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1.
Bioorg Chem ; 148: 107488, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38797066

RESUMO

Progressive loss of dopaminergic neurons leads to the depletion of the striatal neurotransmitter dopamine, which is the main cause of Parkinson's disease (PD) motor symptoms. Simultaneous inhibition of the two key dopamine metabolic enzymes, catechol-O-methyltransferase (COMT) and monoamine oxidase B (MAO-B), could potentially be a breakthrough in achieving clinical efficacy. Representative compound C12 exhibits good COMT inhibitory activity (IC50 = 0.37 µM), metal chelation ability, and BBB permeability. Furthermore, results from in vivo biological activity evaluations indicate that C12 can improve dopamine levels and ameliorate MPTP-induced PD symptoms in mice. Preliminary in vivo and in vitro study results highlight the potential of compound C12 in PD treatment.


Assuntos
Dopamina , Inibidores da Monoaminoxidase , Monoaminoxidase , Doença de Parkinson , Animais , Camundongos , Dopamina/metabolismo , Relação Estrutura-Atividade , Monoaminoxidase/metabolismo , Estrutura Molecular , Inibidores da Monoaminoxidase/farmacologia , Inibidores da Monoaminoxidase/química , Inibidores da Monoaminoxidase/síntese química , Doença de Parkinson/tratamento farmacológico , Doença de Parkinson/metabolismo , Catecol O-Metiltransferase/metabolismo , Camundongos Endogâmicos C57BL , Masculino , Inibidores de Catecol O-Metiltransferase/farmacologia , Inibidores de Catecol O-Metiltransferase/química , Inibidores de Catecol O-Metiltransferase/síntese química , Humanos , Relação Dose-Resposta a Droga , Antiparkinsonianos/farmacologia , Antiparkinsonianos/química , Antiparkinsonianos/síntese química , Antiparkinsonianos/uso terapêutico
2.
Guang Pu Xue Yu Guang Pu Fen Xi ; 31(9): 2503-7, 2011 Sep.
Artigo em Chinês | MEDLINE | ID: mdl-22097858

RESUMO

The changing law between interelectrode current, discharge characteristic and jet characteristic of plasma ignitor under different inlet Ar pressure and working current was researched by adopting self-made plasma ignitor. Still, four channels CCD spectrometer was adopted to measure the spectrum characteristic at the exit of ignitor and electron temperature of plasma was calculated according to the spectrum characteristic. The results show that the interelectrode current gradually reduced with rising inlet Ar pressure; The jet length of plasma ignitor firstly increased then reduced with rising inlet Ar flowrate, and also increased with rising working current; The working current of plasma ignitor reduced with rising inlet Ar flowrate, and increased with rising source output current; the electron temperature of plasma ignitor jet increased with rising working current and reduced with rising Ar flowrate. The research results are of certain guidance meanings and reference values for the practical application of plasma ignition system in aeroengine.

3.
Guang Pu Xue Yu Guang Pu Fen Xi ; 31(4): 898-901, 2011 Apr.
Artigo em Chinês | MEDLINE | ID: mdl-21714224

RESUMO

The emission spectra of air dielectric barrier discharge were measured through dielectric barrier discharge experiment system, and the influence of argon fraction on the emission spectra of air dielectric barrier discharge was studied in the present paper. In the wavelength range of 280-500 nm, the second positive band system of nitrogen N2 (C3 pi(u)-B 3 pi(g)) and the first negative band system of nitrogen ion N2+ (B 3sigma(u)(+) -X 2 sigma(g)+) were found. Adding 10% argon under the same conditions, initial discharge voltage reduced from 26 to 23 kV, both dielectric barrier discharge and its emission spectra intensity were enhanced, and the full width at half maximum increased. With increasing argon fraction, the trends of each nitrogen second positive band system line were different and two nitrogen ion first negative band system lines (391.44 and 427.81 nm) were reduced.

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