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The goal of the current work was to assess the nutritional profile and phytochemical properties of cucurbit (Cucurbita maxima L.) seeds, seed oils and oil extraction by-products (e.g., seed-cakes). Our results suggest a high nutritional value for both cucurbit seeds and cucurbit cake, while γ-tocopherol was the richest compound, with traces of α, β and δ-tocopherol compounds also detected. Regarding the free sugars composition, there were recorded significant statistical differences between seeds and cucurbit seed-cake, although sucrose content was the highest for both matrices (1.97 and 2.9 g/100 g dw, respectively) followed by trehalose (0.26 and 0.25 g/100 g dw, respectively), fructose (0.20 and 0.34 g/100 g dw, respectively) and glucose (0.21 and 0.19 g/100 g dw, respectively). In terms of organic acids, oxalic was the only compound detected in seed cake (0.006 g/100 g dw), while in seeds only traces of oxalic and malic acid were detected. In relation to fatty acid composition, linolenic acid was the most abundant compound in both seeds and seed-cake (43.9% and 41.5%, respectively), while oleic acid (37.0% and 36.3%, respectively), palmitic acid (12.2% and 14.0%, respectively) and stearic acid (4.83% and 5.46%, respectively) were detected in lesser amounts. Moreover, polyunsaturated fatty acids (PUFA) were the major fatty acids class (44.5% and 42.3% in seeds and seed cake, respectively) compared to monounsaturated fatty acids (MUFA; 37.4% and 36.7% in seeds and seed cake, respectively) and saturated fatty acids (SFA; 18.1% and 21.0% in seeds and seed cake, respectively) which were detected in lower amounts. Furthermore, the tested extracts did not present any cytotoxic or hepatoxic activity at the maximum tested concentration (GI50 > 400 μg/mL), while seed oils presented satisfactory antimicrobial properties with inhibitory activity against the studied bacterial strains and fungi. Our findings provide valuable knowledge regarding the exploitation of pumpkin seeds and seed by-products as valuable natural sources of nutrients and phytochemicals in the food industry sector within the context of a circular economy. [ABSTRACT FROM AUTHOR]

Wound healing, a complex physiological process orchestrating intricate cellular and molecular events, seeks to restore tissue integrity. The burgeoning interest in leveraging the therapeutic potential of natural substances for advanced wound dressings is a recent phenomenon. Notably, Sericin, a silk-derived protein, and Chelidonium majus L. (C. majus), a botanical agent, have emerged as compelling candidates, providing a unique combination of natural elements that may revolutionize conventional wound care approaches. Sericin, renowned for its diverse properties, displays unique properties that accelerate the wound healing process. Simultaneously, C. majus, with its diverse pharmacological compounds, shows promise in reducing inflammation and promoting tissue regeneration. As the demand for innovative wound care solutions increases, understanding the therapeutic potential of natural products becomes imperative. This review synthesizes current knowledge on Sericin and C. majus, envisioning their future roles in advancing wound management strategies. The exploration of these natural substances as constituents of wound dressings provides a promising avenue for developing sustainable, effective, and biocompatible materials that could significantly impact the field of wound healing. [ABSTRACT FROM AUTHOR]

Coriander, caraway, and mystical cumin are famous for their aromatic properties and widely used in Moroccan cuisine. The nutritional/phytochemical composition of their seeds (used for food flavoring and preservation) were compared. Their antioxidant, anti-inflammatory, cytotoxic and hepatotoxic effects were also explored. The fat content was similar among the samples (13%), with monounsaturated fatty acids being predominant. The coriander and mystical cumin seeds were extremely rich in C18:1n9c (81 and 85%, respectively) while, in the caraway, C18:1n12 (25%) was found together with C18:1n9c (32%). The caraway seeds also presented a higher proportion of C18:2n6c (34%) than the other seeds (13 and 8%, correspondingly). γ-Tocotrienol was the major vitamin E form in all the samples. The caraway seeds contained double the amount of protein (~18%) compared to the other seeds (~8%) but, qualitatively, the amino acid profiles among all seeds were similar. The seeds were also rich in dietary fiber (40–53%); however, differences were found in their fiber profiles. Caraway showed the highest antioxidant profile and anti-inflammatory activity and an LC-DAD-ESI/MSn analysis revealed great differences in the phenolic profiles of the samples. Cytotoxicity (NCI-H460, AGS, MCF-7, and CaCo2) and hepatotoxicity (RAW 264.7) were not observed. In sum, besides their flavoring/preservation properties, these seeds are also relevant source of bioactive compounds with health-promoting activities. [ABSTRACT FROM AUTHOR]

The gut microbiota establishes a mutually beneficial relationship with the host starting from birth, impacting diverse metabolic and immunological processes. Dysbiosis, characterized by an imbalance of microorganisms, is linked to numerous medical conditions, including gastrointestinal disorders, cardiovascular diseases, and autoimmune disorders. This imbalance promotes the proliferation of toxin-producing bacteria, disrupts the host's equilibrium, and initiates inflammation. Genetic factors, dietary choices, and drug use can modify the gut microbiota. However, there is optimism. Several therapeutic approaches, such as probiotics, prebiotics, synbiotics, postbiotics, microbe-derived products, and microbial substrates, aim to alter the microbiome. This review thoroughly explores the therapeutic potential of these microbiota modulators, analysing recent studies to evaluate their efficacy and limitations. It underscores the promise of microbiota-based therapies for treating dysbiosis-related conditions. This article aims to ensure practitioners feel well-informed and up to date on the most influential methods in this evolving field by providing a comprehensive review of current research. [ABSTRACT FROM AUTHOR]

Since the early twentieth century, research on vitamins has revealed their therapeutic potential beyond their role as essential micronutrients. Riboflavin, known as vitamin B2, stands out for its unique characteristics. Despite numerous studies, riboflavin remains vital, with implications for human health. Abundantly present in various foods, riboflavin acts as a coenzyme in numerous enzymatic reactions crucial for human metabolism. Its role in energy production, erythrocyte synthesis, and vitamin metabolism underscores its importance in maintaining homeostasis. The impact of riboflavin extends to neurological function, skin health, and cardiovascular well-being, with adequate levels linked to reduced risks of various ailments. However, inadequate intake or physiological stress can lead to deficiency, a condition that poses serious health risks, including severe complications. This underscores the importance of maintaining sufficient levels of riboflavin for general wellness. The essential role of riboflavin in immune function further emphasises its significance for human health and vitality. This paper examines the diverse effects of riboflavin on health and stresses the importance of maintaining sufficient levels for overall well-being. [ABSTRACT FROM AUTHOR]

The Lamiaceae family, which includes several well-known aromatic plants, is scientifically relevant due to its essential oils (EOs). In this work, four EOs from Mediterranean species, namely Origanum vulgare L., Rosmarinus officinalis L., Salvia officinalis L., and Thymus vulgaris L., were evaluated for their volatile profiles and the biological activity in vitro to assess their potential use in the food and cosmetic sector. GC/MS analysis revealed dominant compounds, such as carvacrol, thymol, and eucalyptol. Regarding biological action, the samples exhibited antioxidant, cytotoxic, anti-inflammatory, antimicrobial, and antifungal activities, with O. vulgare and T. officinalis standing out. T. vulgaris showed the lowest EC50 in the reducing power assay, and O. vulgare had the lowest EC50 in the DPPH assay. Most EOs also displayed excellent anti-inflammatory responses and antifungal properties, with O. vulgare and T. vulgaris also demonstrating antibacterial activity. All EOs from Mediterranean species showed cytotoxicity against tumoral cell lines. Overall, the selected EOs stood out for their interesting bioactivities, with the obtained results underscoring their potential as natural preservatives and bioactive agents in various industrial applications, including food, pharmaceuticals, and cosmetics. [ABSTRACT FROM AUTHOR]

