Evaluation of antitumoral and antioxidant activities of the hydroalcoholic extract and fractions obtained from the fruit pericarp of Sapindus saponaria L.

The fruits of Sapindus saponaria L., popularly known as 'saboeiro', have been used in medicine. This study evaluated the antioxidant and antitumor activities of the hydroethanolic extract (HAE) and fractions obtained from the fruit pericarp of S. saponaria. The HAE was obtained from the S. saponaria fruit pericarp by maceration; this was followed by fractionation using reversed-phase solid-phase extraction, resulting in fractions enriched with acyclic sesquiterpenic oligoglycosides (ASOG) and saponins (SAP1, and SAP2), confirmed by mass spectrometry with electrospray ionization (ESI-QTOF-MS). The greatest citotoxic activity was observed with the SAP1 fraction against the CaCo2 cell line with a GI50 of 8.1 µg mL-1, while the SAP2 fraction had a GI50 of 13.6 µg mL-1 against CaCo2. The HAE demonstrated the greatest antioxidant activity. S. saponaria has potential therapeutic use in the pharmaceutical industry as a natural anti-oxidant or antitumor product.

Chemical Characterization, Bioactivity and Toxicity of European Flora Plant Extracts in Search for Potential Natural Origin Preservatives.

Consumer demand for natural and healthier products has led to an increasing interest in the bioactive and therapeutic properties of plant extracts. In this study, we evaluated the phenolic compounds profile, bioactivities, and toxicities of plant extracts from eight European flora species, including Calendula officinalis L., Calluna vulgaris (L.) Hull, Hippophae rhamnoides L., Juglans regia L., Mentha cervina L., Rubus idaeus L., Sambucus nigra L., and Vitis vinifera L. The aim was to identify potential preservatives of natural origin. Phenolic compounds were identified by HPLC-DAD-ESI-MS. Caffeic acid derivatives, ellagitannins, flavonols, and flavones were the major phenolic compounds identified. The total phenolic content varied from 16.0 ± 0.2 (V. vinifera) to 123 ± 2 mg/g (H. rhamnoides) of dry extract. All extracts showed antioxidant potential and exhibited activity against some of the microorganisms tested. S. nigra showed the highest activity in the inhibition of oxidative hemolysis (OxHLIA) assay and H. rhamnoides, notably, had the lowest IC50 values in TBARS and DPPH assays, as well as the lowest minimum inhibitory concentration (MIC) values. Regarding in vitro cytotoxicity, in tumor and non-tumor cell lines, although some extracts revealed toxicity against normal cells, it was found that the samples C. vulgaris, V. vinifera and R. idaeus might be used against tumor cells since the active concentration is much lower than the one causing toxicity. In vivo acute toxicity tests using Artemia franciscana suggest low toxicity for most extracts, with LC50 > 400 mg/L. These results showed the potential of the studied extracts as natural preservatives, given their richness in compounds with bioactive properties, highlight their potential value to the production chain.

Cellular Antioxidant, Anti-Inflammatory, and Antiproliferative Activities from the Flowers, Leaves and Fruits of Gallesia integrifolia Spreng Harms.

Gallesia integrifolia, a notable species in the Atlantic Forest, has been traditionally employed in folk medicine for treating rheumatism, asthma, and worms. This study investigated the cellular antioxidant, antiproliferative, and anti-inflammatory activities of the essential oils (EOs) and crude extracts (CEs) from G. integrifolia flowers, fruits, and leaves. The chemical identification of EOs was performed by GC-MS and CEs by UHPLC-MS. Cellular antioxidant and anti-inflammatory activities were assessed through mouse macrophage cell culture. In addition, the antiproliferative potential was evaluated in gastric, colorectal, breast, and lung tumor cell lines and non-tumor VERO cells. EOs predominantly contained organosulfur compounds in flowers (96.29%), fruits (94.94%), and leaves (90.72%). We found the main compound is 2,2'-Disulfanediyldiethanethiol in the EOs of flowers (47.00%), leaves (41.82%), and fruits (44.39%). Phenolic compounds were identified in CEs. The EOs and CEs demonstrated potential against the tumor cell lines tested (GI50 between 51 and 230 µg/mL). The selectivity index values were greater than 1.0 (1.01 to 3.37), suggesting a relative safety profile. Moreover, the anti-inflammatory activity IC50 ranged from 36.00 to 268 µg/mL, and the cellular oxidation inhibition ranged from 69% to 82%. The results suggest that oils and extracts derived from G. integrifolia have potential for use in various industrial sectors.

