| 微生物转化法从雷公藤甲素合成雷腾舒 |
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| 引用本文： | 赵舜波,黄海华,陈笑艳,李秀立,钟大放.微生物转化法从雷公藤甲素合成雷腾舒[J].中国新药杂志,2012(3):303-309. |
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| 作者姓名： | 赵舜波 黄海华 陈笑艳 李秀立 钟大放 |
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| 作者单位： | 浙江工业大学;中国科学院上海药物研究所 |
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| 基金项目： | 国家自然科学基金(30901831) |
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| 摘 要： | 目的:以雷公藤甲素为原料,采用微生物转化法合成新型抗类风湿药物雷腾舒。方法:筛选10株小克银汉霉菌,采用HPLC法检测转化液中目标产物雷腾舒的浓度并计算产率,优化转化系统。结果:模型菌株雅致小克银汉霉ATCC36112在pH 4.5、底物浓度400μg.mL-1和转化10 d等条件下,雷腾舒产率>70%。结论:小克银汉霉ATCC36112转化雷公藤甲素,为活性代谢产物雷腾舒的合成开辟了一条新途径。
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| 关 键 词： | 雷腾舒 雷公藤甲素 微生物转化 雅致小克银汉霉菌 液相色谱法 |
Biotransformation of triptolide to (5R)-5-hydroxytriptolide |
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| ZHAO Shun-bo,HUANG Hai-hua,CHEN Xiao-yan,LI Xiu-li,ZHONG Da-fang.Biotransformation of triptolide to (5R)-5-hydroxytriptolide[J].Chinese Journal of New Drugs,2012(3):303-309. |
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| Authors: | ZHAO Shun-bo HUANG Hai-hua CHEN Xiao-yan LI Xiu-li ZHONG Da-fang |
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| Institution: | 1,2 (1 Zhejiang University of Technology,Hangzhou 310014,China;2 Shanghai Institute of Materia Medica, Chinese Academy of Sciences,Shanghai 201203,China) |
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| Abstract: | Objective: To synthesize(5R)-5-hydroxytriptolide by microbial transformation of triptolide.Methods: Among 10 strains of Cunninghamella screened,Cunninghamella elegans ATCC36112 was selected as a suitable bioconverter.To calculate the transformation yield,the concentration of(5R)-5-hydroxytriptolide in the fermentation fluids was determined by HPLC.Factors influencing biotransformation system were optimized to increase the yield of(5R)-5-hydroxytriptolide.Results: The optimized conditions were pH 4.5,400 μg·mL-1 of substrate concentration and 10 d of transformation.A yield of > 70% was achieved.Conclusion: We have proved that biotransformation of triptolide to(5R)-5-hydroxytriptolide by Cunninghamella elegans ATCC36112 is a new approach for the synthesis of(5R)-5-hydroxytriptolide. |
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| Keywords: | (5R)-5-hydroxytriptolide triptolide microbial transformation Cunninghamella elegans HPLC |
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