Bioactive Potential Research Articles

Bioactivity and application potential of O/W emulsions derived from carboxylic acid-based NADES-extracted total saponins from Polygonatum cyrtonema Hua

This study focuses on evaluating new methods for the green extraction of saponin compounds from Polygonatum cyrtonema Hua (PCH). This study utilized a combination of carboxylic acid-based natural deep eutectic solvents (NADES) and various extraction techniques including conventional heat reflux-, ultrasound-, and microwave-assisted extraction. The primary objectives were to assess total saponin yield, antioxidant capacity, and enzyme inhibition efficiency. Additionally, the solvents and extracts were evaluated for their antibacterial activity. Oil-in-water (O/W) emulsions of NADES extracts were also characterized and analyzed for stability. Results indicated that three NADES systems were effective in extracting saponins, with choline chloride and lactic acid (ChCl-LA) system being the most efficient. The ChCl:LA extract exhibited antimicrobial and antioxidant activities superior to conventional organic solvent extracts. Additionally, it demonstrated maximum inhibitory activity (IC50 values: 0.98 ± 0.03 and 1.46 ± 0.07 mg/mL, respectively) against α-glucosidase and α-amylase. The NADES extract as an aqueous phase significantly improved the stationarity of the O/W emulsion. Collectively, the study highlights the antimicrobial and technological advantages of NADES as a potential solvent for extracting saponin compounds from PCH.

Valorization of Grape Pomace: A Review of Phenolic Composition, Bioactivity, and Therapeutic Potential.

Vitis vinifera L., commonly known as grapes, is one of the most widely cultivated crops worldwide, with over 80% used for wine production. However, the winemaking process generates substantial residues, including grape pomace (GP), wine lees, and wastewater, which can pose significant environmental and economic challenges. Among these, GP stands out not only as a waste product but also as a rich source of polyphenols-bioactive compounds with recognized antioxidant and anti-inflammatory properties. Recent advancements have expanded the application of GP-derived extracts, particularly in the health and food industries, due to their potent bioactive properties. This review provides a comprehensive overview of the valorization of GP, focusing on its phenolic composition and therapeutic potential. It evokes innovative, environmentally friendly extraction techniques and integrated methods for the chemical analysis of these valuable compounds. Additionally, the health benefits of GP polyphenols are explored, with recent experimental findings examining their metabolism and highlighting the key role of gut microbiota in these processes. These insights contribute to a deeper understanding of the biological activity of GP extracts and underscore their growing significance as a high-added-value product. By illustrating how winemaking by-products can be transformed into natural therapeutic agents, this review emphasizes the importance of sustainable development and eco-friendly waste management practices, significantly contributing to the advancement of a circular economy.

Antioxidant potentials of Acanthus ilicifolius leaves from Southwest Coastal Region of Bangladesh

This research delves into the antioxidant potential of Acanthus ilicifolius leaves harvested from the southwestern coastal region of Bangladesh. Four distinct solvents—methanol, ethanol, acetone, and ethyl acetate—were utilized to determine antioxidant activities. Initial phytochemical screening unveiled the existence of many secondary metabolites, including as flavonoids, phenols, alkaloids, and others. Total phenolic content, total flavonoid content, and total proanthocyanidin content were determined using quantitative analysis. The assessment of antioxidant activity was conducted using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2-Azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) scavenging assays. Notably, the acetone extract of Acanthus ilicifolius exhibited the highest total phenolic content (24.75 mg of GA/g), total flavonoid content (12.9 mg of catechin/g), and total proanthocyanidins content (11.47 mg of catechin/g). The ethanol extract displayed the most robust antioxidant activity in both DPPH (91.41 %) and ABTS (66.78 %) scavenging assays among the crude extracts, underscoring its potential as a valuable source of antioxidants. The results emphasise the crucial importance of choosing the appropriate solvent in the extraction procedure and suggest that Acanthus ilicifolius leaves, particularly when extracted with ethanol, acetone, or methanol, hold promise as a natural source of antioxidants. This study offers valuable insights into the bioactive potential of Acanthus ilicifolius leaves.

