Search Results (110)

Toxoplasma gondii, an obligate intracellular protozoan parasite infecting nucleated cells of warm-blooded vertebrates, causes severe complications in immunocompromised hosts. Current therapies remain limited by suboptimal efficacy and toxicity, necessitating novel anti-toxoplasmic agents. Piceatannol (PIC), a natural stilbenoid, demonstrates multifaceted bioactivity including antimicrobial and anti-parasitic effects, suggesting therapeutic potential against T. gondii. Our previous study revealed PIC’s potent anti-parasitic activity, selectively inhibiting T. gondii proliferation and altering parasite morphology without host cytotoxicity. In this study, mechanistic analyses indicated that PIC disrupts mitochondrial integrity in tachyzoites, reducing mitochondrial membrane potential and ATP production while elevating ROS levels. Transcriptomic profiling identified significant suppression of oxidative phosphorylation-related genes, consistent with mitochondrial dysfunction. These findings establish PIC as a promising candidate targeting T. gondii through the mechanism of mitochondrial impairment. Full article

Passion fruit (Passiflora edulis) is consumed worldwide, and its processing generates a substantial amount of waste, particularly from the seeds and peels. This study investigated the potential of valorizing passion fruit seeds by adding them to high-fiber snack bars. Seed-enriched snack bars were evaluated for their sensory qualities, antioxidant activities, and nutritional compositions. Seed addition markedly increased the dietary fiber content (from 4.17% to 5.66%), fat content (from 15.02% to 19.63%), and antioxidant activity (e.g., 83.38% vs. 82.47% DPPH inhibition at 50 ppm) compared to the control. This was mainly due to the presence of piceatannol, a potent bioactive molecule. The overall phenolic content decreased from 90.11 to 65.37 mg GAE/100 g, suggesting intricate matrix interactions. The control bars exhibited a higher overall acceptability score, whereas the seed bars remained within the acceptable sensory range and required only minor texture adjustments. Microbiological analyses confirmed that both formulations retained their safety for 7 days at +4 °C, with appropriate levels of yeast and total viable count and no mold growth. These results suggest that passion fruit seeds have the potential to be used as a sustainable functional food ingredient. Further research is warranted to improve the sensory qualities and shelf-life stability. Full article

The traditional aging of cachaça has been performed with different types of wood barrels. Although it is efficient for incorporating phenolics, volatiles, and color into the drink, it is time-consuming for the industry. Alternative aging processes, such as the use of wood chips, have been proposed, and they have the advantage of achieving aging in a shorter time and producing a quality and innovative drink. Therefore, the influence of jackfruit wood barrel and chips and micro-aeration was investigated during cachaça aging. For that, five treatments were used—stainless steel tank (control); stainless steel tank and micro-aeration (control); jackfruit wood barrel; stainless steel tank with jackfruit chips; and stainless steel tank with jackfruit chips and micro-aeration—during two aging times (40 and 79 days). Aging cachaça with jackfruit wood led to increased physicochemical, color, and total phenolic contents, whereas alcoholic degree, lightness, and copper contents decreased. No influence was observed on higher alcohols. Nineteen phenolic compounds were identified in the jackfruit wood aged cachaça by HPLC-DAD-FLD. Myricetin was predominant, a potential marker for jackfruit wood. Longer aging time decreased the alcoholic degree and total ester, but it increased dry extract, density, total and volatile acidity, and it improved the quality of cachaça. The use of chips accelerated aging, whereas micro-aeration led to decreased myricetin. PCA and HCA clustered the samples into three groups: the first was correlated with several flavonoids and coumarins; the second with myricetin, piceatannol, and trans-ferulic acid; and the last with ellagic acid. The use of jackfruit chips in the aging of cachaça has been shown to be a promising innovation. Full article

