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

文獻(xiàn)鏈接：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：

利用配體與受體的特異性結(jié)合作為靶向策略，促進(jìn)藥物脂質(zhì)體在*癥組織中的積累。葉酸受體已被發(fā)現(xiàn)在侵襲性乳腺*癥細(xì)胞上過表達(dá)。本研究合成了三種葉酸類似物-脂質(zhì)偶聯(lián)物，并將其作為葉酸受體的靶向配體，用于修飾藥物脂質(zhì)體，以提高侵襲性乳腺*癥的治療效果。

方法：選擇三種葉酸類似物，氨基蝶呤、培美曲塞和拉替曲塞作為靶向分子，并與N-羥基琥珀酰亞胺基-聚乙二醇二硬脂酰-磷脂酰乙醇胺（DSPE-PEG2000-NHS）偶聯(lián)。通過基質(zhì)輔助激光解吸/電離飛行時(shí)間質(zhì)譜（MALDI-TOF-MS）證實(shí)了合成的偶聯(lián)物。

隨后，通過將這些靶向偶聯(lián)物分別摻入脂質(zhì)體表面，開發(fā)了納米結(jié)構(gòu)靶向脂質(zhì)體。

相關(guān)推薦產(chǎn)品：

DSPE-PEG-NBD

DSPE-PEG-TRITC

DSPE-PEG-Comarin

DSPE-PEG-ICG

DSPE-PEG-Pyrene

DSPE-PEG-Ce6

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