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J Ocul Pharmacol Ther ; 37(5): 290-300, 2021 06.
Artigo em Inglês | MEDLINE | ID: mdl-33761287

RESUMO

Purpose: This study investigated the safety and therapeutic efficacy of licarin A (LCA) in the treatment of intraocular inflammation. Methods:In vitro safety of LCA in retinal pigmented epithelial cells (ARPE-19) and human embryonic stem cell derived-retinal pigmented epithelial cells (hES-RPE) was evaluated using CellTiter-Blue® kit. The chorioallantoic membrane (CAM) assay was used to investigate LCA safety and antiangiogenic activity. In vivo safety of intravitreal LCA was accomplished by clinical examination (including assessment of intraocular pressure), electroretinography (ERG), and histopathology. Uveitis was induced in rats by subcutaneous and intravitreal injection of bacillus Calmette-Guérin (BCG) antigen of Mycobacterium bovis. Intraocular inflammation was graded by slit-lamp and fundus examination, ERG, and histopathology. Results: LCA was safe to cells and to the CAM at concentration below 12.0 µM. LCA significantly reduced the percentage of blood vessels in the CAM. Retinal safety and anti-inflammatory efficacy of intravitreal injection of LCA 6.0 µM were confirmed through clinical, functional, and histopathological evaluation. Significant reduction of inflammatory cytokines (tumor necrosis factor-α and interleukin-6) was also found, when compared to untreated animals. Conclusion: The results suggest that LCA is a potential new drug for the treatment of inflammatory eye disease.


Assuntos
Inibidores da Angiogênese/farmacologia , Inflamação/tratamento farmacológico , Lignanas/farmacologia , Epitélio Pigmentado da Retina/efeitos dos fármacos , Inibidores da Angiogênese/administração & dosagem , Inibidores da Angiogênese/uso terapêutico , Animais , Anti-Inflamatórios/farmacologia , Membrana Corioalantoide/metabolismo , Modelos Animais de Doenças , Descoberta de Drogas , Eletrorretinografia/métodos , Oftalmopatias/patologia , Inflamação/diagnóstico , Pressão Intraocular/efeitos dos fármacos , Injeções Intravítreas , Lignanas/administração & dosagem , Lignanas/uso terapêutico , Masculino , Ratos , Ratos Wistar , Epitélio Pigmentado da Retina/citologia , Epitélio Pigmentado da Retina/embriologia , Segurança , Resultado do Tratamento , Uveíte/induzido quimicamente , Uveíte/patologia
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