In vitro and in vivo effects of inhibitors on actin and myosin

Research output: Contribution to journalResearch articleContributedpeer-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 languageEnglish
Article number115928
JournalBioorganic and Medicinal Chemistry
Volume30
Publication statusPublished - 15 Jan 2021
Peer-reviewedYes

External IDs

PubMed 33341499

Keywords

Keywords

  • Actin, Cell migration, Flavonoids, Myosin, Pseudilins, Toxicity