Two novel rare earth tungstosilicic polyoxometalate containing 5-fluorouracil,K26(C4H4FN2O2)8Pr(SiW11O39)4·10H2O(FPSW) and K26(C4H4FN2O2)8Sm(SiW11O39)4·9H2O(FSSW),were synthesized and their structure were ch...Two novel rare earth tungstosilicic polyoxometalate containing 5-fluorouracil,K26(C4H4FN2O2)8Pr(SiW11O39)4·10H2O(FPSW) and K26(C4H4FN2O2)8Sm(SiW11O39)4·9H2O(FSSW),were synthesized and their structure were characterized by using elemental analysis,FTIR spectra,X-ray powder diffraction and TG.The antitumor activity tests of the compounds FPSW and FSSW were carried out by the methyl thiazolyl tetrazolium method in hepatocellular carcinoma cell HepG-2.The results showed that FPSW and FSSW could inhibit the HepG-2 cells in vitro significantly.The EC50 of FPSW and FSSW is 1.94×10-5 and 1.32×10-5 mol·L-1 respectively.The therapeutic index of FPSW and FSSW is 0.76 and 1.58 respectively.展开更多
Traditional Chinese herbal medicine(TCM)has been shown to enhance the efficacy of standard anticancer agents.However,there are only a limited number of well-controlled preclinical and clinical studies documenting the ...Traditional Chinese herbal medicine(TCM)has been shown to enhance the efficacy of standard anticancer agents.However,there are only a limited number of well-controlled preclinical and clinical studies documenting the potential benefit of TCM.OBJECTIVE To identify biologically active formulas that were effective against colorectal cancer(CRC)by screening TCM formulas in in vitro and in vivo animal models.METHODS Cell growth assays,cell cycle analysis,immunoblot analysis and qRT-PCR were performed to investigate the mechanism(s)of action of the formulason human CRC cells.In vivo animal models were used to evaluate the antitumor activity of formulasalone and in combination with 5-FU.RESULTS We identified Huangqin Gegen Tang(HQGGT)which suppressed the in vivo growth of human CRC HT-29 xenografts.HQGGT significantly inhibited the growth of CRC cell lines.HQGGT enhanced the cytotoxicity of 5-FU against human 5-FU-resistant cells(H630R1)and mouse colon cancer cells(MC38).This synergy was the result of suppression of thymidylate synthase expression by HQGGT.HQGGT significantly enhanced the antitumor effect of 5-FU in mice bearing MC38 xenografts.Ongoing studies have identified Huangqin as the herb responsible for TS inhibi⁃tion.CONCLUSION These findings provide support for the potential role of HQGGT as a novel modulator of fluoropyrim⁃idine chemotherapy for CRC treatment.展开更多
基金Project supported by Institution of Chemical Materials,China Academy of Engineering Physics
文摘Two novel rare earth tungstosilicic polyoxometalate containing 5-fluorouracil,K26(C4H4FN2O2)8Pr(SiW11O39)4·10H2O(FPSW) and K26(C4H4FN2O2)8Sm(SiW11O39)4·9H2O(FSSW),were synthesized and their structure were characterized by using elemental analysis,FTIR spectra,X-ray powder diffraction and TG.The antitumor activity tests of the compounds FPSW and FSSW were carried out by the methyl thiazolyl tetrazolium method in hepatocellular carcinoma cell HepG-2.The results showed that FPSW and FSSW could inhibit the HepG-2 cells in vitro significantly.The EC50 of FPSW and FSSW is 1.94×10-5 and 1.32×10-5 mol·L-1 respectively.The therapeutic index of FPSW and FSSW is 0.76 and 1.58 respectively.
文摘Traditional Chinese herbal medicine(TCM)has been shown to enhance the efficacy of standard anticancer agents.However,there are only a limited number of well-controlled preclinical and clinical studies documenting the potential benefit of TCM.OBJECTIVE To identify biologically active formulas that were effective against colorectal cancer(CRC)by screening TCM formulas in in vitro and in vivo animal models.METHODS Cell growth assays,cell cycle analysis,immunoblot analysis and qRT-PCR were performed to investigate the mechanism(s)of action of the formulason human CRC cells.In vivo animal models were used to evaluate the antitumor activity of formulasalone and in combination with 5-FU.RESULTS We identified Huangqin Gegen Tang(HQGGT)which suppressed the in vivo growth of human CRC HT-29 xenografts.HQGGT significantly inhibited the growth of CRC cell lines.HQGGT enhanced the cytotoxicity of 5-FU against human 5-FU-resistant cells(H630R1)and mouse colon cancer cells(MC38).This synergy was the result of suppression of thymidylate synthase expression by HQGGT.HQGGT significantly enhanced the antitumor effect of 5-FU in mice bearing MC38 xenografts.Ongoing studies have identified Huangqin as the herb responsible for TS inhibi⁃tion.CONCLUSION These findings provide support for the potential role of HQGGT as a novel modulator of fluoropyrim⁃idine chemotherapy for CRC treatment.
