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用于前哨淋巴结检测的新型大分子的合成:99mTc-甘氨酰-甘露糖基-葡聚糖。

The synthesis of a new macromolecule for the sentinel node detection: 99mTc-gly-mannosyl-dextran.

作者信息

Wang Gang, Wu Erming, Wang Yang, Huang Heyun, Zhou Yanfang, Chen Zhiming

机构信息

Key Laboratory of Nuclear Medicine, Ministry of Health, Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi, China.

出版信息

Nucl Med Commun. 2019 Feb;40(2):131-135. doi: 10.1097/MNM.0000000000000951.

DOI:10.1097/MNM.0000000000000951
PMID:30461697
Abstract

OBJECTIVE

We aimed to design and synthesize a new macromolecule for sentinel node detection to improve the imaging quality and avoid possible adverse effect.

BACKGROUND

The imaging of sentinel lymph node has been an important field in the nuclear medicine. A lot of imaging agents have been developed, including Tc-sulfer colloid, Tc-labeled dextrans and the latest Tc-DTPA-mannosyl-dextran. With the technology advanced, the imaging ability of the agents has been better and better. However, there are still some drawbacks.

MATERIALS AND METHODS

The new macromolecule agent was based on the dextran macromolecule backbone. Then the gly-gly-gly and mannose molecules were conjugated onto the backbone proportionally by targeting two different reaction sites. Once the new macromolecule was labelled with Tc, its imaging ability was tested by single-photon emission computed tomography scanning with Tc-sulfur colloid as the comparison.

RESULTS

The average numbers of gly-gyl-gyl and mannosyl groups on the dextran backbone are determined to be ∼1: 2 per dextran. The average molecular diameter and molecular weight are measured to be 5.4±0.7 nm and 10 324 g/mol, respectively. The macromolecule is labelled by Tc with 93.2±2.4% radiochemical yield. The lymphatic imaging by single-photon emission computed tomography with the labeled compound showed no worse imaging ability but cost less time than the commercially available Tc-sulfur colloid.

CONCLUSION

A new macromolecule imaging agent for sentinel node detection has been synthesized with better imaging ability and less imaging time cost.

摘要

目的

我们旨在设计并合成一种用于前哨淋巴结检测的新型大分子,以提高成像质量并避免可能的不良反应。

背景

前哨淋巴结成像一直是核医学中的一个重要领域。已经开发了许多成像剂,包括锝-硫胶体、锝标记的葡聚糖以及最新的锝-二乙三胺五乙酸-甘露糖基-葡聚糖。随着技术的进步,这些试剂的成像能力越来越好。然而,仍然存在一些缺点。

材料与方法

新型大分子试剂基于葡聚糖大分子骨架。然后通过靶向两个不同的反应位点,将甘氨酰-甘氨酰-甘氨酸和甘露糖分子按比例连接到骨架上。一旦用锝标记了新型大分子,就以锝-硫胶体作为对照,通过单光子发射计算机断层扫描来测试其成像能力。

结果

确定葡聚糖骨架上甘氨酰-甘氨酰-甘氨酸和甘露糖基的平均数量约为每个葡聚糖1:2。测得平均分子直径和分子量分别为5.4±0.7nm和10324g/mol。该大分子用锝标记,放射化学产率为93.2±2.4%。用标记化合物进行单光子发射计算机断层扫描的淋巴成像显示,其成像能力不低于市售的锝-硫胶体,但成像时间更短。

结论

已合成一种用于前哨淋巴结检测的新型大分子成像剂,具有更好的成像能力和更短的成像时间成本。

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