Key Laboratory of Natural Medicine and Immune Engineering of Henan Province, Henan University, Kaifeng, China.
Chem Biol Drug Des. 2018 Jan;91(1):285-293. doi: 10.1111/cbdd.13080. Epub 2017 Aug 31.
The modified quantum dots (QDs) have been used in intracellular probing and drug delivery because of their special chemical and physical properties. In this paper, two β-cyclodextrin (β-CD)-modified CdSe/ZnS QDs with strong optical emission properties were synthesized as drug carriers to induce apoptosis. The positively charged l-Arginine (l-Arg) and neutral l-Tryptophan (l-Trp) were selected as ligands to compare the effect of charge on bioactivity of QDs nanoparticles. The in vitro assays revealed that these modified QDs showed good Dox carrier ability and significantly high inhibition rate to cancer cells. Especially, the more positively charged β-CD-l-Arg-polyamine-coated CdSe/ZnS QDs could effectively deliver the doxorubicin (Dox) into cells and exhibit excellent cell selectivity in cancer versus normal cells. The Dox-loaded QDs could enter intracellular, which showed that the Dox can efficiently go through the membranes at the existence of β-CD. Several lines of evidence suggest that the Dox-loaded QDs can efficiently induce apoptosis likely related to the production of ROS. We expect that the modified QDs can enhance the amount of hydrophobic antitumor drugs in cells and can also be used as fluorescent imaging agents.
经过修饰的量子点（QDs）具有特殊的化学和物理性质，因此被用于细胞内探测和药物输送。本文合成了两种具有强光学发射特性的β-环糊精（β-CD）修饰的 CdSe/ZnS QDs 作为药物载体来诱导细胞凋亡。选择带正电荷的 l-精氨酸（l-Arg）和不带电荷的 l-色氨酸（l-Trp）作为配体，比较了电荷对 QDs 纳米颗粒生物活性的影响。体外实验表明，这些修饰的 QDs 具有良好的载药能力，并对癌细胞具有显著的高抑制率。特别是带更多正电荷的β-CD-l-Arg-聚胺修饰的 CdSe/ZnS QDs 能够有效地将阿霉素（Dox）递送到细胞内，并在癌细胞与正常细胞之间表现出优异的细胞选择性。载有 Dox 的 QDs 可以进入细胞内，这表明 Dox 可以在β-CD 的存在下有效地穿过细胞膜。有几条证据表明，载有 Dox 的 QDs 可以有效地诱导细胞凋亡，这可能与 ROS 的产生有关。我们期望修饰后的 QDs 能够增加细胞内疏水性抗肿瘤药物的含量，并可用作荧光成像剂。