Fish milt and roe‐derived functional proteins and peptides: composition, bioactivities, and applications

SummaryAn expanding list of marine species has been identified and evaluated for their potential bioactivity and nutritional values. Most attention is directed toward utilising protein‐rich by‐products of fish processing for their bioactive functionalities, which can aid in minimising waste and add value to underutilised resources. Milt and roe, the reproductive constituents of fish, are known to contain a high concentration of nutritional content. Bioactive peptides derived from these constituents have shown several biological activities including antihypertensive, antibacterial, anticoagulant, anti‐inflammatory, anti‐obesity, anti‐cancer, and antioxidant activities. These peptides are commonly extracted by enzymatic hydrolysis and purified by different chromatographic methods according to their mass, molecular size, and composition. This review discusses the approaches to produce, purify, and characterise the protein hydrolysates from fish milt and roe and delves into the compositions of the nutraceutical compounds derived from milt and roe. The review also highlights the bioactive properties of the milt and roe‐derived peptides that can have potential applications in the food, nutraceutical, pharmaceutical, and cosmeceutical industries.

Bioactive potential of unpurified hydrothermal xylooligosaccharides: Implications for prebiotic formulations from sugarcane bagasse

This study explored the bioactive potential of xylooligosaccharides (XOS) obtained from sugarcane bagasse through one-step hydrothermal process approach, applied here without the typical purification or further processing steps commonly required to produce XOS for use as prebiotic. We investigated various processing conditions to optimize the yield and biofunctional properties of these unpurified, hydrothermally produced XOS-rich hemicellulose hydrolysates from sugarcane bagasse. The prebiotic efficacy of these unpurified XOS-rich hydrolysates was evaluated by their ability to support the metabolism of bifidobacteria in anaerobic fermentation. The results revealed that the chain length of XOS significantly influenced their effectiveness as a carbon source, with longer chains (beyond hexoses) being less efficient. Despite the presence of lignin and sugar degradation by-products, generally considered detrimental in such processes, they did not negatively affect bifidobacteria growth. In addition, variations in the degree of acetyl substitutions on the XOS mildly influenced the production of short-chain fatty acids. Importantly, unpurified XOS-rich hydrolysates produced under selected hydrothermal conditions demonstrated bioactive performance that was comparable to, or even superior to, commercial prebiotics. These findings confirm the practical viability of using unpurified, hydrothermally derived XOS-rich hydrolysates from sugarcane bagasse as prebiotics, emphasizing the innovative approach of eliminating purification and additional processing, thereby simplifying the production process while still maintaining high prebiotic efficacy.

Bioactive Properties of Enzymatic Gelatin Hydrolysates Based on In Silico, In Vitro, and In Vivo Studies.

This current study aims to analyze the potential bioactivities possessed by the enzymatic hydrolysates of commercial bovine, porcine, and tilapia gelatins using bioinformatics in combination with in vitro and in vivo studies. The hydrolysate with superior inhibition of angiotensin converting enzyme (ACE) activity was used to treat the D-galactose (DG)-induced amnesic mice. In silico digestion of the gelatins led to the identification of peptide sequences with potential antioxidant, ACE-inhibitory, and anti-amnestic properties. The results of in vitro digestion revealed that the <1 kDa peptide fraction of porcine gelatin hydrolysate obtained after 1 h digestion with papain (PP) (PP1, <1 kDa) potently inhibited ACE, acetylcholinesterase, and prolyl endopeptidase activities at 87.42%, 21.24%, and 48.07%, respectively. Administering the PP1 to DG-induced amnesic mice ameliorated the spatial cognitive impairment and Morris water maze learning abilities. The dentate area morphology in the PP1-treated mice was relatively similar to the control group. In addition, PP1 enhanced the antioxidant capacity in the DG-induced amnesic mice. This study suggests that PP1 could serve as a potential treatment tool against oxidative stress, hypertension, and neurodegenerative diseases.

Theoretical investigation of complexes of uranyl(II), vanadyl(II) and zirconyl(II) with vitamin B13 as candidate compounds as anti-nonalcoholic fatty liver disease and Diabetes mellitus targets

