UHPLC-ESI-QTOF-MS metabolite profiles of different extracts from Pelargonium endlicherianum parts and their biological properties based on network pharmacological approaches.

In the present study, we aimed to investigate the chemical profiles and biological activities of different extracts (ethyl acetate, dichloromethane, ethanol, and water) of Pelargonium endlicherianum parts (aerial parts and roots). Free radical scavenging, reducing power, phosphomolybdenum, and metal chelating were assayed for antioxidant properties. To detect enzyme inhibitory properties, cholinesterase, amylase, glucosidase, and tyrosinase were chosen as target enzymes. The ethanol extract of the aerial parts contained higher amounts of total bioactive compounds (120.53 mg GAE/g-24.46 mg RE/g). The ethanol and water extracts of these parts were tentatively characterized by UHPLC-ESI-QTOF-MS and 95 compounds were annotated. In addition, the highest acetylcholiesterase (3.74 mg GALAE/g) and butyrylcholinesterase (3.92 mg GALAE/g) abilities were observed by the ethanol extract of roots. The water extract from aerial parts exhibited the most pronounced inhibitory effects on multiple cancer cell lines, especially A549 (IC50: 23.2 µg/mL) and HT-29 (IC50: 27.43 µg/mL) cells. Using network pharmacology, P. endlicherianum compounds were studied against cancer, revealing well-connected targets such as epidermal growth factor receptor (EGFR), phosphoinositide-3-kinase (PI3K), AKT, receptor tyrosine-protein kinase erbB-2, and growth factor receptor bound protein 2 (GRB2) with significant impact on cancer-related pathways. The results could open a new path from natural treasure to functional applications with P. endlicherianum and highlight a new study on other uninvestigated Pelargonium species.

Valorization applications of pineapple and papaya byproducts in food industry.

The recent increase in the harvesting and industrial processing of tropical fruits such as pineapple and papaya is leading to unavoidable amounts of byproducts rich in valuable compounds. Given the significance of the chemical composition of these byproducts, new research avenues are opening up to exploit them in the food industry. In this sense, the revalorization of pineapple and papaya byproducts is an emerging trend that is encouraging the full harnessing of these tropical fruits, offering the opportunity for developing innovative value-added products. Therefore, the main aim of this review is to provide an overview of the state of the art of the current valorization applications of pineapple and papaya byproducts in the field of food industry. For that proposal, comprehensive research of valorization applications developed in the last years has been conducted using scientific databases, databases, digital libraries, and scientific search engines. The latest valorization applications of pineapple and papaya byproducts in the food industry have been systematically revised and gathered with the objective of synthesizing and critically analyzing existing scientific literature in order to contribute to the advancement of knowledge in the field of tropical byproduct revalorization providing a solid foundation for further research and highlighting scientific gaps and new challenges that should be addressed in the future.

Selectivity Tuning by Natural Deep Eutectic Solvents (NADESs) for Extraction of Bioactive Compounds from Cytinus hypocistis-Studies of Antioxidative, Enzyme-Inhibitive Properties and LC-MS Profiles.

In the present study, the extracts of Cytinus hypocistis (L.) L using both traditional solvents (hexane, ethyl acetate, dichloromethane, ethanol, ethanol/water, and water) and natural deep eutectic solvents (NADESs) were investigated in terms of their total polyphenolic contents and antioxidant and enzyme-inhibitive properties. The extracts were found to possess total phenolic and total flavonoid contents in the ranges of 26.47-186.13 mg GAE/g and 0.68-12.55 mg RE/g, respectively. Higher total phenolic contents were obtained for NADES extracts. Compositional differences were reported in relation to antioxidant potential studied by several assays (DPPH: 70.19-939.35 mg TE/g, ABTS: 172.56-4026.50 mg TE/g; CUPRAC: 97.41-1730.38 mg TE/g, FRAP: 84.11-1534.85 mg TE/g). Application of NADESs (choline chloride-urea 1:2, a so-called Reline) allowed one to obtain the highest number of extracts having antioxidant potential in the radical scavenging and reducing assays. NADES-B (protonated by HCl L-proline-xylitol 5:1) was the only extractant from the studied solvents that isolated a specific fraction without chelating activity. Reline extract exhibited the highest acetylcholinesterase inhibition compared to NADES-B and NADES-C (protonated by H2SO4 L-proline-xylitol 5:1) extracts, which showed no inhibition. The NADES extracts were observed to have higher tyrosinase inhibitory properties compared to extracts obtained by traditional organic solvents. Furthermore, the NADES extracts were relatively better inhibitors of the diabetic enzymes. These findings provided an interesting comparison in terms of total polyphenolic content yields, antioxidant and enzyme inhibitory properties (cholinesterase, amylase, glucosidase, and tyrosinase) between traditional solvent extracts and NADES extracts, used as an alternative. While the organic solvents showed better antioxidant activity, the NADES extracts were found to have some other improved properties, such as higher total phenolic content and enzyme-inhibiting properties, suggesting functional prospects for their use in phytonutrient extraction and fractionation. The obtained results could also be used to give a broad overview of the different biological potentials of C. hypocistis.

