新型半合成强心甾内酯类似物3β-[2-(1-金刚烷胺)-1-氧代乙胺]-洋地黄毒苷元（AMANTADIG）有效抑制人白血病和泌尿系统肿瘤细胞系的细胞生长。

The New Semisynthetic Cardenolide Analog 3β-[2-(1-Amantadine)-1-on-ethylamine]-digitoxigenin (AMANTADIG) Efficiently Suppresses Cell Growth in Human Leukemia and Urological Tumor Cell Lines.

作者信息

Nolte Elke, Sobel Anna, Wach Sven, Hertlein Heidi, Ebert Nadja, Müller-Uri Frieder, Slany Robert, Taubert Helge, Wullich Bernd, Kreis Wolfgang

机构信息

Department of Urology, University Hospital Erlangen, Erlangen, Germany

Department of Biology, Friedrich Alexander University Erlangen-Nürnberg, Erlangen, Germany.

出版信息

Anticancer Res. 2015 Oct;35(10):5271-5.

PMID:26408686

Abstract

BACKGROUND/AIM: The use of cardenolides in the treatment of cardiac insufficiency is well-established. However, the potential of cardenolides in tumor therapy has not been comprehensively studied. The aim of the present study was to characterize the cytotoxic effects of the new semisynthetic cardenolide analog AMANTADIG (3β-[2-(1-amantadine)-1-on-ethylamine]-digitoxigenin), and the cardenolide digitoxin on leukemia and urological tumor cell lines.

MATERIALS AND METHODS

The anti-proliferative effects of AMANTADIG and digitoxin on leukemia and urological cancer cell lines were analyzed using (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) tetrazolium reduction viability assay.

RESULTS

AMANTADIG and digitoxin exhibited anti-proliferative activities against the leukemia cell lines in the low nanomolar range. The prostate cancer and renal cell carcinoma cell lines were equally sensitive to AMANTADIG and digitoxin, however, the leukemia cell lines were more sensitive to both cardenolides.

CONCLUSION

The new cardenolide analog AMANTADIG appears effective in cell growth inhibition of leukemia and urological tumor cell lines.

摘要

背景/目的：强心甾类化合物用于治疗心脏功能不全已得到充分证实。然而，强心甾类化合物在肿瘤治疗中的潜力尚未得到全面研究。本研究的目的是表征新型半合成强心甾类类似物AMANTADIG（3β-[2-(1-金刚烷)-1-氧代乙胺]-洋地黄毒苷元）和强心甾类化合物洋地黄毒苷对白血病和泌尿系统肿瘤细胞系的细胞毒性作用。