a Faculty of Life Science and Technology , Kunming University of Science and Technology , Kunming 650500 , P.R. China.
J Biomater Sci Polym Ed. 2014;25(6):594-607. doi: 10.1080/09205063.2014.884875. Epub 2014 Feb 20.
The inclusion complexation behavior of scutellarein (SCUE) with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) has been investigated in both solution and in the solid state. SCUE/HP-β-CD solid system was prepared by suspension method. The formation of SCUE/HP-β-CD complex in aqueous solution was demonstrated by fluorescence spectroscopy, and the Job plot showed a maximum at a molar fraction of 0.5, indicating 1:1 inclusion complexation between SCUE and HP-β-CD. However, SCUE/HP-β-CD inclusion complex was characterized by means of XRD, DSC, (1)H, and two-dimensional NMR. Through the complexation between HP-β-CD and SCUE, the water solubility and antitumor activity of SCUE were obviously increased. This satisfactory water solubility and high antitumor activity of the SCUE/HP-β-CD complex will be potentially useful for its application on human colon cancer chemotherapies.
以水为溶剂，通过荧光光谱法研究了灯盏乙素（SCUE）与 2-羟丙基-β-环糊精（HP-β-CD）在溶液中和固态中的包合作用，采用悬浮法制备了 SCUE/HP-β-CD 固体体系。荧光光谱表明，在水溶液中形成了 SCUE/HP-β-CD 包合物，且根据 Job 图，当摩尔分数为 0.5 时，出现最大值，表明 SCUE 与 HP-β-CD 之间为 1:1 的包合作用。然而，通过 XRD、DSC、（1）H 和二维 NMR 对 SCUE/HP-β-CD 包合物进行了表征。通过 HP-β-CD 与 SCUE 的包合作用，SCUE 的水溶性和抗肿瘤活性明显提高。SCUE/HP-β-CD 复合物具有令人满意的水溶性和高抗肿瘤活性，有望应用于人类结肠癌的化疗。
