文献：Synthesis and evaluations of three folate analogue-lipid conjugates as the targeting materials for treatment of invasive breast cancer

文献链接：https://xueshu.baidu.com/usercenter/paper/show?paperid=124c0t30bt340ps01e5106r0c8030546&site=xueshu_se

作者：Rui-Jun，Ju，Wan-Liang，Lu

摘要：

Objective:Specific binding between ligand and receptor is used as a targeting strategy to enhance the accumulation of drug-loaded liposomes in the cancer tissues.Folate receptor has been found to be overexpressed on invasive breast cancer cells.In the present study,three kinds of folate analogue-lipid conjugates were synthetized and evaluated as the targeting ligands of folate receptor for modifying drug-toaded liposomes to improve the efficacy in treatment of invasive breast cancer.Methods:Three folate analogues,aminopterin,pemetrexed and raltitrexed,were selected as the targeting molecules and were conjugated with N-hydroxysuccinimidyl-polyethylene glycol distearoylphosphatidyl ethanolamine(DSPE-PEG2000-NHS).The synthesized conjugates were confirmed by a matrix-assisted laser desorption/ionization time of flight mass spectrometry(MALDI-TOF-MS).Nanostructured targeting liposomes were subsequently developed by incorporating these targeting conjugates onto the surface of liposomes,respectively.

目的：

利用配体与受体的特异性结合作为靶向策略，促进药物脂质体在*症组织中的积累。叶酸受体已被发现在侵袭性乳腺*症细胞上过表达。本研究合成了三种叶酸类似物-脂质偶联物，并将其作为叶酸受体的靶向配体，用于修饰药物脂质体，以提高侵袭性乳腺*症的治疗效果。

方法：选择三种叶酸类似物，氨基蝶呤、培美曲塞和拉替曲塞作为靶向分子，并与N-羟基琥珀酰亚胺基-聚乙二醇二硬脂酰-磷脂酰乙醇胺（DSPE-PEG2000-NHS）偶联。通过基质辅助激光解吸/电离飞行时间质谱（MALDI-TOF-MS）证实了合成的偶联物。

随后，通过将这些靶向偶联物分别掺入脂质体表面，开发了纳米结构靶向脂质体。

相关推荐产品：

DSPE-PEG-NBD

DSPE-PEG-TRITC

DSPE-PEG-Comarin

DSPE-PEG-ICG

DSPE-PEG-Pyrene

DSPE-PEG-Ce6

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