Human thioredoxin reductase (TrxR) system is associated with cancer cell growth and anti-apoptosis process. Effects of 1,2-bis(1,2-benzisoselenazolone-3(2H)-ketone)ethane (BBSKE),a novel TrxR inhibitor,were investigat...Human thioredoxin reductase (TrxR) system is associated with cancer cell growth and anti-apoptosis process. Effects of 1,2-bis(1,2-benzisoselenazolone-3(2H)-ketone)ethane (BBSKE),a novel TrxR inhibitor,were investigated on human leu-kemia cell lines HL-60 and K562. BBSKE treatment induced cell growth inhibition and apoptosis in both cell lines. Apoptosis induced by BBSKE is through Bcl-2/Bax and caspase-3 pathways. Ehrlich's ascites carcinoma-bearing mice were used to inves-tigate the anti-tumor effect of BBSKE in vivo. Tumor-bearing mice treated with BBSKE showed an increase of life span with a comparable effect to cyclophosphamide (CTX). These results suggest a potential usage of BBSKE as a therapeutic agent against non-solid tumors.展开更多
Two novel silver（I） complexes [Ag（DPEphos）（dppe）]Cl O4（1） and [Ag（DPEphos）-（dppe）]SCN（2）（DPEphos = bis[2-（diphenylphosphino）phenyl]ether, dppe = bis（diphenylphosphino）ethane） are synthesized and ch...Two novel silver（I） complexes [Ag（DPEphos）（dppe）]Cl O4（1） and [Ag（DPEphos）-（dppe）]SCN（2）（DPEphos = bis[2-（diphenylphosphino）phenyl]ether, dppe = bis（diphenylphosphino）ethane） are synthesized and characterized by IR, 1H/31 P NMR spectroscopy and fluorescence spectra. Complex 1 crystallizes in monoclinic, space group P21/c with a = 14.8821（12）, b = 12.6620（11）, c = 36.025（3） ？, β = 112.633（2）°, V = 6265.7（9） ？3, C62H52 Cl O5P4Ag, Mr = 1144.24, Z = 4, Dc = 1.213 g/cm3, F（000） = 2352, μ = 0.510 mm-1, the final R = 0.0616 and w R = 0.1192 for 4003 observed reflections（I 〉 2σ（I））. Complex 2 crystallizes in monoclinic, space group P21/c with a = 14.9021（13）, b = 12.6100（11）, c = 35.920（3） A, β = 112.852（2）°, V = 6220.2（9） A3, C63H52NOP4 SAg, Mr = 1102.87, Z = 4, Dc = 1.178 g/cm3, F（000） = 2272, μ = 0.498 mm-1, the final R = 0.0912 and w R = 0.1706 for 3287 observed reflections（I 〉 2σ（I））. In mono-nuclear complexes 1 and 2, the Ag（I） atom is chelated by DPEphos and dppe ligand. In the 31 P NMR spectra, there are splitting signals（doublets or triplets） which can be attributed to the coupling of the 107,109Ag–31P（from DPEphos or dppe ligand）. All the emission peaks of these complexes are attributed to ligand-centered（π-π＊） transitions.展开更多
基金Project (No.30472036) supported by the National Natural Science Foundation of China
文摘Human thioredoxin reductase (TrxR) system is associated with cancer cell growth and anti-apoptosis process. Effects of 1,2-bis(1,2-benzisoselenazolone-3(2H)-ketone)ethane (BBSKE),a novel TrxR inhibitor,were investigated on human leu-kemia cell lines HL-60 and K562. BBSKE treatment induced cell growth inhibition and apoptosis in both cell lines. Apoptosis induced by BBSKE is through Bcl-2/Bax and caspase-3 pathways. Ehrlich's ascites carcinoma-bearing mice were used to inves-tigate the anti-tumor effect of BBSKE in vivo. Tumor-bearing mice treated with BBSKE showed an increase of life span with a comparable effect to cyclophosphamide (CTX). These results suggest a potential usage of BBSKE as a therapeutic agent against non-solid tumors.
基金supported by the National Natural Science Foundation of China(Nos.21171119 and 81573822)the National High Technology Research and Development Program 863 of China(No.2012AA063201)+1 种基金the Technology Foundation for Selected Overseas Chinese,the Beijing Municipal Education Commission(KM201510028006)the Scientific Research Base Development Program of the Beijing Municipal Commission of Education
文摘Two novel silver（I） complexes [Ag（DPEphos）（dppe）]Cl O4（1） and [Ag（DPEphos）-（dppe）]SCN（2）（DPEphos = bis[2-（diphenylphosphino）phenyl]ether, dppe = bis（diphenylphosphino）ethane） are synthesized and characterized by IR, 1H/31 P NMR spectroscopy and fluorescence spectra. Complex 1 crystallizes in monoclinic, space group P21/c with a = 14.8821（12）, b = 12.6620（11）, c = 36.025（3） ？, β = 112.633（2）°, V = 6265.7（9） ？3, C62H52 Cl O5P4Ag, Mr = 1144.24, Z = 4, Dc = 1.213 g/cm3, F（000） = 2352, μ = 0.510 mm-1, the final R = 0.0616 and w R = 0.1192 for 4003 observed reflections（I 〉 2σ（I））. Complex 2 crystallizes in monoclinic, space group P21/c with a = 14.9021（13）, b = 12.6100（11）, c = 35.920（3） A, β = 112.852（2）°, V = 6220.2（9） A3, C63H52NOP4 SAg, Mr = 1102.87, Z = 4, Dc = 1.178 g/cm3, F（000） = 2272, μ = 0.498 mm-1, the final R = 0.0912 and w R = 0.1706 for 3287 observed reflections（I 〉 2σ（I））. In mono-nuclear complexes 1 and 2, the Ag（I） atom is chelated by DPEphos and dppe ligand. In the 31 P NMR spectra, there are splitting signals（doublets or triplets） which can be attributed to the coupling of the 107,109Ag–31P（from DPEphos or dppe ligand）. All the emission peaks of these complexes are attributed to ligand-centered（π-π＊） transitions.