Brazilian berry waste as a source of bioactive compounds: grumixama (Eugenia brasiliensis Lam.) as a case study.

Grumixama, Eugenia brasiliensis Lam., is a Brazilian berry little explored commercially and scientifically. However, local small producers market this fruit in the form of frozen pulp, which generates bioresidues, composed of seeds and peels. With the view to propose strategies for valuing grumixama, this study aimed to determine the chemical composition and assess the bioactivities of the hydroethanolic extracts of the whole residue (GR), seed (GS) and peel (GP) fractions of E. brasiliensis. From the results, GP had the highest concentration of organic acids (oxalic, malic, ascorbic and citric acids), total tocopherols, condensed tannins, anthocyanins, and other flavonoids. On the other hand, GS showed the highest content of monounsaturated fatty acids and hydrolysable tannins, whereas GR displayed a mixture of compounds detected in each of its parts. Regarding the bioactivities, low extract concentrations were required in two in vitro antioxidant assays, namely TBARS (EC50 = 0.90-1.34 µg mL-1) and OxHLIA (IC50 = 21-65 µg mL-1). Furthermore, GP had the highest inhibition activity of cellular oxidation in the CAA assay (80 ± 0.6%), while GS showed the highest anti-inflammatory activity via nitric oxide production inhibition (EC50 = 98.0 ± 0.5 µg mL-1). All samples induced cell growth inhibition of the tested tumor cells (GI50 = 14.7-186 µg mL-1) besides antibacterial and antifungal effects at low concentrations, but all samples were harmful to normal cells at moderate concentrations (GI50 = 145-268 µg mL-1). Therefore, E. brasiliensis residue could be a good source of bioactive compounds to be used in several areas. However, additional studies are needed to confirm its safety as well as to unravel the mechanisms behind its biological activities.

Antimalarial and Cytotoxic Activity of Native Plants Used in Cabo Verde Traditional Medicine.

Medicinal plants have historically been a source of drugs in multiple applications, including the treatment of malaria infections. The Cabo Verde archipelago harbors a rich diversity of native plants, most of which are used for medicinal purposes. The present study investigated the in vitro antiplasmodial activities of four native plants from Cabo Verde (i.e., Artemisia gorgonum, Lavandula rotundifolia, Sideroxylon marginatum, and Tamarix senegalensis). Traditional preparations of these medicinal plants, namely aqueous extracts (infusions) and ethanolic extracts, were tested against both chloroquine-sensitive (3D7) and chloroquine-resistant (Dd2) Plasmodium falciparum strains using the SYBR Green detection method. The in vitro cytotoxicity was evaluated in Caco-2 and PLP2 cells using a sulforhodamine B colorimetric assay. An ethanolic extract of A. gorgonum and infusions of T. senegalensis exhibited high antiplasmodial activities (EC50 < 5 µg/mL) without cytotoxicity (GI50 > 400 µg/mL). Extracts of L. rotundifolia and S. marginatum exhibited moderate activities, with EC50 values ranging from 10-30 µg/mL. The A. gorgonum ethanolic extract showed activity toward early ring stages, and parasites treated with the T. senegalensis infusions progressed to the early trophozoite stage, although did not develop further to the late trophozoite or schizont stages. Antimalarial activities and the lack of cytotoxicity of the extracts are reported in the present study and support previous claims by traditional practitioners for the use of these plants against malaria while suggesting their ethnopharmacological usefulness as future antimalarials.

Purple tea: chemical characterization and evaluation as inhibitor of pancreatic lipase and fat digestion in mice.

