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Methoxychalcones as potential anticancer agents for colon cancer: Is membrane perturbing potency relevant?
Palko-Labuz, Anna; Wesolowska, Olga; Blaszczyk, Maria; Uryga, Anna; Sobieszczanska, Beata; Skonieczna, Magdalena; Kostrzewa-Suslow, Edyta; Janeczko, Tomasz; Sroda-Pomianek, Kamila.
Afiliación
  • Palko-Labuz A; Department of Biophysics and Neuroscience, Wroclaw Medical University, Wroclaw, Poland. Electronic address: anna.palko-labuz@umw.edu.pl.
  • Wesolowska O; Department of Biophysics and Neuroscience, Wroclaw Medical University, Wroclaw, Poland.
  • Blaszczyk M; Department of Biophysics and Neuroscience, Wroclaw Medical University, Wroclaw, Poland.
  • Uryga A; Department of Biophysics and Neuroscience, Wroclaw Medical University, Wroclaw, Poland.
  • Sobieszczanska B; Department of Microbiology, Wroclaw Medical University, Wroclaw, Poland.
  • Skonieczna M; Department of Systems Biology and Engineering, The Silesian University of Technology, Gliwice, Poland; Biotechnology Centre, Silesian University of Technology, Gliwice, Poland.
  • Kostrzewa-Suslow E; Department of Food Chemistry and Biocatalysis, Wroclaw University of Environmental and Life Sciences, Wroclaw, Poland.
  • Janeczko T; Department of Food Chemistry and Biocatalysis, Wroclaw University of Environmental and Life Sciences, Wroclaw, Poland.
  • Sroda-Pomianek K; Department of Biophysics and Neuroscience, Wroclaw Medical University, Wroclaw, Poland.
Biochim Biophys Acta Gen Subj ; 1868(4): 130581, 2024 Apr.
Article en En | MEDLINE | ID: mdl-38336309
ABSTRACT
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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Neoplasias del Colon / Chalconas / Antineoplásicos Límite: Humans Idioma: En Revista: Biochim Biophys Acta Gen Subj Año: 2024 Tipo del documento: Article Pais de publicación: Países Bajos

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Neoplasias del Colon / Chalconas / Antineoplásicos Límite: Humans Idioma: En Revista: Biochim Biophys Acta Gen Subj Año: 2024 Tipo del documento: Article Pais de publicación: Países Bajos