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1.
Drug Discov Today ; 28(8): 103629, 2023 08.
Artigo em Inglês | MEDLINE | ID: mdl-37230283

RESUMO

Microbial resistance is a major concern for public health worldwide, mainly because of the inappropriate use of antimicrobials. In this scenario, antimicrobial peptides (AMPs) have emerged as a potential therapeutic alternative means by which to control infectious diseases, because of their broad spectrum of action. However, some challenges can make their clinical application problematic, including metabolic instability and toxicity. Here, we provide a clear description of AMPs as promising molecules for the development of unusual antimicrobial drugs. We also describe current strategies used to overcome the main difficulties related to AMP clinical application, including different peptide designs and nanoformulation.


Assuntos
Anti-Infecciosos , Peptídeos Catiônicos Antimicrobianos , Peptídeos Catiônicos Antimicrobianos/farmacologia , Peptídeos Catiônicos Antimicrobianos/uso terapêutico , Peptídeos Antimicrobianos , Anti-Infecciosos/farmacologia , Anti-Infecciosos/uso terapêutico , Anti-Infecciosos/química , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Antibacterianos/química
2.
Molecules ; 24(23)2019 Nov 28.
Artigo em Inglês | MEDLINE | ID: mdl-31795088

RESUMO

The Indianmeal moth, Plodia interpunctella, is one of the most damaging pests of stored products. We investigated the insecticidal properties of ApKTI, a Kunitz trypsin inhibitor from Adenanthera pavonina seeds, against P. interpunctella larvae through bioassays with artificial diet. ApKTI-fed larvae showed reduction of up to 88% on larval weight and 75% in survival. Trypsin enzymes extracted from P. interpunctella larvae were inhibited by ApKTI, which also demonstrated capacity to bind to chitin. Kinetic studies revealed a non-competitive inhibition mechanism of ApKTI for trypsin, which were further corroborated by molecular docking studies. Furthermore, we have demonstrated that ApKTI exhibits a hydrophobic pocket near the reactive site loop probably involved in chitin interactions. Taken together, these data suggested that the insecticidal activity of ApKTI for P. interpunctella larvae involves a dual and promiscuous mechanisms biding to two completely different targets. Both processes might impair the P. interpunctella larval digestive process, leading to larvae death before reaching the pupal stage. Further studies are encouraged using ApKTI as a biotechnological tool to control insect pests in field conditions.


Assuntos
Fabaceae/química , Inseticidas/química , Inseticidas/farmacologia , Mariposas/efeitos dos fármacos , Inibidores da Tripsina/química , Inibidores da Tripsina/farmacologia , Animais , Biomassa , Quitina , Inseticidas/isolamento & purificação , Larva , Modelos Moleculares , Conformação Proteica , Sementes/química , Relação Estrutura-Atividade , Tripsina/química , Inibidores da Tripsina/isolamento & purificação
4.
Clin Physiol Funct Imaging ; 36(2): 139-45, 2016 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-25523909

RESUMO

The association of ageing with obesity commits elderly women and has been correlated with multiple degenerative processes, which could be occasioned by an enhancing in levels of matrix metalloproteinase-2 and metalloproteinase-9 (MMPs) as well by an cytokine unbalance that included an enhancing on interleukin-6 (IL-6). Furthermore, other factors could be also related to degenerative process, as they could be reduced by eccentric resistance exercise (ERE), which seems particularly important to initiate resistance training in obese older adults. In this view, this study aims to determinate the effects of an acute ERE session on serum MMP-2, MMP-9 and IL-6 in elderly obese women. Ten elderly obese women participated in this study and completed a 10 repetitions maximum test (10 RM) utilizing leg extension exercise. Subjects then completed an acute ERE session consisting of seven sets of 10 repetitions at 110% of 10 RM with a rest of 3 min between sets. Blood samples were collected before, immediately after, 3, 24 and 48 h following the ERE session. Zymograms were utilized to measure the MMP-2 and MMP-9 enzymes from all individuals. Moreover, IL-6 concentration was also determinated. After ERE session, MMP-2 and MMP-9 decreased, remaining significantly below baseline values after 48 h (P<0·05). Although not statistically significant, there was a tendency for IL-6 to decrease 48 h after the ERE when compared with 3 h (P = 0·06). An acute ERE session decreases MMP-9, MMP-2 and IL-6 in elderly obese women, possibly indicating a transient protection against the low grade inflammation present in this specific population.


Assuntos
Metaloproteinase 2 da Matriz/sangue , Metaloproteinase 9 da Matriz/sangue , Obesidade/enzimologia , Treinamento Resistido , Fatores Etários , Idoso , Regulação para Baixo , Feminino , Humanos , Mediadores da Inflamação/sangue , Interleucina-6/sangue , Pessoa de Meia-Idade , Obesidade/sangue , Obesidade/diagnóstico , Obesidade/fisiopatologia , Fatores Sexuais , Fatores de Tempo
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