Red rice has been proposed as a super-food. Accordingly, the nutritional properties (AOAC), as well as its chemical composition, including sugars (HPLC-RI), organic acids (UFLC-PDA), tocopherols (HPLD-FD), and phenolic compounds (LC-DAD-ESI/MSn), together with the main bioactive properties (antioxidant, cytotoxic, antiproliferative, and antibacterial activities), were evaluated to access its nutritional benefits and health improvement potential. The most abundant macronutrients found were carbohydrates (87.2 g/100 g dw), proceeded by proteins (9.1 g/100 g dw), fat (2.6 g/100 g dw), and ash (1.1 g/100 g dw). Sucrose and raffinose were the only detected sugars, with sucrose presenting the maximum concentration (0.74 g/100 g dw). MUFAs and PUFAs were the predominant fatty acids (40.7% and 31%, respectively). Among the two detected tocopherol isoforms, γ-tocopherol (0.67 mg/100 g dw) predominated over α-tocopherol. The phenolic compounds profile, majorly composed of flavan-3-ols, should be associated with the detected bioactivities, which may provide biological benefits to human health beyond the primary nutritional effect. Overall, the bioactive potential of red rice was comprehensively accessed. [ABSTRACT FROM AUTHOR]

Chronic diseases (CD) may result from a combination of genetic factors, lifestyle and social behaviours, healthcare system influences, community factors, and environmental determinants of health. These risk factors frequently coexist and interact with one another. Ongoing research and a focus on personalized interventions are pivotal strategies for preventing and managing chronic disease outcomes. A wealth of literature suggests the potential involvement of gut microbiota in influencing host metabolism, thereby impacting various risk factors associated with chronic diseases. Dysbiosis, the perturbation of the composition and activity of the gut microbiota, is crucial in the etiopathogenesis of multiple CD. Recent studies indicate that specific microorganism-derived metabolites, including trimethylamine N-oxide, lipopolysaccharide and uremic toxins, contribute to subclinical inflammatory processes implicated in CD. Various factors, including diet, lifestyle, and medications, can alter the taxonomic species or abundance of gut microbiota. Researchers are currently dedicating efforts to understanding how the natural progression of microbiome development in humans affects health outcomes. Simultaneously, there is a focus on enhancing the understanding of microbiome–host molecular interactions. These endeavours ultimately aim to devise practical approaches for rehabilitating dysregulated human microbial ecosystems, intending to restore health and prevent diseases. This review investigates how the gut microbiome contributes to CD and explains ways to modulate it for managing or preventing chronic conditions. [ABSTRACT FROM AUTHOR]

Despite past efforts towards therapeutical innovation, cancer remains a highly incident and lethal disease, with current treatments lacking efficiency and leading to severe side effects. Hence, it is imperative to develop new, more efficient, and safer therapies. Bee venom has proven to have multiple and synergistic bioactivities, including antitumor effects. Nevertheless, some toxic effects have been associated with its administration. To tackle these issues, in this work, bee venom-loaded niosomes were developed, for cancer treatment. The vesicles had a small (150 nm) and homogeneous (polydispersity index of 0.162) particle size, and revealed good therapeutic efficacy in in vitro gastric, colorectal, breast, lung, and cervical cancer models (inhibitory concentrations between 12.37 ng/mL and 14.72 ng/mL). Additionally, they also revealed substantial anti-inflammatory activity (inhibitory concentration of 28.98 ng/mL), effects complementary to direct antitumor activity. Niosome safety was also assessed, both in vitro (skin, liver, and kidney cells) and ex vivo (hen's egg chorioallantoic membrane), and results showed that compound encapsulation increased its safety. Hence, small, and homogeneous bee venom-loaded niosomes were successfully developed, with substantial anticancer and anti-inflammatory effects, making them potentially promising primary or adjuvant cancer therapies. Future research should focus on evaluating the potential of the developed platform in in vivo models. [ABSTRACT FROM AUTHOR]

Nowadays, bee products are commended by consumers for their medicinal and dietary properties. This study aimed to differentiate between monofloral bee pollens originating from Portugal using phenolic and volatile profiles and investigate their antioxidant and cytotoxic activity. Total phenolic and flavonoid compounds were recorded between 2.9–35.8 mg GAE/g and 0.7–4.8 mg QE/g, respectively. The LC/DAD/ESI-MSn analytical results allowed us to identify and quantify a total of 72 compounds, including phenolic and phenylamide compounds, whereas GC-MS results revealed the presence of 49 different compounds, mostly ketones, aldehydes, esters, hydrocarbons, and terpenes. The highest DPPH• radical scavenging activity, EC50: 0.07 mg/mL, was recorded in the sample dominated by Castanae sp. pollen, whereas the Rubus sp. (1.59 mM Trolox/mg) and Cistaceae sp. (0.09 mg GAE/g) pollen species exhibited the highest antioxidant activity in ABTS•+ and reducing power assays, respectively. Regarding the anti-carcinogenic activity, only Carduus sp. showed remarkable cytotoxic potential against MCF-7. [ABSTRACT FROM AUTHOR]

The aim of this study was to evaluate the chemical profile of the flesh and yield parameters of Greek pumpkin genotypes, including nine local landraces and two commercially available cultivars, focusing on valorizing the genetic pool of Cucurbita sp. with high added value products. Yield parameters (mean fruit weight and total fruit yield) recorded high variability with genotypes V8 and V2 showing the highest fruit yield. Moreover, genotype V11 was the most abundant in glucose and total sugars and scored the highest sweetness index suggesting good taste and promising marketing attributes. The highest antioxidant activity (OxHLIA assay) was assessed in the V8 genotype, while the V2 genotype showed the highest α-, β- and total tocopherols content. Oxalic acid was the main organic acid, followed by malic and citric acids, while organic acid composition varied among the tested genotypes. Moreover, the flesh extracts showed varied antimicrobial activity against several bacteria and fungi, while no toxicity against non-tumor cells was recorded. In conclusion, our results make evident the presence of high innate variability in terms of crop performance, chemical composition and bioactive properties not only between the different genotypes but also at the intra-populational level. This finding is of high importance for the valorization of the local genetic pool of Cucurbita species through the selection of elite genotypes with high yield and quality of fruit, contributing to the conservation of valuable genetic material and limitation of the risk of genetic erosion due to neglect of local landraces. [ABSTRACT FROM AUTHOR]

Background: Grape agri-food wastes, such as skin, seeds, and other discarded by-products, contain phytochemical compounds that offer potential health benefits. Methods: This study aimed to investigate the polyphenol composition and bioactivities of different extracts obtained from grape marc and seeds, with the goal of exploring their potential for application as natural food additives. Results: Regardless of the extraction method used (dynamic maceration, ultrasound-assisted extraction (UAE), and microwave-assisted extraction (MAE)), all extracts exhibited relatively high concentrations of phenolic compounds. The chemical characterization of the extracts revealed the presence of specific compounds and chemical groups associated with each extraction methodology. Moreover, the extracts displayed satisfactory antioxidant activities, especially in inhibiting lipoperoxidation as assessed by the TBARS assay. Additionally, the extracts demonstrated effective inhibition against different strains of bacteria and fungi known as food contaminants. Taken together, these findings indicate that those extracts have the potential to be tested as natural antioxidants and preservatives with sustainable origins in food and beverage systems. Among the extraction methods evaluated, traditional maceration and UAE provided extracts with the highest antioxidant and antimicrobial activities. Conclusions: Our results suggest the opportunity to explore grape marc and seeds discarded by the winery industry in Portugal as natural sources of bioactive compounds, which could be employed as functional food ingredients or technological additives. The valorization of grape biowastes offers a promising strategy to reduce waste and harness their potential health benefits. [ABSTRACT FROM AUTHOR]

This study assessed the halophyte species Limonium spathulatum (Desf.) as a possible source of natural ingredients with the capacity to inhibit enzymes related to relevant human health disorders and food browning. Extracts using food-grade solvents such as water and ethanol were prepared by maceration from dried L. spathulatum leaves. They were evaluated for in vitro inhibition activity of enzymes such as acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), α-glucosidase, tyrosinase and lipase, related to Alzheimer's disease, type-2-diabetes mellitus, skin hyperpigmentation, and obesity, respectively. These extracts were also appraised for in vitro acute toxicity on tumoral and non-tumoral cell lines and their chemical composition by high-performance liquid chromatography coupled with electrospray ionization mass spectrometry (HPLC-ESI-MS/MS). The extracts were more effective towards BChE than AChE. The best results were obtained with the hydroethanolic and water extracts, with IC50 values of 0.03 mg/mL and 0.06 mg/mL, respectively. The hydroethanolic extract had the highest capacity to inhibit α-glucosidase (IC50: 0.04 mg/mL), higher than the positive control used (acarbose, IC50 = 3.14 mg/mL). The ethanol extract displayed the best inhibitory activity against tyrosinase (IC50 = 0.34 mg/mL). The tested samples did not inhibit lipase and exhibited low to moderate cytotoxic activity against the tested cell lines. The hydroethanolic extract had a higher diversity of compounds, followed by the ethanol and water samples. Similar molecules were identified in all the extracts and were mainly hydroxybenzoic acids, hydroxycinnamic acids, and flavonoids. Taken together, these results suggest that L. spathulatum should be further explored as a source of bioactive ingredients for the food, cosmetic, and pharmaceutical industries. [ABSTRACT FROM AUTHOR]