Density functional theory (DFT) calculations were carried out utilizing the B3LYP functional in conjunction with the 6-311G++ and LanL2DZ basis sets to explore the molecular properties and geometries of Vitamin (Vit) B13 and its complexes with Uranyl (II), Vanadyl (II), and Zirconyl (II). The optimized structures, molecular electrostatic potential maps, key molecular properties, and HOMO-LUMO energy gaps of these compounds were systematically examined to gain insights into their electronic characteristics and stability. Bioactivity screenings of the synthesized complexes were performed using molecular docking studies to investigate their interactions with diabetes mellitus (DM) target proteins, specifically the Insulin Receptor (IR) (PDB ID: 1IR3) and the peroxisome proliferator-activated receptor-γ (PPARγ) (PDB ID: 3K8S). These receptors play pivotal roles in the PPAR and AMP-activated protein kinase (AMPK) signaling pathways, which are essential for protecting against nonalcoholic fatty liver disease (NAFLD). The docking results highlighted the binding affinities and potential bioactivity of Vit B13 and its metal complexes, suggesting their promise as therapeutic agents against DM and NAFLD. This comprehensive computational study provides valuable insights into the molecular interactions and electronic properties of these compounds, paving the way for further experimental validation and potential pharmaceutical applications. KEY WORDS: Vitamin B13, Metal complexes, Diabetes mellitus, Molecular docking, DFT Bull. Chem. Soc. Ethiop. 2024, 38(6), 1743-1757. DOI: https://dx.doi.org/10.4314/bcse.v38i6.19

Solid-state fermentation with Bacillus subtillis co-cultured with probiotic Lactobacillus spp. enhances the bioactive peptides, nutritional and antioxidative potentials of tamarind seed

The effect of natural or controlled solid-state fermentation using single or mixed probiotic strains on the nutritional, bioactive and phytochemical constituents, and antioxidant activities of tamarind seeds was evaluated. Tamarind seeds were subjected to either controlled solid-state fermentation (37 °C, 72 h) using either Bacillus subtilis only or Bacillus subtilis co-cultured with probiotics Lactobacillus spp. (Lactobacillus fermentum, Lactobacillus rhamnosus GG, Lactobacillus brevis, and Lactobacillus delbrueckii) or natural fermentation while unfermented tamarind seeds served as control. The changes in the nutritional composition, peptide content, antioxidative properties (Ferric reducing antioxidant power (FRAP) and DPPH radical scavenging activities) and total viable count of probiotics in fermented tamarind seed were evaluated using standard methods. The peptide content, crude protein, fat, and fibre (100.19 mg/g, 51.35, 9.50 and 5.10%), and FRAP and DPPH (0.55 and 21.60%) in unfermented tamarind seed were significantly (p < 0.05) lower than fermented tamarind seed (271.00–308 mg/g, 12, 62.84–64.02, 12.21–13.11 and 6.01–6.90, and 1.42–2.92 and 26.66–35.70%, respectively), after 72 h of fermentation. The total viable count in the tamarind seed fermented with Bacillus subtilis only was 1.2 × 109 CFU/g while that co-cultured with probiotics ranged from 6 × 108 to 9.9 × 108 CFU/g after 72 h of fermentation. This study showed that a controlled solid-state fermentation using probiotics Lactobacillus co-cultured with Bacillus subtilis can significantly increase the peptide contents, and enhance the nutritional and antioxidant activities of tamarind seed while producing a condiment with significant probiotic potential.

Insights into phytochemistry and bioactive potential of saffron (Crocus sativus L) petal

AbstractThe principal by‐product of saffron processing, which is produced at a large level but has little market value, is saffron petals. Numerous constituents with profound bioactive potential, including safranal, crocin, picrocin, anthocyanins, glycosides, alkaloids, and kaempferol, are present in saffron petals. Saffron petal is an appropriate substitute for a variety of uses because it is less expensive and produced in greater quantities than saffron stigma. In this review, many pharmaceutical characteristics of the saffron petal have been discussed, including its anti‐bacterial, antifungal, antispasmodic, immunomodulatory, antidepressant, antinociceptive, hepatoprotective, renoprotective, antihypertensive, antidiabetic, and antioxidant activity. This review also provides insight into the pharmacological characteristics of saffron and its components along with the related mechanisms of action.

