In Vitro Anticancer Activity, Toxicity and Structure-Activity Relationships of Phyllostictine A, a Natural Oxazatricycloalkenone Produced by the Fungus Phyllosticta cirsii. (Articolo in rivista)

Type
Label
  • In Vitro Anticancer Activity, Toxicity and Structure-Activity Relationships of Phyllostictine A, a Natural Oxazatricycloalkenone Produced by the Fungus Phyllosticta cirsii. (Articolo in rivista) (literal)
Anno
  • 2011-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1016/j.taap.2011.03.027 (literal)
Alternative label
  • Le Calvé B., Lallemand B., Perrone C., Lenglet G., Depauw S., Van Goietsenoven G., Mbury M., Vurro M., Herphelin F., Andolfi A., Zonno M.C., Mathieu V., Dufrasne F., Van Antwerpen P., Poumay Y., David-Cordonnier M.H., Evidente A., Kiss R., (2011)
    In Vitro Anticancer Activity, Toxicity and Structure-Activity Relationships of Phyllostictine A, a Natural Oxazatricycloalkenone Produced by the Fungus Phyllosticta cirsii.
    in Toxicology and applied pharmacology
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Le Calvé B., Lallemand B., Perrone C., Lenglet G., Depauw S., Van Goietsenoven G., Mbury M., Vurro M., Herphelin F., Andolfi A., Zonno M.C., Mathieu V., Dufrasne F., Van Antwerpen P., Poumay Y., David-Cordonnier M.H., Evidente A., Kiss R., (literal)
Pagina inizio
  • 8 (literal)
Pagina fine
  • 17 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 254 (literal)
Rivista
Note
  • ISI Web of Science (WOS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • a Laboratoire de Toxicologie, Faculté de Pharmacie de Pharmacie, Université Libre de Bruxelles (ULB), Brussels, Belgium b Laboratoire de Chimie Analytique, Toxicologie et de Chimie Physique Appliquée, Faculté de Pharmacie de Pharmacie, Université Libre de Bruxelles (ULB), Brussels, Belgium c Dipartimento di Scienze, del Suolo, della Pianta, dell'Ambiente e delle Produzioni Animali, Università di Napoli Federico II, Portici, Italy d INSERM U-837, Jean-Pierre Aubert Research Center (JPARC), Team Molecular and Cellular Targeting for Cancer Treatment, Institut pour la Recherche sur le Cancer de Lille, Lille, France e Istituto di Scienze delle Produzioni Alimentari, CNR, Bari, Italy f Cell and Tissue Laboratory, URPHYM, University of Namur (FUNDP), Namur, Belgium g Laboratoire de Chimie Pharmaceutique Organique, Faculté de Pharmacie de Pharmacie, Université Libre de Bruxelles (ULB), Brussels, Belgium h Plate-Forme Analytique, Faculté de Pharmacie de Pharmacie, Université Libre de Bruxelles (ULB), Brussels, Belgium (literal)
Titolo
  • In Vitro Anticancer Activity, Toxicity and Structure-Activity Relationships of Phyllostictine A, a Natural Oxazatricycloalkenone Produced by the Fungus Phyllosticta cirsii. (literal)
Abstract
  • The in vitro anticancer activity and toxicity of phyllostictine A, a novel oxazatricycloalkenone recently isolated from a plant-pathogenic fungus (Phyllosticta cirsii) was characterized in six normal and five cancer cell lines. Phyllostictine A displays in vitro growth-inhibitory activity both in normal and cancer cells without actual bioselectivity, while proliferating cells appear significantly more sensitive to phyllostictine A than nonproliferating ones. The main mechanism of action by which phyllostictine displays cytotoxic effects in cancer cells does not seem to relate to a direct activation of apoptosis. In the same manner, phyllostictine A seems not to bind or bond with DNA as part of its mechanism of action. In contrast, phyllostictine A strongly reacts with GSH, which is a bionucleophile. The experimental data from the present study are in favor of a bonding process between GSH and phyllostictine A to form a complex though Michael attack at C=C bond at the acrylamide-like system. Considering the data obtained, two new hemisynthesized phyllostictine A derivatives together with three other natural phyllostictines (B, C and D) were also tested in vitro in five cancer cell lines. Compared to phyllostictine A, the two derivatives displayed a higher, phyllostictines B and D a lower, and phyllostictine C an almost equal, growth-inhibitory activity, respectively. These results led us to propose preliminary conclusions in terms of the structure-activity relationship (SAR) analyses for the anticancer activity of phyllostictine A and its related compounds, at least in vitro. (literal)
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