Methoxychalcones as potential anticancer agents for colon cancer: Is membrane perturbing potency relevant?

Chalcones are naturally produced by many plants, and constitute precursors for the synthesis of flavons and flavanons. They were shown to possess antibacterial, antifungal, anti-cancer, and anti- inflammatory properties. The goal of the study was to assess the suitability of three synthetic methoxyc...

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Published in:Biochimica et biophysica acta. General subjects 2024-04, Vol.1868 (4), p.130581-130581, Article 130581
Main Authors: Palko-Łabuz, Anna, Wesołowska, Olga, Błaszczyk, Maria, Uryga, Anna, Sobieszczańska, Beata, Skonieczna, Magdalena, Kostrzewa-Susłow, Edyta, Janeczko, Tomasz, Środa-Pomianek, Kamila
Format: Article
Language:English
Subjects:
Apoptosis
colon cancer
Lipid rafts
Membrane interaction
Methoxychalcones
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Summary:Chalcones are naturally produced by many plants, and constitute precursors for the synthesis of flavons and flavanons. They were shown to possess antibacterial, antifungal, anti-cancer, and anti- inflammatory properties. The goal of the study was to assess the suitability of three synthetic methoxychalcones as potential anticancer agents. In a panel of colon cancer cell lines they were demonstrated to be cytotoxic, proapoptotic, causing cell cycle arrest, and increasing intracellular level of reactive oxygen species. Anticancer activity of the compounds was not diminished in the presence of stool extract containing microbial enzymes that could change the structure of chalcones. Moreover, methoxychalcones interacted strongly with model phosphatidylcholine membranes as detected by differential scanning calorimetry. Metohoxychalcones particularly affected the properties of lipid domains in giant unilamellar liposomes formed from raft-mimicking lipid composition. This may be of importance since many molecular targets for therapy of metastatic colon cancer are raft-associated receptors (e.g., receptor tyrosine kinases). The importance of membrane perturbing potency of methoxychalcones for their biological activity was additionally corroborated by the results obtained by molecular modelling. [Display omitted] •methoxychalcones reduce colon cancer cells growth.•they possess anticancer activity even in presence of metabolizing enzyme.•methoxychalcones cause colon cancer cell cycle arrest in G2/M phase.•the compounds interact with model lipid membranes.
ISSN:0304-4165
1872-8006
DOI:10.1016/j.bbagen.2024.130581