Bioactive Phenolics Research Articles

Enzyme-Assisted Coextraction of Phenolics and Polysaccharides from Padina gymnospora.

Brown seaweed is a promising source of polysaccharides and phenolics with industrial utility. This work reports the development of a green enzyme-assisted extraction method for simultaneously extracting polysaccharides and phenolics from the brown seaweed Padina gymnospora. Different enzymes (Cellulast, Pectinex, and Alcalase), individually and in combination, were investigated, with Alcalase alone showing the highest efficiency for the simultaneous extraction of polysaccharides and phenolics. Yields from Alcalase-assisted aqueous extraction were higher than those obtained using either water alone or conventional ethanol extraction. Alcalase-assisted extraction was subsequently optimized using a response surface methodology to maximize compound recovery. Maximal polysaccharide and phenolic recovery was obtained under the following extraction conditions: a water-to-sample ratio of 61.31 mL/g, enzyme loading of 0.32%, temperature of 60.5 °C, and extraction time of 1.95 h. The extract was then fractionated to obtain alginate-, fucoidan-, and phenolic-rich fractions. Fractions exhibited potent 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity with IC50 values of 140.55 µg/mL, 126.21 µg/mL, and 48.17 µg/mL, respectively, which were higher than those obtained from conventional extraction methods. The current work shows that bioactive polysaccharides and phenolics can be obtained together in high yield through a single aqueous-only green and efficient Alcalase-assisted extraction.

Bioactive Phenolics and Flavonoids, Antioxidants, Anti-Inflammatory, Enzyme-Inhibitory and Cytotoxic Activities of Aerial part of Trachyspermum roxburghianum (DC.) Craib.

Trachyspermum roxburghianum (DC.) Craib is an edible plant found in Northern and Northeastern Thailand. This plant is used in household remedies to relieve carminative and digestive problems, hiccups, vomiting, bladder pain, etc. This study aims to assess the bioactive compounds, consisting of phenolics and flavonoids, and evaluate the biological activities of this plant. The aerial portion was macerated in EtOH1 to obtain EtOH1 crude extracts. Then, the EtOH1 was divided and separated by the solvents’ polarity to obtain Petr, EtOAc, and EtOH2 crude extracts. All crude extracts were assessed for their total phenolics and flavonoids and subsequentially evaluated for their antioxidants (using DPPH, ABTS and FRAP), enzymatic inhibitory effects (on tyrosinase and collagenase), anti-inflammatory activity (protein denaturation assay) and cytotoxicity (MTT assay). The results presented that a high amount of phenolics and flavonoids were observed in EtOH2 (56.57 mg GAE/g ext. and 22.75 mg QE/g ext.) followed by EtOAc (57.95 mg GAE/g ext. and 7.41 mg QE/g ext.), EtOH1 (47.14 mg GAE/g ext. and 4.23 mg QE/g ext.), and Petr (37.05 mg GAE/g ext. and 2.08 mg QE/g ext.), respectively. All crude extracts represented antioxidants in all assays; EtOAc presented a high level of antioxidants on ABTS (IC50 54.96 µg/mL) and DPPH (IC50 133.32 µg/mL), while EtOH2 revealed a high ability to reduce the Fe3+-TPTZ complex (155.85 Fe2+g ext.). Remarkably, for all crude extracts used for anti-collagenase enzyme activity, the percentage of inhibition ranged from 78.35 - 97.96 %. Besides, only Petr and EtOH2 showed the activity of the anti-protein denaturation (IC50 1.926 and 2.578 mg/mL). The cytotoxicity test showed that EtOH1, Petr, and EtOAc exhibited a concentration-dependent manner of inducing cell death in 24 and 48 h, while EtOH2 showed less toxicity to the cell line. This information would be valuable and pave the way for future study and application of this plant to other products. HIGHLIGHTS Trachyspermum roxburghianum (DC.) Craib from Northern Thailand High antioxidant and high anti-collagenase activities of Trachyspermum roxburghianum (DC.) Craib ethanolic extracts. GRAPHICAL ABSTRACT

Antioxidative, Metabolic and Vascular Medicinal Potentials of Natural Products in the Non-Edible Wastes of Fruits Belonging to the Citrus and Prunus Genera: A Review.

