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首页> 外文期刊>Journal of Materials Chemistry, B. materials for biology and medicine >Selenadiazole derivatives as theranostic agents for simultaneous cancer chemo-/radiotherapy by targeting thioredoxin reductase
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Selenadiazole derivatives as theranostic agents for simultaneous cancer chemo-/radiotherapy by targeting thioredoxin reductase

机译：硒代唑衍生物作为治疗剂，用于通过靶向硫氧嗪还原酶同时癌症化学/放射疗法

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摘要

The lack of early and timely diagnosis of tumors and the monitoring of their response to therapeutics have limited the successful cancer treatments. Theranostic agents are expected to realize the dual-purpose of simultaneous diagnosis and therapy for treatments of cancers. In the present study, we have examined the effects of the chemical structure of selenadiazole derivatives (SeDs) on their anticancer efficacy and radio-sensitization against clinically used X-rays. The results showed that the introduction of a nitro group (-NO2) into SeD-3 significantly enhanced the anticancer activity of SeDs. The higher lipophilicity endowed SeD-3 with higher cellular internalization ability, resulting in higher cellular uptake and anticancer efficacy. Specifically, the capacity of autofluorescence allowed the use of SeD-3 as a promising theranostic agent to directly monitor the cellular uptake, localization and biodistribution in vitro and in vivo. Interestingly, SeD-3 also significantly enhanced the sensitivity of HeLa cervical cells to X-ray-induced apoptosis by targeting the inhibition of TrxR and promoting intracellular ROS overproduction, which activated the downstream ROS-mediated signaling pathways to regulate cell apoptosis. Furthermore, SeD-3 exhibited satisfactory in vivo antitumor efficacy through the inhibition of tumor proliferation and induction of tumor cell apoptosis, and showed no toxicity to the main organs. Moreover, from the results of hematological analysis, we found that not only inhibiting the tumor growth, treatment of SeD-3 also alleviated the damage of liver, kidney and heart function of nude mice induced by HeLa xenografts. Taken together, this study demonstrates that SeDs could be further developed as an effective and safe theranostic agent for simultaneous cancer chemo-/radiotherapy.
机译：缺乏早期和及时​​诊断肿瘤以及监测对治疗剂的反应有限于成功的癌症治疗方法。预计治疗剂将实现同时诊断和治疗癌症治疗的两用目的。在本研究中，我们研究了Selenadiazole衍生物（SED）的化学结构对临床使用的X射线的抗癌疗效和无线电致敏的影响。结果表明，将硝基群（-NO2）引入SED-3显着增强了SED的抗癌活动。更高的亲脂性赋予SED-3，细胞内化能力较高，导致细胞摄取和抗癌效果更高。具体地，自发荧光的能力允许使用SED-3作为有前途的治疗剂，以直接监测体外和体内体外细胞吸收，定位和生物分布。有趣的是，SED-3还通过靶向TRXR的抑制和促进细胞内ROS过量生产来显着提高HELA宫颈细胞对X射线诱导的细胞凋亡的敏感性，其激活下游ROS介导的信号传导途径来调节细胞凋亡。此外，SED-3通过抑制肿瘤增殖和肿瘤细胞凋亡诱导，对体内抗肿瘤功效表现出令人满意的，对主器官没有毒性。此外，从血液学分析的结果，我们发现不仅抑制肿瘤生长，SED-3的治疗也缓解了Hela异种移植物诱导的裸鼠肝，肾和心脏功能的损害。这项研究表明，可以进一步开发出SEDS作为同时癌症化学/放射治疗的有效和安全的治疗剂。

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