Summary: Integrins such as αvβ3, α5β31 play a key role in angiogenesis regulation, invasion and metastasis, inflammation, wound healing, etc. The up-regulation of integrin αvβ3 after cerebral ischemic stroke ca...Summary: Integrins such as αvβ3, α5β31 play a key role in angiogenesis regulation, invasion and metastasis, inflammation, wound healing, etc. The up-regulation of integrin αvβ3 after cerebral ischemic stroke can promote angiogenesis, which in turn improves functional recovery. In addition, the integrin αvβ3 inhibitor can block the blood-brain barrier (BBB) leakage induced by vascular endothelial growth factor (VEGF) and also can reduce inflammatory reaction, decrease the deposition of fibrinogen. Other studies showed that integrin αvβ3 is not essential in revascularization. Therefore, the effect of integrin αvβ3 in the whole process of brain function recovery merits further study.展开更多
Antibody targeted delivery is an effective strategy to improve the diagnostic imaging outcome of nanoscale imaging agents in the focal areas. Dual targeting micelles encapsulating superparamagnetic iron oxide were pre...Antibody targeted delivery is an effective strategy to improve the diagnostic imaging outcome of nanoscale imaging agents in the focal areas. Dual targeting micelles encapsulating superparamagnetic iron oxide were prepared from the amphiphilic block copolymer poly(ethylene glycol)-poly(e-caprolactone) (PEG-b-PCL) with different targeting ligands cRGD and scFv-ErbB single chain antibody conjugated to the distal ends of PEG block. The breast cancer animal model was established by subcutaneous injecting the BT474 cells into the BALB/c-nu female nude mice and then employed to assess the potential of the dual ligand targeted magnetic micelles as a novel MRI contrast agent on a 1.5 T clinical MR/scanner. The T2 signal intensity of the tumor in animals receiving the dual ligand targeted magnetic micelles via tail vein decreased more significantly than the single ligand targeted and nontargeted magnetic micelles. These results indicate that the dual ligand targeted magnetic micelles, cRGD/scFv-ErbB-PEG-PCL-SPION, have great potential to act as a new type of effective nanoscale MRI contrast agent for early diagnosis of breast cancer.展开更多
目的:建立反相高效液相色谱法(RP-HPLC)测定卡维地洛片有关物质。方法:采用YMC-Pack Pro C8色谱柱(150 mm×4.6 mm,5μm),以乙腈-0.02 mol·L-1磷酸二氢钾溶液(用磷酸调p H 2.0)为流动相进行梯度洗脱,流速1.0 m L·...目的:建立反相高效液相色谱法(RP-HPLC)测定卡维地洛片有关物质。方法:采用YMC-Pack Pro C8色谱柱(150 mm×4.6 mm,5μm),以乙腈-0.02 mol·L-1磷酸二氢钾溶液(用磷酸调p H 2.0)为流动相进行梯度洗脱,流速1.0 m L·min-1,柱温30℃,检测波长为220 nm(杂质E)和240 nm(其他杂质)。结果:卡维地洛与已知杂质及强制破坏实验产生的降解产物均能获得良好的分离,杂质D(4-环氧丙烷氧基咔唑)与杂质E[2-(2-甲氧基苯氧基)乙胺]质量浓度分别在0.063 98~12.80μg·m L-1(r=0.999 9)和0.089 33~8.933μg·m L-1(r=1.000)范围内与峰面积呈良好的线性关系。杂质D高、中、低浓度的回收率(n=3)分别为98.6%、96.5%、94.2%,RSD分别为1.1%、0.8%、1.4%;杂质E高、中、低浓度的回收率(n=3)分别为99.2%、86%、92.7%,RSD分别为0.15%、0.65%、9.5%。杂质D和杂质E精密度试验的RSD(n=6)分别为1.4%和0.31%,建立的方法与现行中国药典收载的方法相比能分离检测到更多的杂质。结论:本方法经方法学验证,可用于卡维地洛有关物质的检测和质量控制。展开更多
文摘Summary: Integrins such as αvβ3, α5β31 play a key role in angiogenesis regulation, invasion and metastasis, inflammation, wound healing, etc. The up-regulation of integrin αvβ3 after cerebral ischemic stroke can promote angiogenesis, which in turn improves functional recovery. In addition, the integrin αvβ3 inhibitor can block the blood-brain barrier (BBB) leakage induced by vascular endothelial growth factor (VEGF) and also can reduce inflammatory reaction, decrease the deposition of fibrinogen. Other studies showed that integrin αvβ3 is not essential in revascularization. Therefore, the effect of integrin αvβ3 in the whole process of brain function recovery merits further study.
基金supported by the 863 Programs of China(No.2009AA03Z310)National Natural Science Foundation of China(Nos.21174166,30973419)+5 种基金the Ph.D.Programs Foundation of Ministry of Education of China(No.20100171110011)the Postdoctoral Foundation(No.201003370)Natural Science Foundation(Nos.9351027501000003,S2011020003140)S&T Programs of Guangdong Province(Nos.2010B031500011,2009B030803003,2009B030801107,2012B031800135)SYSU Projects for Promotion of Key and Emerging Interdisciplinary Researches(10ykjc18)Young Teachers(11lgpy44)
文摘Antibody targeted delivery is an effective strategy to improve the diagnostic imaging outcome of nanoscale imaging agents in the focal areas. Dual targeting micelles encapsulating superparamagnetic iron oxide were prepared from the amphiphilic block copolymer poly(ethylene glycol)-poly(e-caprolactone) (PEG-b-PCL) with different targeting ligands cRGD and scFv-ErbB single chain antibody conjugated to the distal ends of PEG block. The breast cancer animal model was established by subcutaneous injecting the BT474 cells into the BALB/c-nu female nude mice and then employed to assess the potential of the dual ligand targeted magnetic micelles as a novel MRI contrast agent on a 1.5 T clinical MR/scanner. The T2 signal intensity of the tumor in animals receiving the dual ligand targeted magnetic micelles via tail vein decreased more significantly than the single ligand targeted and nontargeted magnetic micelles. These results indicate that the dual ligand targeted magnetic micelles, cRGD/scFv-ErbB-PEG-PCL-SPION, have great potential to act as a new type of effective nanoscale MRI contrast agent for early diagnosis of breast cancer.