Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, TN 38105, USA.
Biomaterials. 2011 Apr;32(10):2540-5. doi: 10.1016/j.biomaterials.2010.12.031. Epub 2011 Jan 12.
A dual-ligand gold nanoparticle (DLGNP) was designed and synthesized to explore the therapeutic benefits of multivalent interactions between gold nanoparticles (GNPs) and cancer cells. DLGNP was tested on human epidermal cancer cells (KB), which had high expression of folate receptor. The cellular uptake of DLGNP was increased by 3.9 and 12.7 folds compared with GNP-folate or GNP-glucose. The enhanced cell recognition was due to multivalent interactions between both ligands on GNPs and cancer cells as shown by the ligand competition experiments. Furthermore, the multivalent interactions increased contrast between cells with high and low expression of folate receptors. The enhanced cell recognition enabled DLGNP to kill KB cells under X-ray irradiation at a dose that was safe to folate receptor low-expression (such as normal) cells. Thus DLGNP has the potential to be a cancer-specific nano-theranostic agent.
设计并合成了一种双配体金纳米粒子(DLGNP),以探索金纳米粒子(GNPs)与癌细胞之间多价相互作用的治疗益处。在人表皮癌细胞(KB)上测试了 DLGNP,该细胞高表达叶酸受体。与 GNP-叶酸或 GNP-葡萄糖相比,DLGNP 的细胞摄取量分别增加了 3.9 倍和 12.7 倍。通过配体竞争实验表明,这是由于 GNPs 上的两种配体与癌细胞之间的多价相互作用所致。此外,多价相互作用增加了高表达和低表达叶酸受体的细胞之间的对比度。增强的细胞识别使 DLGNP 能够在 X 射线照射下杀死 KB 细胞,而 X 射线照射的剂量对低表达叶酸受体(如正常)细胞是安全的。因此,DLGNP 有可能成为一种针对癌症的纳米治疗剂。