In this work, a comparison between the extracts of dehydrated yerba mate (Ilex paraguariensis) and bio-waste of yerba mate leaves from the Brazilian industry was made. The incorporation of the functional extract as a preservative/functional ingredient in a pastry product (pancakes) was tested. The individual profile of phenolic compounds was determined by HPLC-DAD-ESI/MS, and the bioactive potential was assessed using in vitro assays for antioxidant, anti-inflammatory, antimicrobial, and cytotoxic activities. The yerba mate extracts revealed a high antimicrobial potential against the tested strains and a very promising antioxidant and anti-inflammatory action. Additionally, revealed a cytotoxic capacity for MCF-7, CaCo and AGS tumor cell-lines. In the three types of pancakes, after 3 days of storage, the chemical and nutritional characteristics remain unchanged, proving the preservative efficiency of the extract. This study showed the benefits of the use bio-waste from agro-industrial sector, focusing on sustainable production and the development of circular economy. [ABSTRACT FROM AUTHOR]

Withania chevalieri, endogenous from Cape Verde, is a medicinal plant used in ethnomedicine with a large spectrum of applications, such as treating skin fungal infections caused by dermatophytes. The aim of this work was to chemically characterize the W. chevalieri crude ethanolic extract (WcCEE), and evaluate its bioactivities as antidermatophytic, antioxidant, anti-inflammatory and anticancer, as well as its cytotoxicity. WcCEE was chemically characterized via HPLC–MS. The minimal inhibitory concentration, minimal fungicidal concentration, time-kill and checkerboard assays were used to study the antidermatophytic activity of WcCEE. As an approach to the mechanism of action, the cell wall components, β-1,3-glucan and chitin, and cell membrane ergosterol were quantified. Transmission electron microscopy (TEM) allowed for the study of the fungal ultrastructure. WcCEE contained phenolic acids, flavonoids and terpenes. It had a concentration-dependent fungicidal activity, not inducing relevant resistance, and was endowed with synergistic effects, especially terbinafine. TEM showed severely damaged fungi; the cell membrane and cell wall components levels had slight modifications. The extract had antioxidant, anti-inflammatory and anti-cancer activities, with low toxicity to non-tumoral cell lines. The results demonstrated the potential of WcCEE as an antidermatophytic agent, with antioxidant, anti-inflammatory and anticancer activity, to be safely used in pharmaceutical and dermocosmetic applications. [ABSTRACT FROM AUTHOR]

Opportunities for the valorisation of agro-industrial residues of the chestnut (Castanea sativa Mill.) production chain have been fostered with the production of multifunctional polyphenol-rich extracts with the potential to be introduced as natural additives or active components in several products. Nonetheless, it is crucial to explore the feasibility of different extracts from the various by-products for these applications through the exhaustive study of their composition and bioactivities without losing sight of the sustainable character of the process. This work aimed at the screening of the phenolic compound composition and bioactivities of different green extracts of chestnut burs, shells and leaves, as the first step to establish their potential application as natural ingredients, primarily as food preservatives. To this end, maceration (MAC) as a conventional extraction method besides ultrasound and microwave-assisted extractions (UAE and MAE) was employed to obtain the extracts from chestnut by-products using water (W) and hydroethanolic solution (HE) as solvents. Phenolic compounds were analysed by HPLC-DAD-(ESI-)MS/MS; the antioxidant capacity was assessed by colourimetric assays, and the antimicrobial activity was evaluated against several strains of food-borne bacteria and fungi. The leaf extracts obtained by MAC-HE and UAE-HE presented the highest concentration of phenolic compounds (70.92 ± 2.72 and 53.97 ± 2.41 mg.g−1 extract dw, respectively), whereas, for burs and shells, the highest recovery of total phenolic compounds was achieved by using UAE-HE and UAE-W (36.87 ± 1.09 and 23.03 ± 0.26 mg.g−1 extract dw, respectively). Bis-HHDP-glucose isomers, chestanin and gallic acid were among the most abundant compounds. Bur extracts (MAC-HE and UAE-HE) generally presented the highest antioxidant capacity as measured by TBARS, while the best results in DPPH and reducing power assays were found for shell extracts (MAE-W and MAC-HE). Promising antibacterial activity was noticed for the aqueous extracts of burs, leaves and hydroethanolic extracts of shells, with emphasis on the MAE-W extract of burs that showed bactericidal activity against E. cloacae, P. aeruginosa and S. aureus (MBC 5 mg.mL−1). Overall, it can be concluded that chestnut by-products, including burs, shells and leaves, are sources of polyphenolic compounds with significant antioxidant and antimicrobial activities. The choice of extraction method and solvent greatly influenced the composition and bioactivity of the extracts. These findings highlight the potential of chestnut by-products for the development of natural additives, particularly for food preservation, while also emphasizing the importance of sustainable utilization of agricultural waste materials. Further research is warranted to optimize extraction techniques and explore additional applications for these valuable bioactive compounds. [ABSTRACT FROM AUTHOR]

Aromatic plants are a remarkable source of natural products. Aloysia citrodora Paláu (Verbenaceae), commonly known as lemon verbena, is a relevant source of essential oils with potential applications due to its lemony scent and bioactive properties. Studies carried out on this species have focused on the volatile composition of the essential oil obtained by Clevenger hydrodistillation (CHD), with little information available on alternative extraction methodologies or the biological properties of the oil. Therefore, this work aimed to compare the volatile composition, antioxidant activity, cytotoxicity, anti-inflammatory and antibacterial activities of the essential oil extracted by conventional hydrodistillation by Clevenger (CHD) and Microwave-Assisted Hydrodistillation (MAHD). Significant differences (p < 0.05) were observed for some compounds, including the two major ones, geranial (18.7–21.1%) and neral (15.3–16.2%). Better antioxidant activity was exhibited by the MAHD essential oil in DPPH radical scavenging and reducing power assays, while no differences were observed in the cellular antioxidant assay. The MADH essential oil also presented higher inhibition against four tumoral cell lines and exhibited lower cytotoxicity in non-tumoral cells as compared with Clevenger-extracted essential oil. In contrast, the latter showed higher anti-inflammatory activity. Both essential oils were able to inhibit the growth of eleven out of the fifteen bacterial strains tested. [ABSTRACT FROM AUTHOR]

Essential oils (EOs) obtained from Juniperus communis L. are frequently used in the production of bioproducts. However, there are no studies regarding industrial crops' production, allowing for better control of the quality and production of juniper EOs. To select the plant material for developing future crops of this species in northern Spain, four locations where this shrub species grows in the wild were selected and samples of both genera were collected. The EOs were obtained by steam distillation, and their chemical composition and bioactivity were evaluated. The results showed that the yield of EOs from male and female samples were within the usual reported ranges, varying between 0.24 and 0.58% (dry basis, d.b.). However, limonene content in three locations varied between 15 and 25%, which is between 100% and 200% higher than the values usually reported for other European countries. The antibacterial activity was determined by broth microdilution and showed that gram-positive bacteria were more susceptible to the tested EOs since, in general, lower MIC values were obtained compared to gram-negatives. The EOs from location 1 (L1F) and 2 (L2M) inhibited the growth of six out of the eight clinical strains tested. Samples from location 1 were particularly effective, exhibiting MBC against two gram-negative (E. coli and P. mirabilis) and one gram-positive bacteria (E. faecalis). Moreover, the majority of the EOs tested showed anti-inflammatory activity. Cytotoxic effect has been demonstrated in tumor cell lines, with the best results observed against gastric carcinoma (AGS) cells (GI50 between 7 to 77 µg/mL). Although generally presenting higher GI50, most samples also inhibited the growth of non-tumoral cells, particularly hepatocytes (PLP2 cells). Therefore, its use for their anti-proliferative activity should consider specific conditions to avoid damaging normal cells. Finally, the results and conclusions obtained led to the selection of the female shrubs from location 1 (L1F) as the plant material to be propagated in order to produce plants for a future juniper crop. [ABSTRACT FROM AUTHOR]

