Targeted tumour theranostics in mice via carbon quantum dots structurally mimicking large amino acids
Targeted tumour theranostics in mice via carbon quantum dots structurally mimicking large amino acids
复制标题
通过结构模仿大氨基酸的碳量子点对小鼠进行靶向肿瘤治疗诊断
DOI：
10.1038/s41551-020-0540-y
复制
发表时间：
2020-03-30
影响因子：
28.1
通讯作者：
Zhou, Jiangbing
中科院分区：
文献类型：
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作者：
Li, Shuhua;Su, Wen;Zhou, Jiangbing
选择性成像和向肿瘤递送药物的策略通常利用癌细胞上差异上调的表面分子。在这里，我们表明，静脉注射的碳量子点，功能化与多个配对的α-羧基和氨基结合的大中性氨基酸转运蛋白1（这是在大多数肿瘤中表达），选择性地积累在小鼠和原位小鼠模型的人类肿瘤异种移植物中的人类胶质瘤。功能化的量子点，其结构上模拟大的氨基酸，并可以通过π-π堆积相互作用负载芳香族药物，在没有可检测的毒性的情况下，能够实现肿瘤的近红外荧光和光声成像，并在将化疗药物靶向递送至肿瘤后减少肿瘤负荷。功能化的多功能性和高肿瘤选择性的量子点使它们广泛适用于肿瘤特异性成像和药物delivery. Intraperitoneal注射功能化的碳量子点，结合到大的中性氨基酸转运蛋白1和结构上模仿大的氨基酸选择性地积累在小鼠的人类肿瘤中，促进靶向治疗诊断。
Strategies for selectively imaging and delivering drugs to tumours typically leverage differentially upregulated surface molecules on cancer cells. Here, we show that intravenously injected carbon quantum dots, functionalized with multiple paired alpha-carboxyl and amino groups that bind to the large neutral amino acid transporter 1 (which is expressed in most tumours), selectively accumulate in human tumour xenografts in mice and in an orthotopic mouse model of human glioma. The functionalized quantum dots, which structurally mimic large amino acids and can be loaded with aromatic drugs through pi-pi stacking interactions, enabled-in the absence of detectable toxicity-near-infrared fluorescence and photoacoustic imaging of the tumours and a reduction in tumour burden after the targeted delivery of chemotherapeutics to the tumours. The versatility of functionalization and high tumour selectivity of the quantum dots make them broadly suitable for tumour-specific imaging and drug delivery.Intravenously injected functionalized carbon quantum dots that bind to the large neutral amino acid transporter 1 and that structurally mimic large amino acids selectively accumulate in human tumours in mice, facilitating targeted theranostics.