Conjugating an anticancer drug of high biological efficacy but large cytotoxicity with a “transporting” molecule of low toxicity constitutes a valuable approach to design safe drug delivery system. In the present study, doxorubicin (DOX) a drug of large cardiotoxicity was chemically conjugated to a C60-fullerene. The synthesized molecule, a fullerene-doxorubicin conjugate (Ful-DOX), was characterized using the 1H NMR and MALDI TOF mass spectrometry. The absorption and fluorescence spectra and dynamic light scattering of the conjugate were recorded in an aqueous solution, while the impact on viability of several cancer cell lines of the free DOX and the conjugate was compared using the SRB and WST-1 assays. A low antiproliferative activity of the conjugate as compared to the free DOX is a consequence of the presence of fullerene moiety in the former, which is also responsible for the conjugate aggregation in an aqueous solution. Unlike free DOX, these aggregates cannot pass through the nuclear membrane (as demonstrated by the confocal microscopy measurements), which makes them marginally cytotoxic.

中文翻译：

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与 C60 富勒烯结合的阿霉素的细胞毒性。结构和体外研究

将生物药效高但细胞毒性大的抗癌药物与低毒的“运输”分子结合，是设计安全给药系统的重要途径。在本研究中，多柔比星 (DOX) 是一种具有大心脏毒性的药物，与 C60-富勒烯进行化学偶联。合成的分子，富勒烯-阿霉素缀合物 (Ful-DOX)，使用 1 H NMR 和 MALDI TOF 质谱法进行表征。结合物的吸收和荧光光谱以及动态光散射在水溶液中记录，同时使用 SRB 和 WST-1 测定比较游离 DOX 和结合物对几种癌细胞系活力的影响。与游离 DOX 相比，缀合物的低抗增殖活性是前者中富勒烯部分存在的结果，这也是水溶液中缀合物聚集的原因。与游离 DOX 不同，这些聚集体不能穿过核膜（如共聚焦显微镜测量所示），这使得它们具有轻微的细胞毒性。