Investigation of inclusion complex of epothilone A with cyclodextrins.
Investigation of inclusion complex of epothilone A with cyclodextrins.
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DOI：
10.1016/j.carbpol.2013.11.049
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发表时间：
2014-02
影响因子：
11.2
通讯作者：
Chuan-Fan Xiao;Ke Li;Rong Huang;Guo-Jin He;Jianqiang Zhang;Li Zhu;Qing-Yi Yang;Kunming Jiang;Yi Jin;Jun Lin
中科院分区：
文献类型：
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作者：
Chuan-Fan Xiao;Ke Li;Rong Huang;Guo-Jin He;Jianqiang Zhang;Li Zhu;Qing-Yi Yang;Kunming Jiang;Yi Jin;Jun Lin
以天然环糊精(β-或γ-CD)及其衍生物羟丙基-β-环糊精(HP-β-CD)为包结剂，制备了环己酮A包合物。通过紫外-可见光谱、核磁共振、X射线衍射仪、差示扫描量热仪和扫描电子显微镜对其在溶液和固体中的行为、表征和结合能力进行了研究。结果表明，环糊精包合物的水溶性和溶液稳定性明显提高。同时，包合物对A549和MCF-7细胞仍具有类似的抗癌活性，具有良好的水溶性、较高的溶液稳定性和较高的抗癌活性，有望成为潜在的抗癌药物。
The inclusion complexation of Epothilone A with native cyclodextrin (β- or γ-CD) and its derivative hydroxypropyl-β-cyclodextrin (HPβCD) were prepared. Their behavior, characterization, and binding ability were investigated in both solution and the solid state by means of UV–vis, NMR, XRD, DSC and SEM. The results show that the water solubility and solution stability obviously increased in the inclusion complex with cyclodextrins. Meanwhile, the inclusion complexes still retained anticancer activity against A549 and MCF-7 cells, similar to free Epothilone A. This satisfactory water solubility, high solution stability, and high anticancer activity of the Epothilone A/CD complexes will be potentially useful as an anticancer therapy.