Juniperus communis L. is a species commonly grown in regions of the Northern Hemisphere, and is a good candidate to be cultivated in marginal lands. Plants coming from a pruning performed in a natural population located in Spain were used to assess the yield and quality of different products obtained following the cascade principle. A total of 1050 kg of foliage biomass were crushed, steam-distilled, and separated into fractions to produce biochar and absorbents for the pet industry using pilot plants. The obtained products were analysed. The essential oil, with a yield of 0.45% dry basis and a qualitative chemical composition similar to that described for the berries in international standards or monographs, showed antioxidant activity with promising CAA results (inhibition of 89% of the cell's oxidation). However, regarding antibacterial and antifungal activities, it only inhibited the growth of microorganisms at the maximum concentration tested, 2.5%. Concerning the hydrolate, it did not show bioactivity. Regarding the biochar, whose yield was 28.79% dry basis, interesting results were obtained for its characterisation as a possible soil improver for agronomic purposes (PFC 3(A)). Finally, promising results were obtained regarding the use of common juniper as absorbent, taking into account the physical characterisation and odour control capacity. [ABSTRACT FROM AUTHOR]

The industrial processing of mangosteen (Garcinia mangostana L.) generates high amounts of waste, as ~60% of the fruit is formed by an inedible pericarp. However, its pericarp has been explored as a source of xanthones; nevertheless, studies addressing the recovery of other chemical compounds from such biomass are still scarce. Hence, this study intended to elucidate the chemical composition of the mangosteen pericarp, including fat-soluble (tocopherols and fatty acids) and water-soluble (organic acids and phenolic compound non-xanthones) compounds present in the following extracts: hydroethanolic (MT80), ethanolic (MTE), and aqueous (MTW). In addition, the antioxidant, anti-inflammatory, antiproliferative and antibacterial potentials of the extracts were assessed. The mangosteen pericarp showed a composition with seven organic acids, three tocopherol isomers, four fatty acids and fifteen phenolic compounds. Regarding the extraction of phenolics, the MT80 was the most efficient (54 mg/g extract), followed by MTE (19.79 mg/g extract) and MTW (4.011 mg/g extract). All extracts showed antioxidant and antibacterial activities; however, MT80 and MTE extracts were more efficient than MTW. Only MTW did not show anti-inflammatory properties, whereas MTE and MT80 showed inhibitory activities towards tumor cell lines. Notwithstanding, MTE showed cytotoxicity towards normal cells. Our findings support the idea that the ripe mangosteen pericarp is a source of bioactive compounds, although their recovery is dependent on the extraction solvent. [ABSTRACT FROM AUTHOR]

Plants are rich in bioactive phytochemicals that often display medicinal properties. These can play an important role in the production of health-promoting food additives and the replacement of artificial ones. In this sense, this study aimed to characterise the polyphenolic profile and bioactive properties of the decoctions, infusions and hydroethanolic extracts of three plants: lemon balm (Melissa officinalis L.), sage (Salvia officinalis L.) and spearmint (Mentha spicata L.). Total phenolic content ranged from 38.79 mg/g extract to 84.51 mg/g extract, depending on the extract. The main phenolic compound detected in all cases was rosmarinic acid. The results highlighted that some of these extracts may have the ability to prevent food spoilage (due to antibacterial and antifungal effects) and promote health benefits (due to anti-inflammatory and antioxidant capacities) while not displaying toxicity against healthy cells. Furthermore, although no anti-inflammatory capacity was observed from sage extracts, these stood out for often displaying the best outcomes in terms of other bioactivities. Overall, the results of our research provide insight into the potential of plant extracts as a source of active phytochemicals and as natural food additives. They also support the current trends in the food industry of replacing synthetic additives and developing foods with added beneficial health effects beyond basic nutrition. [ABSTRACT FROM AUTHOR]

Aesculus hippocastanum L., also known as horse chestnut, is an ornamental tree whose seeds are mostly discarded in landfills in the regions where they are grown. However, recent studies have shown that these seeds can be a source of interesting compounds for several industries. This work aimed to chemically characterize horse chestnut seeds at the level of compounds recognized for their wide bioactivity, i.e., organic acids, including phenolic compounds, using chromatographic methodologies (UFLC-DAD and LC-DAD-ESI/MSn). In addition, the bioactivity of these seeds was evaluated by in vitro methodologies, seeking to relate the respective (bio)activity to the compounds present in the endocarp (husk), seed coat (skin), and peeled seed (pulp). The antioxidant activity (lipid peroxidation inhibition and oxidative haemolysis inhibition), antibacterial potential (against Gram-positive and Gram-negative bacteria) and cytotoxicity (in human tumour cell lines and porcine liver primary cells) were evaluated. Kaempferol-O-pentoside-O-hexoside-O-hexoside was the main phenolic identified in the pulp. At the same time, (-)-epicatechin and β-type (epi)catechin dimer were the major phenolics present in husk and skin, respectively. In general, A. hippocastanum extracts presented antioxidant and antibacterial potential, without toxicity up to the maximal tested dose. Overall, these findings anticipate potential applications of A. hippocastanum seeds in food- or pharmaceutical-related uses. [ABSTRACT FROM AUTHOR]

Since the dawn of man, inflammation has been known to humanity, as it is marked by pain. Inflammation processes are related to serious chronic diseases with irreversible damage to the organism, being crucial for the development of anti-inflammatory agents. Among the existing anti-inflammatory drugs, non-steroidal and glucocorticoids are commonly used; however, these compounds have been described as responsible for the increased risk of upper gastrointestinal complications and many other side effects. Therefore, it is not shocking that ethnobotany leads most modern studies on the discovery of anti-inflammatory agents obtained from natural matrices. Extracts from plants and isolated substances have demonstrated anti-inflammatory effects in a set of in vitro and in vivo anti-inflammatory models. This review describes inflammation processes with an emphasis on the most common related diseases, while also describing the most promising natural anti-inflammatory agents, by reporting on their obtention processes, mechanisms of action, and applications. [ABSTRACT FROM AUTHOR]

Coffee is one of the most popular and consumed products in the world, generating tons of solid waste known as spent coffee grounds (SCG), containing several bioactive compounds. Here, the antifungal activity of ethanolic SCG extract from caffeinated and decaffeinated coffee capsules was evaluated against yeasts and filamentous fungi. These extracts had antifungal activity against Candida krusei, Candida parapsilosis, Trichophyton mentagrophytes, and Trichophyton rubrum, all skin fungal agents. Moreover, SCG had fungicidal activity against T. mentagrophytes and T. rubrum. To understand the underlying mechanisms of the antifungal activity, fungal cell membrane and cell wall components were quantified. SCG caused a significant reduction of the ergosterol, chitin, and β-(1,3)-glucan content of C. parapsilosis, revealing the synthesis of this membrane component and cell wall components as possible targets of these extracts. These extracts were cytotoxic for the tumoral cell lines tested but not for the non-tumoral PLP2 cell line. The analysis of the phenolic compounds of these extracts revealed the presence of caffeoylquinic acid, feruloylquinic acid, and caffeoylshikimic acid derivatives. Overall, this confirmed the antifungal activity of spent coffee grounds, presenting a potential increase in the sustainability of the life cycle of coffee grounds, as a source for the development of novel antifungal formulations, especially for skin or mucosal fungal infections. [ABSTRACT FROM AUTHOR]

Mushrooms are valued worldwide for their nutritional, organoleptic and chemical properties. The aim of this study was to determine the chemical composition (free sugars, organic acids, fatty acids, tocopherols and phenolic compounds) and bioactivity of three wild mushrooms (Lactarius piperatus, Lactarius quietus and Lactarius vellereus) from Serbia. Chemical analysis was performed with HPLC-RI and UFLC-PDA (for hydrophilic compounds) and with GC-FID and HPLC-FP (for lipophilic compounds). The analysis of phenolic compounds was performed by UFLC-DAD. Biological activities were evaluated using three different assays (microdilution, TBARS and SRB assays). The results showed that the fruiting bodies were rich in mannitol and trehalose. The main organic acids were oxalic acid and citric acid. As for lipophilic components, stearic, oleic and linoleic acids and β-tocopherol dominated in all the species studied. In addition, the methanolic and ethanolic extracts obtained showed antibacterial, antibiofilm and antioxidant properties. As for cytotoxicity, the extracts were not toxic or only moderately toxic toward different tumor cell lines. According to the results, the selected Serbian mushrooms are a rich source of bioactive compounds, and due to their good biological potential, they can be further exploited as functional ingredients beneficial to human health (antimicrobial agents, antioxidants). [ABSTRACT FROM AUTHOR]