Background/Objectives: Periodontal disease involves chronic immunoinflammatory processes and microbial dysbiosis, making phytochemicals with anti-inflammatory properties potential therapeutic agents. This study aimed to assess the modulatory effects of yellow passion fruit bagasse extract (PFBE) on periodontal cells under microbial condition. Methods: A human periodontal ligament (PDL) cell line was exposed to F. nucleatum ATCC 25586 to simulate a microbial environment in vitro in the presence and absence of PFBE containing three different concentrations (0.25, 0.50, and 1.00 µg/mL) of piceatannol. Pro-inflammatory markers (TNF-α, IL-8, CCL2), the antioxidant enzyme SOD2, and the protease marker MMP-1 were analyzed by real-time PCR. Protein levels were assessed via ELISA and NF-κB nuclear translocation by immunofluorescence. Cell viability was investigated using live/dead and alamarBlue assays, and in vitro wound healing was evaluated by an automated scratch assay. Results: PDL cells exposed to F. nucleatum significantly increased the gene and protein expression of all inflammatory markers. The stimulatory effects of F. nucleatum were significantly reduced when PDL cells were simultaneously exposed to PFBE. F. nucleatum triggered the NF-κB nuclear translocation while PFBE abrogated the F. nucleatum-stimulated NF-κB nuclear translocation at 60 min. Viability assays demonstrated that neither PFBE nor F. nucleatum were toxic or significantly affected PDL cell viability. In vitro wound closure was improved by the addition of PFBE to F. nucleatum. Conclusions: PFBE exhibited anti-inflammatory and anti-proteolytic effects while improving in vitro wound healing, suggesting a potential modulatory role of PFBE in periodontal disease prevention and treatment. Full article

Rheumatoid arthritis (RA) is a highly prevalent systemic autoimmune disease. Recently, natural small molecules have been explored as alternative therapeutic agents. Iris halophila Pall is the traditional herbal medicine, and it is rich in active ingredients with anti-inflammatory and immunomodulatory effects. In our previous study, LC-MS analysis revealed that piceatannol (PIC) is one of the primary active ingredients in the root of Iris tectorum. The purpose of this study was to explore the immunomodulatory effects of PIC on the maturation and function of dendritic cells, as well as on experimental arthritis induced by complete Freund’s adjuvant (CFA) and incomplete Freund’s adjuvant (IFA). Additionally, we aimed to probe into the potential mechanisms underlying the effects of PIC. We first verified the immunosuppressive effect of PIC using flow cytometry and an ELISA. The immunosuppressive mechanism of PIC on dendritic cells (DCs) was investigated through a joint analysis of network pharmacology and Western blotting. Our findings revealed that under Lipopolysaccharide (LPS)-induced inflammatory conditions, PIC could restrain the maturation and function of DCs (p < 0.001) and decrease the secretion of inflammatory cytokines (p < 0.001) compared to the LPS group. Furthermore, PIC suppressed the activation and polarization of CD4⁺ T cells, resulting in a decreased proportion of Th1 and Th17 cells (p < 0.001), ultimately improving the symptoms of CFA-induced arthritis in comparison to the model group. The PIC-induced shift in the T helper cell differentiation correlated with the secretion of polarizing cytokines from DCs in the AIA model. Mechanistically, PIC exerted its immunosuppressive function mainly by down-regulating the Mitogen-Activated Protein Kinase (MAPK) and Nuclear Factor kappa-B (NF-κB) signaling pathways. Collectively, these data unveil the anti-inflammatory mechanisms of a traditional medicine via the inhibition of the immune activation function of DCs in vivo and open up a therapeutic approach for autoinflammatory diseases. Full article

Plant-based stilbenes are low-molecular-weight polyphenolic compounds that exhibit anti-oxidant, anti-microbial, anti-fungal, anti-inflammatory, anti-diabetic, cardioprotective, neuroprotective, and anti-cancer activities. They are phytoalexins produced in diverse plant species in response to stress, such as fungal and bacterial infections or excessive UV irradiation. Plant-derived dietary products containing stilbenes are common components of the human diet. Stilbenes appear to be promising chemopreventive and chemotherapeutic agents. Accumulating evidence indicates that stilbenes are able to trigger both apoptotic and autophagic molecular pathways in many human cancer cell lines. Of note, the molecular crosstalk between autophagy and apoptosis under cellular stress conditions determines the cell fate. The autophagy and apoptosis relationship is complex and depends on the cellular context, e.g., cell type and cellular stress level. Apoptosis is a type of regulated cell death, whereas autophagy may act as a pro-survival or pro-death mechanism depending on the context. The interplay between autophagy and apoptosis may have an important impact on chemotherapy efficiency. This review focuses on the in vitro effects of stilbenes in different human cancer cell lines concerning the interplay between autophagy and apoptosis. Full article

