Host-guest inclusion system of 1, 2-O, O-Diacetyllycorine (DALY) and α-cyclodextrin: Preparation, characterization, inclusion modes and anticancer activity

1, 2-O, O-Diacetyllycorine (DALY) is one of the lycorine derivatives which has various biological properties. However, the bioavailability and clinical application of DALY was restrained because of its low water solubility and moderate antitumor activities . In order to improve its physicochemical properties, we prepared the inclusion complex of DALY with α-cyclodextrin (α-CD). The inclusion complex was characterized by UV, XRD, DSC , TG, 1 H, 2D NMR spectroscopy and its anticancer activity was evaluated in vitro against the human cell lines HCT116, A549, HepG2 and K562. The results demonstrated that DALY was encapsulated into the cavity of α-CD to form the complexes with 1:1 stoichiometry . The water solubility of DALY significantly increased for about 49 times after the inclusion complexation with α-CD. Furthermore, the cytotoxicity of DALY/α-CD against the examined cell lines was significantly increased for about 80 times compared to that of the free DALY. The improved physicochemical and biological properties of the inclusion complexes will be beneficial for its potential applications in the design and formulation of natural medicines.