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Inclusion Complex of Podophyllotoxin with γ ‐Cyclodextrin: Preparation, Characterization, Anticancer Activity, Water‐Solubility and Toxicity
Author(s) -
Guo Yafei,
Zhang Yushun,
Li Jiuling,
Zhao Fen,
Liu Yang,
Su Min,
Jiang Yubo,
Liu Yuqi,
Zhang Jihong,
Yang Bo,
Yang Rui
Publication year - 2016
Publication title -
chinese journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.28
H-Index - 41
eISSN - 1614-7065
pISSN - 1001-604X
DOI - 10.1002/cjoc.201500692
Subject(s) - chemistry , solubility , podophyllotoxin , cyclodextrin , nuclear chemistry , stability constants of complexes , thermogravimetry , differential scanning calorimetry , combinatorial chemistry , aqueous solution , stereochemistry , organic chemistry , inorganic chemistry , physics , thermodynamics
An inclusion complex of podophyllotoxin (PPT) with γ ‐cyclodextrin ( γ ‐CD) was prepared. The behavior, characterization, and water solubility of the inclusion complex were carefully investigated via fluorescence spectroscopy, thermogravimetry, differential scanning calorimetry, X‐ray diffraction analysis, and 1 H 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 K s (4245.5 L·mol −1 ). 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 podophyllotoxin inclusion complex reduced and became more safety to mice which will be great valuable to research its applications as a kind of antitumor drug to human in the further.