| 引用本文: | 冯昭龙,刘纯慧.肝素前体heparosan的制备及药学应用研究进展[J].中国现代应用药学,2019,36(1):114-119. |
| FENG Zhaolong,LIU Chunhui.Research Progress of the Preparation and Pharmaceutical Applications of Heparosan[J].Chin J Mod Appl Pharm(中国现代应用药学),2019,36(1):114-119. |
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| 摘要: |
| 目的 综述肝素前体heparosan的制备技术及其在药学领域应用的最新研究进展，为其进一步研究和开发提供参考。方法 查阅国内外关于heparosan的制备方法及药学应用的文献，对其分析、概括和总结。结果 现有heparosan的制备方法主要包括微生物发酵提取法、代谢工程改造菌生产法、体外重组酶合成法；heparosan不仅可作为起始原料用于非动物源肝素的生物合成和非抗凝肝素衍生物的制备，还可作为药物载体。结论 发酵工程、代谢工程及酶工程等技术的成功应用推动heparosan的制备规模显著提高，但尚难以定制合成分子量可控的heparosan及衍生物；目前heparosan在药学领域的应用发展迅速，新的制备与结构改造策略将进一步拓宽其在药物发现与研究中的应用。 |
| 关键词: heparosan 肝素 多糖 制备方法 药学应用 |
| DOI：10.13748/j.cnki.issn1007-7693.2019.01.024 |
| 分类号:R943 |
| 基金项目:国家自然科学基金（21372146）；山东省科技重大专项（2015ZDJS04002） |
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| Research Progress of the Preparation and Pharmaceutical Applications of Heparosan |
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FENG Zhaolong, LIU Chunhui
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School of Pharmaceutical Sciences & National Glycoengineering Research Center, Shandong University, Jinan 250012, China
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| Abstract: |
| OBJECTIVE To systematically review the latest research achievement in the preparation and the pharmaceutical applications of heparosan to provide a reference for its further research and development. METHODS The literatures at home and abroad were collected, summarized and analyzed on preparation methods of heparosan and its pharmaceutical application. RESULTS The present methods for the preparation of heparosan mainly included extraction from bacterial fermentation liquid, production by metabolic engineering bacteria and in vitro synthesis using recombinant enzymes. Heparosan could be used for the biosynthesis of non-animal derived heparin and preparation of non-anticoagulant heparin analogs as starting materials, as well as for drug delivery. CONCLUSION Heparosan has been produced at a large scale due to the successful application of fermentation engineering, metabolic engineering, and enzyme engineering, nevertheless, which still can't allow for tailored synthesis of heparosan with controllable molecular weight and its derivatives. To date, heparosan has been rapidly applied in the pharmaceutical field, and new strategies for the production and structure modifications will further expand its application in drug discovery and research. |
| Key words: heparosan heparin polysaccharide preparation methods pharmaceutical application |
