Toward multitasking pharmacological COX-targeting agents: Non-steroidal anti-inflammatory prodrugs with antiproliferative effects

The antitumor activity of certain anti-inflammatory drugs is often attributed to an indirect effect based on the inhibition of COX enzymes. In the case of anti-inflammatory prodrugs, this property could be attributed to the parent molecules with mechanism other than COX inhibition, particularly through formulations capable of slowing down their metabolic conversion. In this work, a pilot docking study aimed at comparing the interaction of two prodrugs, nabumetone (NB) and its tricyclic analog 7-methoxy-2, 3-dihydro-1H-cyclopenta[b]naphthalen-1-one (MC), and their common active metabolite 6-methoxy-2-naphthylacetic acid (MNA) with the COX binding site, was carried out. Cytotoxicity, cytofluorimetry, and protein expression assays on prodrugs were also performed to assess their potential as antiproliferative agents that could help hypothesize an effective use as anticancer therapeutics. Encouraging results suggest that the studied compounds could act not only as precursors of the anti-inflammatory metabolite, but also as direct antiproliferative agents. © 2021 by the authors. Licensee MDPI, Basel, Switzerland

Controle biológico da murcha bacteriana do tomateiro, por Pseudomonas spp. fluorescentes Biological control of bacterial wilt of tomato by fluorescent Pseudomonas spp

Esta revisão bibliográfica teve como objetivo avaliar o potencial de antagonismo de espécies de Pseudomonas fluorescentes a Pseudomonas solanacearum, agente causal da murcha bacteriana do tomateiro. Devido a dificuldade encontrada nas estratégias utilizadas para o controle da Murcha Bacteriana por meio de métodos convencionais, alguns outros tem sido estudados, como o uso de microrganismos benéficos. As rizobactérias vem proporcionando solução viável a algumas doenças consideradas de difícil manejo. Dentre os mecanismos que tem sido sugeridos para o controle microbiano de patógenos de plantas, através do uso de rizobactérias fluorescentes, citamse produção de antibióticos, bactericinas, enzimas titicas, competição por espaço e nutrientes. Possuem uma alta capacidade de colonização e sobrevivência no hospedeiro, falares que são importantes no estabelecimento e introdução de microrganismos na rizosfera. Estas bactérias podem também incitar um aumento no desenvolvimento e na produção do hospedeiro, sendo denominadas de rizobactérias promotoras de crescimento de plantas.<br>This literature review has the objetive of evaluating the antagonism potential of species of florescem Pseudomonas to Pseudomonas solanacearum which is the causal agent of bacterial wilt on the tomato crop. Due to serious limitation in the ejficiency of conventional methods of contrai, other strategies have been siudied, such as the use o/beneficiai microrganisms. Rhizobacteria have shown to be a viable alternative in the contrai of some diseases of difficult managmenl. Among the mechanisms which have been suggestedfor microbian control of plantpathogens with fluorescent rhizobacteria, can be used antibiotic production, bacteriocin, uric emimes and competition for colonization and survival capacity on the host. The survival capacity is very important in the introduction and stablishment ofthe microrganisms in the rhizosphere. These bacteria can aiso increse the development and yield of the host and can be calledplant growth promete rhizobacteria