Conjugation with α-linolenic acid improves cancer cell uptake and cytotoxicity of doxorubicin

The synthetic DOX–LNA conjugate was characterized by proton nuclear magnetic resonance and mass spectrometry. In addition, the purity of the conjugate was analyzed by reverse-phase high-performance liquid chromatography. The cellular uptake, intracellular distribution, and cytotoxicity of DOX–LNA were assessed by flow cytometry, fluorescence microscopy, liquid chromatography/electrospray ionization tandem mass spectrometry, and the tetrazolium dye assay using the in vitro cell models. The DOX–LNA conjugate showed substantially higher tumor-specific cytotoxicity compared with DOX.

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