Analysis of anti-tumor active components and preparation of self-assembled polymeric micelles in taxus chinensis seeds.

OBJECTIVE

Seeds of Taxus chinensis contain effective anti-tumor substances. In this study, the main anti-tumor active compound was screened from Taxus chinensis seeds, which was combined with TPGS and mPEG-PCL to make micelles, improve its solubility and anti-tumor activity, and reduce the toxic side effects.

METHODS

Organic solvent extraction, silica gel column chromatography, thin layer chromatography and other separation and purification techniques were used, combined with MTT method, to screen out the anti-tumor active fraction F5 (BE) from the ethanol extract of Taxus chinensis seeds, and then the main compound of BE, 20-hydroxyecdyone (20-HE), was obtained. High-pressure liquid chromatography (HPLC) was used to establish the in vitro analysis of BE and 20-HE. Afterward, BE micelle (BE-M) system was constructed via solvent injection combined with TPGS and mPEG-PCL and optimized using the single-factor screening experiment.

RESULTS

BE-M were spherical micelles with particle size (34.37 ± 0.11) nm and polydispersity index (PDI) 0.152 ± 0. 003, possessing a high encapsulation rate (86.53 ± 1.54) % and drug loading (21.63 ± 0.87) %. The critical micelle concentration (CMC) value was very low at 0.881 μg/mL, indicating that BE-M has good stability. X-ray diffraction analysis (XRD) and Fourier transform infrared analysis (FT-IR) showed that BE had been successfully encapsulated in BE-M.

CONCLUSION

The results of MTT assay showed that the IC50 values of BE-M against HepG2, A549 and U251 were lower than those of BE. This observation indicates that BE-M significantly improved the in vitro anti-tumor effect of BE.