于立华,黄海华,司端运,李智峰,钟大放
YU Li hua 1; HUANG Hai hua 1; SI Duan yun 2; LI Zhi feng 1; ZHONG Da fang 2 (1. School of Pharmaceutical Engineering;

• 1:沈阳药科大学制药工程学院
• 2:沈阳药科大学制药工程学院
• 3:沈阳药科大学药物代谢与药物动力学实验室
• 4:沈阳药科大学制药工程学院

摘要(Abstract)：

目的研究拟低聚氨基糖类系列化合物异戊他定的微生物转化特征。方法采用微生物转化法 ,选择 1 1株丝状霉菌和 9株细菌对异戊他定主要组分进行代谢转化 ,用液相色谱 多级质谱检测转化液中的代谢产物。结果黑曲霉、青霉、从土壤中分离出的丝状霉菌 2 82 9、0 2 35 1 9和 8菌株可使异戊他定发生相似的水解反应 ,对 2 82 9菌株的转化特点进行了较深入的探讨 ,发现其产生的葡萄糖苷水解酶可使异戊他定系列组分从非还原性末端外切脱去葡萄糖残基生成低分子质量的同系物 ;嗜热脂肪芽孢杆菌IFFI 1 0 0 91对异戊他定具有转糖苷反应能力。结论异戊他定组分经2 82 9菌株转化后 ,具有非还原性末端的葡萄糖残基均发生了较完全的降解 ,其化学组成明显简化。
Objective To investigate microbial transformations of isovalertatins, which are homologous complex of pseudooligosaccharides and used as an α amylase inhibitor. Methods Eleven strains of molds and nine strains of bacteria were applied to evaluating the transformation abilities and the metabolites were determined by LC MS n. Results Aspergillus niger, Penicillium and the mycelioid mold strains 2829, 0235 19 and 8 showed the degradation activities against the isovalertatins. The experiments to the mold strain 2829 concluded that it could secrete the glucosidase, spliting the glucose residue from the non reducing end for isovalertatins. Bacillus stearothermophilus could transform the glucosidic group. Conclusion Almost all the analogues possessing the glucose units in the non reducing end were degradated by the mold 2829. The chemical composition of isovalertatins was, then, simplified to some extent.

关键词(KeyWords)： 异戊他定;拟寡糖;微生物转化;药物代谢;液相色谱质谱联用法
isovalertatins; pseudooligosaccharides; microbial transformation; drug metabolism; liquid chromatography mass spectrometry

Abstract:

Keywords:

基金项目(Foundation): 国家自然科学基金资助项目 ( 39930 1 80 )

作者(Authors): 于立华,黄海华,司端运,李智峰,钟大放
YU Li hua 1; HUANG Hai hua 1; SI Duan yun 2; LI Zhi feng 1; ZHONG Da fang 2 (1. School of Pharmaceutical Engineering;

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