The Potential Neuroprotective Effect of Cyperus esculentus L. Extract in Scopolamine-Induced Cognitive Impairment in Rats: Extensive Biological and Metabolomics Approaches.

The aim of the present study is to investigate the phytochemical composition of tiger nut (TN) (Cyperus esculentus L.) and its neuroprotective potential in scopolamine (Scop)-induced cognitive impairment in rats. The UHPLC-ESI-QTOF-MS analysis enabled the putative annotation of 88 metabolites, such as saccharides, amino acids, organic acids, fatty acids, phenolic compounds and flavonoids. Treatment with TN extract restored Scop-induced learning and memory impairments. In parallel, TN extract succeeded in lowering amyloid beta, ß-secretase protein expression and acetylcholine esterase (AChE) activity in the hippocampus of rats. TN extract decreased malondialdehyde levels, restored antioxidant levels and reduced proinflammatory cytokines as well as the Bax/Bcl2 ratio. Histopathological analysis demonstrated marked neuroprotection in TN-treated groups. In conclusion, the present study reveals that TN extract attenuates Scop-induced memory impairments by diminishing amyloid beta aggregates, as well as its anti-inflammatory, antioxidant, anti-apoptotic and anti-AChE activities.

A Prospective of Multiple Biopharmaceutical Activities of Procyanidins-Rich Uapaca togoensis Pax Extracts: HPLC-ESI-TOF-MS Coupled with Bioinformatics Analysis.

The article reports the chemical composition, antioxidant, six key enzymes inhibitory and antimicrobial activities of two solvent extracts (water and methanol) of leaves and stem bark of Uapaca togoensis. For chemical composition, methanol extract of stem bark exhibited significant higher total phenolic (129.86 mg GAE/g) and flavanol (10.44 mg CE/g) contents. Methanol extract of leaves and water extract of stem bark showed high flavonoids (20.94 mg RE/g) and phenolic acid (90.40 mg CAE/g) content, respectively. In addition, HPLC-ESI-TOF-MS analysis revealed that U. togoensis was rich in procyanidins. The methanol and water extracts of stem bark had overall superior antioxidant activity; however, only methanol extract of stem bark showed higher inhibition of cholinesterase (AChE: 2.57 mg GALAE/g; BChE: 4.69 mg GALAE/g), tyrosinase (69.53 mg KAE/g) and elastase (2.73 mmol CE/g). Potent metal chelating ability was showed by water extract of leaves (18.94 mg EDTAE/g), higher inhibition of amylase was detected for water extracts of leaves (0.94 mmol ACAE/g) and stem bark (0.92 mmol ACAE/g). The tested extracts have shown wide-spectrum antibacterial properties and these effects have shown to be more effective against Aspergillus ochraceus, Penicillium funiculosum, Trichoderma viride, Bacillus cereus, Escherichia coli and Pseudomonas aeruginosa. The results revealed that the antioxidant, enzyme inhibitory and antimicrobial activities depended on the extraction solvents and the parts of plant. Bioinformatics analysis on the 17 major compounds showed modulation of pathway associated with cancer. In brief, U. togoensis might be valuable as potential source of natural agents for therapeutic application.

The Role of High-Resolution Analytical Techniques in the Development of Functional Foods.

