Document Detail


Inhibitors directed towards caspase-1 and -3 are less effective than pan caspase inhibition in preventing renal proximal tubular cell apoptosis.
MedLine Citation:
PMID:  14988591     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
BACKGROUND: Uncontrolled apoptosis contributes to tubular cell deletion in renal scarring. Caspase-3 has a central role in the execution of apoptosis and may provide a target for regulating cell death. Here we evaluate three caspase inhibitors: B-D-FMK (pan caspase inhibitor), Z-DEVDFMK (predominantly Caspase-3 inhibitor) and Z-VAD-FMK (predominantly Caspase-1 and -3 inhibitor) to ameliorate apoptosis induced by cisplatin in rat proximal tubular (RPT) cells. METHODS: Caspase-3 activity (substrate cleavage assay) and protein (immunocytochemistry and Western blotting), apoptosis (Annexin V flow cytometry, in situend labelling of fragmented DNA, light/electron microscopy and DNA laddering) and cell survival (trypan blue exclusion and propidium iodide flow cytometry) were determined in RPT cells exposed to cisplatin with and without caspase inhibitors. RESULTS: Cisplatin induced a dose-dependent increase in Caspase-3 activity and 8-fold of increase in apoptosis (p < 0.01) when applied for 24 h at 100 microM. B-D-FMK (40 microM), Z-DEVD-FMK (15 microM) and Z-VAD-FMK (22 microM) almost completely inhibited the 25-fold increase in Caspase-3 activity and decreased apoptosis from 15.9 +/- 4.4 to 2.0 +/- 0.6% (p < 0.01), 15.0 +/- 2.2 and 15.0 +/- 2.2% respectively. DNA ladders were visible in cisplatin-treated cells, which disappeared following addition of B-D-FMK and decreased with Z-VAD-FMK and Z-DEVD-FMK. Cisplatin reduced cell survival to 61% by trypan blue exclusion. B-D-FMK and Z-VAD-FMK increased this to 87 and 75%, but Z-DEVD-FMK had no significant effect. CONCLUSIONS: Cisplatin causes an increase in RPT apoptosis that is associated with increased Caspase-3 activity. All caspase inhibitors were equally effective at reducing Caspase-3 activity, however the pan caspase inhibitor B-D-FMK was more effective at preventing apoptosis and increasing cell survival. Therefore, pan caspase inhibition offers the greatest potential for the prevention of renal tubular cell deletion by uncontrolled apoptosis.
Authors:
Bin Yang; A Meguid El Nahas; Marie Fisher; Bart Wagner; Linhong Huang; Ian Storie; David Barnett; Jonathan Barratt; Alice C Smith; Timothy S Johnson
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Nephron. Experimental nephrology     Volume:  96     ISSN:  1660-2129     ISO Abbreviation:  Nephron Exp. Nephrol.     Publication Date:  2004  
Date Detail:
Created Date:  2004-02-27     Completed Date:  2004-05-10     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  101159770     Medline TA:  Nephron Exp Nephrol     Country:  Switzerland    
Other Details:
Languages:  eng     Pagination:  e39-51     Citation Subset:  IM    
Copyright Information:
Copyright 2004 S. Karger AG, Basel
Affiliation:
Sheffield Kidney Institute, Sheffield University Division of Clinical Sciences, Sheffield, UK.
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MeSH Terms
Descriptor/Qualifier:
Amino Acid Chloromethyl Ketones / pharmacology
Animals
Apoptosis / drug effects*
Caspase 1 / antagonists & inhibitors
Caspase 3
Caspases / analysis,  antagonists & inhibitors*,  metabolism
Cell Line
Cell Survival / drug effects
Cisplatin / antagonists & inhibitors
Cysteine Proteinase Inhibitors / pharmacology*
DNA Fragmentation / drug effects
Flow Cytometry
Kidney Tubules, Proximal / cytology*,  drug effects,  enzymology
Necrosis
Oligopeptides / pharmacology
Rats
Chemical
Reg. No./Substance:
0/Amino Acid Chloromethyl Ketones; 0/Cysteine Proteinase Inhibitors; 0/Oligopeptides; 0/benzoylcarbonyl-aspartyl-glutamyl-valyl-aspartyl-fluoromethyl ketone; 0/benzyloxycarbonylvalyl-alanyl-aspartyl fluoromethyl ketone; 0/butyloxycarbonyl-O-methyl-aspartyl-fluoromethyl ketone; 15663-27-1/Cisplatin; EC 3.4.22.-/Casp3 protein, rat; EC 3.4.22.-/Caspase 3; EC 3.4.22.-/Caspases; EC 3.4.22.36/Caspase 1

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