title: Preparation, characterisation and bioactivity evaluation of the inclusion complex formed between picoplatin and γ-cyclodextrin.
abstract: The inclusion complex of picoplatin with γ-cyclodextrin (γ-CD) was prepared and characterised by different analytical methods, including NMR, FTIR, TGA, phase solubility as well as SEM. All of these approaches indicated that picoplatin was able to form an inclusion complex with γ-CD, and that the picoplatin/γ-CD inclusion compounds exhibited different spectroscopic features and properties from free picoplatin. The stoichiometry of the complex was 1:1; the pyridine group of picoplatin was deeply inserted into the cavity of γ-CD and the amine platinum group of picoplatin was near the narrower rim of γ-CD. The calculated apparent stability constant of the complex was 10,318M(-1). Moreover, the water solubility of picoplatin was significantly improved, according to phase-solubility studies. The complex maintained its anticancer activity, as shown by an in vitro cell-survival assay on A549 and MCF-7 cancer cell lines. All of these results showed that inclusion complexation may be a promising strategy to design a novel formulation of picoplatin as an anticancer therapy.
authors.affiliation: Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091, PR China.
authors.forename: Jian-Qiang
authors.initials: JQ
authors.lastname: Zhang
authors.affiliation: The First Department of Medical Oncology, The Third Affiliated Hospital of Kunming Medical University, Kunming 650031, PR China.
authors.forename: Ke
authors.initials: K
authors.lastname: Li
authors.affiliation: Kunming Guiyan Pharmaceutical Co., Ltd, Kunming 650093, PR China.
authors.forename: Yan-Wei
authors.initials: YW
authors.lastname: Cong
authors.affiliation: Kunming Guiyan Pharmaceutical Co., Ltd, Kunming 650093, PR China.
authors.forename: Shao-Ping
authors.initials: SP
authors.lastname: Pu
authors.affiliation: Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091, PR China.
authors.forename: Hong-You
authors.initials: HY
authors.lastname: Zhu
authors.affiliation: Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091, PR China.
authors.forename: Xiao-Guang
authors.initials: XG
authors.lastname: Xie
authors.affiliation: Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091, PR China. Electronic address: jinyi@ynu.edu.cn.
authors.forename: Yi
authors.initials: Y
authors.lastname: Jin
authors.affiliation: Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091, PR China. Electronic address: linjun@ynu.edu.cn.
authors.forename: Jun
authors.initials: J
authors.lastname: Lin
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D002152:Calorimetry, Differential Scanning; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D009944:Organoplatinum Compounds / Q000737:chemistry* / Q000494:pharmacology; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013816:Thermodynamics; D014961:X-Ray Diffraction; D047408:gamma-Cyclodextrins / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D009944:Organoplatinum Compounds; C110525:amminedichloro(2-methylpyridine)platinum(II); D047408:gamma-Cyclodextrins
keywords: Anti-tumour activity; Characterisation; Cyclodextrin; Inclusion complex; Picoplatin