Hydrogen peroxide is one of the most important reactive oxygen species, which plays a vital role in many physiological and pathological processes. A dramatic increase in H2O2 levels is a prominent feature of cancer. Therefore, rapid and sensitive detection of H2O2 in vivo is quite conducive to an early cancer diagnosis. On the other hand, the therapeutic potential of estrogen receptor beta (ERβ) has been implicated in many diseases including prostate cancer, and this target has attracted intensive attention recently. In this work, we report the development of the first H2O2-triggered ERβ-targeted near-infrared fluorescence (NIR) probe and its application in imaging of prostate cancer both in vitro and in vivo. The probe showed good ERβ selective binding affinity, excellent H2O2 responsiveness and near infrared imaging potential. Moreover, in vivo and ex vivo imaging studies indicated that the probe could selectively bind to DU-145 prostate cancer cells and rapidly visualizes H2O2 in DU-145 xenograft tumors. Mechanistic studies such as high-resolution mass spectrometry (HRMS) and density functional theory (DFT) calculations indicated that the borate ester group is vital for the H2O2 response turn-on fluorescence of the probe. Therefore, this probe might be a promising imaging tool for monitoring the H2O2 levels and early diagnosis studies in prostate cancer research.

中文翻译：

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开发由内源性过氧化氢触发的高效雌激素受体 β 靶向近红外荧光探针，用于前列腺癌的诊断成像。

过氧化氢是最重要的活性氧之一，在许多生理和病理过程中起着至关重要的作用。H2O2 水平的急剧增加是癌症的显着特征。因此，快速、灵敏地检测体内H2O2有利于癌症的早期诊断。另一方面，雌激素受体β（ERβ）的治疗潜力与包括前列腺癌在内的许多疾病有关，该靶点最近引起了广泛关注。在这项工作中，我们报告了第一个 H2O2 触发的 ERβ 靶向近红外荧光 (NIR) 探针的开发及其在体外和体内前列腺癌成像中的应用。该探针显示出良好的 ERβ 选择性结合亲和力、出色的 H2O2 响应性和近红外成像潜力。而且，体内和离体成像研究表明，该探针可以选择性地结合 DU-145 前列腺癌细胞，并快速可视化 DU-145 异种移植肿瘤中的 H2O2。高分辨率质谱 (HRMS) 和密度泛函理论 (DFT) 计算等机理研究表明，硼酸酯基团对于探针的 H2O2 响应开启荧光至关重要。因此，该探针可能是一种很有前途的成像工具，用于监测前列腺癌研究中的 H2O2 水平和早期诊断研究。高分辨率质谱 (HRMS) 和密度泛函理论 (DFT) 计算等机理研究表明，硼酸酯基团对于探针的 H2O2 响应开启荧光至关重要。因此，该探针可能是一种很有前途的成像工具，用于监测前列腺癌研究中的 H2O2 水平和早期诊断研究。高分辨率质谱 (HRMS) 和密度泛函理论 (DFT) 计算等机理研究表明，硼酸酯基团对于探针的 H2O2 响应开启荧光至关重要。因此，该探针可能是一种很有前途的成像工具，用于监测前列腺癌研究中的 H2O2 水平和早期诊断研究。