ABSTRACT
Objective: A transferrin and folic acid co-modified Coicis Semen oil-tripterine microemulsion (Tf/FA-CT-MEs) was developed to improve the tumor targeting and thereby enhance the in vitro antitumor efficacy. Methods: FA-PEG 400 was synthesized by classic condensation and together with transferrin as targeting ligands. The structures were characterized by FT-IR and H-NMR. Tf/FA-CT-MEs were prepared by aqueous titration method using Coicis Semen oil as oil phase, followed by anchoring Tf on the surface of prepared particles mentioned-above in aqueous environment. The physiochemical properties and morphology were detected by dynamic light scattering (DLS) and transmission electron microscopy (TEM), respectively. The A549 and MCF-7 cellular uptake of various microemulsions was detected through employing fluorescein isothiocyanate (FITC) as a fluorescence probe. The in vitro antitumor efficacy of the microemulsions against A549 and MCF-7 cells were determined by MTT assay and cell apoptosis kit. Results: FA-PEG 400 was synthesized and characterized as a target ligand. The Tf/FA-CT-MEs with spherical shape had a small droplet size (52.52 ± 0.11) nm, narrow polydispersion index (PDI, 0.124 ± 0.019), and negative Zeta potential (-21.50 ± 1.70) mV, respectively, with good in vitro stability. In in vitro antitumor efficacy, the half proliferation inhibitory concentration (IC50) of Tf/FA-CT-MEs was 0.77 μmol/L on MCF-7 cell model and 0.85 μmol/L on A549 cell model. The cellular uptake results suggested that the fluorescence intensity of MCF-7 and A549 cells was 2782.33 ± 131.77 and 2762.91 ± 23.18 for 4 h, respectively. Besides, (70.60 ± 6.92)% of MCF-7 cells were induced to apoptosis by Tf/FA-CT-MEs. Conclusion: Tf/FA-CT-MEs could improve in vitro targeting and cytotoxicity toward MCF-7 cells. This study suggests that the modification with dul-targeted ligands could be a promising strategy for developing tumor-specific nanomedicines.
ABSTRACT
Objective To investigate the inhibitory effect of Coicis Semen oil on human prostate cancer PC-3 cell. Methods A Nude mice xenograft model was established with human prostate cancer PC-3 cells. Meanwhile, intragastric administration with Coicis Semen oil 2 mL/kg and 6 mL/kg was run for once daily and growth-curve was drawn through measuring the tumor volume until 26 d. At the end of the experiment, tumor weights were measured and the tumor inhibition rate of each group was calculated. The activity of fatty acid synthase (FAS) was determined through UV-VIS spectrophotometry. PC-3 cells were cultured in vitro. SYBR Green I real-time quantitative RT-PCR was used to determine the relative expression of FAS mRNA. Results The tumor inhibition rate of Coicis Semen oil 6 mL/kg group was 43.9%. Compared with model group, FAS activity in this tumor tissue decreased by 44.7% (P < 0.05). The expression of FAS mRNA was significantly decreased at 20 μL/mL of Coicis Semen oil group (P < 0.05). Conclusion Coicis Semen oil on human prostate cancer PC-3 cells has a significant inhibitory effect. FAS activity and mRNA expression decline may be related to its main anti-cancer mechanism.
ABSTRACT
Objective: To establish the fusion-fingerprint of Coicis Semen oil. Methods: The Coicis Semen oil was analyzed by GC-MS and HPLC-ELSD, and the fusion-fingerprint was originated from the Computer Aided Similarity Evaluation software based on the normalized data acquired by the above two methods. Results: Twenty-one common peaks existed in the fusion-fingerprint of which there were 13 kinds of aliphatic esters detected by GC-MS and 8 kinds of triglyceride ingredients detected by HPLC-ELSD. Conclusion: The fusion-fingerprint established on GC-MS combined with HPLC-ELSD could provide integrity and more information for the quality control of Chinese materia medica.