ABSTRACT
OBJECTIVE: To design and synthesize two kinds of allyl-substituted quercetin and investigate their anti-oxidation and anti-tumor activities in vitro. METHODS: The target compounds 1 and 2 were first synthesized from quercetin by hydroxyl protection, allylation,Claisen rearrangement and deprotection. The anti-oxidation and anti-tumor activities of the target compounds and intermediate products were evaluated by DPPH and MTT assay. RESULTS: Eight compounds were synthesized,including six intermediates and two target compounds,in which four were new compounds. All of them were confirmed by 1H-NMR,13C-NMR and LC-MS spectra. The anti-oxidation and anti-tumor tests showed that compounds 1,2,5,6,8 and 9 had anti-oxidation activities and compound 5 inhibited A549 lung cancer cell proliferation. Compound 9 could inhibit the proliferation of lung cancer A549 cells and HepG2 cells. CONCLUSION: The compounds with electron-donating groups have significant anti-oxidant activity. When acetyl and methyl ether groups are used as the protecting groups,the position of introducing allyl group to quercetin has obvious impact on the anti-tumor activity.
ABSTRACT
OBJECTIVE: To improve the water solubility of ginsenoside Rg3, using mesoporous silica nanoparticles MCM-41 loading ginsenoside Rg3 and study the mechanism of promoting drug absorption with human lung cancer cells A549 as a model. METHODS: The mesoporous silica nanoparticles MCM-41, as a carrier, loading ginsenoside Rg3 by adsorption method. The morphology and particle size of MCM-41 were investigated by transmission electron microscopy (TEM) and laser particle size analyzer. The solid state characterization of ginsenoside Rg3 were investigated by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and Fourier transform infrared spectroscopy method (FTIR), respectively. In vitro dissolution experiments investigated the dissolution rate of ginsenoside Rg3. Cytotoxicity assay and cell uptake experiments explored the effect of the administration system of A549 cells and the mechanism of inhibiting cell proliferation. RESULTS: We have been successfully prepared the mesoporous silica nanoparticles MCM-41. In vitro dissolution experiments showed that MCM-41 can significantly improve the dissolution rates of ginsenoside Rg3. Administration system can be uptaked into A549 cells and inhibit cell proliferation. CONCLUSION: The mesoporous silica nanoparticles MCM-41 has a good solubilization effect for ginsenoside Rg3, and MCM-41 has potential as a carrier for the treatment of lung cancer.
ABSTRACT
Aim To study the apoptosis effect of Sir-aitia grosvenorii extract on human lung cancer cells A549 and its mechanisms.Methods MTT assay was applied to determine A549 cell proliferation.Hoechst 33258 staining was applied to investigate morphological changes in A549 cells.To find out the cause of cell growth inhibition,several experiments on cell cycle distribution and apoptosis were performed by flow cy-tometry analysis.The expression of p21 and Bcl-2 was determined by Western blot.Results Flow cytometry analysis showed that treatment with mogrol arrested A549 cells in the G0 /G1 phase and induced apoptosis. After treatment with Siraitia grosvenorii extract,West-ern blot experiment showed cell cycle regulator p21 was up-regulaed,while the apoptosis inhibitor Bcl-2 was down-regulated.Conclusion Treatment with Siraitia grosvenorii extract arrests the A549 cells at G0 /G1 phase and induces apoptosis that may contribute to the anti-proliferation activity of mogrol through the regula-tion of p21 and Bcl-2 expression.