The purpose of the present study was to characterize the chemical composition, lipid oxidation, and physical characteristics of fresh sausages produced with meat from the pectoralis major muscle ...affected by deep pectoral myopathy. For the characterization of myopathy, samples were collected from broiler chickens slaughtered between 42- and 46-days old in a slaughterhouse in the state of São Paulo. The experiment consisted of samples from pectoralis major muscle of birds affected or not by DPM (normal—absence of myopathy and DPM category 3—progressive degeneration of the pectoralis minor with a greenish appearance). After classification of the samples, a part of raw products with the pectoralis minor removed, was submitted to microbiological and physical analyses for the characterization of DPM. Afterward, only the pectoralis major muscle was used to manufacture fresh sausages and 2 groups were established. The evaluated parameters were: color, pH, water-holding capacity (WHC), cooking loss (CL), shear force (SF), water activity (Aw), and chemical composition. Meat pH was higher (P < 0.05) in meats with DPM, however, WHC values were lower (71.92%), which made CL value increase (25.31%). In addition, the coloring increased and the technological characteristics of raw breasts were less favorable with the presence of DPM. All fresh sausages’ color (except a* higher control group), pH, and Aw values were higher in DPM group. No effect on SF values was observed between fresh sausages. In chemical composition, only protein content increased in fresh sausages with DPM. Microbiological analyses did not indicate bacterial contamination of raw samples and fresh sausages. Data obtained in the present study suggest fresh sausages produced with breasts affected by DPM are a viable alternative and may confer more favorable qualitative characteristics to sausages than the raw marketed meat.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
Free radicals act as secondary messengers, modulating a number of important biological processes, including gene expression, ion mobilization in transport systems, protein interactions and enzymatic ...functions, cell growth, cell cycle, redox homeostasis, among others. In the cardiovascular system, the physiological generation of free radicals ensures the integrity and function of cardiomyocytes, endothelial cells, and adjacent smooth muscle cells. In physiological conditions, there is a balance between free radicals generation and the activity of enzymatic and non-enzymatic antioxidant systems. Redox imbalance, caused by increased free radical's production and/or reduced antioxidant defense, plays an important role in the development of cardiovascular diseases, contributing to cardiac hypertrophy and heart failure, endothelial dysfunction, hypertrophy and hypercontractility of vascular smooth muscle. Excessive production of oxidizing agents in detriment of antioxidant defenses in the cardiovascular system has been described in obesity, diabetes mellitus, hypertension, and atherosclerosis. The transcription factor Nrf2 (nuclear factor erythroid 2-related factor 2), a major regulator of antioxidant and cellular protective genes, is primarily activated in response to oxidative stress. Under physiological conditions, Nrf2 is constitutively expressed in the cytoplasm of cells and is usually associated with Keap-1, a repressor protein. This association maintains low levels of free Nrf2. Stressors, such as free radicals, favor the translocation of Nrf2 to the cell nucleus. The accumulation of nuclear Nrf2 allows the binding of this protein to the antioxidant response element of genes that code antioxidant proteins. Although little information on the role of Nrf2 in the cardiovascular system is available, growing evidence indicates that decreased Nrf2 activity contributes to oxidative stress, favoring the pathophysiology of cardiovascular disorders found in obesity, diabetes mellitus, and atherosclerosis. The present mini-review will provide a comprehensive overview of the role of Nrf2 as a contributing factor to cardiovascular risk in metabolic diseases.
This paper describes a comparative analysis of the physicochemical and structural properties of prodrugs and their corresponding drugs with regard to drug‐likeness rules. The dataset used in this ...work was obtained from the DrugBank. Sixty‐five pairs of prodrugs/drugs were retrieved and divided into the following categories: carrier‐linked to increase hydrophilic character, carrier‐linked to increase absorption, and bioprecursors. We compared the physicochemical properties related to drug‐likeness between prodrugs and drugs. Our results show that prodrugs do not always follow Lipinski's Rule of 5, especially as we observed 15 prodrugs with more than 10 hydrogen bond acceptors and 18 with a molecular weight greater than 500 Da. This fact highlights the importance of extending Lipinski's rules to encompass other parameters as both strategies (filtering of drug‐like chemical libraries and prodrug design) aim to improve the bioavailability of compounds. Therefore, critical reasoning is fundamental to determine whether a structure has drug‐like properties or could be considered a potential orally active compound in the drug‐design pipeline.
Breaking the rules: Drug‐likeness rules exist for the design of orally active compounds. We compared the physicochemical and structural properties of oral prodrugs and their active metabolites to evaluate whether prodrugs also are inside drug‐likeness chemical space. Critical reasoning and insights beyond the rules are essential to select compounds for biological testing depending on the assay and expected application.
