RESUMO
BACKGROUND: Organophosphorus pesticides exert their toxic effects mainly by the inhibition of acetylcholinesterase (AChE), which is related to emotional disorders, such as depression. Atropine-oximes therapy is commonly used; however, the efficacy of oximes in the reactivation of AChE has been inconsistent. The objective of this study was to investigate the possible neuroprotective effect of (3Z)-5-Chloro-3-(hydroxyimino)indolin-2-one (Câ-HIN), a compound that combines the isatin and oxime functional groups, in rats exposed to malathion. The effect of Câ-HIN on the AChE activity and the BDNF-Trkß pathway in the prefrontal cortex of malathion-exposed rats were tested. METHODS: Wistar male rats were co-treated with Câ-HIN [50 mg/kg (p.o.) (3 mL/kg)] and/or malathion [250 mg/kg (i.p.) (5 mL/kg)] and performed behavioral tests twelve hours after these exposures. RESULTS: The Câ-HIN reversed the increased immobility time in the forced swimming test and the decreased grooming time in the splash test induced by malathion, but any significant difference was observed in locomotion analysis. These results demonstrate the antidepressant-like effect of Câ-HIN. The cortical AChE activity was reactivated by Câ-HIN in rats exposed to malathion. Malathion induced an increase in Trkß and a decrease in BDNF levels in the prefrontal cortex of rats, which were avoided by Câ-HIN. CONCLUSION: These findings support the hypothesis that Câ-HIN is an AChE reactivator with antidepressant-like properties, which is related to the improvement of BDNF-Trkß signaling after acute exposure to malathion in rats. Thus, the results allow suggesting the potential use of Câ-HIN as an oxime-based therapy against the neurotoxic effects of malathion.
Assuntos
Acetilcolinesterase/metabolismo , Antidepressivos/farmacologia , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Indóis/farmacologia , Malation/toxicidade , Oxindóis/farmacologia , Receptor trkB/metabolismo , Transdução de Sinais , Animais , Antidepressivos/administração & dosagem , Antidepressivos/química , Antidepressivos/uso terapêutico , Comportamento Animal/efeitos dos fármacos , Depressão/tratamento farmacológico , Indóis/administração & dosagem , Indóis/química , Indóis/uso terapêutico , Masculino , Atividade Motora/efeitos dos fármacos , Fármacos Neuroprotetores/farmacologia , Fármacos Neuroprotetores/uso terapêutico , Oxindóis/administração & dosagem , Oxindóis/química , Oxindóis/uso terapêutico , Ratos Wistar , Transdução de Sinais/efeitos dos fármacosRESUMO
In the title compound, [Cu2(C11H13N3O3S)2(C2H6OS)2], the Cu(II) cation is N,N',O-chelated by a deprotonated hy-droxy-imino-tosyl-hydrazone ligand and coordinated by a dimethyl sulfoxide mol-ecule. One O atom from the adjacent hy-droxy-imino-tosyl-hydrazone ligand bridges the Cu(II) cation, forming the centrosymmetric dimeric complex. The cation is in an overall distorted N2O3 square-pyramidal coordination environment. The methyl-benzene ring is twisted with respect to the hydrazine fragment, with a dihedral angle of 89.54â (9)° between the planes. An intra-molecular C-Hâ¯O hydrogen bond occurs. In the crystal, mol-ecules are linked by weak C-Hâ¯O and C-Hâ¯S inter-actions. Weak π-π stacking is also observed between parallel benzene rings of adjacent mol-ecules, the centroid-centroid distance being 3.9592â (17)â Å.
RESUMO
The reaction of cadmium acetate dihydrate with 2-acetyl-pyridine (4-phenyl-thio-semicarbazone) yielded the title compound, [Cd(C(14)H(13)N(4)S)(2)]. The Cd(II) atom is six-coordin-ated in a distorted octa-hedral environment by two deproton-ated thio-semicarbazone ligands acting in a tridentate chelating mode through two N and one S atoms, forming metalla-rings. In the crystal, mol-ecules are connected through inversion centers via pairs of N-Hâ¯S inter-actions, building a one-dimensional hydrogen-bonded polymer along [0-1-1].
RESUMO
In the title compound, C(11)H(15)N(3)O(3)S, the C-S-N(H)-N linkage is nonplanar, the torsion angle being 75.70â (12)°. The compound has two almost planar fragments linked to the S atom: the hydrazone-derivative fragment [(HONC(4)H(6))N-N(H)-] and the tolyl fragment (C(7)H(7)-) have maximum deviations from the mean plane through the non-H atoms of 0.0260â (10) and 0.0148â (14)â Å, respectively. The two planar fragments make an inter-planar angle of 79.47â (5)°. In the crystal, mol-ecules are connected through inversion centers via pairs of N-Hâ¯O and O-Hâ¯N hydrogen bonds.