Sterile bracts can represent 80% of Araucaria angustifolia pinecone and are a rich source of phenolic compounds. This study aimed to optimize the extraction of the phenolic compounds from Araucaria angustifolia bracts using response surface methodology; the bioactivity properties were also investigated. The effects of the ethanol concentration, solute/solvent ratio, and temperature in relation to the phenolic composition and antioxidant activity were evaluated. The quantification and identification of the individual phenolic compounds (using high-performance liquid chromatography) and their bioactivity were evaluated. The optimized extraction conditions, which detected gallic acid, catechin, epicatechin, quercetin, and kaempferol, were obtained using 60% ethanol at a ratio of 1:38 (w/v) and a temperature of 80 °C. The extract showed high levels of phenolic classes and antioxidant activity. The extract also showed an inhibitory activity for pathogenic (approximately 80%, 10,000 µg/mL) and lactic acid (27.9%, 15,000 µg/mL) bacteria strains. The α-glucosidase inhibitory activity was approximately ten times greater than acarbose, demonstrating its high antiglycemic potential. No antioxidant and anti-inflammatory cellular activity were determined; however, a high cytotoxicity for non-tumor cells and the antiproliferative activity against the tumor cells were observed. Overall, the phenolic extract showed promising action in relation to the fight against the diseases related to oxidative stress and, hopefully, the application of the safe concentrations of the extract, based on bioavailability assays, can be verified. [ABSTRACT FROM AUTHOR]

Silk is a natural composite fiber composed mainly of hydrophobic fibroin and hydrophilic sericin, produced by the silkworm Bombyx mori. In the textile industry, the cocoons of B. mori are processed into silk fabric, where the sericin is substantially removed and usually discarded in wastewater. This wastewater pollutes the environment and water sources. However, sericin has been recognized as a potential biomaterial due to its biocompatibility, immunocompatibility, biodegradability, anti-inflammatory, antibacterial, antioxidant and photoprotective properties. Moreover, sericin can produce hydrogels, films, sponges, foams, dressings, particles, fibers, etc., for various biomedical and pharmaceutical applications (e.g., tissue engineering, wound healing, drug delivery, cosmetics). Given the severe environmental pollution caused by the disposal of sericin and its beneficial properties, there has been growing interest in upcycling this biomaterial, which could have a strong and positive economic, social and environmental impact. [ABSTRACT FROM AUTHOR]

Several scientific studies have been proving the bioactive effects of many aromatic and medicinal plants associated with the presence of a high number of bioactive compounds, namely phenolic compounds. The antioxidant, anti-inflammatory, and antimicrobial capacities of these molecules have aroused high interest in some industrial sectors, including food, pharmaceuticals, and cosmetics. This work aimed to determine the phenolic profiles of the infusions and hydroethanolic extracts of five plants (Carpobrotus edulis, Genista tridentata, Verbascum sinuatum, Cytisus multiflorus, and Calluna vulgaris) that have been employed in many traditional preparations. In addition, the antioxidant, antimicrobial, anti-inflammatory, and anti-tumoral activity of each different preparation was evaluated using in vitro assays. The HPLC-DAD-ESI/MS profile revealed the presence of eighty phenolic compounds, belonging to seven different families of compounds. Regarding antioxidant properties, the hydroethanolic extract of C. edulis showed a potent effect in the TBARS assay (IC50 = 1.20 µg/mL), while G. tridentata hydroethanolic extract achieved better results in the OxHLIA test (IC50 = 76 µg/mL). For cytotoxic and anti-inflammatory results, V. sinuatum infusions stood out significantly, with GI50 = 59.1–92.1 µg/mL and IC50 = 121.1 µg/mL, respectively. Finally, C. edulis hydroethanolic extract displayed the most relevant antibacterial activity, showing MBC values of 0.25–1 mg/mL, while G. tridentata hydroethanolic extract exerted the greatest antifungal effects (MFC of 0.5–1 mg/mL). The results of this study deepen the knowledge of the phenolic profiles and also provide evidence on the bioactive properties of the species selected, which could be considered highly valuable options for research and application in several sectors, namely food, cosmetics, and pharmaceuticals. [ABSTRACT FROM AUTHOR]

The nutritional quality of kiwifruit has been highlighted by several studies, while its peel is typically discarded as a by-product with no commercial value. This study was carried out to optimize the ultrasound-assisted extraction (UAE) of phenolic compounds from kiwi peel. Three independent variables (time (t), ultrasonic power (P) and ethanol concentration (EtOH)) were combined in a five-level central composite rotatable design coupled with the response surface methodology (RSM). The extraction yield determined gravimetrically and the content of phenolic compounds identified by HPLC-DAD-ESI/MSn (namely two quercetin glycosides, one catechin isomer and one B-type (epi)catechin dimer) were the experimental responses used in the optimization. The polynomial models were successfully fitted to the experimental data and used to determine the optimal UAE conditions. The sonication of the sample at 94.4 W for 14.8 min, using 68.4% ethanol, resulted in a maximum of 1.51 ± 0.04 mg of flavonoids per g of extract, a result that allowed the experimental validation of the predictive model. The kiwi peel extract obtained under optimized conditions showed somehow promising bioactive properties, including antioxidant and antimicrobial effects, and no toxicity to Vero cells. Overall, this study contributes to the valorization of kiwi peel as a low-cost raw material for the development of natural ingredients (such as food preservatives) and also to the resource-use efficiency and circular bioeconomy. [ABSTRACT FROM AUTHOR]

Featured Application: Vegetable oils are a rich source of fatty acids and bioactive compounds with numerous beneficial effects to human health. The presented results showed that seed oils of linseed, purslane, luffa, and pumpkin have significant antimicrobial properties that could find application in the food industry as functional ingredients or as non-synthetic antimicrobial agents in the design of new healthy food products. Moreover, they could be used in mixtures with other oils to design new vegetable oils with functional properties and enhance content in omega-3 fatty acids. In the present study, the antimicrobial and cytotoxic activities, as well as the fatty acids composition in vegetable seed oils from linseed, purslane, luffa, and pumpkin were evaluated. For this purpose, two linseed oils and one luffa oil were commercially obtained, while purslane and pumpkin oils were obtained from own cultivated seeds. The results showed a variable fatty acids composition among the tested oils, with α-linolenic, linoleic, oleic, palmitic, and stearic acid being the most abundant compounds. In regards to particular oils, linseed oils were a rich source of α-linolenic acid, luffa and pumpkin oil were abundant in linoleic acid, while purslane oil presented a balanced composition with an almost similar amount of both fatty acids. Luffa oil was the most effective against two of the tested cancer cell lines, namely HeLa (cervical carcinoma) and NCI-H460 (non-small cell lung cancer), while it also showed moderate toxicity against non-tumor cells (PLP2 cell line). Regarding the antibacterial activity, linseed oil 3 and pumpkin oil showed the highest activity against most of the tested bacteria (especially against Enterobacter cloacae and Escherichia coli) with MIC and MBC values similar to the used positive controls (E211 and E224). All the tested oils showed significant antifungal activities, especially luffa and pumpkin oil, and for most of the tested fungi they were more effective than the positive controls, as for example in the case of Aspergillus versicolor, A. niger, and Penicillium verrucosum var. cyclopium. In conclusion, the results of our study showed promising antimicrobial and cytotoxic properties for the studied seed oils which could be partly attributed to their fatty acids composition, especially the long-chain ones with 12–18 carbons. [ABSTRACT FROM AUTHOR]

