ABSTRACT
Objective: To investigate the effects of magnolol in combination with 5-fluorouracil (5-FU) on the proliferation of human colon cancer HCT-8 cells and the expression of secreted frizzled-related protein-4 (SFRP-4). Methods: After treatment with magnolol and 5-FU alone or magnolol in combination with 5-FU, the proliferation of colon cancer HCT-8 cells was detected by MTT method, and the cell cycle distribution and the apoptosis of HCT-8 cells were examined by flow cytometry (FCM) and Hoechst 33258 nucleic acid staining, respectively. The expression levels of SFRP-4 and p-catenin proteins in HCT-8 cells were examined by Western blotting. Results: The proliferation of HCT-8 cells was inhibited by magnolol and 5-FU alone or mamgnolol in combination with 5-FU (all P 2/M phases were decreased in 5-FU alone group and the combination treatment group (both P < 0.05). The expression levels of SFRP-4 in HCT-8 cells in all three treatment groups were higher than that in the blank control group (without any treatment) (P < 0.05), while the expression level of p-catenin in HCT-8 cells in combination treatment group was lower than those in 5-FU and magnolol alone groups (P < 0.05). Conclusion: Magnolol in combination with 5-FU can enhance the inhibition effect on proliferation of human colon cancer HCT-8 cells, and arrest the cells at G0/G1 phase. This mechanism may be related to regulating the expressions of SFRP-4 and p-catenin proteins.
ABSTRACT
The study is designed to synthesize nano-carrier Tyr-RGD (cyclo-[Arg-Gly-Asp-d-Tyr-Lys]) and poly(ethylene glycol) modified polyethylenimine (Tyr-RGD-PEG-PEI) targeting vascular endothelial cells, then analyze its nanoparticle properties and the characteristics of drug carrying and targeting properties in vivo / in vitro tumor. The nano-carrier Tyr-RGD-PEG-PEI was synthesized with the method of chemical synthesis and the properties of this nanoparticle and drug carrying characteristics were identified. Its effect of targeting vascular endothelial cells in vitro was studied with the method of competitive binding assay. The fluorescent labeled nano-drug was injected into tumor-bearing nude mice to observe its tumor-targeting. The mean size of nano-carrier Tyr-RGD-PEG-PE was about 145 nm, good in encapsulation efficiency of siRNA. After incubation in plasma for half an hour, only about 3 percent of siRNA out. It was confirmed that it was a single spot with TLC analysis, the R(f) value was 0.65. Receptor competition experiments showed that the nano could effectively compete with RGD in binding the receptors on endothelial cells. Tumor-bearing nude mice experiments showed that when containing a fluorescent-labeled siRNA of Tyr-RGD-PEG-PEI nano-drug was injected into mice, after 24 hours this nano-drug mainly distributed within the tumor tissue. However, nano-drug without Tyr-RGD appeared in tumor tissue as well as other organs such as livers, lungs, etc. The Tyr-RGD-targeted gene vector Tyr-RGD-PEG-PEI synthesized in this study has good nanoparticle properties and high efficiency of gene-drug encapsulation. Study of nude mice shows that the ability of its tumor-targeting is significantly better than nano-drug without Tyr-RGD.
Subject(s)
Animals , Humans , Mice , Endothelial Cells , Metabolism , Gene Transfer Techniques , Genetic Vectors , Integrins , Mice, Nude , Nanoparticles , Oligopeptides , Pharmacology , RNA, Small InterferingABSTRACT
<p><b>OBJECTIVE</b>To study the difference of glucose metabolic rate in non-small cell lung cancer (NSCLC) patients with blood stasis syndrome and with non-blood stasis syndrome.</p><p><b>METHODS</b>Whole body positron emission tomography (PET) and functional agent 2-[fluorine-18] fluorine-2-deoxy-glucose (18FDG) were used to detect the 18FDG uptake value in regions of interest (ROI) in tumor tissue of patients.</p><p><b>RESULTS</b>In patients with same pathologic type, the maximum and mean standardized uptake value (Max SUV and Mean SUV) were significantly higher in the blood stasis group than those in the non-blood stasis group (P < 0.01); it also showed the same in patients with NSCLC of phase I, II and III (P < 0.05), but the 18FDG uptake rate was obviously enhanced in patients of phase IV (P < 0.01).</p><p><b>CONCLUSION</b>The glucose uptake in NSCLC patients of blood stasis syndrome was higher than that in those with of non-blood stasis syndrome.</p>