14 documents found, page 1 of 2
Development of eugenol derivatives with 5-LOX inhibitory activity
Filho, José L. Pereira; Pereira, Renato B.; Vieira, Tatiana F.; Sousa, Sérgio F.; Coelho, José Ricardo Alves; Pinto, Nuno F. S.; Coelho, Catarina M. M.Eugenol (4-allyl-2-methoxyphenol), is the major chemical constituent in the essential oil of numerous plant species. Several biological properties have been described for this molecule, including modulation of enzymatic targets relevant for the inflammatory response, such as 5-lipoxygenase (5-LOX). As so, there is interest in expanding the chemical space of this molecule to develop new molecules to be used in i...
New supramolecular hydrogels based on diastereomeric dehydrotripeptide mixtures...
Oliveira, Carlos B. P.; Carvalho, André; Pereira, Renato B.; Pereira, David M.; Hilliou, L.; Jervis, Peter J.; Martins, J. A. R.; Ferreira, Paula M. T.Self-assembly of peptide building blocks offers unique opportunities for bottom-up preparation of exquisite nanostructures, nanoarchitectures, and nanostructured bulk materials, namely hydrogels. In this work we describe the synthesis, characterization, gelation, and rheological properties of new dehydrotripeptides, Cbz-L-Lys(Cbz)-L,D-Asp-∆Phe-OH and (2-Naph)-L-Lys(2-Naph)-L,D-Asp-∆Phe-OH, containing a N-termin...
Global burden of chronic respiratory diseases and risk factors, 1990-2019: an u...
Momtazmanesh, Sara; Moghaddam, Sahar Saeedi; Ghamari, Seyyed-Hadi; Rad, Elaheh Malakan; Rezaei, Negar; Shobeiri, Parnian; Aali, AmiraliBackground Updated data on chronic respiratory diseases (CRDs) are vital in their prevention, control, and treatment in the path to achieving the third UN Sustainable Development Goals (SDGs), a one-third reduction in premature mortality from non-communicable diseases by 2030. We provided global, regional, and national estimates of the burden of CRDs and their attributable risks from 1990 to 2019. Methods Using...
An injectable, naproxen-conjugated, supramolecular hydrogel with ultra-low crit...
Oliveira, Carlos Bruno Pereira; Veloso, Sérgio Rafael Silva; Castanheira, Elisabete M. S.; Figueiredo, Pedro R.; Carvalho, Alexandra T.P.; Hilliou, L.Short peptides capped on the N-terminus with aromatic groups are often able to form supramolecular hydrogels—self-assembled networks of fibrils able to trap water molecules. Typically, these hydrogelators can form stiff gels at concentrations of 0.1 to 1.0 wt%—i.e. they consist of mainly water. The properties of these soft materials mimic those of the extracellular matrix (ECM) of biological tissue and therefor...
Aryl-capped lysine-dehydroamino acid dipeptide supergelators as potential drug ...
Oliveira, Carlos B. P.; Pereira, Renato B.; Pereira, David M.; Hilliou, L.; Castro, Tarsila Gabriel; Martins, J. A. R.; Jervis, Peter JohnEmploying amino acids and peptides as molecular building blocks provides unique opportunities for generating supramolecular hydrogels, owing to their inherent biological origin, bioactivity, biocompatibility, and biodegradability. However, they can suffer from proteolytic degradation. Short peptides (<8 amino acids) attached to an aromatic capping group are particularly attractive alternatives for minimalistic ...
Liposomal formulations loaded with a eugenol derivative for application as inse...
Fernandes, Maria José Gomes; Pereira, Renato B.; Rodrigues, Ana Rita Oliveira; Vieira, Tatiana F.; Fortes, A. Gil; Pereira, David M.; Sousa, Sérgio F.A recently synthesized new eugenol derivative, ethyl 4-(2-methoxy-4-(oxiran-2-ylmethyl)phenoxy)butanoate, with a high insecticidal activity against Sf9 (Spodoptera frugiperda) insect cells, was encapsulated in the liposomal formulations of egg-phosphatidylcholine/cholesterol (Egg-PC:Ch) 70:30 and 100% dioleoylphosphatidylglycerol (DOPG), aiming at the future application as insecticides. Compound-loaded DOPG lip...
Eugenol β-amino/β-alkoxy alcohols with selective anticancer activity
Teixeira, Cláudia; Pereira, Renato B.; Pinto, Nuno F. S.; Coelho, Catarina M. M.; Fernandes, Maria José G.; Fortes, A. Gil; Gonçalves, M. Sameiro T.Eugenol, 4-allyl-2-methoxyphenol, is the main constituent of clove essential oil and has demonstrated relevant biological activity, namely anticancer activity. Aiming to increase this activity, we synthesized a series of eugenol β-amino alcohol and β-alkoxy alcohol derivatives, which were then tested against two human cancer cell lines, namely gastric adenocarcinoma cells (AGS) and lung adenocarcinoma cells (A5...
Discovery of the anticancer activity for lung and gastric cancer of a brominate...
González-Berdullas, Patricia; Pereira, Renato B.; Teixeira, Cláudia; Silva, José Pedro; Magalhães, Carla M.; Rodríguez-Borges, José E.Cancer is still a challenging disease to treat, both in terms of harmful side effects and therapeutic efficiency of the available treatments. Herein, to develop new therapeutic molecules, we have investigated the anticancer activity of halogenated derivatives of different components of the bioluminescent system of marine Coelenterazine: Coelenterazine (<b>Clz</b>) itself, Coelenteramide (<b>Clmd</b>), and Coele...
Synthesis, computational and nanoencapsulation studies on eugenol-derived insec...
Coelho, Catarina M. M.; Pereira, Renato B.; Vieira, Tatiana F.; Teixeira, Cláudia M.; Fernandes, Maria José Gomes; Rodrigues, Ana Rita O.A new set of alkoxy alcohols were synthesised by reaction of eugenol oxirane with aliphatic and aromatic alcohols. These eugenol derivatives were evaluated against their effect upon the viability of the insect cell line Sf9 (Spodoptera frugiperda). The most promising compounds, 4-(3-(tert-butoxy)-2-hydroxypropyl)-2-methoxyphenol and 4-(2-((4-fluorobenzyl)oxy)-3-hydroxypropyl)-2-methoxyphenol were submitted to i...
New carvacrol and thymol derivatives as potential insecticides: synthesis, biol...
Natal, Carolina M.; Fernandes, Maria José Gomes; Pinto, Nuno F. S.; Pereira, Renato B.; Vieira, Tatiana F.; Rodrigues, Ana Rita OliveiraNew compounds with potential insecticide activity were synthesized by structural modifications performed in the monoterpenoids phenolic moieties of carvacrol and thymol, resulting in a set of derivatives with the ether function containing the propyl, chloropropyl or hydroxypropyl chains, as well as a bicyclic ether with an unsaturated chain containing a carboxylic acid terminal. In addition, an analogue of carv...