Consumers are very concerned with following a healthy diet, along with some precautions that may influence environmental impact. Solanum melongena L. is one of the most consumed vegetables due to its excellent nutritional value and antioxidant action. Associated with its high consumption, considerable amounts of agro-food wastes are produced. This work targets the valorization of this matrix, through the use of its bio-residues to study the obtention of coloring pigments, applying innovative technologies. Its nutritional value, chemical composition, and bioactive potential were evaluated, and the ultrasound-assisted extraction to obtain coloring pigments of high industrial interest was optimized. Considering the results, low contents of fat and carbohydrates and energy value were evident, as well as the presence of compounds of interest (free sugars, organic acids, unsaturated fatty acids, and phenolic acids). In addition, the antioxidant and antimicrobial potential was detected. Response surface methodology was performed to optimize the extraction of natural pigments, showing a concentration of 11.9 mg/g of anthocyanins/g of extract, applying optimal conditions of time, solvent, and solid/liquid ratio of 0.5 min, 68.2% (v/v) and 5 g/L, respectively. S. melongena proved to be a good source of bioactive compounds and natural pigments, which can generate great interest in the food industry. [ABSTRACT FROM AUTHOR]

Azadirachta indica A. Juss (neem) extracts have been used in pharmaceutical applications as antitumor agents, due to their terpenes and phenolic compounds. To obtain extracts from neem leaves with potential antiproliferative effect, a sequential process of pressurized liquid extraction was carried out in a fixed bed extractor at 25 °C and 100 bar, using hexane (SH), ethyl acetate (SEA), and ethanol (SE) as solvents. Extractions using only ethanol (EE) was also conducted to compare the characteristics of the fractionated extracts. The results obtained by liquid chromatography-electrospray ionization mass spectrometry suggested a higher concentration of terpenes in the SEA extract in comparison to SH, SE, and EE extracts. Therefore, antiproliferative activity showed that SEA extracts were the most efficient inhibitor to human tumor cells MCF-7, NCI-H460, HeLa, and HepG2. Hepatocellular cells were more resistant to SH, SEA, SE, and EE compared to breast, lung, hepatocellular, and cervical malignant cells. Neem fractioned extracts obtained in the present study seem to be more selective for malignant cells compared to the non-tumor cells. [ABSTRACT FROM AUTHOR]

Bee bread (BB) is a fermented mixture of plant pollen, honey, and bee saliva that worker bees use as food for larvae, and for young bees to produce royal jelly. In the present study, five BB samples, collected from Apis mellifera iberiensis hives located in different apiaries near Bragança, in the northeast region of Portugal, and one BB commercial sample were characterized by high-performance liquid chromatography coupled to a diode array detector and electrospray mass spectrometry (HPLC-DAD-ESI/MS) in terms of phenolic compounds, such as flavonoid glycoside derivatives. Furthermore, the samples were screened, using in vitro assays, against different human tumor cell lines, MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer), HeLa (cervical carcinoma) and HepG2 (hepatocellular carcinoma), and also against non-tumor liver cells (porcine liver cells, PLP2). The main phenolic compounds found were flavonol derivatives, mainly quercetin, kaempferol, myricetin, isorhamnetin and herbacetrin glycoside derivatives. Thirty-two compounds were identified in the six BB samples, presenting BB1 and BB3 with the highest contents (6802 and 6480 μg/g extract, respectively) and the highest number of identified compounds. Two isorhamnetin glycoside derivatives, isrohamnetin-O-hexosyl-O-rutinoside and isorhamnetin-O-pentosyl-hexoside, were the most abundant compounds present in BB1; on the other hand, quercetin-3-O-rhamnoside was the most abundant flavonol in BB3. However, it was not possible to establish a correlation between the flavonoids and the observed low to moderate cytotoxicity (ranging from >400 to 68 μg/mL), in which HeLa and NCI-H460 cell lines were the most susceptible to the inhibition. To the authors' knowledge, this is the first report characterizing glycosidic flavonoids in BB samples, contributing to the chemical knowledge of this less explored bee product. [ABSTRACT FROM AUTHOR]

The cosmetic industry is in a constant search for natural compounds or extracts with relevant bioactive properties, which became valuable ingredients to design cosmeceutical formulations. Mushrooms have been markedly studied in terms of nutritional value and medicinal properties. However, there is still slow progress in the biotechnological application of mushroom extracts in cosmetic formulations, either as antioxidants, anti-aging, antimicrobial, and anti-inflammatory agents or as hyperpigmentation correctors. In the present work, the cosmeceutical potential of ethanolic extracts prepared from Agaricus bisporus, Pleurotus ostreatus, and Lentinula edodes was analyzed in terms of anti-inflammatory, anti-tyrosinase, antioxidant, and antibacterial activities. The extracts were characterized in terms of phenolic acids and ergosterol composition, and further incorporated in a base cosmetic cream to achieve the same bioactive purposes. From the results obtained, the final cosmeceutical formulations presented 85%–100% of the phenolic acids and ergosterol levels found in the mushroom extracts, suggesting that there was no significant loss of bioactive compounds. The final cosmeceutical formulation also displayed all the ascribed bioactivities and as such, mushrooms can further be exploited as natural cosmeceutical ingredients. [ABSTRACT FROM AUTHOR]

Tabebuia impetiginosa (Mart. ex DC.) Standl. has been used in traditional medicine for many centuries, being nowadays marketed as dried plant material (inner bark) for infusions, pills, and syrups. The main objective of the present work was to validate its popular use through the bioactivity evaluation of the inner bark (methanolic extract and infusion) and of two different formulations (pills and syrup) also based on the same plant-material. The antioxidant activity was evaluated by in vitro assays testing free radical scavenging activity, reducing power and inhibition of lipid peroxidation in brain homogenates. The cytotoxicity was determined in four human tumor cell lines (MCF-7, NCI-H460, HeLa and HepG2, and also in non-tumor cells (porcine liver primary cells, PLP2)). Furthermore, the sample was chemically characterized regarding free sugars, organic acids, fatty acids, and tocopherols. Syrup and methanolic extract showed the highest antioxidant activity, related to their highest amount of phenolics and flavonoids. Methanolic extract was the only sample showing cytotoxic effects on the tested human tumor cell lines, but none of the samples showed toxicity in PLP2. Glucose and oxalic acid were, respectively, the most abundant sugar and organic acid in the sample. Unsaturated predominated over the saturated fatty acids, due to oleic, linoleic, and linolenic acids expression. α- and γ-Tocopherols were also identified and quantified. Overall, T. impetiginosa might be used in different phytoformulations, taking advantage of its interesting bioactive properties and chemical composition. [ABSTRACT FROM AUTHOR]

Three aminodi(hetero)arylamines were prepared via a palladium-catalyzed C-N Buchwald-Hartwig coupling of methyl 3-aminothieno[3,2-b]pyridine-2-carboxylate with different bromonitrobenzenes, followed by reduction of the nitro groups of the coupling products to the corresponding amino compounds. The aminodi(hetero)arylamines thus obtained were evaluated for their growth inhibitory effect on four human tumor cell lines MCF-7 (breast adenocarcinoma), A375-C5 (melanoma), NCI-H460 (non-small cell lung cancer) and HepG2 (hepatocellular carcinoma). The toxicity to non-tumor cells was also evaluated using a porcine liver primary cell culture (PLP1), established by us. The aminodi(hetero)arylamine with the NH2 group in the ortho position and an OMe group in the para position to the NH of the di(hetero)arylamine, is the most promising compound giving the lowest GI50 values (1.30-1.63 μM) in all the tested human tumor cell lines, presenting no toxicity to PLP1 at those concentrations. The effect of this compound on the cell cycle and induction of apoptosis was analyzed in the NCI-H460 cell line. It was observed that it altered the cell cycle profile causing a decrease in the percentage of cells in the G0/G1 phase and an increase of the apoptosis levels. [ABSTRACT FROM AUTHOR]

Cupressus sempervirens L., Juniperus communis L. and Cistus ladanifer L. are Mediterranean arboreal and shrub species that possess essential oils (EO) in their leaves and branches. This study aimed at characterizing the EOs obtained by steam distillation from the three species collected in different locations from Spain (Almazán, Andévalo, Barriomartín, Cerezal, Ermitas and Huéscar). For this purpose, volatiles composition was determined by GC-MS, and different bioactivities were evaluated. The highest content in terpenes was observed in C. sempervirens (Huéscar origin) followed by J. communis (Almazán origin), corresponding to 92% and 91.9% of total compounds, respectively. With exception of C. ladanifer from Cerezal that presented viridiflorol as the most abundant compound, all the three species presented in common the α-pinene as the major compound. The EOs from C. ladanifer showed high antibacterial potential, presenting MIC values from 0.3 to 1.25 mg/mL. Concerning other bioactivities, C. ladanifer EO revealed an oxidation inhibition of 83%, while J. communis showed cytotoxicity in the MCF-7 cell line, and C. sempervirens and C. ladanifer EOs exhibited the highest potential on NCI-H460 cell lines. Nevertheless, some EOs revealed toxicity against non-tumoral cells but generally presented a GI50 value higher than that of the tumor cell lines. [ABSTRACT FROM AUTHOR]

