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1.
Bioorg Med Chem Lett ; 30(11): 127173, 2020 06 01.
Artigo em Inglês | MEDLINE | ID: mdl-32278513

RESUMO

A group of 2-methyl-4-phenylquinoline-chalcone analogs (2a-2x) was synthesized and investigated for anti-depressant, anti-inflammatory, and analgesic effects as cyclooxygenase-2 inhibitors. Pharmacological experiments identified 24 analogs that exhibited anti-depressant, anti-inflammatory, and analgesic activities. In particular, compounds 2c, 2k, and 2w markedly shortened immobility times and exhibited the most anti-depressant activity. In addition, the mechanisms of action of the analogs 2c, 2k, and 2w were likely related to increased serotonin levels in the central nervous system. Compounds 2c, 2k, and 2w displayed reasonable cyclooxygenase-2 inhibitory effects (IC50 values from 0.21 to 0.29 µmol/L) similar to celecoxib (IC50: 0.19 µmol/L) in vitro. A molecular docking study of compound 2k also was conducted.


Assuntos
Analgésicos/química , Anti-Inflamatórios/química , Antidepressivos/química , Chalcona/química , Inibidores de Ciclo-Oxigenase 2/química , Ciclo-Oxigenase 2/metabolismo , Analgésicos/metabolismo , Anti-Inflamatórios/metabolismo , Antidepressivos/metabolismo , Sítios de Ligação , Celecoxib/química , Chalcona/metabolismo , Ciclo-Oxigenase 1/química , Ciclo-Oxigenase 1/metabolismo , Ciclo-Oxigenase 2/química , Inibidores de Ciclo-Oxigenase 2/metabolismo , Desenho de Fármacos , Humanos , Simulação de Acoplamento Molecular , Relação Estrutura-Atividade
2.
World J Clin Cases ; 9(14): 3227-3237, 2021 May 16.
Artigo em Inglês | MEDLINE | ID: mdl-34002132

RESUMO

This review focuses on the available evidence regarding the molecular mechanisms and treatment potential of several non-surgical physical therapies for managing flap ischemia to propose a non-invasive, economical, and simple treatment to improve flap survival. A review of the literature was conducted on the topics of various non-invasive methods for the treatment of ischemic necrosis of the distal end of the flap between 1988 and 2019. A total of 52 published studies were reviewed on the applications of hyperbaric oxygen therapy, electrical stimulation therapy, heat stress pretreatment, phototherapy, and vibration therapy to manage skin flap necrosis. The underlying molecular mechanisms of these physical therapies on revitalizing the dying skin flaps were discussed and preliminary clinical uses of these therapies to salvage the necrotic skin flaps were pooled and summarized for clarifying the safety and feasibility of these methods. Various physical therapy regimens have been ushered to manage necrotic development in cutaneous flaps. With the refinement of these new technologies and enhancement of related basic science research on vascular revitalization, the prevention and treatment of flap ischemia will enter a new era.

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