中国医学计算机成像杂志
中國醫學計算機成像雜誌
중국의학계산궤성상잡지
CHINESE JOURNAL OF MEDICAL COMPUTED IMAGING
2010年
1期
46-51
,共6页
李树平%冯晓源%梁春敏%何慧瑾%孟庆刚%占昌友%李瑾%顾炳%佘振珏%邱龙华%杨波%陈路平
李樹平%馮曉源%樑春敏%何慧瑾%孟慶剛%佔昌友%李瑾%顧炳%佘振玨%邱龍華%楊波%陳路平
리수평%풍효원%량춘민%하혜근%맹경강%점창우%리근%고병%사진각%구룡화%양파%진로평
磁共振造影剂前体%合成%表征%BSA-(Gd-DTPA)_n
磁共振造影劑前體%閤成%錶徵%BSA-(Gd-DTPA)_n
자공진조영제전체%합성%표정%BSA-(Gd-DTPA)_n
MRI contrast agent precursor%Synthesis%Characterization%BSA- (Gd- DTPA)_n
目的:改进BSA-(Gd-DTPA)_n制备及纯化方法,探讨其作为磁共振造影剂前体的优势及应用前景.方法:BSA与二乙烯三胺五乙酸环酐反应生成BSA-(DTPA)_n,并与GdCb螯合生成BSA-(Gd-DTPA)_n.紫外光谱法鉴定其结构,并定量测定其中DTPA对BSA的偶联率.测定配合物体外弛豫时间T_1、T_2,分析其弛豫性能R1、R2.小鼠急性毒性试验评价药物安全性.大鼠磁共振增强扫描评价其活体内代谢及分布情况.结果:本研究制得的BSA-(Gd-DTPA)n配合物中n=26.体外弛豫性能RI约为7.00×10~(-3) L·mmol~(-1)·ms~(-1).比小分子Gd-DTPA的弛豫性能(3.52×10~(-3) L·mmol~(-1)·ms~(-1))提高近1倍.大鼠磁共振增强扫描显示BSA-(Gd-DTPA)-n和白蛋白一样具有长循环特性.结论:本实验改进方法可制备出磁共振造影剂前体BSA-(Gd-DTPA)_n,该配合物具备长循环特性,且具有多个可供修饰的氨基,可作为一种潜在的磁共振造影剂前体.
目的:改進BSA-(Gd-DTPA)_n製備及純化方法,探討其作為磁共振造影劑前體的優勢及應用前景.方法:BSA與二乙烯三胺五乙痠環酐反應生成BSA-(DTPA)_n,併與GdCb螯閤生成BSA-(Gd-DTPA)_n.紫外光譜法鑒定其結構,併定量測定其中DTPA對BSA的偶聯率.測定配閤物體外弛豫時間T_1、T_2,分析其弛豫性能R1、R2.小鼠急性毒性試驗評價藥物安全性.大鼠磁共振增彊掃描評價其活體內代謝及分佈情況.結果:本研究製得的BSA-(Gd-DTPA)n配閤物中n=26.體外弛豫性能RI約為7.00×10~(-3) L·mmol~(-1)·ms~(-1).比小分子Gd-DTPA的弛豫性能(3.52×10~(-3) L·mmol~(-1)·ms~(-1))提高近1倍.大鼠磁共振增彊掃描顯示BSA-(Gd-DTPA)-n和白蛋白一樣具有長循環特性.結論:本實驗改進方法可製備齣磁共振造影劑前體BSA-(Gd-DTPA)_n,該配閤物具備長循環特性,且具有多箇可供脩飾的氨基,可作為一種潛在的磁共振造影劑前體.
목적:개진BSA-(Gd-DTPA)_n제비급순화방법,탐토기작위자공진조영제전체적우세급응용전경.방법:BSA여이을희삼알오을산배항반응생성BSA-(DTPA)_n,병여GdCb오합생성BSA-(Gd-DTPA)_n.자외광보법감정기결구,병정량측정기중DTPA대BSA적우련솔.측정배합물체외이예시간T_1、T_2,분석기이예성능R1、R2.소서급성독성시험평개약물안전성.대서자공진증강소묘평개기활체내대사급분포정황.결과:본연구제득적BSA-(Gd-DTPA)n배합물중n=26.체외이예성능RI약위7.00×10~(-3) L·mmol~(-1)·ms~(-1).비소분자Gd-DTPA적이예성능(3.52×10~(-3) L·mmol~(-1)·ms~(-1))제고근1배.대서자공진증강소묘현시BSA-(Gd-DTPA)-n화백단백일양구유장순배특성.결론:본실험개진방법가제비출자공진조영제전체BSA-(Gd-DTPA)_n,해배합물구비장순배특성,차구유다개가공수식적안기,가작위일충잠재적자공진조영제전체.
Purpose: To improve the synthesis and purification methods of BSA - (Gd - DTPA)_n, and to explore its advantages and application prospect as a high - performance relaxation magnetic resonance imaging agent precursor. Methods: Bovine serum albumin (BSA) reacted with diethylenetriamine pen-taacetic acid cyclic anhydride (DTPACA) under the condition pH = 9, and produced the conjugate BSA -(DTPA)_n, GdCl_3 was further chelated to the conjugate to produce BSA- (Gd- DTPA)_n. BSA- (Gd - DT-PA)_n was characterized and identified by UV spectroscopy . The coupling ratio of DTPA and BSA was quantitatively determined by ICP/AES. The relaxation rates of R1/R2 were further analyzed by measur-ing the relaxation time T_1/ T_2 of the complex in vitro. The drug safety was evaluated by acute toxicity test. The preliminary evaluation of its metabolism and distributions in vivo was done by magnetic reso-nance multi - phase enhanced scanning for multi - organs in rats. Results: In the obtained complex BSA -(Gd-DTPA)_n, n = 26. The relaxation property R1 in vitro was about 7.00×10~(-3) L·mmol~(-1)·ms~(-1) at 0.5T in 32℃, about twice of the relaxation property of the small - molecule Gd - DTPA(3.52×10~(-3) L· mmol~(-1)·ms~(-1)). The enhanced MRI scans in SD rats showed that vessels were obviously enhanced at the same time that the renal pelvis already bad been filled by the contrast agent. This indicated that BSA-(Gd - DTPA)_n had notable long - circulating characteristic as albumin, and this was conducive to its fully integration with the targeted lesions and displaying the vessels.Conclusion: The high relaxation per-formance magnetic resonance contrast agent precursor BSA - (Gd- DTPA)_n can be prepared and purified by the improved methods in this experiment, it has notable long - circulating characteristic, and has many amino - groups for modification, so it can be used as a potential MRI targeting contrast agent pre-cursor.
