title: Antioxidant potential of new pyrazoline derivatives to prevent oxidative damage.
abstract: The antioxidant capacity of a series of six novel synthetic pyrazoline derivatives (i) 5-hydroxy-3-methyl-5-trifluoromethyl-4,5-dihydro-1H-carbaldehyde-pyrazole, (ii) 5-hydroxy-3-methyl-5-trifluoromethyl-4,5-dihydro-1H-1-acetyl-pyrazole, (iii) 5-hydroxy-3-methyl-5-trifluoromethyl-4,5-dihydro-1H-carboxyamide-pyrazole, (iv) 5-hydroxy-3-methyl-5-trifluoromethyl-4,5-dihydro-1H-1-benzoyl-pyrazole, (v) 5-hydroxy-3-methyl-5-trifluoromethyl-4,5-dihydro-1H-1-(2-hydroxybenzoyl)-pyrazole and (vi) 5-hydroxy-3-methyl-5-trifluoromethyl-4,5-dihydro-1H-1-(4-methoxybenzoyl)-pyrazole was evaluated as the capacity of compounds to transfer a hydrogen atom (protection against brain lipid peroxidation and glutathione oxidation) and their capacity to transfer a single electron [ferric-reducing antioxidant power (FRAP) and 1,1-diphenyl-2-picrylhydrazyl radical scavenging (DPPH) assays]. Compound 5 had the highest free radical scavenging capacity in the DPPH assay, while compound 2 had the highest FRAP value (P < 0.05). Only compounds 1, 4 and 5 protected against lipid peroxidation in rat brain homogenate. However, compound 5 was the most effective to prevent basal and iron-, sodium nitroprusside- and H(2)O(2)-stimulated lipid peroxidation (IC(50) < 15 microM) and the only one effective to block glutathione oxidation-mediated by H(2)O(2) (at 150 microM). Our results indicate that compound 5 has the greatest potential to prevent oxidative damage in brain homogenates.
authors.affiliation: Graduate Program on Pharmacology, Center of Health Sciences, Federal University of Santa Maria, Manta Maria, Rio Grande do Sul, Brazil.
authors.forename: Daniele M
authors.initials: DM
authors.lastname: Martins
authors.forename: Bruna G
authors.initials: BG
authors.lastname: Torres
authors.forename: Patrícia R
authors.initials: PR
authors.lastname: Spohr
authors.forename: Pablo
authors.initials: P
authors.lastname: Machado
authors.forename: Helio G
authors.initials: HG
authors.lastname: Bonacorso
authors.forename: Nilo
authors.initials: N
authors.lastname: Zanatta
authors.forename: Marcos A P
authors.initials: MA
authors.lastname: Martins
authors.forename: Tatiana
authors.initials: T
authors.lastname: Emanuelli
mesh_terms: D000818:Animals; D016166:Free Radical Scavengers / Q000737:chemistry / Q000494:pharmacology*; D005978:Glutathione / Q000378:metabolism; D066298:In Vitro Techniques; D015227:Lipid Peroxidation / Q000187:drug effects; D008297:Male; D018384:Oxidative Stress / Q000187:drug effects*; D016548:Prosencephalon / Q000187:drug effects* / Q000378:metabolism; D011720:Pyrazoles / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D017382:Reactive Oxygen Species / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D016166:Free Radical Scavengers; D011720:Pyrazoles; D017382:Reactive Oxygen Species; D005978:Glutathione