The approaches based on high-resolution analytical techniques, such as nuclear magnetic resonance or mass spectrometry coupled to chromatographic techniques, have a determining role in several of the stages necessary for the development of functional foods. The analyses of botanical extracts rich in bioactive compounds is one of the fundamental steps in order to identify and quantify their phytochemical composition. However, the compounds characterized in the extracts are not always responsible for the bioactive properties because they generally undergo metabolic reactions before reaching the therapeutic targets. For this reason, analytical techniques are also applied to analyze biological samples to know the bioavailability, pharmacokinetics and/or metabolism of the compounds ingested by animal or human models in nutritional intervention studies. In addition, these studies have also been applied to determine changes of endogenous metabolites caused by prolonged intake of compounds with bioactive potential. This review aims to describe the main types and modes of application of high-resolution analytical techniques in all these steps for functional food development.

LC-MS and Spectrophotometric Approaches for Evaluation of Bioactive Compounds from Peru Cocoa By-Products for Commercial Applications.

Peru is one of the main areas where there are large cocoa crops with special relevance to the economy of this country. In fact, cocoa is a major, economically important, international crop which has been linked to several benefits, such as anti-allergenic, anti-atherogenic, anti-inflammatory, anti-microbial, anti-oxidant, anti-thrombotic, cardioprotective and vasodilatory properties, relating to its bioactive compound content. However, in cocoa industrial processing, several residues or wastes, which are commonly discarded generating a negative impact on the environment, are produced in large amounts. Some of the cocoa by-products, which go underutilized, could be a good source of bioactive compounds with high utility for the development of innovative products in nutraceutical, medical or pharmaceutical industries. For this reason, the aim of this study is to qualitatively determine the phytochemical composition of husk and bean extracts from different cocoa-growing areas and processes from Peru by high performance liquid chromatography coupled to mass spectrometry. Furthermore, we aim to evaluate their phenolic and flavan-3-ol contents and antioxidant capacities for the purpose of highlighting the potential of cocoa by-products from these cultivars as functional ingredients. In total, 49 chemical compounds were detected in the analyzed extracts. Comparing both husks and beans, bean extracts were characterized by high content in flavonoids whereas husk extracts had a higher content of phenolic acids. The presence of these compounds together with the bioactivity results suggest that these matrices may be further studied for their revaluation in the development of high added-value products in nutraceutical, medical, and pharmaceutical industries.

Innovative perspectives on Pulicaria dysenterica extracts: phyto-pharmaceutical properties, chemical characterization and multivariate analysis.

BACKGROUND: In this study, we aimed to evaluate the influence of different extraction procedures [decoction, homogenizer-assisted extraction (HAE), infusion, maceration, Soxhlet and ultrasound-assisted extraction (UAE)] on the chemical profiling and biological properties of methanol and water extracts of Pulicaria dysenterica (L.) Bernh. The chemical profiles of the extracts were evaluated by high-performance liquid chromatography coupled to electrospray ionization and time-of-flight mass spectrometry (HPLC-ESI-TOF-MS). The antioxidant properties and enzymes (lipase, α-amylase, α-glucosidase, tyrosinase and cholinesterases) inhibitory potential of the extracts were evaluated. RESULTS: The chemical profiles were dependent on the type of extraction methods as well as on the type of solvent. The methanolic extracts showed higher levels of total phenolic, flavonoid, and phenolic acid content, while the highest total flavonol content was observed in the HAE-water extract. Forty different compounds were identified from P. dysenterica. In relation to the potential in vitro anti-diabetic effects, the highest activity against the studied key enzymes was observed for the macerated extract (α-amylase: 0.58 ± 0.03 and α- glucosidase: 1.65 ± 0.03 mmol ACAE g-1 ). The HAE-methanol extract was the most potent inhibitor of cholisterases, whereas the highest activities against tyrosinase were observed for UAE-methanol extract, followed by macerated and Soxhlet. The inhibitory activity of the studied extracts against lipase were in the order: soxhlet > macerated> HAE-methanol > UAE-methanol. CONCLUSION: This study has established scientific baseline data on the therapeutic properties of P. dysentrica, thereby advocating the need for further investigations in an endeavour to develop novel pharmaceuticals from this plant. © 2019 Society of Chemical Industry.

Metabolite Profiling of Colvillea racemosa via UPLC-ESI-QTOF-MS Analysis in Correlation to the In Vitro Antioxidant and Cytotoxic Potential against A549 Non-Small Cell Lung Cancer Cell Line.