Enhancement of phenolic compounds bioaccessibility in jabuticaba wine through fermentation by Saccharomyces cerevisiae

Jabuticaba (Plinia cauliflora), a fruit native to Brazil, is known for the high phenolic content in its peel, which is usually discarded. The development of jabuticaba wine is an alternative for better nutritional and technological utilization of the fruit. In this context, the study is the first to investigate the biotransformation of phenolic compounds in jabuticaba during alcoholic fermentation by Saccharomyces cerevisiae and maturation. The research also explored the antioxidant and antiproliferative effects of the beverages, as well as their ability to inhibit α-glucosidase and lipase. Fermentation of jabuticaba significantly increased total phenolic compounds (4.91 ± 0.07-fold), total anthocyanins (5.62 ± 1.17-fold), cyanidin-3-glucoside (2.05 ± 0.74-fold), gallic acid (57.02 ± 3.70-fold), and protocatechuic acid (3.70 ± 0.51-fold), as well as the bioaccessibility of these compounds. The beverages also showed antiproliferative effects against cancer cells, antioxidant activities, and enzyme inhibition properties. Maturation at 4 ± 2 °C for 30 days reduced the cytotoxicity of the samples. Despite a reduction in phenolic concentration after digestion, the samples retained bioactive potential. These results establish reference data on the chemical composition and bioactive potential of jabuticaba wine.

Cookies Fortified with Polyphenols Extracts: Impact on Phenolic Content, Antioxidant Activity, Inhibition of α-Amylase and α-Glucosidase Enzyme, Colour and Sensory Attractiveness.

The goal of the research was to determine the impact of fortification with polyphenolic compounds on (i) sensory attractiveness (global satisfaction, appearance, colour, odour, flavour, sweetness, bitterness), (ii) content of polyphenols and colour (L*, a*, b*) after the baking process and (iii) their bioactive potential (antioxidants activity and inhibiting of α-amylase and α-glucosidase enzyme). Fortification was made with extracts of polyphenolic compounds of selected plant raw materials rich in polyphenols from quince (fruits), tilia (flowers), pomegranate (skin), passion fruit (endocarp), sour cherries (leaves), haskap and chokeberry (berries), silver skin (coffee beans), rosehip (seeds). Depending on the nature of the polyphenol extract, flavan-3-ols (monomeric and polymeric), phenolic acid, flavonols and anthocyanins were identified in the product in amounts ranging from 53.7 to 212.6 mg/100 g DM. Cookies' colour (L*, a*, b*) depended on the type of polyphenol extract used for fortification. Cookies with haskap, chokeberry and sour cherry presented the highest antioxidant potential. Cookies with chokeberry, haskap and rosehip presented high activity in inhibiting α-amylase (65.5, 60.6 and 62.2% of inhibition, respectively), but cookies with haskap, silver skin and quince in inhibiting α-glucosidase activity (23.0, 20.4 and 21.4% of inhibition, respectively). In the sensory evaluation, the most attractive were cookies with rosehip and pomegranate (6.3 and 5.8 score, respectively), but the lowest ratings were given to cookies with passion fruit and silver skin but especially quince cookies, which obtained the lowest desirability (3.7 score). The acceptability of fortified cookies was determined to the least extent by monomeric flavan-3-ols and phenolic acids (in minus in odour/flavour, bitterness, sweetness and global satisfaction), but anthocyanins, polymeric procyanidins and flavonols had the most significant positive impact on consumer acceptance of the assessed features, i.e., global satisfaction, odour/flavour, sweetness and bitterness (positive consumer drivers).

Synthesis, antifungal activity, and 3d-QSAR study of L-carvone-based pyrazole-oxime ester compounds

Natural products can provide versatile substructures with potential bioactivity and biocompatibility for exploring bioactive compounds. Herein, to explore novel natural product-derived antifungal agents, 21 unreported L -carvone-based pyrazole-oxime ester compounds 6a-6u were synthesised using L-carvone as raw material, and structurally characterised by means of FT-IR,1H NMR,13C NMR, and HRMS. The results of the in vitro bioactivity tests showed that the target compounds exhibited certain antifungal activity against the eight tested plant fungi at the concentration of 50 mg/L, especially for Physalospora piricola. The inhibition rates of compounds 6e (R = m-Cl) and 6c (R = m-F) against P. piricola were 88.3% and 83.9%, respectively, both better than that of the positive control chlorothalonil. Compound 6e (R= m-Cl) with the most significant antifungal activity deserves further investigation as the potential leading compound. In addition, the structure-activity relationships (SARs) of the target compounds were investigated by establishing an effective three-dimensional quantitative structure-activity relationship (3D-QSAR) model.

Biochemical Characterization of Recombinant Enterococcus faecalis EntV Peptide to Elucidate Its Antihyphal and Antifungal Mechanisms against Candida albicans.

