Ellagic Acid Research Articles

Plantago boissieri : Phytochemical Assessment, Antioxidant, Anti-inflammatoryand Wound Healing Potential.

Plantago is a large genus under family Plantaginaceae. Plantago species were noted for potent antioxidant, anti-inflammatory and wound healing activities. The current research investigated the potential bioactivities as the metabolic content of Plantagoboisserei extract. Results highlighted the rich content of phenolics (450.93 ± 7.4 mg GAE/g extract) and flavonoids (144.2 ± 3.6 mg RE/g extract). HPLC analysis enabled the detection of 17 phenolic constituents among which ellagic acid was found in highest concentration followed by rutin. P. boisserei exhibited a potent antioxidant activity evidenced by the IC50 values in ABTS and H2O2 assays (10.95 and 10.87 µg/mL, respectively) as well as in TAC assay (67.94 mg AAE/g). The anti-microbial activities revealed a moderate activity against Staphylococcus aureus and Proteus vulgaris. In vitro anti-inflammatory potential indicated a characteristic inhibition against COX-1 and COX-2 enzymes with IC50 62.8 and 14.23 µg/mL, respectively, compared to ibuprofen (IC50 8.07 and 6.58, respectively). Additionally, P. boisserei extract achieved a potent wound healing activity using in vivo rat model, this might be attributed to its high content of flavonoids together with other polyphenolic compounds that have a great free radical scavenging potential. P. boisserei is a promising candidate for more extensive phytochemical and biological exploration.

Correlation Analysis Among the Chemical Composition and Cytotoxic and Antioxidative Activities of a Tessaria absinthioides Decoction for Endorsing Its Potential Application in Oncology

Historically, botanical preparations have been used to improve human health. Their active ingredients are influenced by multiple factors such as intraspecies variations, environmental conditions, collection time and methods, and the part of the plant used. To ensure the efficiency and safety of these herbal drugs, qualitative and quantitative analyses are required. A Tessaria absinthioides decoction (DETa) was reported as having hypocholesterolemic, anti-inflammatory, cytotoxic, antitumor, and antioxidative properties. This work aimed to analyze DETa by correlating its chemical composition with cytotoxic and antioxidative properties, with the aim of promoting research on it as an anticancer agent. DETa collections (2017, 2018, 2019, and 2022) were analyzed by UHPLC-DAD, UHPLC-DAD-FLD, and UPLC-MS/MS; cytotoxicity was assessed on the MCF-7 breast cancer cell line; antioxidative capacity was evaluated by the DPPH and FRAP methods; and correlation analysis was used to determine biological and chemical markers. The results provide evidence that biological activities were consistent across the collections. Among the quantified compounds, apigenin, naringin, gallocatechin gallate, ginnalin A, myricetin, epicatechin, OH-tyrosol, quercetin, and chlorogenic, tessaric, p-coumaric, vanillic, caffeic, caftaric, ellagic, and rosmarinic acids correlated as bioactive and chemical markers. Moreover, tessaric acid could be established as a species marker. Altogether, these findings add relevant information to DETa properties, encouraging further exploration of its potential application as an anticancer botanical.

The anti-obesity effects of polyphenols: a comprehensive review of molecular mechanisms and signal pathways in regulating adipocytes

Excess weight gain is a growing concern worldwide, fueled by increased consumption of calorie-dense foods and more sedentary lifestyles. Obesity in China is also becoming increasingly problematic, developing into a major public health concern. Obesity not only increases the risk of associated disease but also imposes a burden on health care systems, and it is thus imperative that an effective intervention approach be identified. Recent studies have demonstrated that the polyphenol-rich Mediterranean diet has considerable potential in this regard. Polyphenols can inhibit the production of adipocytes and reduce adverse reactions, such as inflammation, insulin resistance, and gut microflora imbalance. In this review, we examine four polyphenols (curcumin, ellagic acid, ferulic acid, and quercetin) in terms of their potential as interventions targeting obesity. The mechanisms that help promote adipocyte browning, increase thermogenic factors, increase thermogenesis, and regulate adipocyte differentiation are summarized, and key signaling pathways, including PPARγ, C/EBP-, and others, are reviewed.

A Comprehensive Guide to Whitening Ingredients for Women

Many people think that a fair and glowing complexion is a sign of beauty; however, with the large number of whitening products available in the market of varying quality, the question of how to choose the right whitening product is an important one. This article takes an in-depth look at the whitening ingredients available to users, which include vitamin C, arbutin, niacinamide, kojic acid, glutathione, alpha-hydroxy acids (AHAs), licorice extract, and ellagic acid. For each ingredient, the source, production method, function and details are provided. Results show that different skin types have specific needs. Dry skin requires moisturizing, oily skin benefits from sebum control and light textures, and sensitive skin needs mild ingredients. Each ingredient has its advantages and disadvantages, and potential drawbacks such as stability issues, allergic reactions, and skin irritation are discussed. This paper also emphasizes key points for choosing whitening products, including understanding skin type, considering the pros and cons of each ingredient, researching product source and quality, following correct usage methods, and combining with a comprehensive skincare routine and sun protection. This research is significant as it provides valuable guidance for women in making informed choices about whitening products, helping them achieve a healthy complexion through proper skin care and understanding of different ingredients.

