Preparation and characterization of cucurbitacin B phospholipids complex and its in vitro antitumor activity / 中草药

ABSTRACT

Objective: To prepare cucurbitacin B phospholipids complex (CuB-PLC) and evaluate its physicochemical properties and in vitro antitumor activity. Methods: CuB-PLC was prepared using solvent evaporation method and optimized by Box-Behnken design. The oil-water partition coefficient, particle size, and morphology of CuB-PLC were investigated; X-ray diffraction (XRD) spectroscopy and infrared (IR) spectroscopy were used to analyze the formation machenism of CuB-PLC. MTT method was used to determine the in vitro antitumor activity of CuB-PLC. Results: The optimal formulation protocol for CuB-PLC was as follows Tetrahydrofuran was taken as the reaction medium, phospholipids-cucurbitacin B molar ratio, reaction concentration of cucurbitacin B, reaction temperature and time were 11, 1.5 mg/mL, 60℃, and 3 h, respectively. The complex rate and particle size for the optimized CuB-PLC was 97.15% and (521.30 ± 10.50) nm, and the polydispersity index (PDI) was 0.133 2 ± 0.024 0. MTT experiments showed that the half of the HepG-2 cell proliferation inhibition concentration (IC50) values of CuB and CuB-PLC were 42.55 and 27.61 μmol/L. Conclusion: CuB-PLC is successfully developed under the optimized protocol, possessing high complex rate, and enhanced solubility in water, and the inhibition on HepG-2 cell proliferation is significantly enhanced, which provides the reference for the further research of CuB.