A variety of the classic green tea plant, Camellia sinensis, was developed and is exclusive to Kenya. Due to high content of anthocyanin polyphenols in its leaves, the beverage obtained from this variety is purple in color and is the origin of the name purple tea. This work had two main purposes. The first one was to identify and quantify the major anthocyanin polyphenols in a hot water aqueous extract of the purple tea leaves. The second one was to test the hypothesis if this extract is capable of inhibiting triglyceride absorption considering that anthocyanin polyphenolics have been frequently associated to antilipidemic effects. Parallel experiments were always done with a similar green tea extract for comparison purposes. The antioxidant, anti-inflammatory, and cytotoxic activities of both tea varieties are similar. The purple tea extract, however, was strongly inhibitory toward the pancreatic lipase (minimal IC50 = 67.4 µg mL-1), whereas the green tea preparation was a weak inhibitor. Triglyceride digestion in mice was inhibited by the purple tea extract starting at 100 mg kg-1 dose and with a well-defined dose dependence. Green tea had no effect on triglyceride digestion at doses up to 500 mg kg-1. The latter effect is probably caused by several components in the purple tea extract including non-anthocyanin and anthocyanin polyphenols, the first ones acting solely via the inhibition of the pancreatic lipase and the latter by inhibiting both the lipase and the transport of free fatty acids from the intestinal lumen into the circulating blood. The results suggest that the regular consumption of Kenyan purple tea can be useful in the control of obesity.

Evaluation of the Polyphenolic Composition and Bioactivities of Three Native Cabo Verde Medicinal Plants.

The use of medicinal plants in a variety of health conditions remains essential for the discovery of new treatments. The present study aimed to investigate the bioactive properties of three native plants from Cabo Verde Islands, namely Artemisia gorgonum Webb, Sideroxylon marginatum (Decne. ex Webb) Cout., and Tamarix senegalensis DC., contributing to the characterization of less-known medicinal plants and their potential benefits for human health. Known compounds, such as kaempferol, quercetin, caffeyolquinic, and apigenin derivatives, among others, were detected in the plant species under study. Overall, all species demonstrated good antioxidant capacity, especially the ethanolic extracts of A. gorgonum (EC50 = 0.149 mg/mL) in TBARS assay. Moreover, the ethanolic extracts of the studied plants showed cytotoxic properties against tumor cells, and again the A. gorgonum extract proved to be the most effective in inhibiting tumor growth, mainly in the CaCO2 (GI50 = 17.3 µg/mL) and AGS (GI50 = 18.2 µg/mL) cell lines. Only the ethanolic extracts of T. senegalensis and S. marginatum demonstrated anti-inflammatory activity, albeit weak (EC50 = 35 and 43 µg/mL, respectively). The present study contributed to increased knowledge about the bioactive properties of these plants commonly used in traditional medicine, some of which was discussed for the first time, opening new perspectives for their use in a wider range of health conditions, especially in African countries, where access to modern health care is more limited.

Low-cost alternative for the bioproduction of bioactive phenolic compounds of callus cultures from Cereus hildmannianus (K.) Schum.

The aim of this study was to establish a sustainable alternative callus culture of Cereus hildmannianus for the production and bioactive determination of phenolic compounds from this species. The conventional callus was cultivated using agar and Murashige and Skoog (MS) medium, while for the alternative culture the agar was replaced with a cotton support covered with filter paper and MS medium (incubated at 32 °C with photoperiod of 16 h), and the morphological characteristics and growth index were assessed (8 weeks). Extracts were obtained by maceration followed by partition, characterized by nuclear magnetic resonance - NMR and ultra-high performance liquid chromatography - UHPLC, quantified (phenolic compounds) by UV-Vis methods, and their antioxidant, antitumor activities, as well as cytotoxicity, were evaluated. The establishment of an alternative callus culture was carried out successfully. Characteristic signals of phenolic compounds were determined by NMR, and 46 compounds with fragment ions were identified using UHPLC analysis. The highest concentrations of phenolic compounds, and greatest antioxidant and antitumor activities, were obtained with the dichloromethane fractions of both callus tissue cultures, which were not cytotoxic. The callus culture from C. hildmannianus has shown promise as a source for the sustainable production of phenolic compounds with antioxidant and antiproliferative activities and thus, has potential use as a natural antitumor product.

