Journal
CHEMMEDCHEM
Volume 15, Issue 6, Pages 552-558Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201900686
Keywords
Arsenic; leukemia; mitochondria; PDHC; apoptosis
Categories
Funding
- National Natural Science Foundation of China [21673166, 21873075]
- Fundamental Research Funds for the Central Universities [2015203020212]
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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.
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