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通过三氯-s-三嗪将甲氨蝶呤与磁铁矿（Fe(3)O(4)）纳米颗粒偶联。

Conjugating Methotrexate to magnetite (Fe(3)O(4)) nanoparticles via trichloro-s-triazine.

作者信息

Young Kaylie L, Xu Chenjie, Xie Jin, Sun Shouheng

机构信息

Department of Chemistry, Brown University, Providence, Rhode Island, 02912, USA.

出版信息

J Mater Chem. 2009 Jan 1;19(35):6400-6406. doi: 10.1039/b902373a.

DOI:10.1039/b902373a
PMID:19915686
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2776745/
Abstract

Monodisperse Fe(3)O(4) nanoparticles (NPs) originally synthesized with a hydrophobic oleylamine capping ligand were made water soluble and conjugated to the anticancer drug Methotrexate (MTX) using a new chemistry based on the readily available linker trichloro-s-triazine (TsT). This new linker is much more versatile than those that currently exist for attaching biomolecules to magnetic NPs. The MTX-conjugated NPs were found to be stable under physiological conditions for over 72 hours and MTX was shown to maintain its anticancer activity after conjugation to the NP surface. Through cell viability studies and intracellular uptake studies, MTX-conjugated NPs were shown to have targeting specificity for a tumor cell line (9L rat glioma) over a healthy cell line (Cultured Pulmonary Artery Endothelial). Additionally the MTX-conjugated NPs were visualized inside 9L cells using fluorescence microscopy to help elucidate their path within a cell after internalization.

摘要

最初用疏水性油胺封端配体合成的单分散Fe(3)O(4)纳米颗粒（NPs）通过基于易于获得的连接体三氯-s-三嗪（TsT）的新化学方法制成水溶性，并与抗癌药物甲氨蝶呤（MTX）偶联。这种新的连接体比目前用于将生物分子连接到磁性纳米颗粒的连接体更具通用性。发现MTX偶联的纳米颗粒在生理条件下72小时以上保持稳定，并且MTX在与纳米颗粒表面偶联后仍保持其抗癌活性。通过细胞活力研究和细胞内摄取研究，MTX偶联的纳米颗粒对肿瘤细胞系（9L大鼠胶质瘤）显示出比对健康细胞系（培养的肺动脉内皮细胞）更高的靶向特异性。此外，使用荧光显微镜在9L细胞内观察到MTX偶联的纳米颗粒，以帮助阐明它们内化后在细胞内的路径。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72d9/2776745/9efd8a62204f/nihms142524f7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72d9/2776745/4f21319ea0fc/nihms142524f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72d9/2776745/4cf15d07f663/nihms142524f2.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72d9/2776745/be9110a8ffc6/nihms142524f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72d9/2776745/57aab344c82b/nihms142524f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72d9/2776745/28733ccf7843/nihms142524f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72d9/2776745/9efd8a62204f/nihms142524f7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72d9/2776745/4f21319ea0fc/nihms142524f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72d9/2776745/4cf15d07f663/nihms142524f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72d9/2776745/b664e73a7bc4/nihms142524f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72d9/2776745/be9110a8ffc6/nihms142524f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72d9/2776745/57aab344c82b/nihms142524f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72d9/2776745/28733ccf7843/nihms142524f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72d9/2776745/9efd8a62204f/nihms142524f7.jpg

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