Candida albicans is a common opportunistic fungus in humans, whose morphological switch between yeast and hyphae forms represents a key virulence trait. Developing strategies to inhibit C. albicans hyphal growth may provide insights into designs of novel antivirulent therapeutics. Importantly, the gut commensal bacterium, Enterococcus faecalis, secretes a bacteriocin EntV which has potent antivirulent and antifungal effects against C. albicans in infection models; however, hampered by the challenges to access large quantities of bioactive EntV, the detailed understanding of its mechanisms on C. albicans has remained elusive. In this work, we biochemically reconstituted the proteolytic cleavage reaction to obtain recombinant EntV88-His6 on a large preparative scale, providing facile access to the C-terminal EntV construct. Under in vitro C. albicans hyphal assay with specific inducers, we demonstrated that EntV88-His6 exhibits potent bioactivity against GlcNAc-triggered hyphal growth. Moreover, with fluorescent FITC-EntV88-His6, we revealed that EntV88-His6 enters C. albicans via endocytosis and perturbs the proper localization of the polarisome scaffolding Spa2 protein. Our findings provide important clues on EntV's mechanism of action. Surprisingly, we showed that EntV88-His6 does not affect C. albicans yeast cell growth but potently exerts cytotoxicity against C. albicans under hyphal-inducing conditions in vitro. The combination of EntV88-His6 and GlcNAc displays rapid killing of C. albicans, rendering it a promising antivirulent and antifungal agent.

Characterising the Metabolomic Diversity and Biological Potentials of Extracts from Different Parts of Two Cistus Species Using UHPLC-MS/MS and In Vitro Techniques.

This study investigates the biochemical composition and biological properties of different parts (leaves, roots, and twigs) of two Cistus species (Cistus monspeliasis and Cistus parviflorus). The extracts were analysed using UHPLC-MS/MS to determine their chemical profiling. A range of antioxidant assays were performed to evaluate the extract's antioxidant capabilities. The enzyme inhibition studies focused on acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-amylase, and α-glucosidase and tyrosinase. In addition, the study examined the antimicrobial effects on different bacteria and yeasts and evaluated the toxicity using the MTT assay. Quinic acid, citric acid, gallic acid, catechin, quercetin derivatives, kaempferol, myricetin, ellagic acid, prodelphinidins, procyanidins, scopoletin, and flavogallonic acid dilactone are the main bioactive compounds found in both species. In enzyme inhibition assays, C. monspeliasis roots exhibited significant activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with the values of 2.58 ± 0.02 mg GALAE/g and 11.37 ± 1.93 mg GALAE/g, respectively. Cytotoxicity studies showed mostly weak toxicity, with some samples moderately reducing viability in RAW and HepG2 cells. These findings underscore the diverse biochemical profiles and bioactive potential of Cistus species, suggesting their utility as natural sources of antioxidants and enzyme inhibitors for pharmaceutical and nutraceutical development.

Nanoencapsulation of quinoa oil enhanced the antioxidant potential and inhibited digestive enzymes

Quinoa oil is rich in unsaturated fatty acids and vitamin E, but its instability limits its application in food, pharmaceutical, and cosmetic products. Nanoencapsulation emerges as a promising strategy to promote water dispersibility, preserve and enhance functional properties, and increase the bioavailability of bioactive compounds. This study encapsulated quinoa oil through O/W emulsification, using porcine gelatin (OG) and isolated whey protein (OWG) as encapsulating agents. The particles were characterized by different physical and chemical methods and evaluated in vitro for cytotoxicity using Chinese hamster ovary (CHO) cells, human hepatocarcinoma cells (HepG2) and epithelial cells, and bioactive potential through the determination of Total Antioxidant Capacity (CAT) (acidic and neutral media) and iron chelation, and inhibition of digestive enzymes (α-amylase and amyloglucosidase). OG and OWG particles presented smooth surfaces, with an average size between 161 ± 7 and 264 ± 6 nm, with a polydispersity index of 0.11 ± 0.03 and 0.130 ± 0.04, encapsulation efficiency of 74 ± 1.47 % and 83 ± 2.92 %, and water dispersibility >70 %, respectively. Free and nanoencapsulated quinoa oil did not show cytotoxic effects (cell viability >70 %). Nanoencapsulation promoted the enhancement of the antioxidant activity of quinoa oil in the range of 50–63 % in a neutral medium and 96–153 % in an acidic medium than free oil (p < 0.05). OG and OWG also enhanced the inhibition of the enzymes α-amylase (by 5–7 %) and amyloglucosidase (6–9 times more) than free oil (p < 0.05). The results showed that nanoencapsulation increased the potential for quinoa oil application, enabling the development of innovative products.

