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New hemisynthetic derivatives of sphaeropsidin phytotoxins triggering severe endoplasmic reticulum swelling in cancer cells.
Ingels, Aude; Scott, Robert; Hooper, Annie R; van der Westhuyzen, Aletta E; Wagh, Sachin B; de Meester, Joséphine; Maddau, Lucia; Marko, Doris; Aichinger, Georg; Berger, Walter; Vermeersch, Marjorie; Pérez-Morga, David; Maslivetc, Vladimir A; Evidente, Antonio; van Otterlo, Willem A L; Kornienko, Alexander; Mathieu, Véronique.
Afiliación
  • Ingels A; Department of Pharmacotherapy and Pharmaceutics, Chemistry and Biochemistry, Faculté de Pharmacie, Université Libre de Bruxelles, Brussels, Belgium.
  • Scott R; ULB Cancer Research Center, U-CRC, Université Libre de Bruxelles, Brussels, Belgium.
  • Hooper AR; Department of Chemistry and Biochemistry, Texas State University, San Marcos, TX, 78666, USA.
  • van der Westhuyzen AE; Department of Chemistry and Biochemistry, Texas State University, San Marcos, TX, 78666, USA.
  • Wagh SB; Department of Chemistry and Polymer Science, University of Stellenbosch, Matieland, Stellenbosch, 7600, South Africa.
  • de Meester J; Department of Chemistry and Biochemistry, Texas State University, San Marcos, TX, 78666, USA.
  • Maddau L; Department of Chemistry and Polymer Science, University of Stellenbosch, Matieland, Stellenbosch, 7600, South Africa.
  • Marko D; Department of Agriculture, Section of Plant Pathology and Entomology, University of Sassari, Sassari, Italy.
  • Aichinger G; Department of Food Chemistry and Toxicology, Faculty of Chemistry, University of Vienna, Vienna, Austria.
  • Berger W; Department of Food Chemistry and Toxicology, Faculty of Chemistry, University of Vienna, Vienna, Austria.
  • Vermeersch M; Medical University of Vienna Center for Cancer Research, Vienna, Austria.
  • Pérez-Morga D; Electron Microscopy Laboratory, Center for Microscopy and Molecular Imaging (CMMI), Université Libre de Bruxelles (ULB), Gosselies, Belgium.
  • Maslivetc VA; Electron Microscopy Laboratory, Center for Microscopy and Molecular Imaging (CMMI), Université Libre de Bruxelles (ULB), Gosselies, Belgium.
  • Evidente A; Department of Chemistry and Biochemistry, Texas State University, San Marcos, TX, 78666, USA.
  • van Otterlo WAL; Institute of Biomolecular Chemistry, National Research Council, Pozzuoli, Italy.
  • Kornienko A; Department of Chemistry and Polymer Science, University of Stellenbosch, Matieland, Stellenbosch, 7600, South Africa.
  • Mathieu V; Department of Chemistry and Biochemistry, Texas State University, San Marcos, TX, 78666, USA. a_k76@txstate.edu.
Sci Rep ; 14(1): 14674, 2024 06 25.
Article en En | MEDLINE | ID: mdl-38918539
ABSTRACT
Sphaeropsidins are iso-pimarane diterpenes produced by phytopathogenic fungi that display promising anticancer activities. Sphaeropsidin A, in particular, has been shown to counteract regulatory volume increase, a process used by cancer cells to avoid apoptosis. This study reports the hemi-synthesis of new lipophilic derivatives obtained by modifications of the C15,C16-alkene moiety. Several of these compounds triggered severe ER swelling associated with strong proteasomal inhibition and consequently cell death, a feature that was not observed with respect to mode of action of the natural product. Significantly, an analysis from the National Cancer Institute sixty cell line testing did not reveal any correlations between the most potent derivative and any other compound in the database, except at high concentrations (LC50). This study led to the discovery of a new set of sphaeropsidin derivatives that may be exploited as potential anti-cancer agents, notably due to their maintained activity towards multidrug resistant models.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Retículo Endoplásmico Límite: Humans Idioma: En Revista: Sci Rep Año: 2024 Tipo del documento: Article País de afiliación: Bélgica Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Retículo Endoplásmico Límite: Humans Idioma: En Revista: Sci Rep Año: 2024 Tipo del documento: Article País de afiliación: Bélgica Pais de publicación: Reino Unido