In this study, flower and leaf extracts of Colvillea racemosa were considered a source of bioactive compounds. In this context, the objective of the study focused on investigating the anticancer potential as well as the phytochemical composition of both extracts. The extracts were analyzed by UPLC-ESI-QTOF-MS, and the bioactivity was tested using in vitro antioxidant assays (FRAP, DPPH, and ABTS) in addition to cytotoxic assays on non-small cell lung cancer cell line (A549). Our results clearly indicated the potent radical scavenging capacity of both extracts. Importantly, the flower extract exhibited a greater antioxidant capacity than the leaf extract. In terms of cytotoxic activity, leaf and flower extracts significantly inhibited cell viability with IC50 values of 17.0 and 17.2 µg/mL, respectively. The phytochemical characterization enabled the putative annotation of 42 metabolites, such as saccharides, phenolic acids, flavonoids, amino acids, and fatty acids. Among them, the flavonoid C-glycosides stand out due to their high relative abundance and previous reports on their anticancer bioactivity. For a better understanding of the bioactive mechanisms, four flavonoids (vitexin, kaempferol-3-O-rutinoside, luteolin, and isoorientin) were selected for molecular docking on hallmark protein targets in lung cancer as represented by γ-PI3K, EGFR, and CDK2 through in-silico studies. In these models, kaempferol-3-O-rutinoside and vitexin had the highest binding scores on γ-PI3K and CDK2, followed by isoorientin, so they could be highly responsible for the bioactive properties of C. racemosa extracts.

Evaluation of Olive Leaf Phenolic Compounds' Gastrointestinal Stability Based on Co-Administration and Microencapsulation with Non-Digestible Carbohydrates.

The large generation of olive by-products has motivated their revalorization into high-added-value products. In this regard, olive leaves pose as an interesting source of bioactive compounds, due to their phenolic content with commonly known antioxidant, anti-inflammatory, and immunomodulatory properties, with potential application in non-communicable diseases. However, their effectiveness and applicability into functional foods is limited by their instability under gastrointestinal conditions. Thus, the development of protective formulations is essential. In this study, the spray-drying encapsulation of a phenolic-rich olive leaf extract with inulin as the encapsulating agent was optimized. Then, the behavior of the free extract under gastrointestinal conditions, its co-administration with the encapsulating agent, and the optimized microencapsulated formulation were studied through an in vitro gastrointestinal digestion process following the INFOGEST protocol. Digestion of the free extract resulted in the degradation of most compounds, whereas this was minimized in the co-administration of the non-encapsulated extract with the encapsulating agent. This protective effect, related to its interaction with inulin, was similar to the microencapsulated formulation. Thus, both approaches, co-administration and microencapsulation with inulin, could be promising strategies for the improvement of the stability of these anti-inflammatory and immunomodulatory compounds under gastrointestinal conditions, enhancing their beneficial effect.

Design and in vitro effectiveness evaluation of Echium amoenum extract loaded in bioadhesive phospholipid vesicles tailored for mucosal delivery.

The Echium amoenum Fisch. and C.A. Mey. (E. amoenum) is an herb native from Iranian shrub, and its blue-violet flowers are traditionally used as medical plants. In the present study, an antioxidant phytocomplex was extracted from the flowers of E. amoenum by ultrasounds-assisted hydroalcoholic maceration. The main components, contained in the extract, have been detected using HPLC-DAD, and rosmarinic acid was found to be the most abundant. The antioxidant power of the extract along with the phenolic content were measured using colorimetric assays. The extract was loaded in liposomes, which were enriched adding different bioadhesive polymers (i.e., mucin, xanthan gum and carboxymethyl cellulose sodium salt) individually or in combination. The main physico-chemical properties (i.e. size, size distribution, surface charge) of the prepared vesicles were measured as well as their stability on storage. The viscosity of dispersion and the ability of vesicles to interact with mucus were evaluated measuring their stability in a mucin dispersion and mobility in a mucin film. The biocompatibility and the ability of the formulations to protect keratinocytes from damages caused by hydrogen peroxide and to promote the cell migration were measured in vitro.

Phytochemical Profile and Biological Activities of Different Extracts of Three Parts of Paliurus spina-christi: A Linkage between Structure and Ability.

