University of Jyväskylä, Department of Chemistry, P.O. Box 35, FI-40014 Jyväskylä, Finland.
Steroids. 2012 Feb;77(3):193-203. doi: 10.1016/j.steroids.2011.11.006. Epub 2011 Nov 22.
Design, synthesis, and characterization of six novel bile acid-cysteamine conjugates together with investigation of their structural studies, gelation properties, and preliminary toxicity evaluation, are reported. Solid state properties of selected compounds were studied by means of X-ray diffraction and (13)C CPMAS NMR spectroscopy. N-(2-thioethyl)-3α,7α,12α-trihydroxy-5β-cholan-24-amide was shown to exhibit (pseudo)polymorphism, and a single crystal structure of its non-stoichiometric hydrate is reported herein. Cholyl and dehydrocholyl derivatives bearing three functionalities in their steroidal backbone were shown to undergo self-assembly leading to gelation in certain organic solvents. Preliminary morphology studies of the formed gels by scanning electron microscopy (SEM) were performed. The standard model mouse fibroblast cell line together with the MTT and NR tests were utilized for evaluating the toxicity of the prepared compounds. Lithocholyl, ursodeoxycholyl, and dehydrocholyl derivatives turned out to be relatively non-toxic in the conditions studied.
设计、合成并表征了六种新型胆酸-半胱胺缀合物，同时研究了它们的结构、胶凝性能和初步毒性评价。通过 X 射线衍射和（13）C CPMAS NMR 光谱研究了所选化合物的固态性质。结果表明，N-(2-硫代乙基)-3α,7α,12α-三羟基-5β-胆烷-24-酰胺具有（准）多晶型性，并在此报告了其非化学计量水合物的单晶结构。在甾体骨架中具有三个功能基团的胆酰基和去氢胆酰基衍生物能够进行自组装，在某些有机溶剂中形成凝胶。通过扫描电子显微镜（SEM）对形成的凝胶进行了初步形态学研究。利用标准的小鼠成纤维细胞系以及 MTT 和 NR 试验评估了所制备化合物的毒性。在研究的条件下，胆酸、熊去氧胆酸和去氢胆酸衍生物的毒性相对较低。