The interest in new sources of bioactive compounds has been driven by the search for natural antioxidants capable of attenuating the toxicity of reactive oxygen species, as well as the emergence of pathogens resistant to antimicrobials. In this sense, we explored the potential of the macaúba epicarp. Compounds such as piceatannol, 3,4,5,3′,5′-penta-hydroxy-trans-stilbene (PHS), and in lower amounts, resveratrol were identified in extracts through techniques such as medium-pressure liquid chromatography, HPLC-MS, and imaging mass spectrometry (IMS), which confirmed the exclusive localization of PHS and piceatannol in the outer epicarp. Extraction with aqueous acetone (Me₂CO:H₂O) and its EtOAC fraction showed the highest yields of stilbenes and, moreover, it efficiently increased the tolerance of Saccharomyces cerevisiae to oxidative stress. Additionally, the Me₂CO:H₂O extract presented antibacterial and anti-cryptococcal activity, with piceatannol and resveratrol increasing survival rates of Galleria mellonella subjected to fungal infection. In silico ADMET (absorption, distribution, metabolism, excretion and toxicity) analysis indicates low toxicity for piceatannol, PHS, and resveratrol, in addition to pharmacokinetic parameters that allow their use. These findings indicate the use of macaúba epicarp as a source of bioactive compounds valuable for the food, cosmetic, and pharmaceutical industries. Full article

Stilbenoids are a class of naturally occurring phenolic compounds found in various plant species, characterized by a stilbene backbone with diverse substituents that confer a range of biological activities. These compounds exhibit antioxidant, anti-inflammatory, and antimicrobial properties, making them promising candidates for improving intestinal health. The intestinal tract plays a critical role in nutrient digestion, absorption, and immune defense, and maintaining its integrity is vital for animal growth. Stilbenoids contribute to gut health by enhancing intestinal morphology, supporting mucosal immune responses, regulating gut microbiota composition, modulating metabolic pathways, and maintaining mitochondrial health. This review provides a comprehensive analysis of key stilbenoids, including resveratrol, pterostilbene, piceatannol, and oxyresveratrol, focusing on their biological effects and regulatory mechanisms. By highlighting their roles in mitigating intestinal inflammation and promoting gut function, this review provides a basis for the practical application of stilbenoids in animal health and husbandry. Full article

Gastric cancer remains a significant global health challenge, driving the need for innovative therapeutic approaches. Natural polyphenolic compounds such as resveratrol, piceatannol, curcumin, and quercetin currently show promising results in the prevention and treatment of various cancers, due to their diverse biological activities. This review presents the effects of natural compounds on important processes related to cancer, such as apoptosis, proliferation, migration, invasion, angiogenesis, and autophagy. Resveratrol, naturally found in red grapes, has been shown to induce apoptosis and inhibit the proliferation, migration, and invasion of gastric cancer cells. Piceatannol, a metabolite of resveratrol, shares similar anticancer properties, particularly in modulating autophagy. Curcumin, derived from turmeric, is known for its anti-inflammatory and antioxidant properties, and its ability to inhibit tumor growth and metastasis. Quercetin, a flavonoid found in various fruits and vegetables, induces cell cycle arrest and apoptosis while enhancing the efficacy of conventional therapies. Despite their potential, challenges such as low bioavailability limit their clinical application, necessitating further research into novel delivery systems. Collectively, these compounds represent a promising avenue for enhancing gastric cancer treatment and improving patient outcomes through their multifaceted biological effects. Full article

