Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, PR China.
Carbohydr Polym. 2013 Feb 15;92(2):1308-14. doi: 10.1016/j.carbpol.2012.10.012. Epub 2012 Oct 12.
A series of scutellarin-cyclodextrin conjugates (SCU-CD conjugates), in which scutellarin was covalently bound to one of the primary hydroxyl groups of β-CD, were prepared, and their structures were determined using NMR and MS. These conjugates were further characterized by XRD and TG. The results showed that the aqueous solubility of the conjugates was much higher than that of scutellarin, and the conjugates could hardly be hydrolyzed to scutellarin in aqueous solutions. The cytotoxicity of SCU-CD conjugates on human colon cancer cell lines HT-29, SW480, Lovo and HTC116 indicated that the antitumor activities of the conjugates were better than that of scutellarin. This high antitumor activity, along with the satisfactory aqueous solubility and high stability of the conjugates, will be potentially useful for their application on human colon cancer chemotherapies.
一系列的灯盏花素-环糊精缀合物（SCU-CD 缀合物）被制备出来，其中灯盏花素通过共价键连接到β-CD 的一个伯羟基上，并用 NMR 和 MS 确定了它们的结构。这些缀合物进一步通过 XRD 和 TG 进行了表征。结果表明，缀合物的水溶解度远高于灯盏花素，并且在水溶液中缀合物几乎不能水解为灯盏花素。SCU-CD 缀合物对人结肠癌细胞系 HT-29、SW480、Lovo 和 HTC116 的细胞毒性表明，缀合物的抗肿瘤活性优于灯盏花素。这种高抗肿瘤活性，以及缀合物令人满意的水溶性和高稳定性，将有可能对人结肠癌的化疗应用有用。