Paliurus spina-christi Mill., a member of the Rhamnaceae family, is a traditionally used medicinal plant in the management of a panoply of human ailments. The current research focused on its phytochemical profile and biological properties evaluated by its antioxidant and enzyme inhibitory properties. The methanol extract was found to be the most effective antioxidant as evidenced by its DPPH and ABTS scavenging activities, cupric and ferric reducing power (CUPRAC and FRAP), and high activity in phosphomolybdenum (PBD) assay, and also displayed the highest anti-tyrosinase activity. The n-hexane extract was the most effective AChE inhibitor (8.89 ± 0.08 mg GALAE/g) followed by the methanol (8.64 ± 0.01 mg GALAE/g) while the latter showed the highest BChE inhibition (2.50 ± 0.05 mg GALAE/g). Among the different solvent extracts of the stem, the methanolic extract showed highest antioxidant activity in the following assays: DPPH (909.88 ± 4.25 mg TE/g), ABTS (3358.33 ± 51.14 mg TE/g), CUPRAC (781.88 ± 16.37 mg TE/g), FRAP (996.70 ± 47.28 mg TE/g), and PBD (4.96 ± 0.26 mmol TE/g), while the dichloromethane extract showed the highest MCA (28.80 ± 0.32 mg EDTAE/g). The methanol extracts revealed the highest TPC and TFC among the different solvents used, and as for plant part, the stem extracts had the highest TPC ranging from 22.36 ± 0.26 to 121.78 ± 1.41 (mg GAE/g), while the leaf extracts showed the highest TFC ranging from 8.43 ± 0.03 to 75.36 ± 0.92 (mg RE/g). Our findings tend to provide additional scientific evidence on the biological and chemical activities of P. spina-christi, which may serve as a source of naturally occurring bioactive chemicals with potential biomedical applications.

From Grape By-Products to Enriched Yogurt Containing Pomace Extract Loaded in Nanotechnological Nutriosomes Tailored for Promoting Gastro-Intestinal Wellness.

Grape pomace is the main by-product generated during the winemaking process; since it is still rich in bioactive molecules, especially phenolic compounds with high antioxidant power, its transformation in beneficial and health-promoting foods is an innovative challenge to extend the grape life cycle. Hence, in this work, the phytochemicals still contained in the grape pomace were recovered by an enhanced ultrasound assisted extraction. The extract was incorporated in liposomes prepared with soy lecithin and in nutriosomes obtained combining soy lecithin and Nutriose FM06®, which were further enriched with gelatin (gelatin-liposomes and gelatin-nutriosomes) to increase the samples' stability in modulated pH values, as they were designed for yogurt fortification. The vesicles were sized ~100 nm, homogeneously dispersed (polydispersity index < 0.2) and maintained their characteristics when dispersed in fluids at different pH values (6.75, 1.20 and 7.00), simulating salivary, gastric and intestinal environments. The extract loaded vesicles were biocompatible and effectively protected Caco-2 cells against oxidative stress caused by hydrogen peroxide, to a better extent than the free extract in dispersion. The structural integrity of gelatin-nutriosomes, after dilution with milk whey was confirmed, and the addition of vesicles to the yogurt did not modify its appearance. The results pointed out the promising suitability of vesicles loading the phytocomplex obtained from the grape by-product to enrich the yogurt, offering a new and easy strategy for healthy and nutritional food development.

Application of Response Surface Methodologies to Optimize High-Added Value Products Developments: Cosmetic Formulations as an Example.

In recent years, green and advanced extraction technologies have gained great interest to revalue several food by-products. This by-product revaluation is currently allowing the development of high value-added products, such as functional foods, nutraceuticals, or cosmeceuticals. Among the high valued-added products, cosmeceuticals are innovative cosmetic formulations which have incorporated bioactive natural ingredients providing multiple benefits on skin health. In this context, the extraction techniques are an important step during the elaboration of cosmetic ingredients since they represent the beginning of the formulation process and have a great influence on the quality of the final product. Indeed, these technologies are claimed as efficient methods to retrieve bioactive compounds from natural sources in terms of resource utilization, environmental impact, and costs. This review offers a summary of the most-used green and advanced methodologies to obtain cosmetic ingredients with the maximum performance of these extraction techniques. Response surface methodologies may be applied to enhance the optimization processes, providing a simple way to understand the extraction process as well as to reach the optimum conditions to increase the extraction efficiency. The combination of both assumes an economic improvement to attain high value products that may be applied to develop functional ingredients for cosmetics purposes.