Background:Dendrobium officinale glycolipids (DOG), often left as residues after hot water extraction for polysaccharide production, are often discarded. Methods: This study investigates the optimal extraction of DOG using response surface methodology, focusing on liquid–solid ratios, ethanol concentrations, extraction temperatures, and extraction times, while preliminarily analyzing DOG’s structural properties. Additionally, the differences in antioxidant effects between DOG and ascorbic acid based on intestinal flora metabolism were further evaluated. Results: The optimal parameters for DOG extraction were determined as follows: liquid–solid ratio of 20 mL/g, ethanol concentration of 70%, extraction temperature of 70 °C, and extraction time of 2.5 h, yielding 2.64 ± 0.18%. In addition, DOG was identified as a diglyceride, mainly composed of glucose, mannose, linoleic acid, 9,12,15-octadecatrienoic acid, and presented certain direct free radicals scavenging effects. In animal experiments, unlike the direct free scavenging effects of ascorbic acid, DOG increased intestinal Bacteroides acidifaciens abundance in mice, up-regulated piceatannol expression, and down-regulated 1-naphthol expression, which contributed to antioxidant effects by enhancing the activities of SOD and GSH-Px while reducing MDA content. Conclusions: DOG was a diglyceride isolated from D. officinale residues after hot water extraction, and presented strong antioxidant effects by regulating intestinal flora metabolism. These findings could promote the efficient utilization of D. officinale and support further development of DOG in functional food applications. Full article

Background: Inflammation and immune cell dysfunction are critical facilitators of endometriosis pathophysiology. Macrophages are renowned for stimulating lesion growth, vascularization, innervation, and pain generation. By combining macrophages and endometriotic cells, we determined if resveratrol and its natural analogs can target the immune dysregulation and oxidative imbalance in endometriosis. Methods: After treatment with compounds (5, 10, 25 µM), we evaluated the expression of key inflammatory and oxidative stress markers, cytokines release, and ROS production by applying q-PCR, ELISA, Cytometric Beads Array, and multiplexed fluorogenic staining and flow cytometry analysis with bioimaging. Results: The results showed that endometriosis-related macrophages treated with stilbenes have impaired expression of pro-inflammatory markers (IL6, IL8, IL1B, TNF, CCL2, CXCL10, PTGS2). The effect of resveratrol, pterostilbene, and piceatannol was observed, especially in reducing IL1B, CCL2, and CXCL10 genes up to 3.5-, 5-, and 7.7-fold at 25 µM, respectively. Also, with piceatannol or polydatin exposure, the IL-6 decrease was noticeable. This study reported an antioxidant effect by reducing ROS-positive cells from 96% to 48% by pterostilbene. Results from flow cytometry correlated with the transcript activation of detoxification enzymes (SOD, GPX). Conclusions: Prospects for potential therapy based on regulating the immune microenvironment and reducing the accumulation of free radicals with stilbenes application were described in the article. Full article

Piceatannol is a naturally occurring hydroxylated analogue of the stilbene phytoalexin resveratrol that can be found in grape fruit and derived products. Piceatannol has aroused great interest as it has been shown to surpass some human health-beneficial properties of resveratrol including antioxidant activity, several pharmacological activities and also bioavailability. The plant biosynthetic pathway of piceatannol is still poorly understood, which is a bottleneck for the development of both plant defence and bioproduction strategies. Cell cultures of Vitis vinifera cv. Gamay, when elicited with dimethyl-β-cyclodextrin (MBCD) and methyl jasmonate (MeJA), lead to large increases in the accumulation of resveratrol, and after 120 h of elicitation, piceatannol is also detected due to the regiospecific hydroxylation of resveratrol. Therefore, an ortho-hydroxylase must participate in the biosynthesis of piceatannol. Herein, three possible types of resveratrol hydroxylation enzymatic reactions have been tested, specifically, a reaction catalyzed by an NADPH-dependent cytochrome, P450 hydroxylase, a 2-oxoglutarate-dependent dioxygenase and ortho-hydroxylation, similar to polyphenol oxidase (PPO) cresolase activity. Compared with P450 hydoxylase and the dioxygenase activities, PPO displayed the highest specific activity detected either in the crude extract, the particulate or the soluble fraction obtained from cell cultures elicited with MBCD and MeJA for 120 h. The overall yield of PPO activity present in the crude extract (107.42 EU) was distributed mostly in the soluble fraction (66.15 EU) rather than in the particulate fraction (3.71 EU). Thus, partial purification of the soluble fraction by precipitation with ammonium sulphate, dialysis and ion exchange chromatography was carried out. The soluble fraction precipitated with 80% ammonium sulphate and the chromatographic fractions also showed high levels of PPO activity, and the presence of the PPO protein was confirmed by Western blot and LC-MS/MS. In addition, a kinetic characterization of the cresolase activity of partially purified PPO was carried out for the resveratrol substrate, including Vmax and Km parameters. The Km value was 118.35 ± 49.84 µM, and the Vmax value was 2.18 ± 0.46 µmol min⁻¹ mg⁻¹. Full article

