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《Chinese Traditional and Herbal Drugs》 2015-01
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Preparation and characterization of cucurbitacin B phospholipids complex and its in vitro antitumor activity

WAN Lu;XIAO Yun-zhi;CHENG Ling;XU Ping-hua;LI Xiao-rong;MIN Hong-yan;HAN Jin;YUAN Hai-long;College of Pharmacy, Jiangxi University of Traditional Chinese Medicine;302 Military Hospital of China;  
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 1∶1, 1.5 mg/m L, 60 ℃, and 3 h, respectively. The complex rate and particle size for the optimized Cu B-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 Hep G-2 cell proliferation inhibition concentration(IC50) values of Cu B and Cu B-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 Cu B.
【Fund】: 北京市科委重点项目(Z131100002513005);; 国家教育部留学归国人员科研启动基金(20101561)
【CateGory Index】: R283.6;R285
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