Diet Supplementation with Polyphenol-Rich Salicornia ramosissima Extracts Protects against Tissue Damage in Experimental Models of Cerebral Ischemia.

Strokes are the second most common cause of death worldwide and a leading cause of disability. Regular consumption of polyphenols has been shown to reduce the risk of suffering a cardiovascular event. For this reason, we have investigated the protective effect of Salicornia ramosissima, a seasonal halophyte that synthetizes high amounts of bioactive compounds, including polyphenols, in response to environmental stress. Aqueous, hydroalcoholic, and ethanolic extracts were prepared to investigate if dietary supplementation prior to ischemic challenge can prevent subsequent damage using two animal models. First, we screened the protective effect against hypoxia-reoxygenation in Drosophila melanogaster and observed that both ethanolic and hydroalcoholic extracts protected flies from the deleterious effects of hypoxia. Second, we confirmed the protective effect of S. ramosissima ethanolic extract against brain ischemia using the transient middle cerebral artery occlusion mice model. Four weeks of oral supplementation with the ethanolic extract before artery occlusion reduced infarct volume and lowered the plasma levels of the DNA peroxidant product 8-hydroxydeoxyguanosine. Phytochemical profiling of S. ramosissima ethanolic extract revealed 50 compounds. Thus, it represents a valuable source of bioactive compounds that show promising disease-modifying activities and could be further developed as an effective food supplement for the prevention or treatment of neurovascular disorders.

Recovery of Bioactive Compounds from Pomegranate (Punica granatum L.) Peel Using Pressurized Liquid Extraction.

Pressurized liquid extraction (PLE) is a clean and environmentally friendly alternative for the recovery of bioactive compounds from fruit by-products. Herein we focused on PLE for the extraction of bioactive compounds from pomegranate peel using a combination of pressurized water and ethanol. The main aim was to determine the optimal PLE conditions, i.e., ethanol percentage and process temperature, to obtain a pomegranate peel extract (PPE) with maximum total phenolic content (TPC), punicalagin content, and antimicrobial activity (AMA). The experimental design was conducted using a central composite design with axial points. Response surface methodology was applied to optimize the response variables using the desirability function. Multiple response optimization indicated a process temperature of 200 °C and ethanol of 77% as optimal conditions. The TPC and the punicalagin content of PPE-PLE obtained under optimal conditions were 164.3 ± 10.7 mg GAE/g DW and 17 ± 3.6 mg/g DW, respectively. Our findings support the efficacy of PLE on TPC recovery but not in punicalagin recovery. The AMA against S. aureus was 14 mm. The efficacy of PPE-PLE in food applications must continue to be studied in order to achieve adequate information on its potential for developing new food additives.

Extraction of the antioxidant phytocomplex from wine-making by-products and sustainable loading in phospholipid vesicles specifically tailored for skin protection.

The present study is aimed at valorizing grape pomace, one of the most abundant winery-making by-products of the Mediterranean area, through the extraction of the main bioactive compounds from the skin of grape pomace and using them to manufacture innovative nanoformulations capable of both avoiding skin damages and promoting skincare. The phytochemicals were recovered through maceration in hydroethanolic solution. Catechin, quercetin, fisetin and gallic acid, which are known for their antioxidant power, were detected as the main compounds of the extract. Liposomes and phospholipid vesicles modified with glycerol or Montanov 82® or a combination of both, were used as carriers for the extract. The vesicles were small (~183 nm), slightly polydispersed (PI ≥ 0.28), and highly negatively charged (~-50 mV). The extract was loaded in high amounts in all vesicles (~100%) irrespective of their composition. The antioxidant activity of the extract, measured by using the DPPH (2,2-Diphenyl-1-picrylhydrazyl) test, was 84 ± 1%, and slightly increased when loaded into the vesicles (~89%, P < 0.05). The grape pomace extract loaded vesicles were highly biocompatible and able to protect fibroblasts (3T3) from the oxidative stress induced by hydrogen peroxide.

Development of advanced phospholipid vesicles loaded with Lippia citriodora pressurized liquid extract for the treatment of gastrointestinal disorders.

