根皮素包合物的制备及其体外抗肿瘤活性研究

Preparation of Phloretin Inclusion Complex and Its Anti-tumor Activity

目的制备根皮素/α-环糊精(α-CD)包合物,对其进行结构鉴定和体外抗肿瘤活性研究。方法采用饱和水溶液法制备根皮素/α-CD包合物,用透射电镜(TEM)、傅立叶红外光谱仪(FT-IR)和X射线衍射仪(XRD)对包合物进行结构鉴定,用噻唑蓝(MTT)法检测包合物的抗肿瘤能力。结果根皮素与α-CD可以形成稳定的包合物,水溶液中可自组装形成直径为396 nm的纳米粒子,游离根皮素和包合物抑制结肠癌HCT-8细胞的IC50分别是44.6和22.6μg/mL。结论根皮素与α-CD可以形成包合物纳米粒子,提高了根皮素的释药速率和体外抗肿瘤能力。

Objective To prepared Phloretin/α-cyclodextrin inclusion complex and investigate its structure and its antitumor activity.Methods The inclusion complex of phloretin/α-cyclodextrin was prepared by saturated aqueous solution.The structure of the inclusion complex was identified by transmission electron microscope(TEM),Fourier transform infrared spectroscopy(FT-IR)and X-ray diffractometer(XRD).The anti-tumor ability of inclusion was detected by thiazolyl(MTT)method.Results Phloretin andα-cyclodextrin could form a stable inclusion complex.Nanoparticles with diameter of 396 nm could be self-assembled in aqueous solution.The IC50 of free phloretin and inclusion complex on colon cancer HCT-8 cells were 44.6 ug/mL and 22.6μg/m L,respectively.Conclusion Phloretin andα-cyclodextrin can form a stable inclusion complex,which significantly improves the anti-tumor ability of phloretin.