Diabetes mellitus and related metabolic and vascular impairments are notable health problems. Fruits and vegetables contain phenolics that are beneficial to metabolic and oxidative health and useful in preventing associated disease. Scientific evidence has shown that some bioactive phenolics are more abundant in the non-edible parts (especially the peels) of many fruits than in their respective edible tissues. Fruits belonging to the Citrus and Prunus genera are commonly consumed worldwide, including in South Africa, and their non-edible wastes (peel and seed) have been shown to have antioxidative, metabolic and vascular pharmacological potentials and medicinal phytochemistry. It is therefore imperative to evaluate the pharmacological actions and phytochemical properties of the non-edible wastes of these fruits and understand how they could potentially be of medicinal relevance in oxidative, metabolic and vascular diseases, including diabetes, oxidative stress, obesity, hypertension and related cardiovascular impairments. In the absence of a previous review that has concomitantly presented the medicinal potentials of fruits wastes from both genera, this review presents a critical analysis of previous and recent perspectives on the medicinal potential of the non-edible wastes from the selected Citrus and Prunus fruits in metabolic, vascular and oxidative health. This review further exposes the medicinal phytochemistry, while elucidating the underlying mechanisms through the fruit wastes potentiates their therapeutic effects. A literature search was carried out on "PubMed" to identify peer-reviewed published (mostly 2015 and beyond) studies reporting the antidiabetic, antioxidative, antihypertensive, anti-hyperlipidemic and anti-inflammatory properties of the non-edible parts of the selected fruits. The data of the selected studies were analyzed to understand the bioactive mechanisms, bioactive principles and toxicological profiles. The wastes (seed and peel) of the selected fruits had antioxidant, anti-obesogenic, antihypertensive, anti-inflammatory, antidiabetic and tissue protective potentials. Some phenolic acids and terpenes, as well as flavonoids and glycosides such as narirutin, nobiletin, hesperidin, naringin, naringenin, quercetin, rutin, diosmin, etc., were the possible bioactive principles. The peel and seed of the selected fruits belonging to the Citrus and Prunus genera are potential sources of bioactive compounds that could be of medicinal relevance for improving oxidative, metabolic and vascular health. However, there is a need for appropriate toxicological studies.

Bacopa monnieri Extract As a Neuroprotective and Cognitive Enhancement Agent

Review Bacopa monnieri Extract As a Neuroprotective and Cognitive Enhancement Agent Bevin J. Nishanth 1, Princy Vijayababu 2, * , and Noble K. Kurian 3 1 Department of Biotechnology, Loyola CollegeChennai600034India 2 The Institute of Biotechnological Research, Rajkot 360004, GujaratIndia 3 School of Life Sciences, B.S.Abdur Rahman Crescent Institute of Science and TechnologyChennai600048India * Correspondence: princyvijayababu@gmail.com Received: 14 July 2023 Accepted: 8 August 2023 Published: 27 December 2023 Abstract: Traditional Indian medicine uses the neuroprotective and cognitive-enhancing effects of the spice, Bacopa monnieri, commonly known as Brahmi. This paper provides an overview of the potential neuropharmacological benefits and therapeutic applications of Bacopa monnieri. Bacopa monnieri has therapeutic value due to the inclusion of bioactive compounds, including alkaloids, flavonoids, tannins, and phenolics. Bacoside A, a triterpenoid saponin of the Dammarane family, has been studied most because of its potential to improve memory and cognitive function. Specific brain regions that are affected by bacoside A experience an increase in protein and RNA production, oxidative stress protection, improved cerebral blood flow, and enhanced synaptic activity. By boosting antioxidant defense mechanisms, lowering oxidative stress, and altering neurotransmitter levels, Bacopa monnieri demonstrates neuroprotective effects. By blocking the activity of acetylcholinesterase, lowering the production of β-amyloid plaques, and modifying neurotransmitter levels, it has demonstrated potential for treating neurodegenerative disorders, such as Alzheimer’s and Parkinson’s disease. As a natural neuroprotective and cognitive-improving agent, Bacopa monnieri is generally found to be promising. To completely comprehend its mechanisms of action and assess its long-term toxicity, more studies are necessary. Further research is needed to determine whether Bacopa monnieri can be used as a possible treatment for neurodegenerative diseases.