Optimizing workflow efficiency for analyzing low molecular weight endogenous peptides in colostrum.

Bovine milk and colostrum play pivotal roles in the nutritional support of both human and bovine infants. Colostrum, the initial milk secretion, is crucial for neonatal growth, providing essential nutrients, growth factors, immunity, and defense mechanisms through a diverse array of bioactive compounds, including bioactive proteins and peptides. Peptidomics, leveraging the potential health benefits of peptides derived from food and body fluids, has become prominent in contemporary research. Endogenous peptides (EPs) have gained notable scientific and commercial interest due to their potential biofunctional significance in areas such as immune health, antimicrobial, anti-inflammatory, antihypertensive, and antioxidative studies. In this investigation, we aimed to extract and analyze low molecular weight EPs from colostrum using four distinct peptide extraction methods, previously employed for EPs extraction from other bodily fluids. The efficiency of these methods was systematically compared and analysed to identify the most effective extraction technique for maximizing the identification of low molecular weight EPs from colostrum. This study represents a pioneering effort as no prior research has systematically compared different extraction methods for low molecular weight EPs from colostrum. Given the unique physical and chemical composition of colostrum compared to milk and other body fluids, a comprehensive analysis of EPs extraction methods was deemed essential. In the present study, we successfully extracted over 3200 EPs from colostrum using trichloroacetic acid (TCA) and a molecular weight cut off (MWCO) extraction method. The findings of this study revealed the extraction of EPs from colostrum, demonstrating potential inherent bioactivities as predicted by in silico tools.

Unveiling the Bioactive Potential of Bacterial Isolates from Extreme Environments of Pakistan by In Vitro and In Silico Approaches.

The soil hosts a wide array of bacterial species capable of producing diverse bioactive compounds. This research aimed to screen bacterial isolates for their bioactive potential from extreme environments in Pakistan. Out of the 69 isolates examined, only 7 exhibited antagonistic activity against Bacillus sp. and Escherichia coli test strains. Notably, the B. cereus DS-2 strain demonstrated the highest antibacterial potential (31mm and 15mm) against the Bacillus and E. coli test strains, respectively. Mode-of-action studies suggested that the crude extract might have induced morphological abnormalities in the Bacillus sp. (test strain), causing cell contraction, chain breakage, and deformation. Furthermore, the B. cereus DS-2 strain displayed significant antioxidant potential (64.8%) as revealed by the 2,2-Diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay. Thin-layer chromatography (TLC) of the DS-2crude extract led to the separation of six components, with only spots 3 and 4 exhibiting the antibacterial potential (3mm and 5mm, respectively). Subsequently, gas chromatography-mass spectrometry (GC-MS) analysis of the bioactive fraction extracted from TLC revealed the presence of diisooctyl phthalate, dibutyl phthalate, hexadecanoic acid methyl ester, and octadecanoic acid methyl ester. Molecular docking analysis of diisooctyl phthalate and dibutyl phthalate revealed their binding affinity against E. coli and Bacillus sp. targets. ADMET analysis confirmed the solubility, toxicity, and drug-like properties of the ligands based on Lipinski's rule of five. Current findings suggest that these compounds hold promise as antibacterial agents in drug development. This study underscores the diverse microbial community present in extreme environments and highlights the versatile applications of natural products derived from these strains.

Spatial distribution of antioxidant activity in baguette and its modulation of proinflammatory cytokines in RAW264.7 macrophages

