酶法合成抗癌新药氟铁龙前体——5-FUR  

Enzymatic Synthesis of 5-FUR, a Precursor of a New Anti-cancer Medicine 5'-DFUR

作　　者：闫蓬勃[1] 丁庆豹[1] 邱蔚然[1] 严滢[1] 石佳瑛[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：《华东理工大学学报（自然科学版）》2001年第2期143-146,共4页Journal of East China University of Science and Technology

摘　　要：筛选得到一株核苷磷酸化酶活力高的乙酰短杆菌 ,以该菌体为酶源酶法合成抗癌新药氟铁龙前体 5-氟尿苷 ,所用反应物为鸟苷和 5-氟尿嘧啶。在 1 50 m L的摇瓶装液 1 5m L的条件下进行研究 ,结果显示 :菌体添加量 2 0～ 30 g/L,底物浓度 1 0 0 mmol/L,磷酸盐浓度 50 mmol/L( p H8.0 ) ,60°C,摇床转速 1 60 r/min,反应 4h,5-氟尿苷的转化率可以达到 60A strain of Brevibacterium acetylium QDY2000 that can produce nucleoside phosphorylase has been successfully screened. 5 Fluorouridine which can be used as the precursor of the 5′ deoxy 5 fluorouridine was enzymatically synthesized from guanosine and 5 fluorouracil by QDY2000. The optimal reaction conditions were studied in 150mL shaking bottle with 15mL solution. The conversion yield could reach above 60% while the reaction mixtures, containing 20~30g/L wet cells, 100mmol/L substrates and 50mmol/L phosphate buffer (pH adjusted to 8.0 with NaOH), were incubated at 60°C for 4h at the shaking speed of 160r/min.

关 键 词：酶法合成 5-氟尿苷 乙酰短杆菌 5-氟尿嘧啶 鸟苷 抗癌药物 

分 类 号：R979.1[医药卫生—药品] Q814[医药卫生—药学]