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FZAB, GIS, IJS, KILJ, NLZOH, NUK, OILJ, SBCE, SBMB, UL, UM, UPUK
The aim of this study was to examine the effects of frozen storage for 12 mo on the concentrations of lipids and cholesterol and fatty acid profile of wooden chicken breast meat. A total of 120 ...samples of chicken breasts were selected, according to the degree of “wooden breast” myopathy “severe,” “moderate,” and “normal” (absence of myopathy), from male chickens slaughtered at 42 d of age, from Cobb 500 strain. Part of the samples (n = 20/grade of severity) were evaluated on the day of collection and the remainder were packaged, frozen and stored at −18°C for up to 12 mo. At the beginning (collection day) and at the end of the proposed freezing period (12 mo), analyses of lipid, cholesterol, and fatty acid profile were carried out. Percentage of saturated (SFA), monounsaturated (MUFA), and polyunsaturated (PUFA) fatty acids were evaluated. Meats affected by wooden breast myopathy had lower levels of PUFA that exert beneficial effects on health, such as DHA, EPA and ARA, and this profile is impaired by prolonged storage (12 mo), which results in important nutritional losses for the consumer.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
The objective of the present study was to characterize possible variations in the quality of wooden chicken breast meat during freezing for 12 mo, in order to prove whether the shelf life recommended ...by the industry allows the storage of that type of meat without compromising its consumption. Three hundred samples of male Cobb 500 broilers slaughtered at 42 d of age were used. Part of the samples (n = 20 normal—control group; n = 20 moderate degree; n = 20 severe degree) were analyzed on the day of collection (beginning), previously kept under refrigeration (4°C). The other samples were stored (−18°C) for up to 12 mo. At the end of each proposed freezing period (3, 6, 9, and 12 mo), physical and chemical analyses were performed (per period: n = 20 normal—control group; n = 20 moderate degree; n = 20 severe degree). Color (L*, a*, and b*), pH, water-holding capacity, cooking losses, tenderness, lipid oxidation, chemical composition, cholesterol concentration, mineral profile, and collagen concentration were evaluated. The physicochemical quality of wooden chicken breast meat is significantly altered during frozen storage for 12 mo, being of inferior quality when compared to normal chicken breast meat, which can negatively affect consumer acceptance. However, it should be noted that even after 12 mo of freezing, the meats did not show oxidative rancidity.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
In fruit crops like citrus, weeds coexist throughout their long cycle and can cause several yield losses. Ecological mowing (ECO) is an integrated weed management (IWM) option for citrus, as it ...produces an in‐situ mulch that suppresses the weeds; however, there is a lack of information on the impacts of tree‐row conventional (CONV) and ECO mechanical weed control when combined with residual or non‐residual herbicides, or standard frequent mechanical (MECH) control. This study aimed to evaluate, for 3 years in a young orange orchard, IWM using ECO and conventional mowing when combined with one of five weed control programmes: pre‐emergent (PRE) herbicides (sulfentrazone spring, indaziflam summer), post‐emergence (POST) herbicides (glyphosate spring, saflufenacil summer), PRE + POST herbicides (sulfentrazone + glyphosate spring, indaziflam + saflufenacil summer) and P/P (pre/post‐emergence duality) herbicides (flumioxazin spring, diuron summer). Impacts on cover crop biomass deposition, weed density, population dynamics, biomass accumulation and seed banks were evaluated. Alternanthera tenella Colla (joyweed), Bidens pilosa L. (hairy beggarticks), Digitaria horizontalis Willd (crabgrass), Galinsoga parviflora Cav. (smallflower galinsoga) and Raphanus raphanistrum L. (wild radish) were the most critical weeds with changes in their population dynamics over time. The ECO treatment promoted greater biomass deposition in the tree‐rows (up to ≈8.0 t ha−1), reducing weed density and biomass accumulation by mulch formation; similarly, MECH resulted in low weed density and a reduction in biomass accumulation. The POST and P/P treatments resulted in low levels of weed control, while ECO + PRE + POST led to almost absolute weed control (>95%). Thus, we suggest ECO + PRE + POST is an efficient IWM option in citrus tree‐row crops with low‐risk herbicide resistance (up to 5 MoA year−1 + mulch).
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BFBNIB, DOBA, FZAB, GIS, IJS, IZUM, KILJ, NLZOH, NUK, OILJ, PILJ, PNG, SAZU, SBCE, SBMB, UILJ, UKNU, UL, UM, UPUK
Targeting histone deacetylases (HDACs) and phosphatidylinositol 3‐kinases (PI3Ks) is a very promising approach for cancer treatment. This manuscript describes the design, synthesis, in vitro ...pharmacological profile, and molecular modeling of a novel class of N‐acylhydrazone (NAH) derivatives that act as HDAC6/8 and PI3Kα dual inhibitors. The surprising selectivity for PI3Kα may be related to differences in the conformation in the active site. Cellular studies showed that these compounds act in HDAC6 inhibition and the PI3/K/AKT/mTOR pathway. The compounds that are selective for inhibition of HDAC6/8 and inhibit PI3Kα show potential for the treatment of cancer.
