Chemical constituents from Ganoderma angustisporum and their α-glucosidase inhibitory activities / 中成药

AIM To study the chemical constituents from Ganoderma angustisporum J.H.Xing,B.K.Cui&Y.C.Dai and their α-glucosidase inhibitory activities.METHODS The ethyl acetate extract from G.angustisporum was isolated and purified by silica gel,ODS,TLC and HPLC,then the structures of obtained compounds were identified by physicochemical properties and spectral data.pNPG method was used to evaluate their α-glucosidase inhibitory activities.RESULTS Seven compounds were isolated and identified as N-acetyl-L-phenylalanine ethyl ester(1),N-acetyl-L-phenylalanine methyl ester(2),4-hydroxy-17R-methylincisterol(3),6,8-di-O-methylaverufin(4),aversin(5),methyl 2-(4-hydroxyphenyl)aceate(6),5-toluene-1,3-diol(7).Compounds 1-2,4-7 showed inhibitory activities of α-glucosidase with IC50 values being(33.80±0.47),(45.45±7.95),(48.80±5.86),(39.48±2.82),(41.47±6.68),(55.38±10.12)μmol/L,and compound 1 showed good inhibitory activity.CONCLUSION Compound 1 is a new natural product.Compounds 2-7 are isolated from genus Ganoderma for the first time.Compounds 1-2,4-7 have α-glucosidase inhibitory activities.

Effects of bortezomib combined with 5-azacytidine on the apoptosis of K562 cells and expression of SHIP mRNA / 中国实验血液学杂志

This study was aimed to investigate the effects of bortezomib combined with 5-azacytidine on the apoptosis of K562 cells and expressiom of SHIP mRNA. The K562 cells were cultured and treated with different concentrations of bortezomib, 5-azacytidine or their combination for 24 hours. Then, the expression of SHIP mRNA was detected by RT-PCR,the cell proliferation was analyzed by using MTT assay and flow cytometry. The results showed that 5-20 nmol/L bortezomib could effectively inhibit the proliferation of K562 and this inhibitory effect gradually enhanced along with the increase of bortezomib concentration, the group of bortezomib combined with 5-azacytidine showed more inhibitory effect on K562 cells than that of bortezomib or 5-azacytidine alone.The bortezomib could promote the apoptosis of K562 cells in a dose-dependent manner,and this apoptotic effect was higher in group of bortezomib combined with 5-azacytidine than that in group of bortezomib or 5-azacytidine alone.Bortezomib could down-regulated the expression of SHIP mRNA in a dose-dependent manner,and this down-requlated effect was higher in group of bortezomib combined with 5-azacytidine than that in group of bortezomib or 5-azacytidine alone.It is concluded that bortezomib and 5-azacytidine can induce apoptosis by inhibiting the expression of SHIP mRNA in K562 cells.The combination of bortezomib with 5-azacytidine displays a synergetic effect.