目的:优化8-氯-5,10-二氢-11H-二苯并[b,e][1,4]-二氮-11-酮的制备工艺。方法:重结晶提纯化合物,依据HPLC分析的结果,利用正交试验法,以反应时间、二甲苯用量、多聚磷酸用量和干燥温度作为影响因素,考查其对制备工艺优化的影响。结果:...目的:优化8-氯-5,10-二氢-11H-二苯并[b,e][1,4]-二氮-11-酮的制备工艺。方法:重结晶提纯化合物,依据HPLC分析的结果,利用正交试验法,以反应时间、二甲苯用量、多聚磷酸用量和干燥温度作为影响因素,考查其对制备工艺优化的影响。结果:确立了最优的工艺配方为反应时间21 h,二甲苯用量450 m L,多聚磷酸用量3 m L和干燥温度20℃。结论:经过多次试验证实,通过本文的试验方法制备8-氯-5,10-二氢-11H-二苯并[b,e][1,4]-二氮-11-酮的收率和纯度比文献工艺有了明显的提升,效果显著。展开更多
This study examined the effect of integrin cytoplasmic domain-associated protein 1α (ICAP-1α) and its mutatants T38A and I138A on the adhesion, migration and tube formation of 2H-11 cells.rAAV-ICAP-1α, rAAV-T38A an...This study examined the effect of integrin cytoplasmic domain-associated protein 1α (ICAP-1α) and its mutatants T38A and I138A on the adhesion, migration and tube formation of 2H-11 cells.rAAV-ICAP-1α, rAAV-T38A and rAAV-I138A were constructed.After infection, the expression of ICAP-1α and p-ERK1/2, p-c-Jun protein was measured by Western blotting.Adhesion ability was evaluated by using MTT.Cell migration was determined by using Boyden chamber method.Tube formation test was conducted on Matrigel.The results showed that in ICAP-1α, T38A and I138A groups, ICAP-1α protein expression was increased.In T38A and I138A groups, phospho-ERK1/2, phospho-c-Jun protein expressions were significantly increased as compared with the control group and the GFP group.ICAP-1α group protein expression was obviously decreased when compared with the control group and the GFP group.Cell adhesion ratio was 0.1429±0.0080 in control group, 0.1434±0.0077 in GFP group and the ratio in T38A and I138A groups increased to 0.3210±0.0082 and 0.3250±0.0079, respectively.In ICAP-1α group, the ratio was decreased to 0.1005±0.0073.In T38A and I138A groups, the number of migrating 2H-11 cells was increased to 31.45±3.20 and 33.10±5.40 against 18.51±2.80 in control group and 20.47±3.12 in GFP group.In ICAP-1α group, the number was decreased to 12.06±1.72.The number of tube-like structures was increased to 20.41±2.54 in T38A and to 22.26±3.07 in I138A groups as compared to those of control group 12.45±1.84 and GFP group 13.63±2.71.In ICAP-1α group, the number of tube-like structures was decreased to 8.32±1.24.It was suggested that rAAV-T38A and rAAV-I138A transfection can substantially increase 2H-11 cell adhesion, migration and angiogenisis, while rAAV-ICAP-1α can greatly inhibit the effect.These effects might be correlated with ERK1/2 and c-Jun protein phosphorylation.展开更多
文摘目的:优化8-氯-5,10-二氢-11H-二苯并[b,e][1,4]-二氮-11-酮的制备工艺。方法:重结晶提纯化合物,依据HPLC分析的结果,利用正交试验法,以反应时间、二甲苯用量、多聚磷酸用量和干燥温度作为影响因素,考查其对制备工艺优化的影响。结果:确立了最优的工艺配方为反应时间21 h,二甲苯用量450 m L,多聚磷酸用量3 m L和干燥温度20℃。结论:经过多次试验证实,通过本文的试验方法制备8-氯-5,10-二氢-11H-二苯并[b,e][1,4]-二氮-11-酮的收率和纯度比文献工艺有了明显的提升,效果显著。
基金supported by a grant from the National Natural Science Foundation of China (No.30670856)
文摘This study examined the effect of integrin cytoplasmic domain-associated protein 1α (ICAP-1α) and its mutatants T38A and I138A on the adhesion, migration and tube formation of 2H-11 cells.rAAV-ICAP-1α, rAAV-T38A and rAAV-I138A were constructed.After infection, the expression of ICAP-1α and p-ERK1/2, p-c-Jun protein was measured by Western blotting.Adhesion ability was evaluated by using MTT.Cell migration was determined by using Boyden chamber method.Tube formation test was conducted on Matrigel.The results showed that in ICAP-1α, T38A and I138A groups, ICAP-1α protein expression was increased.In T38A and I138A groups, phospho-ERK1/2, phospho-c-Jun protein expressions were significantly increased as compared with the control group and the GFP group.ICAP-1α group protein expression was obviously decreased when compared with the control group and the GFP group.Cell adhesion ratio was 0.1429±0.0080 in control group, 0.1434±0.0077 in GFP group and the ratio in T38A and I138A groups increased to 0.3210±0.0082 and 0.3250±0.0079, respectively.In ICAP-1α group, the ratio was decreased to 0.1005±0.0073.In T38A and I138A groups, the number of migrating 2H-11 cells was increased to 31.45±3.20 and 33.10±5.40 against 18.51±2.80 in control group and 20.47±3.12 in GFP group.In ICAP-1α group, the number was decreased to 12.06±1.72.The number of tube-like structures was increased to 20.41±2.54 in T38A and to 22.26±3.07 in I138A groups as compared to those of control group 12.45±1.84 and GFP group 13.63±2.71.In ICAP-1α group, the number of tube-like structures was decreased to 8.32±1.24.It was suggested that rAAV-T38A and rAAV-I138A transfection can substantially increase 2H-11 cell adhesion, migration and angiogenisis, while rAAV-ICAP-1α can greatly inhibit the effect.These effects might be correlated with ERK1/2 and c-Jun protein phosphorylation.
