A novel glutathione peroxidase mimic with antioxidant activity.
Many diseases are associated with the overproduction of hydroperoxides that inflict cell damage. A novel cyclodextrin derivative, 6A,6B-diseleninic acid-6A',6B'-selenium bridged beta-cyclodextrin (6-diSeCD), was synthesized to be a functional mimic of glutathione peroxidase (GPX) that normally removes these hydroperoxides. The mimic had high catalytic GPX activity of 13.5 U/micromol, which is 13.6-fold higher than ebselen (PZ51), and was chemically and biologically stable in vitro. Antioxidant activity was studied by ferrous sulfate/ascorbate-induced mitochondria damage model system. These data show that the mimic has great antioxidant activity. Such mimics may result in better clinical therapies for diseases mediated by hydroperoxides.
Ren
X
X
Key Laboratory of Molecular Enzymology and Engineering, Jilin University, Changchan, People's Republic of China.
Yang
L
L
Liu
J
J
Su
D
D
You
D
D
Liu
C
C
Zhang
K
K
Luo
G
G
Mu
Y
Y
Yan
G
G
Shen
J
J
D000818:Animals; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001205:Ascorbic Acid / Q000737:chemistry / Q000494:pharmacology; D002417:Cattle; D003505:Cyclodextrins / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D005296:Ferrous Compounds / Q000737:chemistry / Q000494:pharmacology; D005978:Glutathione / Q000737:chemistry; D008928:Mitochondria / Q000187:drug effects; D008954:Models, Biological; D016566:Organoselenium Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D010084:Oxidation-Reduction / Q000187:drug effects; D017382:Reactive Oxygen Species / Q000378:metabolism; D018036:Selenium Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D047392:beta-Cyclodextrins
C426831:6A,6B-diseleninic acid-6A',6B'-selenium bridged beta-cyclodextrin; D000975:Antioxidants; D003505:Cyclodextrins; D005296:Ferrous Compounds; D016566:Organoselenium Compounds; D017382:Reactive Oxygen Species; D018036:Selenium Compounds; D047392:beta-Cyclodextrins; C020748:ferrous sulfate; D005978:Glutathione; C031215:betadex; D001205:Ascorbic Acid