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印楝素的化学、生物活性、提取与分析:最新进展。

Chemistry, bioactivities, extraction and analysis of azadirachtin: State-of-the-art.

机构信息

Centro de Investigação em Saúde e Ambiente, Escola Superior de Saúde, Instituto Politécnico do Porto, Porto, Portugal; LAQV, REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Porto, Portugal.

Centro de Investigação em Saúde e Ambiente, Escola Superior de Saúde, Instituto Politécnico do Porto, Porto, Portugal; LAQV, REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Porto, Portugal.

出版信息

Fitoterapia. 2019 Apr;134:141-150. doi: 10.1016/j.fitote.2019.02.006. Epub 2019 Feb 6.

DOI:10.1016/j.fitote.2019.02.006
PMID:30738093
Abstract

Azadirachta indica A. Juss. (Neem) is an Indian tree recognized for its activity as pesticide, as well as several pharmacological properties. Among the various compounds already isolated and studied from Neem tree, azadirachtin (AZA) was identified as the main bioactive compound. Azadirachtin can be found at different parts of the Neem plant but assumes its maximum concentration at the seed level. This compound features a quite complex chemical structure, which justifies the 20-plus-year difficulty to identify the synthetic pathway that subsequently permitted to carry out its artificial synthesis. Azadirachtin is widely used as a basis for production of biopesticides; nevertheless, other properties have been recognized for this substance, among which the anticancer and antimalarial activity stand out. The methods available for azadirachtin extraction are diverse, including solid-liquid extraction and extraction with solvents at high or low temperatures. Alcohol based solvents are associated with higher extraction yields and are therefore preferred for the isolation of azadirachtin from plant parts. Clean-up of the extracts is generally required for further purification. The highest azadirachtin levels have been obtained from Neem seeds but concentration values present a large variation between batches. Therefore, in addition to extraction procedures, it is essential to establish routine methods for azadirachtin identification and quantification. Chromatography-based techniques are preferably selected for detection and quantification of azadirachtin in plant matrices. Overall, this process will guarantee a future reproducible, safe and effective use of the extracts in formulations for commercial applications.

摘要

印楝(Azadirachta indica A. Juss.)是一种印度树种,因其具有杀虫剂活性以及多种药理学特性而受到认可。在已经从印楝树中分离和研究的各种化合物中,印楝素(AZA)被鉴定为主要的生物活性化合物。印楝素可以在印楝植物的不同部位找到,但在种子水平上达到最大浓度。该化合物具有相当复杂的化学结构,这也解释了 20 多年来难以确定其合成途径的原因,而随后的人工合成正是基于这一途径。印楝素被广泛用作生产生物农药的基础;然而,人们已经发现了这种物质的其他特性,其中包括抗癌和抗疟活性。提取印楝素的方法多种多样,包括固液萃取和在高温或低温下用溶剂萃取。基于酒精的溶剂与更高的提取产率相关联,因此更适合从植物部分中分离印楝素。通常需要对提取物进行净化以进一步纯化。从印楝种子中获得了最高水平的印楝素,但批次之间的浓度值存在很大差异。因此,除了提取程序外,还必须建立常规方法来鉴定和定量印楝素。基于色谱的技术是在植物基质中检测和定量印楝素的首选方法。总的来说,这个过程将保证未来在商业应用配方中对提取物进行可重复、安全和有效的使用。

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