Document Detail


Nimbolide sensitizes human colon cancer cells to TRAIL through reactive oxygen species- and ERK-dependent up-regulation of death receptors, p53, and Bax.
MedLine Citation:
PMID:  21078664     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
TNF-related apoptosis-inducing ligand (TRAIL) shows promise as a cancer treatment, but acquired tumor resistance to TRAIL is a roadblock. Here we investigated whether nimbolide, a limonoid, could sensitize human colon cancer cells to TRAIL. As indicated by assays that measure esterase activity, sub-G(1) fractions, mitochondrial activity, and activation of caspases, nimbolide potentiated the effect of TRAIL. This limonoid also enhanced expression of death receptors (DRs) DR5 and DR4 in cancer cells. Gene silencing of the receptors reduced the effect of limonoid on TRAIL-induced apoptosis. Using pharmacological inhibitors, we found that activation of ERK and p38 MAPK was required for DR up-regulation by nimbolide. Gene silencing of ERK abolished the enhancement of TRAIL-induced apoptosis. Moreover, our studies indicate that the limonoid induced reactive oxygen species production, which was required for ERK activation, up-regulation of DRs, and sensitization to TRAIL; these effects were mimicked by H(2)O(2). In addition, nimbolide down-regulated cell survival proteins, including I-FLICE, cIAP-1, cIAP-2, Bcl-2, Bcl-xL, survivin, and X-linked inhibitor of apoptosis protein, and up-regulated the pro-apoptotic proteins p53 and Bax. Interestingly, p53 and Bax up-regulation by nimbolide was required for sensitization to TRAIL but not for DR up-regulation. Overall, our results indicate that nimbolide can sensitize colon cancer cells to TRAIL-induced apoptosis through three distinct mechanisms: reactive oxygen species- and ERK-mediated up-regulation of DR5 and DR4, down-regulation of cell survival proteins, and up-regulation of p53 and Bax.
Authors:
Subash C Gupta; Simone Reuter; Kanokkarn Phromnoi; Byoungduck Park; Padmanabhan S Hema; Mangalam Nair; Bharat B Aggarwal
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't     Date:  2010-11-15
Journal Detail:
Title:  The Journal of biological chemistry     Volume:  286     ISSN:  1083-351X     ISO Abbreviation:  J. Biol. Chem.     Publication Date:  2011 Jan 
Date Detail:
Created Date:  2011-01-10     Completed Date:  2011-03-02     Revised Date:  2012-01-16    
Medline Journal Info:
Nlm Unique ID:  2985121R     Medline TA:  J Biol Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1134-46     Citation Subset:  IM    
Affiliation:
Cytokine Research Laboratory, Department of Experimental Therapeutics, The University of Texas M.D. Anderson Cancer Center, Houston, Texas 77030, USA.
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MeSH Terms
Descriptor/Qualifier:
Adenocarcinoma / drug therapy*,  metabolism,  pathology
Antineoplastic Agents / pharmacology*
Apoptosis / drug effects,  physiology
Breast Neoplasms
Colonic Neoplasms / drug therapy*,  metabolism,  pathology
Extracellular Signal-Regulated MAP Kinases / metabolism*
HCT116 Cells
HT29 Cells
Humans
Kidney Neoplasms
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Limonins / pharmacology*
Lung Neoplasms
Multiple Myeloma
Pancreatic Neoplasms
Reactive Oxygen Species / metabolism
Receptors, TNF-Related Apoptosis-Inducing Ligand / metabolism
TNF-Related Apoptosis-Inducing Ligand / metabolism*
Tumor Suppressor Protein p53 / metabolism
bcl-2-Associated X Protein / metabolism
Grant Support
ID/Acronym/Agency:
CA-124787-01A2/CA/NCI NIH HHS; CA016672/CA/NCI NIH HHS
Chemical
Reg. No./Substance:
0/Antineoplastic Agents; 0/Limonins; 0/Reactive Oxygen Species; 0/Receptors, TNF-Related Apoptosis-Inducing Ligand; 0/TNF-Related Apoptosis-Inducing Ligand; 0/TNFRSF10A protein, human; 0/TNFSF10 protein, human; 0/TP53 protein, human; 0/Tumor Suppressor Protein p53; 0/bcl-2-Associated X Protein; 25990-37-8/nimbolide; EC 2.7.11.24/Extracellular Signal-Regulated MAP Kinases

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