Objective An organic layer prepared from the cortex of Morus alba(Moraceae)was studied in order to identify the active compounds for heparinase.Methods Bioassay-guided fractionation resulted in the isolation of sangge...Objective An organic layer prepared from the cortex of Morus alba(Moraceae)was studied in order to identify the active compounds for heparinase.Methods Bioassay-guided fractionation resulted in the isolation of sanggenon G.Results The compound showed inhibitory activity with IC50 of 3.7μmol/L on heparinase in vitro as well as 24μmol/L in invasion assay using MDA-MB231 cells.Sanggenon G also had the moderate cytotoxicity at SW 620(colon)and ACHN(kidney)cancer cell lines with IC50 of 10.96 and 13.44μmol/L,respectively.Conclusion This is the first time that prenylated flavonoid sanggenon G is described as heparinase inhibitor.Besides,this flavonoid would be expected to be a metastasis inhibitor of cancer cells and also a valuable reagent to explore the mechanism of heparinase/heparanase-mediated metastasis.展开更多
基金Scientific Research Foundation for the Returned Overseas Chinese Scholars,State Education Ministry(JWSL-2009-1590)Key Laboratory of Natural Resources of Changbai Mountain & Functional Molecules(Yanbian University)Ministry of Education,China(CSSHZ-2009-05)
文摘Objective An organic layer prepared from the cortex of Morus alba(Moraceae)was studied in order to identify the active compounds for heparinase.Methods Bioassay-guided fractionation resulted in the isolation of sanggenon G.Results The compound showed inhibitory activity with IC50 of 3.7μmol/L on heparinase in vitro as well as 24μmol/L in invasion assay using MDA-MB231 cells.Sanggenon G also had the moderate cytotoxicity at SW 620(colon)and ACHN(kidney)cancer cell lines with IC50 of 10.96 and 13.44μmol/L,respectively.Conclusion This is the first time that prenylated flavonoid sanggenon G is described as heparinase inhibitor.Besides,this flavonoid would be expected to be a metastasis inhibitor of cancer cells and also a valuable reagent to explore the mechanism of heparinase/heparanase-mediated metastasis.
