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.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
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)
