| 5—氟尿苷的微生物转化 |
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| 引用本文： | 阮期平 周长林 等. 5—氟尿苷的微生物转化[J]. 微生物学报, 2002, 42(1): 117-120 |
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| 作者姓名： | 阮期平 周长林 等 |
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| 作者单位： | 中国药科大学生物制药学院 南京210009(阮期平，周长林，窦洁)，中国药科大学生物制药学院 南京210009(吴梧桐) |
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| 基金项目： | 国家医药管理局资助项目 |
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| 摘 要： | 5 氟尿苷 (简称ＦＵＲ)是抗肿瘤核苷药物脱氧氟尿苷 (Ｆｌｏｘｕｒｉｄｉｎｅ ,简称ＤＦＵＲ)的合成中间体。脱氧氟尿苷是一种抗代谢类抗肿瘤药 ,在体内可以部分转化为氟尿嘧啶 (简称ＦＵ) ,二者具有相似的作用途径和抗肿瘤谱。与ＦＵ相比 ,由于ＤＦＵＲ的抗肿瘤活性高且毒副反应小 ,主要用于治疗晚期结直肠癌和各种类型肝癌。在国内 ,采用化学法合成的ＤＦＵＲ业已进入临床研究阶段[1]采用化学合成法生产ＤＦＵＲ时 ,由于反应过程中需将碱基或核糖残基的部分基团进行保护 ,而且产物为多种核苷异构体和其它副产品的混合物 ,需要进一步分离 ,…
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| 关 键 词： | 5－氟尿苷 微生物转化 分离纯化 |
| 文章编号： | 0001-6209(2002)01-0117-04 |
| 修稿时间： | 2001-04-11 |
Studies on Biotransformation of 5-FUR |
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| Ruan Qiping Zhou Changlin Dou Jie Wu Wutong. Studies on Biotransformation of 5-FUR[J]. Acta microbiologica Sinica, 2002, 42(1): 117-120 |
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| Authors: | Ruan Qiping Zhou Changlin Dou Jie Wu Wutong |
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| Affiliation: | School of Biopharmaceutics, China Pharmaceutical University, Nanjing 210009, China. |
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| Abstract: | Conditions for biotransformation and purification of FUR were investigated. The result showed that when the cell concentration of E. aerogenes was 10% (w/v), the temperature and pH were 7.8 and 60 degrees C respectively, 59.7% UR was converted to FUR. It also demonstrated that the ideal procedure for the purification of FUR is silica gel column chromatography by two elution systems (S1:CHCl3:CH3OH:H2O = 61:13:1, and S2; CH3COOCH2CH3:CH3OH:CH3COOH:H2O = 12:3:3:2) with the purity and yield of 98.0% and 86.0% respectively. |
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| Keywords: | FUR Biotransformation Isolation and purification |
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