Farrerol overcomes the invasiveness of lung squamous cell carcinoma cells by regulating the expression of inducers of epithelial mesenchymal transition.

In recent years Epithelial Mesenchymal Transition (EMT) has been proposed as a mechanism indispensable to acquisition of metastatic properties by tumor cells. In this study we tested the ability of Farrerol, a Chinese herb-derived compound to ablate the EMT in human lung squamous cell carcinoma cells. Human lung squamous cell carcinoma cells, Calu-1 were treated with various concentrations of Farrerol for 24 h to examine its effect on their viability by the MTT assay. Only those concentrations which showed least effect on the viability of Calu-1 cells were further used to evaluate the expression of epithelial and mesenchymal markers by western blotting. Furthermore the effect of such concentrations on the migration and invasion of Calu-1 cells was determined by wound healing and transwell invasion assays respectively. The results demonstrated that Farrerol treatment led to the downregulation of Slug and Zeb-1, transcriptional regulators of EMT with the concomitant increase and decrease in the expression of E-cadherin and vimentin respectively. These data were further supported by migration and invasion assays which demonstrated that Farrerol treatment caused inhibited the migration and invasion of Calu-1 lung squamous cell carcinoma cells. Taken together, our results indicate that Farrerol suppresses lung squamous cell carcinoma cell metastatic potential by modulating the expression of EMT proteins.

Ferrerol overcomes the invasiveness of lung squamous cell carcinoma cells by regulating the expression of inducers of Epithelial Mesenchymal Transition.

In recent years Epithelial Mesenchymal Transition (EMT) has been proposed as a mechanism indispensable to acquisition of metastatic properties by tumor cells. In this study we tested the ability of Ferrerol, a Chinese herb-derived compound to ablate the EMT in human lung squamous cell carcinoma cells. Human lung squamous cell carcinoma cells, Calu-1 were treated with various concentrations of Ferrerol for 24 h to examine its effect on their viability by the MTT assay. Only those concentrations which showed least effect on the viability of Calu-1 cells were further used to evaluate the expression of epithelial and mesenchymal markers by western blotting. Furthermore the effect of such concentrations on the migration and invasion of Calu-1 cells was determined by wound healing and transwell invasion assays respectively. The results demonstrated that Ferrerol treatment led to the downregulation of Slug and Zeb-1, transcriptional regulators of EMT with the concomitant increase and decrease in the expression of E-cadherin and vimentin respectively. These data were further supported by migration and invasion assays which demonstrated that Ferrerol treatment caused inhibited the migration and invasion of Calu-1 lung squamous cell carcinoma cells. Taken together, our results indicate that Ferrerol suppresses lung squamous cell carcinoma cell metastatic potential by modulating the expression of EMT proteins.

[Synthesis and characterization of folic acid-conjugated chitosan nanoparticles as a tumor-targeted drug carrier].

OBJECTIVE: To synthesize and characterize paclitaxel (PTX)-loaded folate-conjugated chitosan (FA-CTS/PTX) nanoparticles and evaluate its cytotoxicity in vitro. METHODS: CTS/PTX and FA-CTS/PTX nanoparticles were prepared using reductive amidation and ionic gelation of chitosan with tripolyphosphate anions (TPP). The particle size was determined by laser scattering and the morphology observed using transmission electron microscopy, and the PTX content in the nanoparticles was determined using ultraviolet spectrophotometer at 227 nm. The in vitro cytotoxicity of the nanoparticles against HeLa cells was evaluated by MTT assay. Fluorescence microscopy was used to observe the HeLa cells incubated with FA-chitosan nanoparticles in the presence or absence of folic acid in the culture medium. RESULTS: PTX loading did not cause adhesion of the FA-CTS nanoparticles, which presented with uniform spherical morphology with an average diameter of 282.8 nm. The loading and encapsulation efficiencies of FA-CTS/PTX were 9.0% and 75.4%, respectively. The FA-CTS nanoparticles showed a greater extent of intracellular uptake in the absence of folic acid, indicating that the cellular uptake of the nanoparticles occurred through endocytosis mediated by the folate receptors. The PTX-loaded FA-CTS nanoparticles exhibited potent cytotoxicity against HeLa cells, an effect 2- to 3-fold stronger than that of PTX-loaded CTS nanoparticles. CONCLUSION: FA-CTS can be a promising drug carrier with high efficiency in condensing drug, good tumor-targeting ability and low cytotoxicity.