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1.
Materials (Basel) ; 15(5)2022 Feb 24.
Artigo em Inglês | MEDLINE | ID: mdl-35268927

RESUMO

Plant-oil-based fibre composites for boat hulls are an interesting and growing group of materials. Although many problems are to be tackled at different stages of their preparation, the green composites are already successfully commercialised. Within this paper, the most important chemical and physical characteristics of both natural fibres and sustainable resins are provided in the form of a comprehensive review. Finally, the complex issue of interactions filler-matrix is considered.

2.
Int J Mol Sci ; 22(13)2021 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-34208928

RESUMO

The development of new antiviral drugs against SARS-CoV-2 is a valuable long-term strategy to protect the global population from the COVID-19 pandemic complementary to the vaccination. Considering this, the viral main protease (Mpro) is among the most promising molecular targets in light of its importance during the viral replication cycle. The natural flavonoid quercetin 1 has been recently reported to be a potent Mpro inhibitor in vitro, and we explored the effect produced by the introduction of organoselenium functionalities in this scaffold. In particular, we report here a new synthetic method to prepare previously inaccessible C-8 seleno-quercetin derivatives. By screening a small library of flavonols and flavone derivatives, we observed that some compounds inhibit the protease activity in vitro. For the first time, we demonstrate that quercetin (1) and 8-(p-tolylselenyl)quercetin (2d) block SARS-CoV-2 replication in infected cells at non-toxic concentrations, with an IC50 of 192 µM and 8 µM, respectively. Based on docking experiments driven by experimental evidence, we propose a non-covalent mechanism for Mpro inhibition in which a hydrogen bond between the selenium atom and Gln189 residue in the catalytic pocket could explain the higher Mpro activity of 2d and, as a result, its better antiviral profile.


Assuntos
Antivirais/química , Quercetina/química , SARS-CoV-2/metabolismo , Selênio/química , Proteínas da Matriz Viral/antagonistas & inibidores , Animais , Antivirais/metabolismo , Antivirais/farmacologia , Sítios de Ligação , COVID-19/patologia , COVID-19/virologia , Domínio Catalítico , Chlorocebus aethiops , Humanos , Ligação de Hidrogênio , Simulação de Acoplamento Molecular , Inibidores de Proteases/química , Inibidores de Proteases/metabolismo , Inibidores de Proteases/farmacologia , Quercetina/metabolismo , Quercetina/farmacologia , SARS-CoV-2/isolamento & purificação , Selênio/metabolismo , Células Vero , Proteínas da Matriz Viral/metabolismo , Replicação Viral/efeitos dos fármacos
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