Document Detail


Nuclear permeable ruthenium(II) β-carboline complexes induce autophagy to antagonize mitochondrial-mediated apoptosis.
MedLine Citation:
PMID:  20958054     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The role of autophagy in cancer development and response to cancer therapy has been a subject of debate. Here we demonstrate that a series of ruthenium(II) complexes containing a β-carboline alkaloid as ligand can simultaneously induce autophagy and apoptosis in tumor cells. These Ru(II) complexes are nuclear permeable and highly active against a panel of human cancer cell lines, with complex 3 displaying activities greater than those of cisplatin. The antiproliferative potentialities of 1-3 are in accordance with their relative lipophilicities, cell membrane penetration abilities, and in vitro DNA binding affinities. Complexes 1-3 trigger release of reactive oxygen species (ROS) and attenuation of ROS by scavengers reduced the sub-G1 population, suggesting ROS-dependent apoptosis. Inhibition of ROS generation also reduces autophagy, indicating that ROS triggers autophagy. Further studies show that suppression of autophagy using pharmacological inhibitors (3-methyladenine and chloroquine) enhances apoptotic cell death.
Authors:
Caiping Tan; Sensen Lai; Shouhai Wu; Sheng Hu; Lingjun Zhou; Yu Chen; Minxu Wang; Yiping Zhu; Wu Lian; Wenlie Peng; Liangnian Ji; Anlong Xu
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  53     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2010 Nov 
Date Detail:
Created Date:  2010-11-04     Completed Date:  2010-12-28     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  7613-24     Citation Subset:  IM    
Affiliation:
State Key Laboratory of Biocontrol, Department of Biochemistry, College of Life Sciences, Sun Yat-sen University, Guangzhou, Guangdong 510006, PR China.
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MeSH Terms
Descriptor/Qualifier:
Antineoplastic Agents / chemical synthesis*,  chemistry,  pharmacology
Apoptosis / drug effects*
Autophagy / drug effects*
Carbolines / chemical synthesis*,  chemistry,  pharmacology
Cell Line, Tumor
Cell Membrane Permeability
Cell Nucleus / metabolism*
Coordination Complexes / chemical synthesis*,  chemistry,  pharmacology
DNA / chemistry
Drug Screening Assays, Antitumor
Green Fluorescent Proteins / genetics
Humans
Microscopy, Confocal
Microscopy, Electron, Transmission
Microtubule-Associated Proteins / genetics,  metabolism
Mitochondria / physiology*
Reactive Oxygen Species / metabolism
Ruthenium*
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/Antineoplastic Agents; 0/Carbolines; 0/Coordination Complexes; 0/Microtubule-Associated Proteins; 0/Reactive Oxygen Species; 0/light chain 3, human; 147336-22-9/Green Fluorescent Proteins; 7440-18-8/Ruthenium; 9007-49-2/DNA

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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