Yeasts are the usual contaminants in fruit juices and other beverages, responsible for the decrease in the quality and shelf-life of such products. Preservatives are principally added to these beverages to enhance their shelf-life. With the increasing consumer concern towards chemical food additives, plant-derived antimicrobials have attracted the attention of researchers as efficient and safer anti-yeast agents. However, the methods currently used for determining their anti-yeast activity are time- and material-consuming. In this study, the anti-yeast effect of plant phenolic compounds in apple and orange juice food models using microtiter plates has been evaluated in order to validate the modified broth microdilution method for screening the antimicrobial activity of juice preservative agents. Among the twelve compounds tested, four showed a significant in vitro growth-inhibitory effect against all tested yeasts (Saccharomyces cerevisiae, Zygosaccharomyces bailii, and Zygosaccharomyces rouxii) in both orange and apple juices. The best results were obtained for pterostilbene in both juices with minimum inhibitory concentrations (MICs) ranging from 32 to 128 μg/mL. Other compounds, namely oxyresveratrol, piceatannol, and ferulic acid, exhibited moderate inhibitory effects with MICs of 256–512 μg/mL. Furthermore, the results indicated that differences in the chemical structures of the compounds tested significantly affected the level of yeast inhibition, whereas stilbenes with methoxy and hydroxy groups produced the strongest effect. Furthermore, the innovative assay developed in this study can be used for screening the anti-yeast activity of juice preservative agents because it saves preparatory and analysis time, laboratory supplies, and manpower in comparison to the methods commonly used. Full article

Piceatannol (PIC), a polyphenol abundant in passion fruit seeds, is reported to promote fat metabolism. This study investigated whether PIC affects sirtuin 1 (SIRT1) expression and metabolic factors in C2C12 skeletal muscle cells. C2C12 myotubes were stimulated with PIC, and alterations in gene expression, protein levels, mitochondrial DNA content, and fatty acid levels were assessed using real-time PCR, Western blotting, and Nile red staining. Furthermore, we examined changes in SIRT1 expression following the consumption of a test food containing 100 mg PIC for 2 weeks among adults with varying age and body mass index ranges. Both PIC and passion fruit seed extract induced SIRT1 expression in C2C12 myotubes to a greater extent than resveratrol. PIC also increased the expression of genes associated with mitochondrial biogenesis and fatty acid utilization, increased mitochondrial DNA content, and suppressed oleic acid-induced fat accumulation. Moreover, participants who consumed PIC exhibited significantly higher SIRT1 mRNA expression in whole blood compared to those in the placebo group. These findings suggest that PIC induces SIRT1 expression both in vitro and in the human body, which may promote mitochondrial biosynthesis and fat metabolism. Full article

Piceatannol (PIC) and epigallocatechin gallate (EGCG) are polyphenolic compounds with applications in the treatment of various diseases such as cancer, but their stability is poor. β-lactoglobulin (β-LG) is a natural carrier that provides a protective effect to small molecule compounds and thus improves their stability. To elucidate the mechanism of action of EGCG, PIC, and palmitate (PLM) in binding to β-LG individually and jointly, this study applied molecular docking and molecular dynamics simulations combined with in-depth analyses including noncovalent interaction (NCI) and binding free energy to investigate the binding characteristics between β-LG and compounds of PIC, EGCG, and PLM. Simulations on the binary complexes of β-LG + PIC, β-LG + EGCG, and β-LG + PLM and ternary complexes of (β-LG + PLM) + PIC, (β-LG + PLM) + EGCG, β-LG + PIC) + EGCG, and (β-LG + EGCG) + PIC were performed for comparison and characterizing the interactions between binding compounds. The results demonstrated that the co-bound PIC and EGCG showed non-beneficial effects on each other. However, the centrally located PLM was revealed to be able to adjust the binding conformation of PIC, which led to the increase in binding affinity with β-LG, thus showing a synergistic effect on the co-bound PIC. The current study of β-LG co-encapsulated PLM and PIC provides a theoretical basis and research suggestions for improving the stability of polyphenols. Full article