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促黄体生成激素释放激素(LHRH)功能化聚(酰胺胺)树枝状大分子共轭物的合成、表征及稳定性

Synthesis, characterization and stability of a luteinizing hormone-releasing hormone (LHRH)-functionalized poly(amidoamine) dendrimer conjugate.

作者信息

Bi Xiangdong, Shi Xiangyang, Baker James R

机构信息

Department of Physical Sciences, Charleston Southern University, Charleston, SC 29406, USA.

出版信息

J Biomater Sci Polym Ed. 2008;19(1):131-42. doi: 10.1163/156856208783227686.

Abstract

Cancer targeting is crucial for cancer detection, therapy and targeted drug delivery. A dendrimer-peptide conjugate has been synthesized based on poly(amidoamine) dendrimer generation 5 (PAMAM G5) as a platform and a luteinizing hormone-releasing hormone (LHRH) peptide as a targeting moiety. The synthesized conjugate was fully characterized using nuclear magnetic resonance (NMR), UV-Vis spectrometry, reverse-phase high-performance liquid chromatography (RP-HPLC) and matrix-assisted laser desorption ionization-time of flight (MALDI-TOF) mass spectrometry. Further stability experiments showed that the synthesized conjugate was stable after 72-h incubation in phosphate-buffered saline (PBS) buffer (pH 7.4) at 37 degrees C. The synthesized conjugate may find applications in biomedical targeting, gene delivery and imaging.

摘要

癌症靶向对于癌症检测、治疗和靶向药物递送至关重要。基于第5代聚(酰胺胺)树枝状大分子(PAMAM G5)作为平台以及促黄体生成素释放激素(LHRH)肽作为靶向部分,合成了一种树枝状大分子 - 肽共轭物。使用核磁共振(NMR)、紫外 - 可见光谱法、反相高效液相色谱(RP - HPLC)和基质辅助激光解吸电离飞行时间(MALDI - TOF)质谱对合成的共轭物进行了全面表征。进一步的稳定性实验表明,合成的共轭物在37℃的磷酸盐缓冲盐水(PBS)缓冲液(pH 7.4)中孵育72小时后是稳定的。合成的共轭物可能在生物医学靶向、基因递送和成像方面找到应用。

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