Obtaining Aromatic Extracts from Portuguese Thymus mastichina L. by Hydrodistillation and Supercritical Fluid Extraction with CO2 as Potential Flavouring Additives for Food Applications.

Humans often respond to sensory impulses provided by aromas, and current trends have generated interest in natural sources of fragrances rather than the commonly used synthetic additives. For the first time, the resulting aroma of a selected culture of Thymus mastichina L. was studied as a potential food ingredient. In this context, dried (DR) and fresh (FR) samples were submitted to carbon dioxide (CO2) supercritical extraction (SFE) and hydrodistillation (HD) methods. The extracts were characterised according to their volatile composition by GC-MS, cytotoxicity against a non-tumour cell culture, and sensory attributes (odour threshold and olfactive descriptors). The most abundant aromas were quantified, and the analysis performed by GC-MS revealed an abundance of terpenoids such as thymol chemotype, followed by the precursors α-terpinene and p-cymene. DR and FR extracts (EX) obtained from SFE-CO2 show the highest content of thymol, achieving 52.7% and 72.5% of the isolated volatile fraction. The DR essential oil (EO) contained the highest amount of terpenoids, but it was also the most cytotoxic extract. In contrast, SFE-CO2 products showed the lowest cytotoxic potential. Regarding FR-OE, it had the lowest extraction yield and composition in aroma volatiles. Additionally, all samples were described as having green, fresh and floral sensory notes, with no significant statistical differences regarding the odour detection threshold (ODT) values. Finally, FR-EX of T. mastichina obtained by SFE-CO2 presented the most promising results regarding food application.

Chemical composition and biological activity of cardoon (Cynara cardunculus L. var. altilis) seeds harvested at different maturity stages.

Cardoon seeds collected in Greece at four different maturity stages (samples S1 to S4) were analysed in terms of chemical composition and in vitro bioactivities. The content of phenolic compounds (six compounds in total) increased with increasing maturity, and 3,5-O-dicaffeyolquinic (14.8-33.8 mg/g extract) acid was the compound detected in higher abundance. Mature seeds (sample S4) also revealed the highest content in lipids (23 g/100 g extract) and tocopherols (29.62 mg/100 g dw) and demonstrated the highest cytotoxic (GI50 of 97-216 µg/mL) and anti-inflammatory (IC50 = 148 µg/mL) activities, and capacity to inhibit the formation of thiobarbituric acid reactive substances (TBARS) (IC50 = 5 µg/mL). Cardoon seed hydroethanolic extracts also revealed high antibacterial and antifungal potential, particularly samples S3 and S1, respectively. This study proved the multifaceted potential associated with valorisation of cardoon seeds, while their biological and chemical composition can be influenced by the maturity stage.

Upcycling Fish By-Products into Bioactive Fish Oil: The Suitability of Microwave-Assisted Extraction.

The seafood industry is often left out of the food waste discussion, but this sector is no exception, as it generates large amounts of various by-products. This study aimed to explore the potential of the microwave-assisted extraction (MAE) technique to obtain high-quality oil from fish by-products. The independent variables, which were time (1-30 min), microwave power (50-1000 W), and solid/liquid ratio (70-120 g/L) were combined in a 20-run experimental design coupled with the response surface methodology (RSM) for process optimization. The obtained oil yield values were fitted to a quadratic equation to build the theoretical models, which were statistically validated based on statistical criteria and used to predict the optimal MAE condition. The oil yields were significantly affected by the three independent variables through linear, quadratic, and/or interactive effects. Compared to a conventional Soxhlet extraction (SE), the optimal MAE conditions allowed between 60 and 100% of oil to be recovered in less than 19 min and with less solvent consumption. The fatty acid profiles of the oils obtained through SE and optimized MAE were characterized by gas chromatography with flame ionizing detection (GC-FID) after a derivatization process. These oils were constituted mainly of health, beneficial unsaturated fatty acids, such as oleic, docosahexaenoic (DHA), linoleic, and eicosapentaenoic (EPA) acids, which were not affected (p > 0.05) by the extraction methods. Interestingly, the oils obtained through MAE showed the best microbial growth inhibition results may have been due to thermolabile compounds, preserved via this unconventional non-thermal method. The oils also exhibited anti-inflammatory effects via nitric oxide production inhibition and cytotoxic potential especially, against breast and gastric adenocarcinoma cells. However, the threshold of toxicity should be further investigated. Overall, this work emerges as a future-oriented approach to upcycling fish by-products into high-quality oils that can be used in the formulation of pet food and other products.

