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Anticancer effect of altersolanol A, a metabolite produced by the endophytic fungus Stemphylium globuliferum, mediated by its pro-apoptotic and anti-invasive potential via the inhibition of NF-κB activity.
Teiten, Marie-Hélène; Mack, Fabienne; Debbab, Abdessamad; Aly, Amal H; Dicato, Mario; Proksch, Peter; Diederich, Marc.
Afiliação
  • Teiten MH; Laboratoire de Biologie Moléculaire et Cellulaire du Cancer, Hôpital Kirchberg, 9 Rue Edward Steichen, L-2540 Luxembourg, Luxembourg.
Bioorg Med Chem ; 21(13): 3850-8, 2013 Jul 01.
Article em En | MEDLINE | ID: mdl-23664494
Altersolanol A, a natural product from the endophytic fungus Stemphylium globuliferum isolated from the medicinal plant Mentha pulegium (Lamiaceae) growing in Morocco, shows cytotoxic, cytostatic, anti-inflammatory and anti-migrative activity against human chronic myeloid K562 leukemia and A549 lung cancer cells in a dose dependent manner without affecting the viability of non cancerous cells. Altersolanol A induces cell death by apoptosis through the cleavage of caspase-3 and -9 and through the decrease of anti-apoptotic protein expression. Moreover, we report here the importance of the distinct structural features of altersolanol A by testing other related anthracene derivatives in order to identify preliminary structure-activity relationships. Acetylation of altersolanol A did not improve activity where other derivatives such as tetrahydroaltersolanol B and ampelanol that differ from altersolanol A by reduction of one of a carbonyl group and removal of hydroxyl substituents were inactive in comparison. Altogether our results suggest that altersolanol A may be considered as an interesting lead for further development of chemotherapeutic agents.
Assuntos

Texto completo: 1 Coleções: 01-internacional Temas: Geral / Tipos_de_cancer / Pulmao Base de dados: MEDLINE Assunto principal: Leucemia Mielogênica Crônica BCR-ABL Positiva / NF-kappa B / Antraquinonas / Neoplasias Pulmonares / Anti-Inflamatórios / Antineoplásicos Tipo de estudo: Prognostic_studies Limite: Humans Idioma: En Revista: Bioorg Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2013 Tipo de documento: Article País de afiliação: Luxemburgo

Texto completo: 1 Coleções: 01-internacional Temas: Geral / Tipos_de_cancer / Pulmao Base de dados: MEDLINE Assunto principal: Leucemia Mielogênica Crônica BCR-ABL Positiva / NF-kappa B / Antraquinonas / Neoplasias Pulmonares / Anti-Inflamatórios / Antineoplásicos Tipo de estudo: Prognostic_studies Limite: Humans Idioma: En Revista: Bioorg Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2013 Tipo de documento: Article País de afiliação: Luxemburgo