Inhibitory Effect of Ebselen on Cerebral Acetylcholinesterase Activity In Vitro: Kinetics and Reversibility of Inhibition

Martini, Franciele; Brüning, César Augusto; Soares, Suelen Mendonça; Nogueira, Cristina Wayne; Zeni, Gilson

doi:10.2174/1381612820666141014124319

Cited by 27 publications

(12 citation statements)

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“…2 ). The AChE reduction caused by selenium compounds, such as ebselen and DPDS, have been also been reported in previous studies using rat brains in vitro and mouse ex vivo , respectively [26] , [27] .…”

Section: Discussionsupporting

confidence: 72%

Protective effects of novel organic selenium compounds against oxidative stress in the nematode Caenorhabditis elegans

et al. 2015

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Section: Discussionsupporting

confidence: 72%

Protective effects of novel organic selenium compounds against oxidative stress in the nematode Caenorhabditis elegans

et al. 2015

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“…The studies of Amit and coworkers led a number of investigators to determine whether EtOH drinking by animals could be modified by pharmacological manipulations that either (i) inhibited catalase activity by 3‐aminotriazole (Aragon and Amit, ; Rotzinger et al., ; Tampier et al., ); (ii) trapped acetaldehyde by administration of penicillamine, a synthetic sulfur‐containing amino acid (Font et al., ; Orrico et al., ), or (iii) reduced hydrogen peroxide levels (the cosubstrate of catalase) by administration of scavengers of hydrogen peroxide, such as ebselen a seleno‐organic drug (Ledesma et al., ). Although these studies support the view that acetaldehyde might constitute the “first hit” in EtOH reinforcement, some of the pharmacological agents used have secondary effects (e.g., inhibition of food intake by aminotriazole [Rotzinger et al., ; Tampier et al., ] or inhibition of acetylcholinesterase by ebselen [Martini et al., ]). Recently, Aragon and coworkers (Ledesma et al, ) administered alpha‐lipoic acid, a natural compound with no known secondary effects, which inhibited EtOH voluntary intake by 40%.…”

Section: Brain‐generated Metabolites Of Etohmentioning

confidence: 91%

The “First Hit” Toward Alcohol Reinforcement: Role of Ethanol Metabolites

Israel

Quintanilla

Karahanian

et al. 2015

Alcoholism Clin & Exp Res

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This review analyzes literature that describes the behavioral effects of 2 metabolites of ethanol (EtOH): acetaldehyde and salsolinol (a condensation product of acetaldehyde and dopamine) generated in the brain. These metabolites are self-administered into specific brain areas by animals, showing strong reinforcing effects. A wealth of evidence shows that EtOH, a drug consumed to attain millimolar concentrations, generates brain metabolites that are reinforcing at micromolar and nanomolar concentrations. Salsolinol administration leads to marked increases in voluntary EtOH intake, an effect inhibited by mu-opioid receptor blockers. In animals that have ingested EtOH chronically, the maintenance of alcohol intake is no longer influenced by EtOH metabolites, as intake is taken over by other brain systems. However, after EtOH withdrawal brain acetaldehyde has a major role in promoting binge-like drinking in the condition known as the "alcohol deprivation effect"; a condition seen in animals that have ingested alcohol chronically, are deprived of EtOH for extended periods, and are allowed EtOH re-access. The review also analyzes the behavioral effects of acetate, a metabolite that enters the brain and is responsible for motor incoordination at low doses of EtOH. Also discussed are the paradoxical effects of systemic acetaldehyde. Overall, evidence strongly suggests that brain-generated EtOH metabolites play a major role in the early ("first-hit") development of alcohol reinforcement and in the generation of relapse-like drinking.

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“…Sec is the key element of the enzymes active site that provides GPx with the unique ability to reduce hydrogen peroxide and other reactive oxygen and nitrogen species [ 2 ]. This unique property makes ebselen a potent bioactive molecule which is effective in the treatment of various diseases including diabetes [ 3 , 4 , 5 , 6 ], Alzheimer’s disease [ 7 ], stroke [ 8 ], hearing loss [ 9 ], and cancer [ 10 ]. It is also non-toxic, as the selenium atom incorporated in its structure is not bioavailable [ 11 ].…”

Section: Introductionmentioning

confidence: 99%

New Chiral Ebselen Analogues with Antioxidant and Cytotoxic Potential

et al. 2017

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New chiral camphane-derived benzisoselenazol-3(2H)-ones and corresponding diselenides have been synthetized using a convenient one-pot procedure. Se-N bond was efficiently converted to an Se-Se bond, which could also be easily re-oxidized to the initial benzisoselenazolone moiety. The antioxidant activity of camphor derivatives was evaluated and compared to the reactivity of a series of N-amino acid benzisoselenazol-3(2H)-ones obtained by a modified procedure involving the improved synthesis and isolation of the diseleno bis(dibenzoic) acid. The most efficient peroxide scavengers, N-bornyl and N-leucine methyl ester benzisoselenazol-3(2H)-ones, were further evaluated as cytotoxic agents on four cancer cell lines (MCF-7, HEP G2, HL 6, and DU 145) and normal cell line PNT1A. The highest antiproliferative potential was evaluated for two compounds bearing a 3-methylbutyl carbon chain, N-leucine methyl ester and N-3-methylbutyl benzisoselenazol-3(2H)-ones.

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Inhibitory Effect of Ebselen on Cerebral Acetylcholinesterase Activity In Vitro: Kinetics and Reversibility of Inhibition

Cited by 27 publications

References 0 publications

Protective effects of novel organic selenium compounds against oxidative stress in the nematode Caenorhabditis elegans

Protective effects of novel organic selenium compounds against oxidative stress in the nematode Caenorhabditis elegans

The “First Hit” Toward Alcohol Reinforcement: Role of Ethanol Metabolites

New Chiral Ebselen Analogues with Antioxidant and Cytotoxic Potential

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