期刊
JOURNAL OF INORGANIC BIOCHEMISTRY
卷 166, 期 -, 页码 108-121出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.jinorgbio.2016.11.009
关键词
Apoptosis; Alkynyl gold(I); Thioredoxin reductase; Redox; Cytochrome c; Caco-2 cells
资金
- Ministry of Science and Innovation (FEDER) [CTQ2013-48635-C2-1-P, SAF2013-41651-R]
- Aragon Regional Government [E104]
- Instituto de Salud Carlos III [CB06/03/1012]
The alkynyl gold(l) derivative [Au(CE CPh)(PTA)] (PTA = 1,3,5-triaza-7-phosphaadamantane) induces apoptosis in colorectal carcinoma tumour cells (Caco-2) without affecting to normal enterocytes. [Au(CE CPh)(PTA)] is a slight lipophilic drug, stable in PBS (Phosphate Buffered Saline) and able to bind BSA (Bovin Serum Albumin) by hydrophobic interactions. Once inside the cell, [Au(CE CPh)(PTA)] targets seleno proteins such as Thioredoxin Reductase 1, increasing ROS (Reactive Oxygen Species) levels, reducing cell viability and proliferation and inducing mitochondrial apoptotic pathway, pro-apoptotic and anti-apoptotic protein imbalance, loss of mitochondrial membrane potential, cytochrome c release and activation of caspases 9 and 3. Moreover, unlike other metal based drugs such as cisplatin, [Au(CE CPh)(PTA)] does not target nucleic acid, reducing the risk of side mutation in the DNA. In consequence, our results predict a promising future for [Au(CE CPh)(PTA)] as a chemotherapeutic agent for colorectal carcinoma. (C) 2016 Elsevier Inc. All rights reserved.
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