Anogeissus Latifolia: A Comprehensive Review from Ethanobotanical Insights to Future Pharmacological Frontiers.

Anogeissus latifolia, commonly known as Axlewood, Indian Gum Tree, or Gum Ghatti, belongs to the Combretaceae family and is native to India, Nepal, Myanmar, and Sri Lanka. It thrives in most tropical and subtropical regions of India. Different parts of the plant contain various proteins, carbohydrates, sugars (arabinose, galactose, mannose, xylose, rhamnose, and glucuronic acid), minerals (magnesium and calcium salts of ghattic acid), and a wide range of phytochemicals such as alkaloids, flavonoids, phenols, terpenoids, sterols, saponins, tannins, coumarins, quinine, and ellagic acid. Studies have indicated the potential of Anogeissus latifolia in managing various health conditions, including antimicrobial, anti-inflammatory, anti-diabetic, anti-parasitic, antioxidant, hepatoprotective, wound healing, and hypolipidemic effects. However, like many medicinal plants, Anogeissus latifolia demonstrates a dose-dependent toxicity profile, particularly when administered intraperitoneally. Research efforts have been directed towards elucidating its safety profile, and findings suggest that it can be considered safe when administered within prescribed dosages. This paper aims to provide a comprehensive review encompassing the ethnobotanical significance, morphological characteristics, phytochemistry, pharmacological actions, and toxicological aspects of Anogeissus latifolia. Additionally, it explores future research perspectives in the field of Anogeissus latifolia pharmacology and therapeutics.

In Vitro Assessment of the Neuroprotective Effects of Pomegranate (Punica granatum L.) Polyphenols Against Tau Phosphorylation, Neuroinflammation, and Oxidative Stress

Background: Oxidative stress and chronic inflammation, at both the systemic and the central level, are critical early events in atherosclerosis and Alzheimer’s disease (AD). Purpose: To investigate the oxidative stress-, inflammation-, and Tau-phosphorylation-lowering effects of pomegranate polyphenols (PPs) (punicalagin, ellagic acid, peel, and aril extracts). Methods: We used flow cytometry to quantify the protein expression of proinflammatory cytokines (IL-1β) and anti-inflammatory mediators (IL-10) in THP-1 macrophages, as well as M1/M2 cell-specific marker (CD86 and CD163) expression in human microglia HMC3 cells. The IL-10 protein expression was also quantified in U373-MG human astrocytes. The effect of PPs on human amyloid beta 1-42 (Aβ1-42)-induced oxidative stress was assessed in the microglia by measuring ROS generation and lipid peroxidation, using 2′,7′-dichlorofluorescein diacetate (DCFH-DA) and thiobarbituric acid reactive substance (TBARS) tests, respectively. Neuronal viability and cell apoptotic response to Aβ1-42 toxicity were assayed using the MTT (3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide) assay and the annexin-V-FITC apoptosis detection kit, respectively. Finally, flow cytometry analysis was also performed to evaluate the ability of PPs to modulate Aβ1-42-induced Tau-181 phosphorylation (pTau-181). Results: Our data indicate that PPs are significantly (p < 0.05) effective in countering Aβ1-42-induced inflammation through increasing the anti-inflammatory cytokines (IL-10) in U373-MG astrocytes and THP1 macrophages and decreasing proinflammatory marker (IL-1β) expression in THP1 macrophages. The PPs were also significantly (p < 0.05) effective in inducing the phenotypic transition of THP-1 macrophages and microglial cells from M1 to M2 by decreasing CD86 and increasing CD163 surface receptor expression. Moreover, our treatments have a significant (p < 0.05) beneficial impact on oxidative stress, illustrated in the reduction in TBARS and ROS generation. Our treatments have significant (p < 0.05) cell viability improvement capacities and anti-apoptotic effects on human H4 neurons. Furthermore, our results suggest that Aβ1-42 significantly (p < 0.05) increases pTau-181. This effect is significantly (p < 0.05) attenuated by arils, peels, and punicalagin and drastically reduced by the ellagic acid treatment. Conclusion: Overall, our results attribute to PPs anti-inflammatory, antioxidant, anti-apoptotic, and anti-Tau-pathology potential. Future studies should aim to extend our knowledge of the potential role of PPs in Ab1-42-induced neurodegeneration, particularly concerning its association with the tauopathy involved in AD.

