López-Lázaro Miguel, Palma De La Peña Nieves, Pastor Nuria, Martín-Cordero Carmen, Navarro Eduardo, Cortés Felipe, Ayuso María Jesús, Toro María Victoria
Departamento de Farmacología, Facultad de Farmacia, Universidad de Sevilla, Spain.
Planta Med. 2003 Aug;69(8):701-4. doi: 10.1055/s-2003-42789.
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.
最近的研究表明洋地黄类化合物具有抗癌作用，这表明它们可能用于医学肿瘤学。使用SRB测定法，评估了从海伍德紫花洋地黄叶中获得的四种提取物对三种人类癌细胞系的细胞毒性活性。所有提取物均显示出高细胞毒性，在无毒浓度下，IC50值在0.78 - 15微克/毫升范围内，其中甲醇提取物活性最高。在该甲醇提取物中检测到甾体苷（吉托辛衍生物）。使用三种人类癌细胞系在SRB测定法中评估了吉托辛和地高辛，显示IC50值在0.13 - 2.8微摩尔/升范围内，其中肾腺癌癌细胞系（TK - 10）最为敏感。对甲醇提取物和这两种化合物在TK - 10细胞系上进行的形态学凋亡评估表明，它们的细胞毒性是由凋亡作用介导的。最后，讨论了洋地黄类化合物诱导凋亡可能涉及的机制。
