以低窄壳糖为载体的MR/荧光双功能成像分子 探针的合成及性质研究
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国家自然科学基金项目;海南省国际技术合作专项


Synthesis and Study on Properties of An MR/Fluorescence Imaging Molecular Probe Using LNCS As Carrier
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    摘要:

    摘 要:通过微波辅助氧化法降解壳聚糖制得低聚窄分子量分布壳聚糖(低窄壳糖),LNCS6(聚合度为6,Mw/Mn = 1.08),并以LNCS6为载体,键接7-羟基-8-醛基香豆素(CA)为荧光基团、二乙烯三胺五乙酸(DTPA)为络合基团,络合三价钆离子最终制得一种潜在的核磁共振(MR)/ 荧光双功能成像分子探针Gd[DTPA/CA-LNCS6]。 研究了其磁共振成像效果以及荧光特性,并通过等温微量热滴定法(ITC)测定了产物与牛血清蛋白(BSA)之间的结合常数及热力学参数。实验结果表明,所得产物具有较高的体外磁共振成像效果〔(r1=13.71 L/(mmol • s)〕,远高于目前临床使用的马根维显〔r1=3.63 L/(mmol • s)〕。同时具有显著的荧光特性(λmax=438nm),与牛血清蛋白之间结合常数Ka>104,适用于血液输送,对这类探针精细化工产品的合成具有较好的参考与借鉴作用。

    Abstract:

    Abstract:Low degree of polymerization (DP) and narrow molecular weight distribution chitosan (LNCS6) (DP=6, Mw/Mn = 1.08) was prepared with the method of microwave-assisted oxidative degradation. It was used as a carrier molecular to link 7-hydroxyl-8-formylcoumarin (CA) as the fluorescence emission group, diethylenetriaminepentaacetic acid (DTPA) as complex of gadolinium ions to get the final product Gd[DTPA/CA-LNCS6] as an potential magnetic resonance (MR) /fluorescence bifunctional imaging molecular probe. The magnetic resonance imaging (MRI) efficiency and fluorescence properties were studied, and the binding constants and thermodynamic parameters between Gd[DTPA/CA-LNCS6] and bovine serum albumin (BSA) were measured by isothermal titration calorimetry (ITC). The results showed that Gd[DTPA/CA-LNCS6] exhibited higher MRI relaxation 〔r1=13.71 L/(mmol ∙ s)〕, which was well above the clinically used Magnevist 〔r1=3.63 L/(mmol ∙ s)〕; Meanwhile, the product had significant fluorescence characteristics at 438nm, and the binding constants between Gd[DTPA/CA-LNCS6] and BSA was over 104 which was suitable for blood transportation. This work has good reference for the synthesis of probes like such type of fine chemical.

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刘春玲,贾春满,张岐,钱亚骜,张德拉,杨秋云,杨仪宣.以低窄壳糖为载体的MR/荧光双功能成像分子 探针的合成及性质研究[J].精细化工,2016,33(2):

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  • 收稿日期:2015-10-31
  • 最后修改日期:2015-12-15
  • 录用日期:2015-12-16
  • 在线发布日期: 2016-01-13
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