Research Of Supramolecular Nanoparticles Based On Self-assembly Of Galactose-functionalized Pillar[5]Arene

Purposes:1.To evaluate the inhibitory effects of honokiol,mentholand DOX on human esophageal cancer MCF-7 cells,human gastric cancer MGC-803 cells,human liver cancer SMMC-7721 cells and human prostate cancer PC-3 cells.To evaluate the inhibitory effect of the combination of honokiol and DOX on human breast cancer MCF-7 cells.To evaluate the inhibitory effect of the combination of menthol and DOX on human prostate cancer PC-3 cells.2.To synthesize water-soluble pillar[5]arene and guest molecules modified with natural drug molecules.To construct and evaluate the drug delivery system based on host-guest complex.Methods:1.The inhibitory effects of honokiol,menthol and DOX on MCF-7,MGC-803,SMMC-7721 and PC-3 were evaluated by MTT method.The inhibitory activity ofthe combination of honokiol and DOX on human breast cancer MCF-7 cellswas evaluated by MTT method.The inhibitory activity ofthe combination of menthol and DOX on human prostate cancer PC-3 cellswas evaluated by MTT method.2.Pillar[5]arene modified galactose was treated as the host.And the guest molecule was modified with natural drug.The drug delivery system was constructed based on the self-assembly of the host and guest.In vitro cell evaluation was performed by the MTT method.Results:1.Honokiol,menthol and DOX all showed good inhibitory activity on human esophageal cancer MCF-7 cells,human gastric cancer MGC-803 cells,human liver cancer SMMC-7721 cells and human prostate cancer PC-3 cells.With the concentration and time increasing,the inhibitory effects of these three drugs becomed better.Honokiol exhibited higher inhibitory activity on MCF-7 cells.Menthol exhibited higher inhibitory activity on PC-3 cells.DOX showed good inhibitory activity on all four cells.DOX at 0.5?M exhibited better anti-tumor effect when combined with honokiol and mentholin various concentrations.2.The structures of host and guest were characterized by NMR and HR-MS.The nanocarrier was constructed successfully based on 1:1 complexation of host and guest molecules.DOX loading rate of the drug delivery systemwas 58.6%.DOX-loadeddrug delivery systemshowed better inhibitory activity compared to free DOX on MCF-7in vitro cell experiments.Conclusions:1.Compared with DOX,honokiol and menthol show relatively weak antitumor activity.The inhibitory activity became higher when DOX at 0.5?M was combined with honokiol and menthol.2.The drug delivery system based on galactose functionalized pillar[5]arene was prepared.DOX-loadeddrug delivery system expressed better inhibitory activity compared to free DOX on MCF-7in vitro cell experiments.