Exploring the Multifaceted Potential of Annona squamosa: A Natural Treasure for Health and Wellness

This article gives an in-depth look at the tropical fruit Annona squamosa L., which has a long history of traditional medicinal usage and is discussed in this review for its phytochemical and pharmacological qualities. The botanical specimen showcases an extensive assortment of bioactive constituents, encompassing glycosides, proteins, carbohydrates, saponins, alkaloids, flavonoids, and phenolics, which have significant antioxidant, antibacterial, antiviral, anticancer, antidiabetic, anti-inflammatory, anti-ulcer, and skin-protective properties. The leaves contain high protein content and essential oils amusing in terpenes and sesquiterpenes, which have shown potential in treating health conditions

Exploring the Bioactive Content of Liquid Waste and Byproducts Produced by Two-Phase Olive Mills in Laconia (Greece): Is There a Prospect for Added-Value Applications?

The use of a two-phase decanter (TwPD) for olive-oil extraction produces wastes and byproducts (a small volume of water from oil washing, olive leaves from the defoliator, and a high moisture pomace which can be destoned) that contain valuable bioactive compounds, such as phenolics and/or triterpenic acids. So far, there is no (water) or limited information (leaves and the destoned pomace fraction) on their content of bioactives, especially triterpenic acids. To contribute to the characterization of such streams from cultivars of international interest, in the present study, samples obtained from five mills from the region of Laconia (from one or two harvests) in Greece, where Koroneiki cv dominates, were screened for phenols and/or triterpenic acids. The leaves and pomace were dried at two temperatures (70 °C and/or 140 °C), and the pomace was also destoned before analysis. The liquid wastes contained low amounts of total (TPC) phenols (<140 mg gallic acid/L), hydroxytyrosol (<44 mg/L), and tyrosol (<33 mg/L). The olive leaves varied widely in TPC (12.8-57.4 mg gallic acid/g dry leaf) and oleuropein (0.4-56.8 mg/g dry leaf) but contained an appreciable amount of triterpenic acids, mainly oleanolic acid (~12.5-31 mg/g dry leaf, respectively). A higher drying temperature (140 vs. 70 °C) affected rather positively the TPC/oleuropein content, whereas triterpenic acids were unaffected. The destoned pomace TPC was 15.5-22.0 mg gallic acid/g dw, hydroxytyrosol 3.9-5.6 mg/g dw, and maslinic 5.5-19.3 mg/g dw. Drying at 140 °C preserved better its bioactive phenols, whereas triterpenic acids were not influenced. The present findings indicate that TwPD streams may have a prospect as a source of bioactives for added-value applications. Material handling, including drying conditions, may be critical but only for phenols.

Evaluation of phenolics and bioactivities of Camellia quephongensis leaf extracts as affected by various extraction solvents

Camellia quephongensis is an endemic Theaceae species from Central Vietnam. In the present study, phenolics in extracts from leaves of this plant species were quantified. Additionally, free radical scavenging activities, α-amylase and albumin denaturation inhibitory effects of the extracts were evaluated. Catechins were found at significantly higher concentrations in the methanolic and ethanolic extracts compared to the other extracts. The ethanolic extract showed the most potent radical scavenging activities determined by ABTS and DPPH assays, with IC50 values of 57.88 ± 1.89 and 47.87 ± 0.16 μg/mL, respectively. Furthermore, the capacity of this extract to counteract ABTS radicals was comparable with that of ascorbic acid. The ethyl acetate extract exerted the strongest α-amylase inhibitory activity (IC50 = 985.79 ± 16.37 μg/mL). The aqueous methanolic extract with the lowest IC50 value (57.56 ± 3.28 μg/mL) exhibited the highest protective effect on albumin against denaturation, and this was even higher than that of diclofenac. The correlation analysis demonstrated that catechins and ferulic acid may play important roles in radical scavenging activities while gallic acid, chlorogenic acid, and rutin could contribute to albumin denaturation inhibitory effects of the extracts. The findings of the study improve our understanding of bioactive phenolics and potential health benefits associated with C. quephongensis leaves.

