摘要
利用微生物转化的方法 ,选取小克银汉霉 (Cunninghamella)为转化菌株 ,对新型抗炎镇痛剂 SFZ- 4 7代谢物的种类与产率进行了研究。高效液相色谱法测试结果表明 ,该菌株对 SFZ- 4 7能产生稳定的转化产物 ,且重现性好。单因素改变实验显示 ,菌株对发酵转化初始 p H值极为敏感。正交试验结果发现 ,在 3种较佳的转化条件下共获得 10种代谢物 ,在其中一种条件下 ,同时可得 7种代谢物 ;在另一条件下 ,一主要代谢物的产率高达 4 1.6% ,转化液中残留的母体药物仅为1.1%。
Biotransformation studies of SFZ 47 (3H 1,2 dihydro 2 (4 methylphenyl amino)methyl 1 pyrrolizinone),a new antiinflammatory and analgesic agent,by Cunninghamella were conducted The diversity and yields of the metabolites of SFZ 47 were determined with a high performance liquid chromatographic method It was showed that the strain produced stable metabolites with good repeatability After changing conditions the strain was found very sensitive to the initial pH values for the biotransformation As results of orthogonal experiments,more than 10 metabolites were observed in three biotransformation processes In one experiment,seven metabolites were obtained;in another,a major metabolite was produced with the yield as high as 41 6%,while the residual parent drug was only 1 1%
出处
《药物生物技术》
CAS
CSCD
1997年第3期158-163,共6页
Pharmaceutical Biotechnology
关键词
微生物转化模型
小克银汉霉菌
SFZ-47
药物代谢
Microbial metabolism,Cunninghamella:SFZ 47 (3H 1,2 dihydro 2 (4 methylphenylamino)methyl 1 pyrrolizinone), Metabolites
