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作 者:冯建勋[1] 陈瑞[1] 高兴强[1] 魏东芝[1] 王学东[1]
机构地区:[1]华东理工大学生物反应器工程国家重点实验室,上海200237
出 处:《中国医药工业杂志》2016年第1期25-30,共6页Chinese Journal of Pharmaceuticals
基 金:国家自然科学基金项目(21276083);国家自然科学基金项目(31570079)
摘 要:前期研究筛得1株新金分枝杆菌(Mycobacterium neoaurum),可以转化植物甾醇生成1,4-雄二烯二酮。本研究主要考察了助溶剂Tween-80和羟丙基-?-环糊精(HP-?-CD)对植物甾醇转化产甾体药物中间体效率的影响,并探讨了这些助溶剂对甾醇转化代谢途径的影响。结果显示,当植物甾醇浓度为2.5 g/L,单独添加Tween-80和HP-?-CD时,转化率为70.2%和100%(对照组为36.7%)。单独添加Tween-80时,1,4-雄二烯二酮占总产物比例减小,而雄烯二酮和睾酮比例增加;若单独添加HP-?-CD,1,4-雄二烯二酮比例升高,并且还原性侧链不完全降解产物增多。若两者同时加入,HP-?-CD对植物甾醇转化的影响远大于Tween-80。One strain of Mycobacterium neoaurum was screened in a previous research and it was validated that it could transform phytosterol into androstadienedione (2). In this study, the effects of Tween-80 and hydroxypropyl-β- cyclodextrin (HP-β-CD) on the efficiency of phytosterol biotransformation to drug intermediates were investigated, as well as the effects of two cosolvents on the metabolic pathways. The conversion rates reached 70.2% and 100% in the presence of Tween-80 and HP-β-CD at the phytosterols concerntration of 2.5 g/L, while that of the control group was 36.7 %. When Tween-80 was added, the proportion of 2 decreased, but the proportion of androstenedione and testosterone increased. However, the proportion of 2 increased and side-chain incompletely reduced metabolites were accumulated at the addition of HP-β-CD. Besides, when two cosolvents were used together, the effect of HP-β-CD was much greater than that of Tween-80.
关 键 词:分枝杆菌 植物甾醇 TWEEN-80 羟丙基-β--环糊精 生物转化
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