利用羟丙基-β-环糊精诱导的包合作用改善甾体的生物转化。
Improvement of steroid biotransformation with hydroxypropyl-beta-cyclodextrin induced complexation.
机构信息
Key Laboratory of Industrial Microbiology, Ministry of Education, College of Biotechnology, Tianjin University of Science and Technology, Tianjin, People's Republic of China.
出版信息
Appl Biochem Biotechnol. 2009 Dec;159(3):642-54. doi: 10.1007/s12010-008-8499-2. Epub 2009 Feb 3.
The inclusion complexes induced by cyclodextrins and its derivates have been shown previously to enhance the biotransformation of hydrophobic compounds. Using hydroxypropyl-beta-cyclodextrin (HP-beta-CD; 20% w/v), the water solubility of cortisone acetate increased from 0.039 to 7.382 g L(-1) at 32 degrees C. The solubilization effect of HP-beta-CD was far superior to dimethylformamide (DMF) and ethanol. The dissolution rate also significantly increased in the presence of HP-beta-CD. The enzymatic stability of Delta(1)-dehydrogenase from Arthrobacter simplex TCCC 11037 was not influenced by the increasing concentrations of HP-beta-CD contrary to the organic cosolvents which negatively influenced in the order DMF > ethanol. The activity inhibition effect caused by HP-beta-CD was not so conspicuous as ethanol and DMF. Inactivation constants of ethanol, DMF, and HP-beta-CD were 5.832, 4.541, and 1.216, respectively. The inactivation energy (E (a)) was in the order of HP-beta-CD (55.1 kJ mol(-1)) > ethanol (39.9 kJ mol(-1)) > DMF (37.1 kJ mol(-1)).
先前的研究表明，环糊精及其衍生物形成的包合物能够增强疏水性化合物的生物转化。在 32℃下，使用羟丙基-β-环糊精（HP-β-CD；20%w/v），醋酸可的松的水溶性从 0.039 增加到 7.382 g/L。HP-β-CD 的增溶效果远优于二甲基甲酰胺（DMF）和乙醇。在 HP-β-CD 的存在下，溶解速率也显著提高。相反，与有机助溶剂不同，来自节杆菌属 Simplex TCCC 11037 的Δ1-脱氢酶的酶稳定性不受 HP-β-CD 浓度增加的影响，其影响顺序为 DMF>乙醇。与乙醇和 DMF 相比，HP-β-CD 引起的活性抑制作用并不那么明显。乙醇、DMF 和 HP-β-CD 的失活动力学常数分别为 5.832、4.541 和 1.216。失活能（E(a)）的顺序为 HP-β-CD（55.1 kJ/mol）>乙醇（39.9 kJ/mol）>DMF（37.1 kJ/mol）。
Zotero 插件