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Single-crystal structure and intracellular localization of Zn(II)-thiosemicarbazone complex targeting mitochondrial apoptosis pathways.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-06-09 , DOI: 10.1016/j.bmcl.2020.127340
Jinxu Qi 1 , Wei Zhao 1 , Yunyun Zheng 1 , Ruiya Wang 1 , Qiu Chen 1 , Fu-An Wang 1 , Weiwei Fan 1 , Huashan Gao 1 , Xichao Xia 1
Affiliation  

Tracking of drugs in cancer cells is important for basic biology research and therapeutic applications. Therefore, we designed and synthesised a Zn(II)-thiosemicarbazone complex with photoluminescent property for organelle-specific imaging and anti-cancer proliferation. The Zn(AP44eT)(NO3)2 coordination ratio of metal to ligand was 1:1, which was remarkably superior to 2-((3-aminopyridin-2-yl) methylene)-N, N-diethylhydrazinecarbothioamide (AP44eT·HCl) in many aspects, such as fluorescence and anti-tumour activity. Confocal fluorescence imaging showed that the Zn(AP44eT)(NO3)2 was aggregated in mitochondria. Moreover, Zn(AP44eT)(NO3)2 was more effective than the metal-free AP44eT·HCl in shortening the G2 phase in the MCF-7 cell cycle and promoting apoptosis of cancer cells. Supposedly, the effects of these complexes might be located mainly in the mitochondria and activated caspase-3 and 9 proteins.



中文翻译:

靶向线粒体凋亡途径的Zn(II)-thiosemicarbazone复合物的单晶结构和细胞内定位。

追踪癌细胞中的药物对于基础生物学研究和治疗应用非常重要。因此,我们设计并合成了具有光致发光特性的Zn(II)-硫代半碳酸盐配合物,用于细胞器特异性成像和抗癌增殖。金属与配体的Zn(AP44eT)(NO 32配位比为1:1,明显优于2-((3-氨基吡啶-2-基)亚甲基)-N,N-二乙基肼碳硫代酰胺(AP44eT·HCl) ),例如荧光和抗肿瘤活性。共聚焦荧光成像表明,Zn(AP44eT)(NO 32聚集在线粒体中。此外,Zn(AP44eT)(NO 32在缩短MCF-7细胞周期中的G2期和促进癌细胞凋亡方面,它比无金属AP44eT·HCl更有效。据推测,这些复合物的作用可能主要位于线粒体和激活的caspase-3和9蛋白中。

更新日期:2020-06-09
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