Surprising selectivity: A novel class of N‐acylhydrazone (NAH) derivatives that act as dual HDAC6/8 and PI3Kα inhibitors is described. The surprising selectivity for PI3Kα may be related to differences in the conformation in the active site. Cellular studies showed that these compounds act in HDAC6 inhibition and the PI3K/AKT/mTOR pathway. The compounds that are selective for inhibition of HDAC6/8 and PI3Kα show potential for the treatment of cancer.
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FZAB, GIS, IJS, KILJ, NLZOH, NUK, OILJ, SBCE, SBMB, UL, UM, UPUK
High levels of aldosterone (Aldo) trigger oxidative stress and vascular dysfunction independent of effects on blood pressure. We sought to determine whether Aldo disrupts Nrf2 signaling, the main ...transcriptional factor involved in antioxidant responses that aggravate cell injury. Thoracic aorta from male C57Bl/6J mice and cultured human endothelial cells (EA.hy926) were stimulated with Aldo (100 nM) in the presence of tiron reactive oxygen species (ROS) scavenger, eplerenone mineralocorticoid receptor (MR) antagonist, and L-sulforaphane (SFN; Nrf2 activator). Thoracic aortas were also isolated from mice infused with Aldo (600 μg/kg per day) for 14 days. Aldo decreased endothelium-dependent vasorelaxation and increased ROS generation, effects prevented by tiron and MR blockade. Pharmacological activation of Nrf2 with SFN abrogated Aldo-induced vascular dysfunction and ROS generation. In EA.hy926 cells, Aldo increased ROS generation, which was prevented by eplerenone, tiron, and SFN. At short times, Aldo-induced ROS generation was linked to increased Nrf2 activation. However, after three hours, Aldo decreased the nuclear accumulation of Nrf2. Increased Keap1 protein expression, but not activation of p38 MAPK, was linked to Aldo-induced reduced Nrf2 activity. Arteries from Aldo-infused mice also exhibited decreased nuclear Nrf2 and increased Keap1 expression. Our findings suggest that Aldo reduces vascular Nrf2 transcriptional activity by Keap1-dependent mechanisms, contributing to mineralocorticoid-induced vascular dysfunction.
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IZUM, KILJ, NUK, PILJ, PNG, SAZU, UL, UM, UPUK
This study reports a set of primeval marine incursions identified in two drill cores, 1PS-06-CE, and 1PS-10-CE, which recovered the Barbalha Formation, Araripe Basin, Brazil. Based on a multi-proxy ...approach involving stratigraphy, microbiofacies, ichnofossils, and microfossils, three short-lived marine incursions were identified, designated Araripe Marine Incursions (AMI) 1-3. AMI-1 and AMI-2, which occur within the shales of the Batateira Beds (lower part of the Barbalha Formation), were identified by the occurrence of benthonic foraminifera, calcareous nannofossils, dinocysts, and a mass mortality event of non-marine ostracods. AMI-3 was recognized in the upper part of the Barbalha Formation, based on the occurrence of ichnofossils and planktonic foraminifera. The observation of the planktonic foraminifera genus Leupoldina for the first time in the basin indicates early Aptian/early late Aptian age for these deposits, and the first opportunity of correlation with global foraminifera biozonation. Our findings have implications for the breakup of the Gondwana Supercontinent, as these incursions represent the earliest marine-derived flooding events in the inland basins of northeastern Brazil.
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IZUM, KILJ, NUK, PILJ, PNG, SAZU, UL, UM, UPUK
Conformational stabilization mediated by hydrogen bonds can play an important role in the drug-target recognition process. Non-classical hydrogen bonding is receiving great attention, where C-H Y ...hydrogen bonds are found in some biological systems and are important for molecular recognition, leading to the possibility of exploration of this interaction in drug design projects. Studies that identify and characterize new non-classical interactions in different systems can assist in the rational application of these interactions. In this paper, we describe the serendipitous identification and characterization of a new non-classical hydrogen bond donor moiety found in 3-acyl-substituted furan. We applied a theoretical and experimental approach in the study of several
N
-acylhydrazones containing 3-acyl-substituted furan, where we describe the presence of a hydrogen bond between the C(2)-H bond of 3-acyl-substituted furan with the imine nitrogen in the
syn
conformer of the
N
-acylhydrazone moiety. In addition, we evaluated the strength of this interaction with intermolecular models. Thus, we believe that the 3-acyl-substituted furan moiety can be rationally explored as a hydrogen bond donor moiety in drug design projects.
A serendipitous identification and characterization of a new non-classical hydrogen bond donor moiety found in
N
-acylhydrazones containing 3-acyl-substituted furan subunit is presented.
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