Anti-tumour activity of Digitalis purpurea L. subsp. heywoodii.
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.
López-Lázaro
Miguel
M
Departamento de Farmacología, Facultad de Farmacia, Universidad de Sevilla, Spain.
Palma De La Peña
Nieves
N
Pastor
Nuria
N
Martín-Cordero
Carmen
C
Navarro
Eduardo
E
Cortés
Felipe
F
Ayuso
María Jesús
MJ
Toro
María Victoria
MV
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
D000972:Antineoplastic Agents, Phytogenic; D002298:Cardenolides; D010936:Plant Extracts; D005047:Etoposide; D004077:Digoxin; C007846:gitoxigenin; C005003:gitoxin