74175-13-6Relevant academic research and scientific papers
Dual Inhibition of Pyruvate Dehydrogenase Complex and Respiratory Chain Complex Induces Apoptosis by a Mitochondria-Targeted Fluorescent Organic Arsenical in vitro and in vivo
Fan, Xiao-Yang,Hu, Yan-Jun,Jiang, Feng-Lei,Liu, Yi,Liu, Yu-Jiao,Xia, Yin-Zheng,Zhang, Dong-Dong,Zhou, Fu-Ling
, (2020)
Based on the potential therapeutic value in targeting mitochondria and the fluorophore tracing ability, a fluorescent mitochondria-targeted organic arsenical PDT-PAO-F16 was fabricated, which not only visualized the cellular distribution, but also exerted anti-cancer activity in vitro and in vivo via targeting pyruvate dehydrogenase complex (PDHC) and respiratory chain complexes in mitochondria. In details, PDT-PAO-F16 mainly accumulated into mitochondria within hours and suppressed the activity of PDHC resulting in the inhibition of ATP synthesis and thermogenesis disorder. Moreover, the suppression of respiratory chain complex I and IV accelerated the mitochondrial dysfunction leading to caspase family-dependent apoptosis. In vivo, the acute promyelocytic leukemia was greatly alleviated in the PDT-PAO-F16 treated group in APL mice model. Our results demonstrated the organic arsenical precursor with fluorescence imaging and target-anticancer efficacy is a promising anticancer drug.
A mitochondria-targeted organic arsenical accelerates mitochondrial metabolic disorder and function injury
Fan, Xiao-Yang,Liu, Yu-Jiao,Cai, Yu-Meng,Wang, An-Dong,Xia, Yin-Zheng,Hu, Yan-Jun,Jiang, Feng-Lei,Liu, Yi
, p. 760 - 768 (2019)
Considering the vital role of mitochondria in the anti-cancer mechanism of organic arsenical, the mitochondria-targeted precursor PDT-PAO-TPP was designed and synthesized. PDT-PAO-TPP, as a delocalization lipophilic cation (DLCs) which mainly accumulated
