Brassinosteroids and analogs as neuroprotectors: synthesis and structure-activity relationships.
Identifieur interne : 001278 ( Main/Exploration ); précédent : 001277; suivant : 001279Brassinosteroids and analogs as neuroprotectors: synthesis and structure-activity relationships.
Auteurs : Jihane Ismaili [Canada] ; Martin Boisvert ; Fanny Longpré ; Julie Carange ; Céline Le Gall ; Maria-Grazia Martinoli ; Benoit DaoustSource :
- Steroids [ 1878-5867 ] ; 2012.
English descriptors
- KwdEn :
- 1-Methyl-4-phenylpyridinium (adverse effects), Animals, Antioxidants (chemical synthesis), Antioxidants (pharmacology), Antioxidants (therapeutic use), Brassinosteroids (chemical synthesis), Brassinosteroids (pharmacology), Brassinosteroids (therapeutic use), Dopaminergic Neurons (cytology), Dopaminergic Neurons (drug effects), Dopaminergic Neurons (metabolism), Humans, Molecular Structure, Neuroprotective Agents (chemical synthesis), Neuroprotective Agents (pharmacology), Neuroprotective Agents (therapeutic use), Oxidative Stress, PC12 Cells, Parkinson Disease (metabolism), Parkinson Disease (pathology), Parkinson Disease (prevention & control), Rats, Structure-Activity Relationship.
- MESH :
- chemical , adverse effects : 1-Methyl-4-phenylpyridinium.
- chemical , chemical synthesis : Antioxidants, Brassinosteroids, Neuroprotective Agents.
- chemical , pharmacology : Antioxidants, Brassinosteroids, Neuroprotective Agents.
- chemical , therapeutic use : Antioxidants, Brassinosteroids, Neuroprotective Agents.
- cytology : Dopaminergic Neurons.
- drug effects : Dopaminergic Neurons.
- metabolism : Dopaminergic Neurons, Parkinson Disease.
- pathology : Parkinson Disease.
- prevention & control : Parkinson Disease.
- Animals, Humans, Molecular Structure, Oxidative Stress, PC12 Cells, Rats, Structure-Activity Relationship.
Abstract
We have demonstrated previously that the brassinosteroid (BR) 24-epibrassinolide exerts neuroprotective effects deriving from its antioxidative properties. In this study, we synthesized 2 natural BRs and 5 synthetic analogs and analyzed their neuroprotective actions in neuronal PC12 cells, against 1-methyl-4-phenylpyridinium (MPP(+)), a neurotoxin known to induce oxidative stress and degenerescence of dopaminergic neurons characteristic of Parkinsonian brains. We also tested the neuroprotective potential of 2 commercially available BRs. Our results disclosed that 6 of the 9 BRs and analogs tested protected neuronal PC12 cells against MPP(+) toxicity. In addition, our structure-activity study suggests that the steroid B-ring and lateral chain play an important role for their neuroprotective action.
DOI: 10.1016/j.steroids.2011.10.009
PubMed: 22064216
Affiliations:
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Le document en format XML
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<author><name sortKey="Longpre, Fanny" sort="Longpre, Fanny" uniqKey="Longpre F" first="Fanny" last="Longpré">Fanny Longpré</name>
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<author><name sortKey="Martinoli, Maria Grazia" sort="Martinoli, Maria Grazia" uniqKey="Martinoli M" first="Maria-Grazia" last="Martinoli">Maria-Grazia Martinoli</name>
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<term>Antioxidants (chemical synthesis)</term>
<term>Antioxidants (pharmacology)</term>
<term>Antioxidants (therapeutic use)</term>
<term>Brassinosteroids (chemical synthesis)</term>
<term>Brassinosteroids (pharmacology)</term>
<term>Brassinosteroids (therapeutic use)</term>
<term>Dopaminergic Neurons (cytology)</term>
<term>Dopaminergic Neurons (drug effects)</term>
<term>Dopaminergic Neurons (metabolism)</term>
<term>Humans</term>
<term>Molecular Structure</term>
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<term>Neuroprotective Agents (pharmacology)</term>
<term>Neuroprotective Agents (therapeutic use)</term>
<term>Oxidative Stress</term>
<term>PC12 Cells</term>
<term>Parkinson Disease (metabolism)</term>
<term>Parkinson Disease (pathology)</term>
<term>Parkinson Disease (prevention & control)</term>
<term>Rats</term>
<term>Structure-Activity Relationship</term>
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<keywords scheme="MESH" qualifier="metabolism" xml:lang="en"><term>Dopaminergic Neurons</term>
<term>Parkinson Disease</term>
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<term>Humans</term>
<term>Molecular Structure</term>
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<front><div type="abstract" xml:lang="en">We have demonstrated previously that the brassinosteroid (BR) 24-epibrassinolide exerts neuroprotective effects deriving from its antioxidative properties. In this study, we synthesized 2 natural BRs and 5 synthetic analogs and analyzed their neuroprotective actions in neuronal PC12 cells, against 1-methyl-4-phenylpyridinium (MPP(+)), a neurotoxin known to induce oxidative stress and degenerescence of dopaminergic neurons characteristic of Parkinsonian brains. We also tested the neuroprotective potential of 2 commercially available BRs. Our results disclosed that 6 of the 9 BRs and analogs tested protected neuronal PC12 cells against MPP(+) toxicity. In addition, our structure-activity study suggests that the steroid B-ring and lateral chain play an important role for their neuroprotective action.</div>
</front>
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<affiliations><list><country><li>Canada</li>
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<tree><noCountry><name sortKey="Boisvert, Martin" sort="Boisvert, Martin" uniqKey="Boisvert M" first="Martin" last="Boisvert">Martin Boisvert</name>
<name sortKey="Carange, Julie" sort="Carange, Julie" uniqKey="Carange J" first="Julie" last="Carange">Julie Carange</name>
<name sortKey="Daoust, Benoit" sort="Daoust, Benoit" uniqKey="Daoust B" first="Benoit" last="Daoust">Benoit Daoust</name>
<name sortKey="Le Gall, Celine" sort="Le Gall, Celine" uniqKey="Le Gall C" first="Céline" last="Le Gall">Céline Le Gall</name>
<name sortKey="Longpre, Fanny" sort="Longpre, Fanny" uniqKey="Longpre F" first="Fanny" last="Longpré">Fanny Longpré</name>
<name sortKey="Martinoli, Maria Grazia" sort="Martinoli, Maria Grazia" uniqKey="Martinoli M" first="Maria-Grazia" last="Martinoli">Maria-Grazia Martinoli</name>
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<country name="Canada"><noRegion><name sortKey="Ismaili, Jihane" sort="Ismaili, Jihane" uniqKey="Ismaili J" first="Jihane" last="Ismaili">Jihane Ismaili</name>
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