| In vitro antioxidant properties of calpain inhibitors: leupeptin and calpain inhibitor-1. | |
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MedLine Citation:
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PMID: 12643443 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The aim of this study was 1/ to assess the efficacy of calpain inhibitors: leupeptin and calpain inhibitor-1, to inhibit calpain activity in vitro, 2/ to measure the scavenging abilities of these compounds against free radicals. The efficacy of calpain inhibitors to block calpain activity was tested with azocasein as a substrate for calpain. Leupeptin and calpain inhibitor-1 inhibited calpain activity in the same range of concentrations, the IC50 being 0.14 microM and 0.09 microM, respectively. We measured the antioxidant properties of leupeptin and calpain inhibitor-1 using the allophycocyans assay after identification offree radical species produced by the complex H2O2 + Cu(++). Electron paramagnetic resonance (EPR) spin-trapping studies performed by using DMPO showed that a quartet signal (hyperfine couplings aN = aH = 14.9 G) arisen from DMPO-OH was formed. We found a correlation between leupeptin concentration and oxygen radical absorbance capacity (ORAC) values (r2 = 0.975) indicating an in vivo antioxidant capacity. In contrast, calpain inhibitor-1 showed no protection. In conclusion, our findings indicate that leupeptin and calpain inhibitor-1 are equipotent inhibitors on calpain activity but exhibit diffrent antioxidant efficacy. |
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Authors:
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Caroline Perrin; Catherine Vergely; Marianne Zeller; Luc Rochette |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Cellular and molecular biology (Noisy-le-Grand, France) Volume: 48 Online Pub ISSN: 0145-5680 ISO Abbreviation: Cell. Mol. Biol. (Noisy-le-grand) Publication Date: 2002 |
Date Detail:
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Created Date: 2003-03-19 Completed Date: 2003-09-30 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 9216789 Medline TA: Cell Mol Biol (Noisy-le-grand) Country: France |
Other Details:
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Languages: eng Pagination: OL267-70 Citation Subset: IM |
Affiliation:
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Laboratoire de Physiopathologie et Pharmacologie Cardiovasculaires Expérimentales, Facultés de Médecine et Pharmacie, Dijon, France. caroline.perrin@u-bourgogne.fr |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Antioxidants
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pharmacology* Calpain / antagonists & inhibitors* Electron Spin Resonance Spectroscopy Glycoproteins / pharmacology* Kinetics Leupeptins / pharmacology* Phycocyanin / pharmacology |
| Chemical | |
Reg. No./Substance:
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0/Antioxidants; 0/Glycoproteins; 0/Leupeptins; 0/allophycocyanin; 0/calpain inhibitors; 11016-15-2/Phycocyanin; 24365-47-7/leupeptin; EC 3.4.22.-/Calpain |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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