Research progress on the regulation of oxidative stress by phenolics: the role of gut microbiota and Nrf2 signaling pathway.

In recent years, the increase in high-calorie diets and sedentary lifestyles has made obesity a global public health problem. An unbalanced diet promotes the production of proinflammatory cytokines and causes redox imbalance in the body. Phenolics have potent antioxidant activity and cytoprotective ability. They can scavenge free radicals and reactive oxygen species, and enhance the activity of antioxidant enzymes, thus combating the body's oxidative stress. They can also improve the body's inflammatory response, enhance the enzyme activity of lipid metabolism, and reduce the contents of cholesterol and triglyceride. Most phenolics are biotransformed and absorbed into the blood after the action by gut microbiota; these metabolites then undergo phase I and II metabolism and regulate oxidative stress by scavenging free radicals and increasing expression of antioxidant enzymes. Phenolics induce the expression of genes encoding antioxidant enzymes and phase II detoxification enzymes by stimulating Nrf2 to enter the nucleus and bind to the antioxidant response element after uncoupling from Keap1, thereby promoting the production of antioxidant enzymes and phase II detoxification enzymes. The absorption rate of phenolics in the small intestine is extremely low. Most phenolics reach the colon, where they interact with the microbiota and undergo a series of metabolism. Their metabolites will reach the liver via the portal vein and undergo conjugation reactions. Subsequently, the metabolites reach the whole body to exert biological activity by traveling with the systemic circulation. Phenolics can promote the growth of probiotics, reduce the ratio of Firmicutes/Bacteroidetes (F/B), and improve intestinal microecological imbalance. This paper reviews the nutritional value, bioactivity, and antioxidant mechanism of phenolics in the body, aiming to provide a scientific basis for the development and utilization of natural antioxidants and provide a reference for elucidating the mechanism of action of phenolics for regulating oxidative stress in the body. © 2023 Society of Chemical Industry.

How to Increase the Nutritional Quality of Stinging Nettle Through Controlled Plant Nutrition§.

As food production faces major challenges, modern agricultural practices are increasingly focused on conserving resources, reducing negative environmental impacts and sustainably producing food with a high content of health-promoting phytochemicals. During production, many factors can affect the quality and chemical composition of a final food product. Proper selection of cultivating conditions, especially a balanced nutrition, can significantly increase nutritional value and result in foods with strong biological and functional properties. Stinging nettle is a rich source of minerals, vitamins, pigments, phenols and other bioactive compounds and can be consumed as a green leafy vegetable with beneficial effects on human health. Therefore, the aim of this study is to determine the nutritional quality and antioxidant capacity of stinging nettle leaves under the influence of different nutrient solution (NS) treatments and three harvest cycles. The experiment was conducted in a floating hydroponic system in which treatments with different nutrient solutions were applied and three harvest cycles were carried out. After each harvest, the following treatments were applied: treatment 1 - depletion of nutrient solution by adding water, treatment 2 - supplementation of nutrient solution by adding initial nutrient solution and treatment 3 - correction of nutrient solution by adding nutrients. Among the bioactive compounds, minerals, ascorbic acid, phenols and photosynthetic pigments content, as well as antioxidant capacity were analysed spectrophotometrically, while individual phenols were determined by liquid chromatography. Different nutrition solution treatments and the number of harvest cycles had a significant effect on the content of the analysed bioactive compounds. The highest mass fraction (on fresh mass basis) of total phenols expressed as gallic acid equivalents (377.04 mg/100 g), total flavonoids expressed as catechol equivalents (279.54 mg/100 g), ascorbic acid (112.37 mg/100 g) and pigments (total chlorophylls 1.84, and total carotenoids 0.36 mg/g) as well as the highest antioxidant capacity expressed as Trolox equivalents (35.47 µmol/g) were recorded in the samples supplemented with nutrient solution (treatment NS2) and analysed after the third harvest. This is the first time that stinging nettle leaves have been produced in a floating hydroponic system by controlled plant nutrition. We have set this type of nutritional manipulation with multiple harvest cycles as an innovative technique for the production of novel food with improved nutritional value that can be consumed as green leafy vegetables.

