Lipid droplets (LDs) targeted fluorescence probe have been believed to be an effective tool for diagnosis and therapy of some tumors with abnormal lipid metabolism, while there are very few probes with simultaneous high efficiency in LDs imaging and inhibiting tumor proliferation. Herein we present a biheteroaryl-bridged fluorescence probe with aggregation-induced emission (AIE) characteristic, which show dual functions of LDs-specific bioimaging and photodynamic therapy (PDT) based on human clear cell renal cell carcinoma (ccRCC) tumor cells and clinical samples, both rich in LDs. The highly LDs-specific targeting capability, good biocompatibility, excellent photostability and imaging resolution of the AIE probe in ccRCC tumor cells make it considerably attractive to commercially available LDs-specific dyes. Notably, the fluorescence imaging in fresh human ccRCC tumor tissues further proves its outstanding LDs-targeting specificity and demonstrates its power as a bio-probe for clinical diagnosis in vitro and in vivo. Confirmatory experiments suggest a superior PDT efficacy of the AIE probe in ccRCC tumor cells in comparison to those LDs-poor tumor cells and normal cells without LDs. Mechanism studies further reveal the presented AIE probe enables to induce the DNA damage and cell apoptosis by reactive oxygen species generation, resulting in desirable therapeutic efficiency for clinical ccRCC tumor cells upon visible light irradiation.

人们认为，以脂质液滴（LDs）为目标的荧光探针是诊断和治疗某些脂质代谢异常的肿瘤的有效工具，而在LDs成像和抑制肿瘤增殖的同时具有极高效率的探针却很少。本文中，我们介绍了一种具有聚集诱导发射（AIE）特征的双杂芳基桥联荧光探针，该探针显示了基于人类透明细胞肾细胞癌（ccRCC）肿瘤细胞和临床样品的LDs特异性生物成像和光动力疗法（PDT）的双重功能，两者都有丰富的LD。ccRCC肿瘤细胞中AIE探针的高度LDs特异性靶向能力，良好的生物相容性，出色的光稳定性和成像分辨率，使其对市售LDs特异性染料具有相当大的吸引力。尤其，体外和体内。验证性实验表明，与那些LDs贫乏的肿瘤细胞和不含LDs的正常细胞相比，AIE探针在ccRCC肿瘤细胞中具有更好的PDT功效。机理研究进一步揭示，提出的AIE探针能够通过活性氧的产生诱导DNA损伤和细胞凋亡，从而在可见光照射下对临床ccRCC肿瘤细胞产生理想的治疗效率。