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Acne vulgaris, a high-prevalence skin condition afflicting people, persists as a significant challenge in the absence of effective treatments and emerging antibiotic resistance. To address this pressing concern, exploration of innovative approaches is of the utmost importance. Asparagopsis armata, an invasive red seaweed renowned for its diverse array of bioactive compounds, emerges as a promising candidate. This study seeks to elucidate the potential utility of A. armata biomass in the treatment of acne vulgaris. Crude extracts were obtained through solid–liquid extraction, and fractions were obtained using liquid–liquid extraction. The analyzed bioactivities included antioxidant, antimicrobial, and anti-inflammatory. Also, chemical characterization was performed to identify free fatty acids and compounds through LC-MS and elements. The present findings unveil compelling attributes, including anti-Cutibacterium acnes activity, cytotoxic and non-cytotoxic effects, antioxidant properties, and its ability to reduce nitric oxide production with consequent anti-inflammatory potential. Additionally, chemical characterization provides insights into its mineral elements, free fatty acids, and diverse compounds. The observed antimicrobial efficacy may be linked to halogenated compounds and fatty acids. Cytoprotection appears to be associated with the presence of glycerolipids and glycosylated metabolites. Furthermore, its antioxidant activity, coupled with anti-inflammatory properties, can be attributed to phenolic compounds, such as flavonoids. This study underscores the potential of A. armata as a natural ingredient in skincare formulations, offering an important contribution to the ongoing battle against acne vulgaris. [ABSTRACT FROM AUTHOR]

Wine production is one of the most important agricultural activities. The winemaking process generates a considerable volume of different residues characterized as by-products, such as pomace, seeds, stems, and skins. By-products are rich in polyphenols with antioxidant and antibacterial properties and may act as bacteriostatic or bactericidal agents against food-borne pathogens, improving food safety by enhancing antibiotic efficacy and reducing bacterial resistance. The aim of this study was to evaluate the phenolic composition and antioxidant activity of grape components (skins, seeds, and stems) from three red grape varieties (Periquita, Gamay, and Donzelinho Tinto) and determine their antibacterial activity against antibiotic-resistant bacteria, including Escherichia coli in food-producing animals and Listeria monocytogenes from food products and food-related environments. Ten phenolic compounds were quantified in these red grape varieties, with specific compounds found in different parts of the grape, including phenolic acids and flavonoids. Flavonoids are abundant in seeds and stems, malvidin-3-O-glucoside being the main anthocyanin in skins. The ethanolic extract from the seeds showed in vitro concentration-dependent activity against reactive species like •NO and O2•−. Gamay extract was the most effective, followed by Donzelinho Tinto and Periquita. Extracts showed varying antibacterial activity against Gram-positive and Gram-negative bacteria, with stronger effects on Gram-positive bacteria. L. monocytogenes was more susceptible, while E. coli was limited to three strains. Seeds exhibited the strongest antibacterial activity, followed by stems. The results of our study provide evidence of the potential of grape by-products, particularly seeds, as sources of bioactive compounds with antioxidant and antibacterial properties, offering promising avenues for enhancing food safety and combating antibiotic resistance in food production and related environments. [ABSTRACT FROM AUTHOR]

Background: Sulphur containing natural compounds are among the most biologically relevant metabolites in vivo. Naringenin 8-sulphonate from Parinari excelsa Sabine was evaluated in a previous work, demonstrating ability to act as a natural anti-inflammatory. Although the interference of this molecule against different inflammatory mediators was described, there is no information regarding its potential toxicity and pharmacokinetics, which are essential for its capacity to reach its therapeutic targets. In fact, despite the existence of reports on naringenin ADMET properties, the influence of sulphation patterns on them remains unknown. Objectives: This work aims to assess the in vitro pharmacokinetic and toxicological behavior of naringenin 8-sulphonate, as well as to understand the importance of the presence and position of the sulphur containing group for that. Methods: Naringenin 8-sulphonate physicochemical and ADMET properties were investigated using in silico tools and cell-based in vitro models. At the same time, naringenin and naringenin 4’-O-sulphate were investigated to evaluate the impact of the sulphonate group on the results. ADMETlab 2.0 in silico tool was used to predict the compounds’ physicochemical descriptors. Pharmacokinetic properties were determined experimentally in vitro. While MRC5 lung fibroblasts and HaCaT keratinocytes were used to evaluate the cytotoxicity of samples through MTT and LDH assays, Caco-2 human intestinal epithelial cells were used for the determination of genotoxicity, through alkaline comet assay, and as a permeability model to assess the ability of compounds to cross biological barriers. Results: Experimental determinations showed that none of the compounds was cytotoxic. In terms of genotoxicity, naringenin 8-sulphonate and naringenin caused significant DNA fragmentation, whereas naringenin 4’-O-sulphate did not. When it comes to permeability, the two sulphur-containing compounds with a sulphur containing group were clearly less capable to cross the Caco-2 cell barrier than naringenin. Conclusion: In this study, we conclude that the sulphur containing group from naringenin 8-sulphonate is disadvantageous for the molecule in terms of ADMET properties, being particularly impactful in the permeability in intestinal barrier models. Thus, this work provides important insights regarding the role of flavonoids sulphation and sulphonation upon pharmacokinetics and toxicity. [ABSTRACT FROM AUTHOR]