Inhibitory Effect of Quercetin on Oxidative Endogen Enzymes: A Focus on Putative Binding Modes.

Oxidative stress is defined as an imbalance between the production of free radicals and reactive oxygen species (ROS) and the ability of the body to neutralize them by anti-oxidant defense systems. Cells can produce ROS during physiological processes, but excessive ROS can lead to non-specific and irreversible damage to biological molecules, such as DNA, lipids, and proteins. Mitochondria mainly produce endogenous ROS during both physiological and pathological conditions. Enzymes like nicotinamide adenine dinucleotide phosphate oxidase (NOX), xanthine oxidase (XO), lipoxygenase (LOX), myeloperoxidase (MPO), and monoamine oxidase (MAO) contribute to this process. The body has enzymatic and non-enzymatic defense systems to neutralize ROS. The intake of bioactive phenols, like quercetin (Que), can protect against pro-oxidative damage by quenching ROS through a non-enzymatic system. In this study, we evaluate the ability of Que to target endogenous oxidant enzymes involved in ROS production and explore the mechanisms of action underlying its anti-oxidant properties. Que can act as a free radical scavenger by donating electrons through the negative charges in its phenolic and ketone groups. Additionally, it can effectively inhibit the activity of several endogenous oxidative enzymes by binding them with high affinity and specificity. Que had the best molecular docking results with XO, followed by MAO-A, 5-LOX, NOX, and MPO. Que's binding to these enzymes was confirmed by subsequent molecular dynamics, revealing different stability phases depending on the enzyme bound. The 500 ns simulation showed a net evolution of binding for NOX and MPO. These findings suggest that Que has potential as a natural therapy for diseases related to oxidative stress.

Storage Effects on Bioactive Phenols in Calabrian Monovarietal Extra Virgin Olive Oils Based on the EFSA Health Claim.

The beneficial properties of extra virgin olive oil (EVOO) on lipids blood levels were recognized by the European Food Safety Authority (EFSA) with a health claim, specifically referring to EVOOs containing at least 5 mg of hydroxytyrosol and its secoiridoids derivatives per 20 g of oil. The main purpose of the work was to characterize the phenolic profile of two commercially available Calabrian monovarietal EVOOs (Nocellara del Belice, VN; Dolce di Rossano, VDR), and to study the effect of one-year storage on secoiridoids composition, by monthly controls. A new UHPLC-ESI-HRMS method was developed and validated, thus facilitating the EFSA claim application and allowing producers to valorize their products. Seven biologically active compounds were chosen: tyrosol, hydroxytyrosol, oleocanthal, oleacein, oleuropein aglycone, verbascoside, and oleuropein. LODs and LOQs were 0.001-0.02 mg g-1 and 0.002-0.08 mg g-1, respectively. The variation coefficients were ≤20% and the percentage of recovery was between 89-109%. During the 12-month storage period, the concentration of selected compounds ranged between 1258.78-1478.91 mg Kg-1 for VN, and 1408.22-2071.45 mg Kg-1 for VDR, with a decrease of 15% and 32% respectively. The method allows an accurate quantification of EVOO phenols thus being useful to certify the nutraceutical properties of olive oil.

Optimizing the Integration of Microwave Processing and Enzymatic Extraction to Produce Polyphenol-Rich Extracts from Olive Pomace.