Pressurized liquid extraction was performed to obtain a phytocomplex from Lippia citriodora leaves rich in bioactive compounds. The extract was loaded in phospholipid vesicles to improve its protective effect against oxidative stress in the intestine. The phytochemicals were identified and quantified by HPLC-ESI-TOF-MS. The extract was incorporated in liposomes and penetration enhancer-containing vesicles (PEVs) modified with glucidex, a dextrin, and a biopolymer obtained from Chimaera monstrosa. The PEVs were smaller than liposomes (~150 vs 370 nm) and more stable, according to accelerated aging tests. The integrity of the vesicles in acidic or neutral pH and high ionic strength or in milk whey was assessed. The cytocompatibility of the formulations and their ability to protect Caco-2 cells against oxidative stress were confirmed in vitro and compared with two commercial extracts of L. citriodora. The results confirmed the suitability of formulations to be used in functional foods to protect the intestine from oxidative stress.

Bioactivity assays, chemical characterization, ADMET predictions and network analysis of Khaya senegalensis A. Juss (Meliaceae) extracts.

Khaya senegalensis A. Juss (Meliaceae) is a popular medicinal plant, widely used in the management of various ailments in the African traditional medicine. This study attempts to investigate into the different extraction methods (homogenizer-assisted extraction (HAE), maceration (MAC), infusion and Soxhlet (SE) extraction) on the pharmacological properties and chemical profiles of K. senegalensis. Antioxidant properties and inhibitory potential against key enzymes were assessed and bioinformatics analysis was conducted on selected limonoids to predict putative pharmacokinetics and protein targets underlying the pharmacological effects. Overall, the leaf extracts showed notable flavonoid (20.59-104.43 mg RE/g) content and the stem barks extracts displayed the highest total phenolic (87.69-46.28 mg GAE/g), phenolic acid (62.96-107.22 mg CE/g), flavanol (3.60-135.40 mg CAE/g) contents. All extracts showed remarkable antioxidant activities, with the MAC-Water leaf extract being most active in all the assays. Regarding stem bark, the MAC-MeOH extract exerted the highest free radical scavenging abilities, while HAE and MAC extracts were better sources of reducing agent and metal chelators. The HAE-MeOH, MAC-Water, and SE extracts showed noteworthy inhibitory activity against AChE, BChE (only stem barks), tyrosinase and α-glucosidase (only stem barks). All extracts displayed moderate inhibitory activities against α-amylase. The bioinformatics approach showed that khayanoside A and C interacted with multiple isoforms of metalloproteinase, while humilin B and khayanone interacted with opioid receptors. To sum up, the chemical profiles and biological activities of K. senegalensis were closely dependent on the extraction methods. Results amassed from this study showed that K. senegalensis is a potent source of bioactive compounds which could be explored as a functional food.

Comprehensive Analysis of Antioxidant Compounds from Lippia citriodora and Hibiscus sabdariffa Green Extracts Attained by Response Surface Methodology.

Phenolic compounds have shown to have a high bioactive potential against various pathologies, postulating as an interesting alternative to manage some diseases. In this sense, both Lippia citriodora and Hibiscus sabdariffa are two botanical sources with a demonstrated high bioactive potential, in which their antioxidant capacity stands out. In this work, the optimization of the extraction conditions for the recovery of phytochemicals from L. citriodora leaves and H. sabdariffa calyces has been carried out using Response Surface Methodologies (RSM) considering their total polar compounds measured by HPLC-ESI-TOF/MS and Folin-Ciocalteu assay, and its antioxidant capacity evaluated by Ferric Reducing Antioxidant Power (FRAP) and Trolox Equivalent Antioxidant Capacity (TEAC) assays. The results showed that to maximize the antioxidant capacity in H. sabdariffa, a moderate temperature and high ethanol percentage are needed, while a low temperature and a high percentage of ethanol are needed in L. citriodora. In addition, with the results obtained in the multiple response analysis, it is possible to affirm the importance of this type of analysis to develop functional ingredients, taking into account both total content of phenolic compounds and their bioactivity. Furthermore, as confirmed in this study, these analyses can be extrapolated in different techniques and in different matrices, with phenolic compounds from different families being important to develop new high added value products for food, pharmaceutical or cosmetic industries.