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Vet Microbiol ; 255: 109016, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-33677370

RESUMO

Porcine Reproductive and Respiratory Syndrome (PRRS) is a devastating disease among the most notorious threats to the swine industry worldwide and is characterized by respiratory distress and reproductive failure. Highly evolving porcine reproductive and respiratory syndrome virus (PRRSV) strains with complicated genetic diversity make the current vaccination strategy far from cost-effective and thus urge identification of potent lead candidates to provide prevention and treatment approaches. From an in vitro small molecule screening with the TargetMol Natural Compound Library comprising 623 small molecules, cytopathic effect (CPE) observations and RT-qPCR analysis of viral ORF7 gene expression identified cepharanthine (CEP) to be one of the most protent inhibitors of PRRSV infection in Marc-145 cells. When compared with tilmicosin, which is one of the most commonly used antibiotics in swine industry to inhibit infections, CEP more prominently inhibited PRRSV infection represented by both RNA and protein levels, further reduced the TCID50 by 5.6 times, and thus more remarkably protected Marc-145 cells against PRRSV infection. Mechanistically, western blot analyses of the Marc-145 cells and the porcine alveolar macrophages (PAMs) with or without CEP treatment and PRRSV infection at various time points revealed that CEP can inhibit the expression of integrins ß1 and ß3, integrin-linked kinase (ILK), RACK1 and PKCα, leading to NF-κB suppression and consequent alleviation of PRRSV infection. Collectively, our small molecule screening identified cepharanthine as an inhibitor of PRRSV infection in vitro by suppressing Integrins/ILK/RACK1/PKCα/NF-κB signalling axis, which may enlighten the deeper understanding of the molecular pathogenesis of PRRSV infection and more importantly, suggested CEP as a potential promising drug for PRRS control in veterinary clinics.


Assuntos
Benzilisoquinolinas/farmacologia , Integrinas/metabolismo , Vírus da Síndrome Respiratória e Reprodutiva Suína , Proteína Quinase C-alfa/metabolismo , Proteínas Serina-Treonina Quinases/metabolismo , Receptores de Quinase C Ativada/metabolismo , Animais , Antivirais/farmacologia , Linhagem Celular , Chlorocebus aethiops , Regulação da Expressão Gênica/efeitos dos fármacos , Integrinas/genética , NF-kappa B/genética , NF-kappa B/metabolismo , Síndrome Respiratória e Reprodutiva Suína/tratamento farmacológico , Síndrome Respiratória e Reprodutiva Suína/virologia , Proteína Quinase C-alfa/genética , Proteínas Serina-Treonina Quinases/genética , Receptores de Quinase C Ativada/genética , Transdução de Sinais , Suínos
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