The integration of green technologies such as microwave- and enzyme-assisted extraction (MEAE) has been shown to improve the extraction efficiency of bioactive compounds while reducing processing time and costs. MEAE using tannase alone (MEAE-Tan), or in combination with cellulase and pectinase (MEAE-Tan-Cel-Pec), was optimized to produce enriched phenolic and antioxidant extracts from olive pomace. The individual and integrated impact of enzyme concentration, temperature, and pomace/water ratio were determined using a central composite rotatable design. Optimal extraction conditions for MEAE-Tan (60 °C, 15 min, 2.34% of enzyme (w/w), and 1:15 pomace/water ratio) and MEAE-Tan-Cel-Pec (46 °C, 15 min, 2% of enzymes (w/w), in the proportion of 1:1:1, and 1:20 pomace/water ratio) resulted in extracts containing 7110.6 and 2938.25 mg GAE/kg, respectively. The antioxidant activity of the extracts was correlated with phenolic acid release, which was enzyme-dependent, as determined with HPLC-DAD analysis. Enzyme selection had a significant impact on the phenolic profile of extracts, with tannase releasing high concentrations of chlorogenic acid and the combined use of enzymes releasing high concentrations of hydroxytyrosol and chlorogenic and ferulic acids. The novelty of this study relies on the integration and optimization of two green technologies (microwave- and enzyme-assisted extraction) to improve the extraction efficiency of bioactive phenolics from olive pomace while reducing processing time and costs. While these techniques have been evaluated isolated, the benefits of using both processing strategies simultaneously remain largely unexplored. This study demonstrates the effectiveness of the integration and processing optimization of two environmentally friendly technologies as a promising alternative to treat agro-industrial byproducts.

Bioactive (Poly)phenol Concentrations in Plant-based Milk Alternatives in the US Market

Bioactive (Poly)phenol Concentrations in Plant-based Milk Alternatives in the US Market

Unlocking the Power of Onion Peel Extracts: Antimicrobial and Anti-Inflammatory Effects Improve Wound Healing through Repressing Notch-1/NLRP3/Caspase-1 Signaling.

Onion peels are often discarded, representing an unlimited amount of food by-products; however, they are a valuable source of bioactive phenolics. Thus, we utilized UPLC-MS/MS to analyze the metabolomic profiles of red (RO) and yellow (YO) onion peel extracts. The cytotoxic (SRB assay), anti-inflammatory (Griess assay), and antimicrobial (sensitivity test, MIC, antibiofilm, and SP-SDS tests) properties were assessed in vitro. Additionally, histological analysis, immunohistochemistry, and ELISA tests were conducted to investigate the healing potential in excisional skin wound injury and Candida albicans infection in vivo. RO extract demonstrated antibacterial activity, limited skin infection with C. albicans, and improved the skin's appearance due to the abundance of quercetin and anthocyanin derivatives. Both extracts reduced lipopolysaccharide-induced nitric oxide release in vitro and showed a negligible cytotoxic effect on MCF-7 and HT29 cells. When extracts were tested in vivo for their ability to promote tissue regeneration, it was found that YO peel extract had the greatest impact. Further biochemical analysis revealed that YO extract suppressed NLRP3/caspase-1 signaling and decreased inflammatory cytokines. Furthermore, YO extract decreased Notch-1 levels and boosted VEGF-mediated angiogenesis. Our findings imply that onion peel extract can effectively treat wounds by reducing microbial infection, reducing inflammation, and promoting tissue regeneration.

Uncovering the Phytochemical Profile, Antioxidant Potency, Anti-Inflammatory Effects, and Thrombolytic Activity in Dendrobium lindleyi Steud.

Background. Dendrobium genus has been used in traditional medicine to treat various illnesses. The study aims at examining the phytochemical, antioxidant, anti-inflammatory, and thrombolytic properties of the leaf, stem, and root of Dendrobium lindleyi Steud, and the relationship between phytochemicals and bioactivities is determined. Results. The qualitative screening found a variety of bioactive compounds, including alkaloids, coumarins, cardiac glycosides, glycosides, flavonoids, proteins, phenols, quinines, resins, steroids, saponins, tannins, and terpenoids, in varying amounts. The quantitative screening showed the highest concentration of alkaloids in the leaves (172.15 ± 1.22 mg/g), phenols in the root (203.55 ± 0.75 mg/g), flavonoids in the root (24.35 ± 0.42 mg/g), tannins in the leaves (105.06 ± 0.55 mg/g), and proteins in the root (194.12 ± 0.65 µg/ml). The root extract showed the highest antioxidant activity (IC50 = 58.24 µg/mL), the stem extract had the most increased thrombolytic activity (IC50 = 242.74 µg/mL), and the leaf extract had the most potent anti-inflammatory activity (IC50 = 61.79 µg/mL). Statistical analysis revealed a significant positive relationship (p = 0.05) between alkaloids (r = 0.96) and tannins (r = 0.9) with antioxidant, anti-inflammatory, and thrombolytic properties. Conclusion. The bioactivities of D. lindleyi, including antioxidant (root), thrombolytic (stem), and anti-inflammatory (leaf) activities, are linked to the phytochemicals detected in the screening.