The venom from Apis mellifera intermissa, the main honey bee prevailing in Morocco, has been scarcely studied, despite its known potential for pharmacological applications. In the present work, we investigated the composition, the anti-inflammatory activity, and the venom's cytotoxic properties from fifteen honey bee venom (HBV) samples collected in three regions: northeast, central, and southern Morocco. The chemical assessment of honey bee venom was performed using LC-DAD/ESI/MSn, NIR spectroscopy and AAS spectroscopy. The antiproliferative effect was evaluated using human tumor cell lines, including breast adenocarcinoma, non-small cell lung carcinoma, cervical carcinoma, hepatocellular carcinoma, and malignant melanoma. Likewise, we assessed the anti-inflammatory activity using the murine macrophage cell line. The study provides information on the honey bee venom subspecies' main components, such as melittin, apamin, and phospholipase A2, with compositional variation depending on the region of collection. Contents of toxic elements such as cadmium, chromium, and plumb were detected at a concentration below 5 ppm, which can be regarded as safe for pharmaceutical use. The data presented contribute to the first study in HBV from Apis mellifera intermissa and highlight the remarkable antiproliferative and anti-inflammatory effects of HBV, suggesting it to be a candidate natural medicine to explore. [ABSTRACT FROM AUTHOR]

Simple Summary: Aloesin is a bioactive constituent of Aloe spp. used primarily in cosmetic products. Its recovery from plant materials is affected by several variables that can compromise the process yield and profitability, which is why it is necessary to determine the best processing conditions. This study describes the design and optimization of a method for extraction of aloesin from Aloe vera rind, a leaf part often discarded as a by-product, using the response surface methodology. The effect of the variables time, temperature, solvent composition, and solid/liquid ratio were investigated. Green organic solvents (ethanol, propylene glycol, and glycerol) were used in aqueous mixtures. Aqueous propylene glycol was found to be the most promising solvent for aloesin recovery and a linear increase in extraction yields was verified with the increase in solid/liquid ratio. To assess the bioactivity of the extracts, their ability to inhibit lipid peroxidation and the fungal and bacterial growth, as well as their cytotoxic potential, was tested in vitro. Overall, it was possible to determine the best extraction conditions for aloesin and to better understand the antioxidant and antimicrobial properties of the aloesin-rich extracts, which may be produced and used by the industrial sector. Aloesin is an aromatic chromone with increasing applications in the cosmetic and health food industries. To optimize its extraction from the Aloe vera leaf rind, the independent variables time (10–210 min), temperature (25–95 °C) and organic solvent composition (0–100%, w/w) were combined in a central composite design coupled with response surface methodology. The solvents consisted of binary mixtures of water with ethanol, propylene glycol, or glycerol. The aloesin levels quantified in each extract were used as response for optimization. The theoretical models were fitted to the experimental data, statistically validated, and used to obtain the optimal extraction conditions. Then, a dose–response analysis of the solid/liquid ratio (S/L) was performed under the optimal conditions determined for each alcohol–water system and revealed that a linear improvement in extraction efficiency can be achieved by increasing the S/L ratio by up to 40 g/L. This analysis also allowed to experimentally validate the predictive models. Furthermore, the aloesin-rich extracts revealed antioxidant activity through thiobarbituric acid reactive substances (TBARS) formation inhibition, antimicrobial effects against bacterial and fungal strains, and no toxicity for PLP2 cells. Overall, this study provided optimal extraction conditions for the recovery of aloesin from Aloe vera rind through an eco-friendly extraction process and highlighted its bioactive potential. [ABSTRACT FROM AUTHOR]

Several novel methyl 7-[(hetero)arylamino]thieno[2,3-b]pyrazine-6-carboxylates were synthesized by Pd-catalyzed C–N Buchwald–Hartwig cross-coupling of either methyl 7-aminothieno[3,2-b]pyrazine-6-carboxylate with (hetero)arylhalides or 7-bromothieno[2,3-b]pyrazine-6-carboxylate with (hetero)arylamines in good-to-excellent yields (50% quantitative yield), using different reaction conditions, namely ligands and solvents, due to the different electronic character of the substrates. The antitumoral potential of these compounds was evaluated in four human tumor cell lines: gastric adenocarcinoma (AGS), colorectal adenocarcinoma (CaCo-2), breast carcinoma (MCF7), and non-small-cell lung carcinoma (NCI-H460) using the SRB assay, and it was possible to establish some structure–activity relationships. Furthermore, they did not show relevant toxicity against a non-tumor cell line culture from the African green monkey kidney (Vero). The most promising compounds (GI50 ≤ 11 µM), showed some selectivity either against AGS or CaCo-2 cell lines without toxicity at their GI50 values. The effects of the methoxylated compounds 2b (2-OMeC6H4), 2f and 2g (3,4- or 3,5-diOMeC6H3, respectively) on the cell cycle profile and induction of apoptosis were further studied in the AGS cell line. Nevertheless, even for the most active (GI50 = 7.8 µM) and selective compound (2g) against this cell line, it was observed that a huge number of dead cells gave rise to an atypical distribution on the cell cycle profile and that these cells were not apoptotic, which points to a different mechanism of action for the AGS cell growth inhibition. [ABSTRACT FROM AUTHOR]

This study was carried out with the aim of optimizing the ultrasound-assisted extraction (UAE) of phenolic compounds from male chestnut flowers (C. sativa Mill) to develop a bioactive extract with potential to be used as a natural antioxidant preservative ingredient in the food industry. Time (t, 1–39 min), solvent concentration (S, 0–100%), and ultrasonic power (P, 5–500 W) were used as the independent variables for a 5-level experimental circumscribed central composite design (CCCD) coupled with response surface methodology (RSM) to optimize the extraction of phenolic compounds by UAE. Regarding the variables, the three showed a significant effect on the extraction of phenolic compounds. The content of phenolic compounds (including flavonoids and tannins) and the extraction yield (extract weight gravimetrically assessed) were the response criteria for the optimization. Based on the statistically validated predictive polynomial models, it was possible to reach a maximum content of phenolic compounds at the global optimal conditions of 24 ± 3 min, 259 ± 16 W, and 51 ± 7% ethanol. Additionally, pentagalloyl-glucoside and trigalloyl-hexahydroxydiphenoyl-glucoside were the major phenolic compounds identified. The optimized extract was then analyzed for their biological properties. The bioactive potential of the chestnut flower extract obtained under these optimized conditions was evaluated using in vitro assays for antioxidant, anti-inflammatory, and antimicrobial activity, as well as cytotoxicity and hepatotoxicity tests. The results revealed that the enriched extract has antioxidant, antitumoral, and anti-inflammatory activities without toxicity issues. Overall, this study allowed to define the optimal conditions for the extraction of phenolic compounds from chestnuts male flowers by UAE, to obtain an enriched extract with biological properties that could be further used as a natural antioxidant ingredient with applications on functional foods. [ABSTRACT FROM AUTHOR]