Seasonal variation in bioactive properties and phenolic composition of cardoon (Cynara cardunculus var. altilis) bracts.

Cardoon (Cynara cardunculus L.) bracts were collected at different maturation stages to investigate seasonal changes in the phenolic compounds profile and in vitro bioactivities. Among the 12 phenolic compounds tentatively identified, 3,5-O-dicaffeoylquinic acid (21.83 mg/g extract) and apigenin-7-O-glucuronide (10.6 mg/g extract) were the most abundant. Immature bracts (C1: principal growth stage (PGS) 5) had the highest phenolic compounds content, and anti-inflammatory (IC50 = 72 µg/mL) and cytotoxic (GI50 of 30-79 µg/mL) activities. Moreover, extract C1 inhibited efficiently the formation of thiobarbituric acid reactive substances (TBARS; IC50 = 26.8 µg/mL), while extract C8 (PGS 8/9) was more effective against oxidative haemolysis (IC50 38 and 75 µg/mL). The highest antibacterial and antifungal activities were attributed to samples C1 and C6 (PGS 7/8) and samples C2 (PGS 5/6) and C4 (PGS 6/7), respectively. Overall, the obtained results suggest the seasonal changes of polyphenolic composition and bioactivity of cardoon bracts of variable maturity.

Phenolic profile and effects of acetone fractions obtained from the inflorescences of Calluna vulgaris (L.) Hull on vaginal pathogenic and non-pathogenic bacteria.

The phenolic profile and the antibacterial activity against pathogenic commensal vaginal bacteria exhibited by different fractions of the acetone extract of heather were assessed. The acetone extract of Calluna vulgaris (L.) Hull was fractionated by silica gel column chromatography through an eluent system of increasing polarity, and 10 different fractions (Fr 1 to Fr 10) were obtained. The phenolic profile was analyzed by HPLC-DAD-ESI/MS. Type B (epi)catechin dimers, (-)-epicatechin and (+)-catechin, were the main phenolic compounds present in the fractions. The antibacterial activity was also analyzed against pathogenic bacteria and the effect on the beneficial microflora was also assessed. Some of the obtained fractions revealed the capacity to inhibit pathogenic microorganisms without affecting the beneficial microflora, especially Fr 7 and Fr 8. For instance, Neisseria gonorrhoeae was inhibited by both of the fractions, while Fr 7 was more active against Klebsiella pneumoniae and Morganella morganii, and Fr 8 was active against methicillin resistant Staphylococcus aureus (MRSA) and methicillin susceptible Staphylococcus aureus (MSSA), without affecting the Lactobacillus strains. This study corroborates the therapeutic use of this matrix in traditional medicine.

Calluna vulgaris (L.) Hull: chemical characterization, evaluation of its bioactive properties and effect on the vaginal microbiota.

The inflorescences of Calluna vulgaris were nutritionally and chemically characterized. Furthermore, different organic and aqueous extracts were prepared for the evaluation of their bioactive properties. From the obtained results, carbohydrates were the major compounds, followed by protein, lipid and ashes. It was possible to identify the sugars fructose and glucose, five organic acids, 26 individual fatty acids and the four tocopherol isoforms. Concerning the extract composition, 12 phenolic compounds were identified, with myricetin-3-O-glucoside and myricetin-O-rhamnoside predominating. Concerning the bioactive effects, the more polar extracts showed not only the highest amount in phenolic compounds, but also the strongest antioxidant and antibacterial activities. In contrast, for the anti-inflammatory and cytotoxic potential, the most effective extracts were the n-hexane and the ethyl acetate extracts, respectively. C. vulgaris presented a wide range of biological effects, highlighting their capacity to inhibit pathogenic bacteria without affecting beneficial microflora, corroborating their use in traditional medicine.