Winemaking: “With One Stone, Two Birds”? A Holistic Review of the Bio-Functional Compounds, Applications and Health Benefits of Wine and Wineries’ By-Products

The plethora of bio-functional compounds present in fermented alcoholic beverages like wine, as well as the valorisation of bioactives from wineries’/breweries’ by-products like grape pomace and grape seed, has gained significant interest in the functional foods sector. This functional beverage, wine, has always accompanied humanity, for religion or for health, especially in the Mediterranean, while the benefits of its moderate consumption were documented even by the Greek physician Hippocrates of Kos (460–370 BC). After a big gap, an outbreak of research on wine benefits has surfaced only since the 1990s, when the term “French paradox” was introduced to the US public during a CBS show, while recent evidence has outlined that the beneficial effects of wine consumption are derived by the synergisms of its bio-functional compounds and their digestion-derived metabolites. Within this article, the proposed health benefits of moderate wine consumption, as a functional component of a balanced diet (i.e., the Mediterranean diet) against inflammation-related chronic disorders, is thoroughly reviewed. The various bio-functional compounds of both wine and wineries’ by-products, such as their bioactive phenolics, unsaturated fatty acids, polar lipids and dietary fibres, and their functional antioxidant, anti-inflammatory and antithrombotic health-promoting properties, are also thoroughly evaluated. The mechanisms of action and synergism, by which the health benefits are elicited, are also explored. Functional properties of non-alcoholic wine products are also introduced. Emphasis is also given to applications of wineries’ by-products bioactives, as ingredients of bio-functional foods, supplements and nutraceuticals. Limitations and future perspectives for this popular functional alcoholic beverage (wine) and its rich in bioactives by-products are also addressed.

Impact of ultrasonication on the contents, profiles and biofunctional properties of free and bound phenolics from white desert truffle (Tirmania nivea) and its protein fractions

The molecular and biofunctional properties of protein and phenolic fractions in edible truffles remain largely unknown. This study examined the effect of ultrasonication on the contents, profiles, and bioactive properties of free and bound phenolics (FP and BP) from desert truffle (Tirmania nivea) and its protein fractions. Protein fractions from the Osborne extraction scheme were biochemically and structurally characterized. The albumin fraction showed the highest abundance (16.8%) and yield (35.8%). Total phenolic contents were the highest in non-sonicated samples (3.5–34.1 mg/g), particularly in the albumin fraction and in whole truffle. FP extracted at 30 °C (FP-30 °C) accounted for the largest proportion of total phenolics in all protein fractions, whereas BP-30 °C and FP-60 °C were predominant in non-sonicated and sonicated truffle, respectively. The highest antioxidant activity was obtained with FP-30 °C extracts from non-sonicated albumins, globulins and truffle (91.9, 72.7 and 30.0%), followed by BP-30 °C from non-sonicated albumins (25.4%) and FP-60 °C from sonicated glutelins-1 (24.2%). High inhibition of α-amylase was evidenced in several extracts, including FP-30 °C from non-sonicated glutelins-1 (99.2%) and FP-30 °C from sonicated globulins (72.4%). Several extracts also displayed high inhibition of angiotensin I-converting enzyme (ACE), including FP-60 °C from non-sonicated glutelins-1 (65.1%) and sonicated glutelins-1 (71.1%) and globulins (64.7%). Most extracts were rich in epicatechin, gallic acid, chlorogenic acid and catechin. Correlations between phenolic content, antioxidant activity, anti-α-amylase and anti-ACE activities were influenced by sonication. Sonication reduced the particle size of the proteins and modified their structural characteristics. These findings demonstrate that white desert truffle proteins co-occur with bioactive phenolics whose functionalities can be tailored by protein fractionation and sonication.

