In vitro and in vivo effects of inhibitors on actin and myosin
Research output: Contribution to journal › Research article › Contributed › peer-review
Contributors
Abstract
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.
Details
Original language | English |
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Article number | 115928 |
Journal | Bioorganic and Medicinal Chemistry |
Volume | 30 |
Publication status | Published - 15 Jan 2021 |
Peer-reviewed | Yes |
External IDs
PubMed | 33341499 |
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Keywords
ASJC Scopus subject areas
Keywords
- Actin, Cell migration, Flavonoids, Myosin, Pseudilins, Toxicity