferol and pentahalogenated pseudilins as efficient inhibitors of migration of MDA-MB-231 breast adenocarcinoma cells. The compounds were studied with respect to possible effects on myosin-2-ATPase activity. The pentahalogenated pseudilins inhibited the enzyme activity in vitro. Flavonoids showed no effect on enzyme activity. The polymerization dynamics of actin was measured to test whether the integrity of F-actin is essential for the migration of MDA-MB-231 cells. Quercetin and kaempferol depolymerized F-actin with similar efficiencies as found for the pentahalogenated pseudilins, whereas epigallocatechin showed the weakest effect. As the inhibitory effect on cell migration may be caused by a toxic effect, we have performed a cytotoxicity test and, furthermore, investigated the influence of the test compounds on cardiac function in eleutheroembryos of medaka (Oryzias latipes). Compared with the pentahalogenated pseudilins, the cytotoxic and cardiotoxic effects of flavonoids on medaka embryos were found to be moderate. |
Databáze: | OpenAIRE |
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