Phytochemical Profiling of Dried Palmyrah Haustorium Powder through GC-MS Analysis: Unveiling Novel Bioactive Compounds

Palmyrah seed haustorium is most beneficial (in human health) with its medicinal properties. It contains various volatile compounds and health benefits, preventing many diseases. The present study was carried out with palmyrah haustorium to evaluate the volatile compounds through GC-MS analysis using methanolic extract. The haustorium extract was used to identify the amount of bioactive substances, secondary metabolites, sugars, amino acids, organic acids, fatty acids, and phenolics found in the Palmyrah haustorium using GC-MS analysis. The results indicated that the palmyrah haustorium contains 50 volatile compounds and secondary metabolites. GC-MS analysis of palmyrah haustorium extract revealed volatile compounds with medicinal properties including anti-bacterial, anti-microbial, hepatoprotective, antihistaminic, cardiotonic, diuretic, antioxidant, anti-inflammatory, and anti-cancer activity. It may prevent Alzheimer's and nervous system disorders. Haustorium is used in food and perfumery industries as a flavoring agent and food additives. The study highlights its health benefits and disease preventing potential in palmyrah haustorium.

Response Surface Methodology in Optimising the Extraction of Polyphenolic Antioxidants from Flower Buds of Magnolia × soulangeana Soul.-Bod. var. 'Lennei' and Their Detailed Qualitative and Quantitative Profiling.

A response surface methodology (RSM) with a central composite design (CCD) was developed to predict and apply the best ultrasound-assisted extraction (UAE) conditions, including the extraction time, the composition of aqueous-ethanolic extractants, and the solvent-to-plant-material ratio, for obtaining the highest yields of different types of polyphenolic components from the dried flower buds of Magnolia × soulangeana Soul.-Bod. var. 'Lennei' (MSL). The novel approach in the RSM procedure resulted from the simultaneous optimisation of UAE conditions to obtain extracts with the highest antioxidant and antiradical potential (examined as dependent variables), using appropriate spectrophotometric assays, with Folin-Ciocâlteu and 2,2-diphenyl-1-picrylhydrazyl reagents, respectively. The use of 66.8% (V/V) ethanol as the extraction solvent during the 55.2 min extraction protocol and the ratio of extractant volume to herbal substance of 46.8 mL/g gave the highest total yield of bioactive antioxidant phenolics in the extract obtained. For this herbal preparation, a qualitative and quantitative analysis was performed using combined chromatographic (LC), spectroscopic (PDA), and tandem mass spectrometric (ESI-QToF-MS/MS) techniques. A detailed phytochemical profiling, conducted for the first time, documented substantial amounts of various polyphenolic antioxidants, especially phenylethanoids and flavonoids, in the MSL flower buds. Their average total content exceeded 30.3 and 36.5 mg/g dry weight, respectively.

De novo design of bioactive phenol and chromone derivatives for inhibitors of Spike glycoprotein of SARS-CoV-2 in silico.

This work presents the synthesis of 12 phenol and chromone derivatives, prepared by the analogs, and the possibility of conducting an in silico study of its derivatives as a therapeutic alternative to combat the SARS-CoV-2, pathogen responsible for COVID-19 pandemic, using its S-glycoprotein as a macromolecular target. After the initial screening for the ranking of the products, it was chosen which structure presented the best energy bond with the target. As a result, derivative 4 was submitted to a molecular growth study using artificial intelligence, where 8436 initial structures were obtained that passed through the interaction filters and similarity to the active glycoprotein pocket through the MolAICal computational package. Thus, 557 Hits with active configuration were generated, which is very promising compared to the BLA reference link for inhibiting the biological target. Molecular dynamics also simulated these compounds to verify their stability within the active protein site to seek new therapeutic propositions to fight against the pandemic. The Hit 48 and 250 are the most active compounds against SARS-CoV-2. In summary, the results show that the Hit 250 would be more active than the natural compound, which could be further developed for further testing against SARS-CoV-2. The study employs the de novo approach to design new drugs, combining artificial intelligence and molecular dynamics simulations to create efficient molecular structures. This research aims to contribute to the development of effective therapeutic strategies against the pandemic.