title: Anti-tumour activity of Digitalis purpurea L. subsp. heywoodii.
abstract: Recent research has shown the anticancer effects of digitalis compounds suggesting their possible use in medical oncology. Four extracts obtained from the leaves of Digitalis purpurea subsp. heywoodii have been assessed for cytotoxic activity against three human cancer cell lines, using the SRB assay. All of them showed high cytotoxicity, producing IC50 values in the 0.78 - 15 microg/mL range with the methanolic extract being the most active, in non toxic concentrations. Steroid glycosides (gitoxigenin derivatives) were detected in this methanolic extract. Gitoxigenin and gitoxin were evaluated in the SRB assay using the three human cancer cell lines, showing IC50 values in the 0.13 - 2.8 microM range, with the renal adenocarcinoma cancer cell line (TK-10) being the most sensitive one. Morphological apoptosis evaluation of the methanolic extract and both compounds on the TK-10 cell line showed that their cytotoxicity was mediated by an apoptotic effect. Finally, possible mechanisms involved in apoptosis induction by digitalis compounds are discussed.
authors.affiliation: Departamento de Farmacología, Facultad de Farmacia, Universidad de Sevilla, Spain.
authors.forename: Miguel
authors.initials: M
authors.lastname: López-Lázaro
authors.forename: Nieves
authors.initials: N
authors.lastname: Palma De La Peña
authors.forename: Nuria
authors.initials: N
authors.lastname: Pastor
authors.forename: Carmen
authors.initials: C
authors.lastname: Martín-Cordero
authors.forename: Eduardo
authors.initials: E
authors.lastname: Navarro
authors.forename: Felipe
authors.initials: F
authors.lastname: Cortés
authors.forename: María Jesús
authors.initials: MJ
authors.lastname: Ayuso
authors.forename: María Victoria
authors.initials: MV
authors.lastname: Toro
mesh_terms: D000230:Adenocarcinoma / Q000188:drug therapy; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D002298:Cardenolides / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D045744:Cell Line, Tumor / Q000187:drug effects; D004070:Digitalis; D004077:Digoxin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use; D005047:Etoposide / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D020128:Inhibitory Concentration 50; D007680:Kidney Neoplasms / Q000188:drug therapy; D008517:Phytotherapy; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D018515:Plant Leaves
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D002298:Cardenolides; D010936:Plant Extracts; D005047:Etoposide; D004077:Digoxin; C007846:gitoxigenin; C005003:gitoxin