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首页> 外文期刊>Journal of drug targeting >Methotrexate-conjugated quantum dots: synthesis, characterisation and cytotoxicity in drug resistant cancer cells
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Methotrexate-conjugated quantum dots: synthesis, characterisation and cytotoxicity in drug resistant cancer cells

机译：甲氨蝶呤 - 共轭量子点：耐药性癌细胞中的合成，表征和细胞毒性

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Methotrexate (MTX), a folic acid derivative, is a potent anticancer used for treatment of different malignancies, but possible initiation of drug resistance to MTX by cancer cells has limited its applications. Nanoconjugates (NCs) of MTX to quantum dots (QDs) may favour the cellular uptake via folate receptors (FRs)-mediated endocytosis that circumvents the efflux functions of cancer cells. We synthesised MTX-conjugated l-cysteine capped CdSe QDs (MTX-QD nanoconjugates) and evaluated their internalisation and cytotoxicity in the KB cells with/without resistancy to MTX. The NCs were fully characterised by high resolution transmission electron microscopy (HR-TEM), atomic force microscopy (AFM), dynamic light scattering (DLS) and optical spectroscopy. Upon conjugation with MTX, the photoluminescence (PL) properties of QDs altered, while an obvious quenching in PL of QDs was observed after physical mixing. The MTX-QD nanoconjugates efficiently internalised into the cancer cells, and induced markedly high cytotoxicity (IC50, 12.0 mu g/mL) in the MTX-resistant KB cells as compared to the free MTX molecules (IC50,105.0 mu g/mL), whereas, these values were respectively about 7.0 and 0.6 mu g/mL in the MTX-sensitive KB cells. Based on these findings, the MTX-QD nanoconjugates are proposed for the targeted therapy of MTX-resistant cancers, which may provide an improved outcome in the relapsed FR-overexpressing cancers.
机译：甲氨蝶呤（MTX）是一种叶酸衍生物，是一种用于治疗不同恶性肿瘤的强累性，但是通过癌细胞对MTX的耐药性起始的可能性限制了其应用。 MTX对量子点（QDS）的纳米缀合物（NCS）可以通过叶酸受体（FRS）介导的内吞作用来抑制癌细胞的缺血功能的植物膜受试者。我们合成MTX缀合的L-半胱氨酸封端CDSE QDS（MTX-QD纳米缀合物），并在KB细胞中评价其内化和细胞毒性，用/不具有MTX的阻力。通过高分辨率透射电子显微镜（HR-TEM），原子力显微镜（AFM），动态光散射（DLS）和光学光谱，NCS完全表征。在与MTX缀合时，QD的光致发光（PL）特性改变，而在物理混合后观察到QD的PL中的明显猝灭。与游离MTX分子相比然而，在MTX敏感的KB细胞中，这些值分别为约7.0和0.6μg/ ml。基于这些发现，提出了MTX-QD纳米缀合物用于抗MTX抗性癌症的靶向治疗，其可以在复发的FR过表达癌症中提供改善的结果。

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