Document Detail

Synthesis, Cytotoxicity and Cell Death Profile of Polyaminoanthraquinones as Antitumor Agents.
MedLine Citation:
PMID:  22913275     Owner:  NLM     Status:  Publisher    
Investigation on designed polyaminoanthraquinones revealed that the anthraquinones bearing triamine motifs are generally more potent than their counterparts with diamine or tetraamine motifs. Compared to the reference drug Mitoxantrone (MTX), 9b and 9c exhibited better inhibitory activity on cancerous HepG2 cells and preferable cell selectivity in the further screen of normal QSG7701 cells, although they were not assimilated by cancer cells via the polyamine transporter. The presence of polyamine motifs elevated the interaction of compounds 9b and 9c with lysosomes, and resulted in distinct mode of cell death. 9c and MTX could cause caspases-dependent HepG2 cell apoptotic death involving in mitochondria membrane potential (MMP) loss, cytochrome c release and caspase-3 activation. However, 9b, which contained only one less methylene group in the polyamine tail, produced cytotoxicity by necrosis. In conclusion, the modification of anthraquinones with polyamines may furnish potent anticancer drug candidates against hepatocellular carcinoma undergoing distinct cell death mechanisms. © 2012 John Wiley & Sons A/S.
Jianhong Wang; Ruihong Gao; Qian Li; Songqiang Xie; Jin Zhao; Chaojie Wang
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-8-22
Journal Detail:
Title:  Chemical biology & drug design     Volume:  -     ISSN:  1747-0285     ISO Abbreviation:  Chem Biol Drug Des     Publication Date:  2012 Aug 
Date Detail:
Created Date:  2012-8-23     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101262549     Medline TA:  Chem Biol Drug Des     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
© 2012 John Wiley & Sons A/S.
Key Laboratory of Natural Medicine and Immuno-Engineering, Henan University, Kaifeng 475004, China Institute of Chemistry and Biology, Henan University, Kaifeng 475004, China.
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