Inclusion Complex of Podophyllotoxin with y-Cyclodextrin Preparation, Characterization, Anticancer Activity, Water-Solubility and Toxicity  

作　　者：Yafei Guo Yushun Zhang Jiuling Li Fen Zhao Yang Liu Min Su Yubo Jiang Yuqi Liu Jihong Zhang Bo Yang Rui Yang 

机构地区：[1]Faculty of Science, Kunming University of Science and Technology, Kunming, Yunnan 650500, China [2]Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming, Yunnan 650500, China [3]Key Laboratory of Medicinal Chemistry for Natural Resource, School of Chemical Science and Technology, Yunnan University, Kunming, Yunnan 650500, China

出　　处：《Chinese Journal of Chemistry》2016年第4期425-431,共7页中国化学（英文版）

摘　　要：An inclusion complex of podophyllotoxin （PPT） with 7-cyclodextrin （7-CD） was prepared. The behavior, char- acterization, and water solubility of the inclusion complex were carefully investigated via fluorescence spectroscopy, thermogravimetry, differential scanning calorimetry, X-ray diffraction analysis, and 1H and 2D nuclear magnetic resonance spectroscopy. Furthermore, antitumor activity to human cancer lines and toxicity in mice were studied. Results showed that the inclusion complex formed in a 1 ： 1 ratio with a considerable apparent stability constant Ks （4245.5 Lomol-l）. Water solubility was considerably improved. In addition, the anticancer activity of the inclusion complex was better than that of cis-platinum （DDP, positive control）. Most importantly, the toxicity of podophyl- lotoxin inclusion complex reduced and became more safety to mice which will be great valuable to research its ap- plications as a kind of antitumor drug to human in the further.An inclusion complex of podophyllotoxin （PPT） with 7-cyclodextrin （7-CD） was prepared. The behavior, char- acterization, and water solubility of the inclusion complex were carefully investigated via fluorescence spectroscopy, thermogravimetry, differential scanning calorimetry, X-ray diffraction analysis, and 1H and 2D nuclear magnetic resonance spectroscopy. Furthermore, antitumor activity to human cancer lines and toxicity in mice were studied. Results showed that the inclusion complex formed in a 1 ： 1 ratio with a considerable apparent stability constant Ks （4245.5 Lomol-l）. Water solubility was considerably improved. In addition, the anticancer activity of the inclusion complex was better than that of cis-platinum （DDP, positive control）. Most importantly, the toxicity of podophyl- lotoxin inclusion complex reduced and became more safety to mice which will be great valuable to research its ap- plications as a kind of antitumor drug to human in the further.

关 键 词：CYCLODEXTRIN CYTOTOXICITY podophyllotoxin inclusion complex antitumor activity 

分 类 号：O627.42[理学—有机化学] TQ461[理学—化学]