Drug development and industrial pharmacy · 2025
Analysis of anti-tumor active components and preparation of self-assembled polymeric micelles in taxus chinensis seeds.
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Wang Qilong, Wang Xiaowen, Jiang Xia, Hua Qinyang, Adu-Frimpong Michael, Gong Mingjie, Li Tingyuan, Li Jiaying, Toreniyazov Elmurat, Berdiyar Jollibekov, Cao Xia, Yu Jiangnan, Xu Ximing
Аннотация
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.
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.