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A selective and sensitive near-infrared fluorescent probe for in vivo real time tracking of exogenous and metabolized hydrazine, a genotoxic impurity
Journal of Materials Chemistry B ( IF 6.1 ) Pub Date : 2020-10-04 , DOI: 10.1039/d0tb02063j
Shun Wang 1, 2, 3, 4 , Jian Liu 1, 2, 3, 4 , Linjiang Song 4, 5, 6, 7 , Qingrong Qi 2, 4, 8, 9 , Zicheng Li 1, 2, 3, 4 , Wencai Huang 1, 2, 3, 4
Affiliation  

Hydrazine is a well-known genotoxic impurity which may be present in some important drugs, such as isoniazid and hydralazine. It may be ingested along with the drug or generated as a metabolite in the human body. Hence, monitoring the level of hydrazine in the human body is of great importance. A hemicyanine-based NIR fluorescent probe, Hcy-DB, was designed and synthesized for hydrazine detection. This probe exhibited a dramatic off–on NIR fluorescence response toward hydrazine in PBS–DMSO buffer and the detection limit was calculated to be 4.38 ppb. The bioimaging of hydrazine in living H1975 cells was successfully demonstrated. Moreover, the real time imaging of hydrazine, either injected as a foreign agent or generated as a metabolite of isoniazid, was demonstrated in mice and the results clearly disclosed the hydrazine level variation in the liver and kidneys. The injected exogenous hydrazine was mainly distributed in the kidneys and then excreted slowly. After the intragastric administration of isoniazid, hydrazine was quickly generated as a metabolite in the liver and reached a maximum in about 20 min, and then it was excreted slowly through the kidneys. Generally, the investigation provided a promising tool to monitor the level of hydrazine in vivo and thus help to evaluate and control its toxicity more rationally.

中文翻译:

一种选择性和灵敏的近红外荧光探针,用于体内实时跟踪外源和代谢的肼(一种遗传毒性杂质)

肼是众所周知的遗传毒性杂质,可能存在于一些重要的药物中,例如异烟肼和肼苯哒嗪。它可能与药物一起摄入或在人体中以代谢产物形式产生。因此,监测人体中肼的水平非常重要。基于半花菁的NIR荧光探针Hcy-DB被设计和合成用于肼的检测。该探针在PBS-DMSO缓冲液中对肼具有显着的近红外荧光响应,计算的检出限为4.38 ppb。成功地证明了H1975活细胞中肼的生物成像。此外,在小鼠中显示了作为外来剂注射或作为异烟肼代谢物生成的肼的实时成像,结果清楚地揭示了肝脏和肾脏中肼的水平变化。注射的外源肼主要分布在肾脏中,然后缓慢排泄。胃内注射异烟肼后,肼在肝脏中快速生成为代谢产物,并在约20分钟内达到最大值,然后通过肾脏缓慢排泄。通常,体内,从而有助于更合理地评估和控制其毒性。
更新日期:2020-11-03
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