靶向MC1R的NIR-Ⅱ聚集诱导发射纳米颗粒用于黑色素瘤成像  

MC1R-targeted NIR-Ⅱ aggregation-induced emission nanoparticles for melanoma imaging

作　　者：刘昭颖 裴书锐 温凯凯 彭爱东 马寒 黄辉 Zhaoying Liu;Shurui Pei;Kaikai Wen;Aidong Peng;Han Ma;Hui Huang(Department of Dermatology,Fifth Affiliated Hospital of Sun Yat-sen University,Zhuhai 519000,China;Materials Science and Optoelectronics Engineering,CAS Center for Excellence in Topological Quantum Computation,CAS Key Laboratory of Vacuum Physics,University of Chinese Academy of Sciences,Beijing 100049,China)

机构地区：[1]Department of Dermatology,Fifth Affiliated Hospital of Sun Yat-sen University,Zhuhai 519000,China [2]Materials Science and Optoelectronics Engineering,CAS Center for Excellence in Topological Quantum Computation,CAS Key Laboratory of Vacuum Physics,University of Chinese Academy of Sciences,Beijing 100049,China

出　　处：《Science China Materials》2023年第10期4100-4108,共9页中国科学（材料科学（英文版）

基　　金：supported by Beijing Natural Science Foundation(Z210017);the National Natural Science Foundation of China(21774130 and 51925306);the Science and Technology Innovation Commission of Shenzhen(JCYJ20220530150604009)。

摘　　要：恶性黑色素瘤是最致命的皮肤癌,因此,早期诊断对提高生存率至关重要.黑色素皮质素-1受体(MC1R)在黑色素瘤细胞中过度表达,被认为是黑色素瘤检测的分子靶标.在本工作中,我们基于具有近红外二区(NIR-Ⅱ)发射的聚集诱导发光源TPE-BBT开发了一种新的MC1R靶向荧光探针,命名为MSH-TPE-BBT NPs,并评估了其在黑色素瘤体内成像的潜力.MSH-TPE-BBT NPs具有显著的组织穿透性、光稳定性和生物安全性,并在人类黑色素瘤细胞及其小鼠体内异种移植肿瘤中表现出特异性靶向特性.MSH-TPE-BBT NPs在黑色素瘤小鼠体内成像的成功应用及其良好的生物相容性表明其作为靶向MC1R的黑色素瘤成像探针具有临床应用潜力.Malignant melanoma is the most lethal form of skin cancer for human beings.Thus,developing melanomatargeted fluorescent probes for early diagnosis is important to increase the survival rates.Here,a novel melanocortin-1 receptor-targeted fluorescent probe named melanocyte-stimulating hormone(MSH)-tetraphenylethene(TPE)-benzobisthiadiazole(BBT)nanoparticles(NPs),based on the aggregation-induced emission luminogen(AIEgen)(TPEBBT)with second near-infrared(NIR-Ⅱ)emission was developed for in vivo imaging of melanoma.MSH-TPE-BBT NPs exhibit significant tissue penetration,photostability,biosafety,and specific targeting properties in human melanoma cells and xenograft tumors of human melanoma cells in mice.These findings revealed that these NPs could be an excellent nano-platform for early diagnosis of melanoma.

关 键 词：MELANOMA melanocortin-1 receptor nanoparticles aggregation-induced emission second near-infrared imaging 

分 类 号：O657.3[理学—分析化学] R739.5[理学—化学] TB383.1[医药卫生—肿瘤]