Escherichia coli, including extended-spectrum β-lactamases (ESBL)-producing strains, poses a global health threat due to multidrug resistance, compromising food safety and environmental integrity. In industrial settings, rabbits raised for meat have the highest consumption of antimicrobial agents compared to other food-producing animals. The European Union is facing challenges in rabbit farming as rabbit consumption declines and antibiotic-resistant strains of E. coli cause enteric diseases. The aim of this study was to investigate the antibiotic resistance profile, genetic diversity, and biofilm formation in cefotaxime-resistant E. coli strains isolated from twenty rabbit farms in Northern Portugal to address the effect of the pressing issue of antibiotic resistance in the rabbit farming industry. Resistance to critically antibiotics was observed, with high levels of resistance to several categories, such as tetracycline, ampicillin, aztreonam, and streptomycin. However, all isolates were susceptible to cefoxitin and imipenem. Multidrug resistance was common, with strains showing resistance to all antibiotics tested. The blaCTX-M variants (blaCTX-3G and blaCTX-M9), followed by the tetracycline resistance genes, were the most frequent resistance genes found. ST10 clones exhibiting significant resistance to various categories of antibiotics and harboring different resistance genes were detected. ST457 and ST2325 were important sequence types due to their association with ESBL-E. coli isolates and have been widely distributed in a variety of environments and host species. The strains evaluated showed a high capacity for biofilm formation, which varied when they were grouped by the number of classes of antibiotics to which they showed resistance (i.e., seven different classes of antibiotics, six classes of antibiotics, and three/four/five classes of antibiotics). The One Health approach integrates efforts to combat antimicrobial resistance in rabbit farming through interdisciplinary collaboration of human, animal, and environmental health. Our findings are worrisome and raise concerns. The extensive usage of antibiotics in rabbit farming emphasizes the urgent need to establish active surveillance systems. [ABSTRACT FROM AUTHOR]

The chemistry of bryophytes is not well known. The available data indicate interesting chemical constitutions of some bryophyte species, i.e., active and new compounds are to be found within bryophytes, especially liverworts. In this study, one liverwort and two moss species were studied: Lunularia cruciata (L.) Dumort, Brachytheciastrum velutinum (Hedw) Ignatov & Huttunen and Kindbergia praelonga (Hedw) Ochyra. The phenolic compositions of these bryophyte species have not hitherto been reported. Their methanolic extracts were analyzed by reversed-phase HPLC, coupled to a diode-array detector (DAD). Luteolin-7-O-glucoside and quercetin were found in the L. cruciata extract. The extract obtained from B. velutinum contained four phenolic acids (4-O-caffeoylquinic, 5-O-caffeoylquinic, caffeic and ellagic acids) and three flavonoids (apigenin-7-O-glucoside, luteolin and apigenin). The K. praelonga extract was characterized by the presence of several phenolic acids and their derivatives (4-O-caffeoylquinic, 5-O-caffeoylquinic, caffeic, p-coumaric, ferulic and ellagic acids, and caffeic and p-coumaric acid derivatives) and three flavonoids (apigenin-7-O-glucoside, luteolin, apigenin and an unidentified flavanone). .

Simple Summary: Cancer is the second cause of death worldwide, representing a massive burden on modern society. It is, therefore, urgent to increase the success rates of cancer treatments. With this work, we aim to characterize selectively cytotoxic natural products that act by inducing stress upon the endoplasmic reticulum (ER) of cancer cells. The ER is in charge of the synthesis and folding of most of the cellular proteome. ER stress is a known vulnerability of cancer cells due to their aberrant protein synthesis rates. We identified several natural products that induce selective cytotoxicity on cancer cell lines and act upon the ER. Berberine was the most promising molecule, disrupting Ca2+ homeostasis, inducing UPR target gene expression and ER-resident caspase-4 activation on AGS and A549 cells. Our results indicate that berberine and emodin are potential leads for the development of new pharmacological strategies against cancer. The last century has witnessed the establishment of neoplastic disease as the second cause of death in the world. Nonetheless, the road toward desirable success rates of cancer treatments is still long and paved with uncertainty. This work aims to select natural products that act via endoplasmic reticulum (ER) stress, a known vulnerability of malignant cells, and display selective toxicity against cancer cell lines. Among an in-house chemical library, nontoxic molecules towards noncancer cells were assessed for toxicity towards cancer cells, namely the human gastric adenocarcinoma cell line AGS and the lung adenocarcinoma cell line A549. Active molecules towards at least one of these cell lines were studied in a battery of ensuing assays to clarify the involvement of ER stress and unfolded protein response (UPR) in the cytotoxic effect. Several natural products are selectively cytotoxic against malignant cells, and the effect often relies on ER stress induction. Berberine was the most promising molecule, being active against both cell models by disrupting Ca2+ homeostasis, inducing UPR target gene expression and ER-resident caspase-4 activation. Our results indicate that berberine and emodin are potential leads for the development of more potent ER stressors to be used as selective anticancer agents. [ABSTRACT FROM AUTHOR]

Plant bacterial pathogens can be devastating and compromise entire crops of fruit and vegetables worldwide. The consequences of bacterial plant infections represent not only relevant economical losses, but also the reduction of food availability. Synthetic bactericides have been the most used tool to control bacterial diseases, representing an expensive investment for the producers, since cyclic applications are usually necessary, and are a potential threat to the environment. The development of greener methodologies is of paramount importance, and some options are already available in the market, usually related to genetic manipulation or plant community modulation, as in the case of biocontrol. Seaweeds are one of the richest sources of bioactive compounds, already being used in different industries such as cosmetics, food, medicine, pharmaceutical investigation, and agriculture, among others. They also arise as an eco-friendly alternative to synthetic bactericides. Several studies have already demonstrated their inhibitory activity over relevant bacterial phytopathogens, some of these compounds are known for their eliciting ability to trigger priming defense mechanisms. The present work aims to gather the available information regarding seaweed extracts/compounds with antibacterial activity and eliciting potential to control bacterial phytopathogens, highlighting the extracts from brown algae with protective properties against microbial attack. [ABSTRACT FROM AUTHOR]