Baguette is a globally acclaimed bakery staple, composed by a crispy crust and soft crumb, both containing Maillard reaction products (MRPs) with potential bioactivities. However, MRPs’ impacts on the nutritional and health attributes of baguette, particularly in terms of cellular and biological functions, are yet to be clearly elucidated. This study chemically characterizes the crust and crumb of baguettes and investigates the influence of the Maillard reaction on baguette’s nutritional profile, especially in the antioxidant and anti-inflammatory effects. The findings indicate an increase in browning intensity and advanced glycation end products (AGEs) from the baguette’s interior to its exterior, alongside a significant rise in the antioxidant capacity of the crust, suggesting the Maillard reaction’s role in boosting antioxidative properties. Both the crust and crumb demonstrated strong cytocompatibility with immune cells, capable of reducing cellular oxidative stress and regulating intracellular free radical levels. The crust effectively countered peroxyl radical-induced cell membrane hyperpolarization by 91% and completely neutralized the suppression of oxygen respiration in mitochondria, displaying higher efficacy than the crumb. In contrast, crumb extracts were more potent in inhibiting lipopolysaccharide-induced expression of proinflammatory cytokines, such as interleukins-1β (IL-1β) and IL-6, in macrophages. It could provide the fundamental data and cell-based approach for investigating the biological impacts of bread on immune responses, contributing to the refinement and supplementation of nutritional recommendations.

Antifouling activity and ecotoxicological profile of the cyanobacterial oxadiazine nocuolin A

Pursuing effective and biocompatible natural compounds to supplant current biocidal antifouling (AF) technologies remains crucial and challenging. Among natural products hosts, cyanobacteria are recognized as producers of bioactive secondary metabolites that are underexplored in terms of anti-biofilm and AF potential. Nocuolin A, a natural oxadiazine previously isolated and known to be produced by different cyanobacterial strains, has demonstrated bioactive potential, particularly against tumor cell lines. Considering this potential and its exquisite chemical structure, here nocuolin A was investigated as a potential natural AF agent through an integrative approach including AF bioactivity testing across distinct levels of biological organization, mode of action assessment, ecotoxicity evaluation, and ecological risk predictions. Nocuolin A was found to inhibit the settlement of mussel (Mytilus galloprovincialis) plantigrades (EC50 = 3.905 μM) while showing no toxicity to this biofouling species (LC50 > 100 μM). Additionally, while exhibiting no inhibitory activity against the growth of five marine biofilm-forming bacterial strains, it significantly suppressed the growth of the marine biofilm-forming diatom Navicula sp. (EC50 = 1.561 μM), and had a lethal effect on this diatom species (>3.1 μM). The AF targets of nocuolin A on mussel plantigrades revealed no correlation with acetylcholinesterase and tyrosinase metabolic processes; however, proteins involved in oxidative stress, muscle regulation, and energy production were highlighted. The results also provide insights into the ecological risk of nocuolin A, including its ecotoxicity against Artemia salina nauplii (LC50 = 2.480 μM), Amphibalanus amphitrite nauplii (LC50 = 0.0162 μM), and Danio rerio embryos (LC50 = 0.0584 μM). When matching these results with simulated environmental values, nocuolin A was deemed a considerable threat to the ecosystems. While this research highlights the AF activity of nocuolin A, it also emphasizes the potential adverse environmental impact when applied in preventive coatings.

Social wasp-associated Tsukamurella sp. strains showed promising biosynthetic and bioactive potential for discovery of novel compounds

In the face of escalating antibiotic resistance, the quest for novel antimicrobial compounds is critical. Actinobacteria is known for producing a substantial fraction of bioactive molecules from microorganisms, nonetheless there is the challenge of metabolic redundancy in bioprospecting. New sources of natural products are needed to overcome these current challenges. Our present work proposes an unexplored potential of Neotropical social wasp-associated microbes as reservoirs of novel bioactive compounds. Using social wasp-associated Tsukamurella sp. strains 8F and 8J, we aimed to determine their biosynthetic potential for producing novel antibiotics and evaluated phylogenetic and genomic traits related to environmental and ecological factors that might be associated with promising bioactivity and evolutionary specialization. These strains were isolated from the cuticle of social wasps and subjected to comprehensive genome sequencing. Our genome mining efforts, employing antiSMASH and ARTS, highlight the presence of BGCs with minimal similarity to known compounds, suggesting the novelty of the molecules they may produce. Previous, bioactivity assays of these strains against bacterial species which harbor known human pathogens, revealed inhibitory potential. Further, our study focuses into the phylogenetic and functional landscape of the Tsukamurella genus, employing a throughout phylogenetic analysis that situates strains 8F and 8J within a distinct evolutionary pathway, matching with the environmental and ecological context of the strains reported for this genus. Our findings emphasize the importance of bioprospecting in uncharted biological territories, such as insect-associated microbes as reservoirs of novel bioactive compounds. As such, we posit that Tsukamurella sp. strains 8F and 8J represent promising candidates for the development of new antimicrobials.