| 摘要: |
| 两面针是我国民间常用的传统中药之一,从根部提取分离到的氯化两面针碱是两面针植物多种生物活性的主要有效成分。当前,直接从植物中提取分离有效成分的方法不仅回收率低、成本高,而且氯化两面针碱存在水溶性差和生物利用度低的问题,因此大多学者致力于改造其结构以提高活性和利用度,同时探索高效经济的全合成方法以满足研究和生产的需求。该文以国内外相关文献为基础,对氯化两面针碱的提取、分离纯化、结构化合物的全合成路线以及药理活性机制的研究进展做一综述,总结目前研究中存在的不足,并对今后的研究重点做出展望,旨在为今后深入研究两面针碱及衍生物活性改造、解析作用机制、开发基于此结构的创新药物分子等提供理论依据。 |
| 关键词: 氯化两面针碱, 提取, 全合成, 药理活性 |
| DOI：10.11931/guihaia.gxzw201711019 |
| 分类号:Q946 |
| 文章编号:1000-3142(2018)09-1248-13 |
| Fund project:国家自然科学基金(21602038); 广西植物研究所基本业务费项目(桂植业16002); 广西壮族自治区八桂学者专项项目; 广西植物功能物质研究与利用重点实验室主任基金(ZRJJ2016-2)[Supported by the National Natural Science Foundation of China(21602038); Fundamental Research Fund of Guangxi Institute of Botany(16002); Bagui Scholar Program of the Guangxi Institute of Botany; Director Capital Program of Guangxi Key Laboratory of Functional Phytochemicals Research and Utilization(ZRJJ2016-2)]。 |
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| Research progress on extraction, separation, total synthesis and pharmacological activity of nitidine chloride |
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QIN Shuqin1,2, LI Haiyun1, SONG Jingru2*, LI Dianpeng2
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1. College of Chemistry and Bioengineering, Guilin University of Technology, Guilin 541006, Guangxi, China;2. Guangxi Key
Laboratory of Functional Phytochemicals Research and Utilization, Guangxi Institute of Botany, Guangxi Zhuang
Autonomous Region and Chinese Academy of Sciences, Guilin 541006, Guangxi, China
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| Abstract: |
| Zanthoxylum nitidum, locally called ‘liangmianzhen', is one of the traditional Chinese medicines. Nitidine chloride isolated from the root of Z. nitidium is the main active consitutent of its biological activities. Nowadays, chemists commit themselves to modifing the structure of nitidine, exploring efficient and versatile total synthetic routes to the analogues and evaluating structure-activity relationship. In this review, we summarized the enormous efforts for separation to enhance extraction efficiency, numerous total synthetic methods according to the reaction types and various pharmacolo-gical activities of nitidine chloride on the basis of related literatures from home and abroad. Besides, the review also discussed the deficiencies of current researches and prospected the further research priority. We hope that this review can provide a theoretical basis for the following study of structural modification, of the concise synthetic route using readily available and inexpensive reagents, of the bioactive mechanism, and of exploiting new chemotherapy drugs. |
| Key words: nitidine chloride, extraction, total synthesis, pharmacological activity |
