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Title

Novel hexahydropyridoindole derivative as prospective agent against oxidative damage in pancreatic β cells

Authors
Račková, Lucia
Cumaoğlu, Ahmet
Bağrıacık, E Umit
Štefek, Milan
Karasu, Çimen
Published in Medicinal Chemistry. 2011, vol. 7, no. 6, p. 711-7
Abstract The potential protective effect of (±)-8-methoxy-1,3,4,4a,5,9b-hexahydro-pyrido[4,3-b]indole-2-carboxylic acid ethyl ester (II) was assessed against hydrogen peroxide (H2O2)-cytotoxicity in rat pancreatic INS-1E β cells and compared with the effect of the related pyridoindole, stobadine (I), a promising indole-type reference antioxidant. Only pre-treatment with the compound (II) led to a significant preservation of the metabolic and secretory functions of the cells exposed to H2O2. The caspase-9 and -3 activities, as well as the early apoptotic changes of plasma membrane, were suppressed in the cells pre-incubated with both of compounds tested. However, only pyridoindole (II) inhibited profoundly the time-delayed apoptotic changes, These results suggest that pyridoindole (II) characterized by enhanced intrinsic antioxidant efficiency, may protect β cells against cytotoxic effects of H2O2, involved in the development of both type 1 and type 2 diabetes.
Keywords AnimalsAntioxidants/chemical synthesis/chemistry/pharmacologyApoptosis/drug effectsCaspases/antagonists & inhibitors/metabolismCells, CulturedDose-Response Relationship, DrugDrug Evaluation, PreclinicalEnzyme Inhibitors/chemical synthesis/chemistry/pharmacologyHydrogen Peroxide/antagonists & inhibitors/pharmacologyIndoles/chemical synthesis/chemistry/pharmacologyInsulin-Secreting Cells/cytology/drug effects/metabolismMolecular StructureOxidative Stress/drug effectsRatsStructure-Activity Relationship
Identifiers
PMID: 22313311
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Structures
Research group Mitochondries et sécrétion d'insuline (671)
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RAČKOVÁ, Lucia et al. Novel hexahydropyridoindole derivative as prospective agent against oxidative damage in pancreatic β cells. In: Medicinal Chemistry, 2011, vol. 7, n° 6, p. 711-7. https://archive-ouverte.unige.ch/unige:25508

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Deposited on : 2013-01-14

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