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印楝素与天然和甲基化环糊精的包合物:增溶作用和结合能力。

Inclusion complexes of azadirachtin with native and methylated cyclodextrins: solubilization and binding ability.

作者信息

Liu Yu, Chen Guo-Song, Chen Yong, Lin Jun

机构信息

Department of Chemistry, State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, PR China.

出版信息

Bioorg Med Chem. 2005 Jun 2;13(12):4037-42. doi: 10.1016/j.bmc.2005.03.051. Epub 2005 Apr 25.

Abstract

The inclusion complexation behavior of azadirachtin with several cyclodextrins and their methylated derivatives has been investigated in both solution and the solid state by means of XRD, TG-DTA, DSC, NMR, and UV-vis spectroscopy. The results show that the water solubility of azadirachtin was obviously increased after resulting inclusion complex with cyclodextrins. Typically, beta-cyclodextrin (beta-CD), dimethyl-beta-cyclodextrin (DMbetaCD), permethyl-beta-cyclodextrin (TMbetaCD), and hydroxypropyl-beta-cyclodextrin (HPbetaCD) are found to be able to solubilize azadirachtin to high levels up to 2.7, 1.3, 3.5, and 1.6 mg/mL (calculated as azadirachtin), respectively. This satisfactory water solubility and high thermal stability of the cyclodextrin-azadirachtin complexes, will be potentially useful for their application as herbal medicine or healthcare products.

摘要

通过X射线衍射(XRD)、热重-差热分析(TG-DTA)、差示扫描量热法(DSC)、核磁共振(NMR)和紫外-可见光谱法,研究了印楝素与几种环糊精及其甲基化衍生物在溶液和固态中的包合络合行为。结果表明,印楝素与环糊精形成包合络合物后,其水溶性明显提高。典型的是,发现β-环糊精(β-CD)、二甲基-β-环糊精(DMβCD)、全甲基-β-环糊精(TMβCD)和羟丙基-β-环糊精(HPβCD)分别能够将印楝素溶解到高达2.7、1.3、3.5和1.6mg/mL(以印楝素计)的高水平。环糊精-印楝素络合物这种令人满意的水溶性和高热稳定性,将可能有助于它们作为草药或保健品的应用。

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