Early detection and accurate diagnosis are essential for the effective prevention and treatment of tumors. Optical imaging methods can provide real-time and high-resolution in vivo images for tumor diagnostic applications. Pro-Leu-His-Ser-Thr(PO3H2) (PLHSpT) is an inhibitor of polo-like kinase 1, which is overexpressed in various tumors, and the transactivator of transcription (TAT) is a peptide known to penetrate tumor cells. In this study, we used a fragment of the TAT sequence, YARVRRRGPRR, to produce a YARVRRRGPRR-conjugated PLHSpT peptide using solid-phase peptide synthesis. Subsequently, the cyanine 5 NHS ester (Cy5) fluorescent dye was attached to YARVRRRGPRRPLHSpT (1) to obtain the Cy5-YARVRRRGPRRPLHSpT peptide (2), which was used to identify tumor targets through optical imaging. 2 was injected into HeLa xenograft tumor-bearing mice. After in vivo imaging at 3 h, 6 h, and 24 h post-injection, mice were sacrificed for ex vivo fluorescence intensity assessment. Optical imaging scans of 2 revealed significantly high uptake by tumor cells at all in vivo scan times. The highest fluorescence intensity difference between tumor and muscles was observed at 6 h. Ex vivo results also showed a high variation in the tumor-to-muscle uptake ratios at 6 h. In conclusion, we synthesized and evaluated 2 for cancer diagnosis in mice. Our optical imaging results demonstrated that 2 has remarkable cancer-detection ability in vivo, establishing this peptide as a potential imaging probe for tumor diagnosis.

中文翻译：

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用于体内肿瘤成像的 polo 样激酶 1 的 TAT 偶联肽抑制剂

早期发现和准确诊断对于有效预防和治疗肿瘤至关重要。光学成像方法可以为肿瘤诊断应用提供实时和高分辨率的体内图像。Pro-Leu-His-Ser-Thr(PO3H2) (PLHSpT) 是 polo 样激酶 1 的抑制剂，它在各种肿瘤中过表达，转录反式激活因子 (TAT) 是一种已知可穿透肿瘤细胞的肽。在本研究中，我们使用 TAT 序列的一个片段 YARVRRRGPRR，通过固相肽合成来生产 YARVRRRGPRR 缀合的 PLHSpT 肽。随后，将花青5 NHS酯（Cy5）荧光染料附着在YARVRRRGPRRPLHSpT（1）上，得到Cy5-YARVRRRGPRRPLHSpT肽（2），用于通过光学成像识别肿瘤靶点。2 被注射到 HeLa 异种移植瘤荷瘤小鼠中。在注射后 3 小时、6 小时和 24 小时进行体内成像后，处死小鼠进行体外荧光强度评估。2 的光学成像扫描显示在所有 体内 扫描时间肿瘤细胞的吸收显着高。在 6 小时观察到肿瘤和肌肉之间的最高荧光强度差异。离体结果还显示 6 小时时肿瘤与肌肉摄取比率的高度变化。总之，我们合成并评估了 2 种用于小鼠癌症诊断。我们的光学成像结果表明，2 具有显着的体内癌症检测能力，确立了该肽作为肿瘤诊断的潜在成像探针。2 的光学成像扫描显示在所有 体内 扫描时间肿瘤细胞的吸收显着高。在 6 小时观察到肿瘤和肌肉之间的最高荧光强度差异。离体结果还显示 6 小时时肿瘤与肌肉摄取比率的高度变化。总之，我们合成并评估了 2 种用于小鼠癌症诊断。我们的光学成像结果表明，2 在体内具有显着的癌症检测能力，确立了该肽作为肿瘤诊断的潜在成像探针。2 的光学成像扫描显示在所有 体内 扫描时间肿瘤细胞的吸收显着高。在 6 小时观察到肿瘤和肌肉之间的最高荧光强度差异。离体结果还显示 6 小时时肿瘤与肌肉摄取比率的高度变化。总之，我们合成并评估了 2 种用于小鼠癌症诊断。我们的光学成像结果表明，2 在体内具有显着的癌症检测能力，确立了该肽作为肿瘤诊断的潜在成像探针。