Institute of Pharmacy, Free University Berlin, Königin-Luise-Str. 2+4, D-14195 Berlin, Germany.
J Chromatogr B Analyt Technol Biomed Life Sci. 2010 Mar 1;878(7-8):713-8. doi: 10.1016/j.jchromb.2010.01.026. Epub 2010 Jan 25.
Saponinum album (Merck), which is a crude mixture of saponins from Gypsophila paniculata L., was shown to improve the anti cancer therapy when used in vivo in combination with saporin-based targeted toxins. Unfortunately saponinum album cannot be used for further development since Merck has ceased its production in the 1990s. As pure saponins are mandatory for use in medical purposes we developed a convenient method for saponin isolation directly from the roots of Gypsophila paniculata L. The developed method is rapid, cheap and scaling up is also possible. By combining dialysis and HPLC three saponins were isolated in a one-step procedure. Chemical structures of the purified saponins were characterized by extensive one and two-dimensional NMR-spectroscopy and by using ESI-TOF-MS. The biological activities of the purified saponins were also investigated. The method presented herein enabled a rapid and cheap isolation of saponins for tumour therapy.
珍珠菜皂素(Merck)是从珍珠菜(Gypsophila paniculata L.)中提取的皂素混合物,当与基于丝氨酸蛋白酶的靶向毒素联合用于体内时,被证明可以改善癌症治疗效果。不幸的是,由于默克公司在 20 世纪 90 年代停止了生产,珍珠菜皂素不能再用于进一步开发。由于纯皂素是用于医疗目的的强制性要求,我们开发了一种从珍珠菜根直接分离皂素的简便方法。该方法快速、廉价,并且可以进行放大。通过结合透析和 HPLC,在一步法中分离出三种皂素。通过广泛的一维和二维 NMR 光谱以及使用 ESI-TOF-MS 对纯化皂素的化学结构进行了表征。还研究了纯化皂素的生物活性。本文所述的方法实现了用于肿瘤治疗的皂素的快速廉价分离。