Achyrocline satureioides (Lam) DC extracts acting as enzyme modulators: digestion, inflammation, and hemostasis / Extratos de Achyrocline satureioides (Lam) DC atuando como moduladores enzimáticos: digestão, inflamação e hemostasia

Achyrocline satureioides is popularly known for its richness in phenolic compounds and medicinal properties (anti-inflammatory, analgesic, and hepatoprotective). The present study aimed at broadening the knowledge about the pharmacological potential exerted by the aqueous and ethanolic extracts of A. satureioides. These extracts were characterized by HPLC and tested for their modulatory action on phospholipases A2 and proteases of snake venoms. In addition, they were tested on the activities of digestive enzymes. Snake venoms were used as tools since they have enzymes with high functional and structural homology to human enzymes. The results demonstrate that the extracts of A. satureioides act as enzymatic inhibitors or potentiators, interfering in processes related to the hemostasis, such as coagulation and thrombus dissolution. In addition, the anti-genotoxic activity and inhibitions exerted on digestive enzymes suggests their potential use in the prevention and/or treatment of several pathologies. New studies could provide information on how the compounds present in the extracts and the different enzymes interact.

A Achyrocline satureioides é popularmente conhecida por sua riqueza em compostos fenólicos e por suas propriedades medicinais (anti-inflamatória, analgésica e hepatoprotetora). No presente estudo, com o objetivo de ampliar o conhecimento sobre o potencial farmacológico exercido por esses extratos, os extratos aquoso e etanólico de A. satureioides foram caracterizados por HPLC e testados quanto à sua ação modulatória sobre as fosfolipases A2 e proteases de peçonhas de serpentes. Além disso, também foram testados em atividades de enzimas digestivas. As peçonhas de serpentes foram usadas como ferramentas por apresentarem enzimas com alta homologia funcional e estrutural às humanas. Os resultados demonstram que os extratos de A. satureioides atuam como inibidores ou potencializadores enzimáticos, interferindo em processos relacionados à hemostasia, como coagulação e dissolução do trombo. Além do mais, destacam seu potencial antigenotóxico e as inibições exercidas sobre as enzimas digestivas direcionando seu potencial de uso na prevenção e/ou tratamento de diversas patologias. Novos estudos poderão fornecer informações sobre os mecanismos de interação entre os compostos presentes nos extratos e as diferentes enzimas.

Exploring the structural and functional aspects of the phospholipase A2 from Naja spp.

Naja spp. venom is a natural source of active compounds with therapeutic application potential. Phospholipase A2 (PLA2) is abundant in the venom of Naja spp. and can perform neurotoxicity, cytotoxicity, cardiotoxicity, and hematological disorders. The PLA2s from Naja spp. venoms are Asp 49 isoenzymes with the exception of PLA2 Cys 49 from Naja sagittifera. When looking at the functional aspects, the neurotoxicity occurs by PLA2 called ß-toxins that have affinity for phosphatidylcholine in nerve endings and synaptosomes membranes, and by α-toxins that block the nicotinic acetylcholine receptors in the neuromuscular junctions. In addition, these neurotoxins may inhibit K+ and Ca++ channels or even interfere with the Na+/K+/ATPase enzyme. The disturbance in the membrane fluidity also results in inhibition of the release of acetylcholine. The PLA2 can act as anticoagulants or procoagulant. The cytotoxicity exerted by PLA2s result from changes in the cardiomyocyte membranes, triggering cardiac failure and hemolysis. The antibacterial activity, however, is the result of alterations that decrease the stability of the lipid bilayer. Thus, the understanding of the structural and functional aspects of PLA2s can contribute to studies on the toxic and therapeutic mechanisms involved in the envenomation by Naja spp. and in the treatment of pathologies.

Antibacterial activity and in vivo wound healing potential of phenolic extracts from jaboticaba skin.

In this study, different phenolic extracts were obtained from the jaboticaba skin meal (JSM), whose phenolic compounds were characterized and their antibacterial activities were assessed. Moreover, the activity of lyophilized ethanolic extract of jaboticaba skin (EEJS) on wound healing was analyzed in rats. The JSM phenolic extracts were obtained in four ways: aqueous, methanolic, ethanolic, and acetone extracts. The phenolic compounds were characterized in these extracts by high-performance liquid chromatography, and their antibacterial activities were evaluated. The in vivo experiment was divided into four groups and received the following treatments: G1-silver sulfadiazine (positive control); G2-EEJS at 10%; G3-EEJS at 5%, and G4-EEJS at 2.5%. The aqueous extract did not inhibit the growing of any bacterium. The ethanolic, acetone, and methanolic extracts inhibited the growing of all bacteria tested at the concentrations of 1.25%, 2.50%, and 5.00%, respectively. The ethanolic extract was the one that showed the highest bacterial inhibition potential and the highest contents of phenolic compounds, especially of catechin, epicatechin gallate, and epicatechin. The G3 and G4 treatments presented faster wound healing compared to the G1 one, as it promoted a less intense inflammatory reaction and full closure of the wounds at an accelerated rate.

Mechanism of firmness loss in guava cv. Pedro Sato during ripening at room temperature

Abstract Guava (Psidium guajava L.) is fruit with very short shelf life due to associated with the loss of firmness in the pulp and information on the activity of enzymes that degrade pectic substances, as well as the amount of pectin, is very contradictory and not clearly defined. This work showed that the firmness of the fruit decreased sharply on the first four day­s of ripening. The identified phenolic compounds had their content increased with fruit maturation. The addition of the enzymes cellulase and hemicellulase in the pectin extraction in fruits of Psidium guajava revealed higher contents of this polyssacaride that the ones reported in literature, highlighting pectin as the responsible for the firmness of these fruits at more adequate contents. β-D-glucosidase was identified as one of the responsible enzymes for the maturation of P. guajava fruits. Thus, studies about possible inhibitory effects of this enzyme in P. guajava fruits may reveal an important tool to reduce pectin release and early maturation of these fruits.

Cereal bars enriched with antioxidant substances and rich in fiber, prepared with flours of acerola residues.

In the processing for obtaining acerola juice, a large amount of residues, which is usually discharged, is generated (seeds and bagasse). Adding value to these by-products is of great interest, since their use can enrich human food as a good source of nutrients and dietary fiber. In this study, acerola seed flours (ASF) and acerola bagasse flours (ABF) were used to develop cereal bars (CB) in different combinations with brown oats: CB 1: control - with the addition of 25% brown oats, CB 2: with the addition of 12.5% ASF and 12.5% ABF, CB 3: with the addition of 6.25% ASF and 18.75% ABF, CB 4: with the addition of 12.5% ASF and 12.5% brown oats and CB 5: with the addition of 12.5% ABF and 12.5% brown oats. These bars were sensorially evaluated and CB 1, CB 4 and CB 5 received the highest scores. We conclude that CB 4 and CB 5 can be considered as products with enhanced nutritional value, containing iron with a low energetic value and high levels of dietary fibre, besides being enriched with antioxidants.