The vibrant colours of many plants are due to secondary metabolites, such as nitrogen-containing compounds, where betacyanins are included. These compounds can be found in plants such as Amaranthus caudatus L. that, due to their high nutritional benefits, have been overproduced, which leads to the accumulation of large amounts of bio-residues. Among these bio-residues, the flowers which have a very intense pink colour and present no economic value or subsequent destination can be exploited as sources of natural colouring agents (betacyanins). This work aimed at characterising the flower's extract in terms of bioactive molecules such as tocopherols, organic acids, but essentially in terms of betacyanins, in order to obtain a natural colouring agent. For the extraction, ultrasound-assisted extraction (UAE) ideal conditions were obtained using the Response Surface Methodology (RSM), allowing the attainment of an enriched extract of betacyanins in high yields and purity. The obtained extracts were analysed for their bioactive potential, namely antioxidant, antimicrobial and cytotoxic properties. From the obtained results, three isoforms of tocopherols were detected, β-tocopherol (0.884 ± 0.003 mg/100 g dry weight (dw)) being the most abundant one. Regarding the organic acids, oxalic (2.48 ± 0.05 mg/100 g dw), shikimic (0.170 ± 0.003 mg/100 g dw) and traces of fumaric acid were found. Four betacyanins were identified and quantified, namely: amaranthine (171 ± 1 mg/g extract), isoamaranthine (38 ± 1 mg/g extract), betanin (1.6 ± 0.1 mg/g), and isobetanin (1.3 ± 0.1 mg/g extract). The obtained extract also presented antioxidant activity with inhibition concentration (IC50 values) of 29.0 ± 0.4 μg/mL and 114 ± 4 μg/mL for Δt of 60 min and 120 min, respectively in the oxidative haemolysis inhibition assay (OxHLIA) assay. The obtained extract also presented an interesting antibacterial activity with minimum inhibitory concentrations ranging from 5 to 20 mg/mL against pathogenic bacteria and revealed no toxicity for normal cells. [ABSTRACT FROM AUTHOR]

Fruit bio-residues can be interesting for the recovery of bioactive molecules, such as phenolic compounds, tocopherols, vitamins, among others. These compounds can be targeted at the food industry and used for the development of functional foods or as food additives. In some cases, fruit epicarps are converted into by-products with non-commercial value, and generally, these fruit parts have a higher content in bioactive compounds than the fruit pulp. From this perspective, S. odorifera, a Brazilian fruit, has an inedible epicarp that could be explored to obtain biological compounds. Therefore, the aims of this study were to evaluate the chemical composition and the antioxidant, anti-proliferative, anti-inflammatory, and antimicrobial bioactivities of this by-product. S. odorifera epicarp showed a total of four organic acids, four phenolic compounds, highlighting the high concentration of anthocyanins (24 ± 1 mg/g dry weight (dw)) and high content of tocopherols (366 ± 2 mg/100 g dw). The hydroethanolic extract showed considerable antioxidant activity (EC50 values of 48.2 ± 0.5 and 27 ± 1 µg/mL for TBARS and OxHLIA assays, respectively), as also antibacterial and antifungal activities (minimal inhibitory concentrations (MICs) ≤ 2.2 mg/mL). The results obtained in this study suggest that Sicana odorifera epicarp represents a reliable option for the development of novel natural-based colorants with functional/bioactive proprieties. [ABSTRACT FROM AUTHOR]

Ruscus aculeatus L. is a subshrub used in traditional medicine in different parts of the world, namely in Europe and the Iberian Peninsula. According to reported folk knowledge, the aerial parts are mainly used as diuretics and the underground organs are used for the treatment of disorders of the urinary system and as a laxative. In this work, the aerial part and the roots and rhizomes of R. aculeatus were chemically characterized with regard to the content of phenolic compounds and bioactive properties. Aqueous (infusions and decoctions) preparations and hydroethanolic extracts from the two mentioned parts of the plant were prepared. Nine phenolic compounds were detected in all the extracts. Apigenin-C-hexoside-C-pentoside isomer II was the major compound in aqueous extracts and, in the hydroethanolic extract was quercetin-O-deoxyhexoside-hexoside followed by apigenin-C-hexoside-C-pentoside isomer II. All extracts revealed antioxidant activity and potential to inhibit some of the assayed bacteria; aqueous extracts of the aerial part and infusions of roots and rhizomes did not show cytotoxic effects on a non-tumor primary cell culture. This preliminary study provides suggestions of the biological potential associated with the empirical uses and knowledge of this species, in particular its bioactivities. [ABSTRACT FROM AUTHOR]

Medicinal and aromatic plants (MAPs), worldwide appreciated and used as condiments, dyes, and preservatives, possess several biological properties that justify their continuous application in the food industry. In the present study, the nutritional and chemical profiles, as well as the bioactive properties of four combinations of condiments, sold for seasoning poultry, meat, fish, and salads, were evaluated. Twenty-five phenolic compounds (HPLC-DAD-ESI/MS) were identified, with apigenin-O-malonyl-pentoside-hexoside as the major compound detected in all extracts. Oxalic and citric acids were identified in all mixtures (UFLC-PDA), as well as all the four tocopherol isoforms (HPLC-fluorescence). Regarding bioactivities, the mixtures for meat and salads (TBARS) and meat and poultry (OxHLIA) stood out for their antioxidant potential, whereas for the anti-inflammatory and antitumor properties, the mixtures revealing the greatest results were those for poultry and salad, respectively. In terms of antimicrobial activity, all the mixtures revealed the capacity to inhibit the growth of some bacterial strains. In brief, condiment mixtures showed to be a good source of bioactive compounds, as they confer health benefits, validating the importance of their inclusion in the human diet as a good dietary practice. [ABSTRACT FROM AUTHOR]

The Mediterranean basin is abundant in wild edible species with numerous health beneficial effects due to the presence of various bioactive phytochemicals. In the present work, the effect of nitrogen fertilization rates (0 ppm, (N0), 200 ppm (N1), 400 ppm (N2), and 600 ppm (N3) of total N) and growth substrate composition (soil or peat/perlite (2/1; v/v)) on the chemical composition and bioactive properties of Centaurea raphanina ssp. mixta plants was evaluated. The results of the study showed that both the tested factors affected nutritional value of the edible leaves, with the soil × N1 treatment being the most beneficial for fat, protein, and carbohydrate content and energetic value. On the other hand, the peat/perlite-grown plants that received 200 ppm of N had the highest content in α-, γ-, and total tocopherols, while the control treatment of soil-grown plants was the richest in individual and total sugars. Oxalic, citric, and total organic acids were the highest in the N2 × soil treatment, while malic acid was the highest in control treatment of the same substrate. The main fatty acids were palmitic, α-linolenic, and linoleic acids, with the highest contents being observed in the N0 × soil, N3 × soil, and N3 × peat/perlite treatments, respectively. The major phenolic compounds were pinocembrim neohesperidoside and pinocembrim acetyl neohesperidoside isomer II, with the highest content being observed in the N1 × soil treatment. The highest antihemolytic activity was observed in the N3 × peat/perlite treatment, while the most effective treatments against lipid peroxidation were N0 (in both soil and peat/perlite combinations) and N1 × peat/perlite. Lastly, all the tested extracts (except for N1 × soil) showed promising cytotoxic effects against HeLa (cervical carcinoma), HepG2 (hepatocellular carcinoma), MCF-7 (breast carcinoma), and NCI-H460 (non-small-cell lung cancer), while all the tested extracts exhibited better antifungal activities (lower minimal inhibition concentration (MIC) values) against Trichoderma viride than the positive controls. Overall, the present results suggest that the application of cost-effective practices such as the nitrogen application and the selection of growth substrate may regulate the chemical composition and the bioactive properties of C. raphanina ssp. mixta species and increase its added value under commercial cultivation conditions. [ABSTRACT FROM AUTHOR]

In the present work, sage (Salvia officinalis L.) and basil (Ocimum basilicum L.) were exploited for their preservative purposes, as viable alternatives to artificial ones. The ultrasound-assisted extraction (UAE) of bioactive compounds was pre-optimized using factorial screening analysis, prior to applying response surface methodology (RSM). The obtained extracts were characterized in terms of phenolic compounds by high-performance liquid chromatography coupled to photodiode array detector and mass spectrometer HPLC-DAD-ESI/MS and bioactivities, namely the antioxidant, antimicrobial and cytotoxic potential. In addition, the most promising extracts were incorporated into yogurts, that were further screened for nutritional and physico-chemical properties and microbial load, over a shelf life of 14 days. According to the obtained results, the solvent percentage is the most relevant factor for obtaining rosmarinic acid-rich extract, followed by the extraction time and ultrasonic power. For the antioxidant and antimicrobial activity, sage showed the best result for both analysis and none of the two plant extracts were hepatotoxic. Finally, both extracts did not show changes in the physicochemical and nutritional characteristics of the yogurts and did not interfere with the growth of lactic acid bacteria, an important microorganism during yogurt fermentation. These results highlight the high potential of sage and basil as natural preservatives. [ABSTRACT FROM AUTHOR]