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短刺小克银汉霉对甘草次酸的生物转化
引用本文:秦宇娟,冯冰,宋新波,周文斌,余河水,赵莉莉,余利岩,马百平.短刺小克银汉霉对甘草次酸的生物转化[J].中国天然药物,2010(5):373-381.
作者姓名:秦宇娟  冯冰  宋新波  周文斌  余河水  赵莉莉  余利岩  马百平
作者单位:[1]北京放射医学研究所,北京100850 [2]天津中医药大学,天津300193 [3]中国医学科学院医药生物技术研究所,北京100050
基金项目:北京市自然科学基金重大项目(No.7090001)Acknowledgements The authors are grateful to Prof. CHEN He-Bing for the NMR spectra.
摘    要:目的:使用生物催化技术探讨甘草次酸(GA)的羟基化反应, 并对转化产物进行抑菌活性的评价。方法:在 30 °C条件下, 用短刺小克银汉霉 AS 3.970 转化 GA, 反应时间为 5 d。结果:对 GA 的转化产物进过分离纯化, 得到 2 个主产物和 4个量较少的产物。其中, 2 个主产物经过 1↑H 和 13↑C NMR 鉴定为 3-酮基-7β-羟基-甘草次酸(GA-1)和 7β-羟基-甘草次酸(GA-2), 其他产物(GA-3-GA-6)使用 HR-ESI-MS 进行结构分析。筛选了底物及其 2 个主产物对 4 株细菌和 1 株酵母菌的抑菌活性。结论:短刺小克银汉霉 AS 3.970 对 GA 具有羟基化作用。GA 和其 2 个主产物对耐药菌粪肠球菌具有良好的抑菌活性。

关 键 词:甘草次酸  短刺小克银汉霉  羟基化反应  生物转化  抑菌活性

Biotransformation of Glycyrrhetinic Acid by Cunninghamella blakesleeana
QIN Yu-Juan,FENG Bing,SONG Xin-Bo,ZHOU Wen-Bin,YU He-Shui,ZHAO Li-Li,YU Li-Yan,MA Bai-Ping.Biotransformation of Glycyrrhetinic Acid by Cunninghamella blakesleeana[J].Chinese JOurnal of Natural Medicines,2010(5):373-381.
Authors:QIN Yu-Juan  FENG Bing  SONG Xin-Bo  ZHOU Wen-Bin  YU He-Shui  ZHAO Li-Li  YU Li-Yan  MA Bai-Ping
Institution:1.Beijing Institute of Radiation Medicine, Beijing 100850; 2.Tianjin University of Traditional Chinese Medicine, Tianjin 300193; 3.Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China)
Abstract:AIM: To study the hydroxylation in glycyrrhetinic acid (GA) by biocatalysis, and evaluate the antibacterial activities of the derivatives. METHODS: The hydroxylation was performed via incubating GA with a fungus, Cunninghamella blakesleeana (C. blakesleeana) AS 3.970 at 30 ℃ for 5 days. RESULTS: GA was converted into two major derivatives and four minor derivatives. The two major derivatives were isolated and elucidated as 3-oxo-7β-hydroxy-glycyrrhetinic acid (GA-1) and 7β-hydroxy-glycyrrhetinic acid (GA-2) based on their spectral data, and other derivatives (GA-3-GA-6) were identified by HR-ESI-MS. The antibacterial activities of substrate and two major derivatives were evaluated on four bacteria strains and one yeast strain. CONCLUSION: Cunninghamella blakesleeana AS 3.970 has the capability of hydroxylation for GA. The two major derivatives and GA were found to have considerable activities against drug-resistant Enterococcusfaecalis.
Keywords:Glycyrrhetinic acid  Cunningharnella blakesleeana  Hydroxylation  Biotransformation  Antibacterial activity
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