The Profile of Phenolic Compounds Identified in Pitaya Fruits, Health Effects, and Food Applications: An Integrative Review

Objective: This integrative review aimed to identify the phenolic compounds present in pitayas (dragon fruit). Methods: We employed a comprehensive search strategy, encompassing full-text articles published between 2013 and 2023 in Portuguese, English, and Spanish from databases indexed in ScienceDirect, Capes Periodics, Scielo, and PubMed. The study’s selection was guided by the question, “What are the main phenolic compounds found in pitaya fruits?”. Results: After screening 601 papers, 57 met the inclusion criteria. The identified phytochemicals have been associated with a range of health benefits, including antioxidant, anti-inflammatory, and anxiolytic properties. Additionally, they exhibit promising applications in the management of cancer, diabetes, and obesity. These 57 studies encompassed various genera, including Hylocereus, Selenicereus, and Stenocereus. Notably, Hylocereus undatus and Hylocereus polyrhizus emerged as the most extensively characterized species regarding polyphenol content. Analysis revealed that flavonoids, particularly kaempferol and rutin, were the predominant phenolic class within the pulp and peel of these fruits. Additionally, hydroxycinnamic and benzoic acid derivatives, especially chlorogenic acid, caffeic, protocatechuic, synaptic, and ellagic acid, were frequently reported. Furthermore, betalains, specifically betacyanins, were identified, contributing to the characteristic purplish-red color of the pitaya peel and pulp. These betalains hold significant potential as natural colorants in the food industry. Conclusion: Therefore, the different pitayas have promising sources for the extraction of pigments for incorporation in the food industry. We recommend further studies investigate their potential as nutraceuticals.

Ellagic Acid Reduces Cadmium Exposure-Induced Apoptosis in HT22 Cells via Inhibiting Oxidative Stress and Mitochondrial Dysfunction and Activating Nrf2/HO-1 Pathway

Exposure to cadmium sulfate (CdSO4) can lead to neurotoxicity. Nevertheless, the precise molecular mechanisms underlying this phenomenon remain unclear, and effective treatment strategies are scarce. This study explored the protective effects of ellagic acid (EA), a natural polyphenolic compound, against CdSO4 exposure-induced neurotoxicity in HT22 cells and the underlying molecular mechanisms. Our findings demonstrated that exposure of HT22 cells to CdSO4 resulted in apoptosis, which was effectively reversed by EA in a dose-dependent manner. EA supplementation also decreased reactive oxygen species (ROS) and mitochondrial ROS production, reduced malondialdehyde (MDA) levels, and restored the activities of superoxide dismutase (SOD) and catalase (CAT). Additionally, EA supplementation at 5–20 μM significantly counteracted Cd-induced the loss of mitochondrial membrane potential and the decrease of ATP and reduced the ratio of Bax/Bcl-2 and cleaved-caspase-3 protein expression. Furthermore, EA supplementation resulted in the upregulation of Nrf2 and HO-1 protein and mRNAs while simultaneously downregulating the phosphorylation of JNK and p38 proteins. The pharmacological inhibition of c-Jun N-terminal kinase (JNK) partially attenuated the activation of the Nrf2/HO-1 pathway induced by CdSO4 and exacerbated its cytotoxic effects. In conclusion, our findings suggest that ethyl acetate (EA) supplementation offers protective effects against CdSO4-induced apoptosis in HT22 cells by inhibiting oxidative stress and activating the Nrf2 signaling pathway. Furthermore, the activation of the JNK pathway appears to play a protective role in CdSO4-induced apoptosis in HT22 cells.

In vitro and computational investigation of antioxidant and anticancer properties of Streptomyces coeruleofuscus SCJ extract on MDA-MB-468 triple-negative breast cancer cells

This study aimed to explore the antioxidant potential of the ethyl acetate extract of Streptomyces coeruleofuscus SCJ strain, along with its inhibitory effects on the triple-negative human breast carcinoma cell line (MDA-MB-468). The ethyl acetate extract’s total phenolic and flavonoid contents were quantified, and its antioxidant activity was investigated using DPPH (1,1-Diphenyl-2-picrylhydrazyl), ABTS (2,2’-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid), and FRAP (Ferric Reducing Antioxidant Power) assays. Furthermore, the cytotoxic effect of the organic extract from Streptomyces coeruleofuscus SCJ on MDA-MB-468 cancer cells was assessed via the crystal violet assay. In tandem, a thorough computational investigation was conducted to explore the pharmacokinetic properties of the identified components of the extract, utilizing the SwissADME and pKCSM web servers. Additionally, the molecular interactions between these components and Estrogen Receptor Beta, identified as a potential target, were probed through molecular docking studies. The results revealed that ethyl acetate extract of SCJ strain exhibited remarkable antioxidant activity, with 39.899 ± 1.56% and 35.798 ± 0.082% scavenging activities against DPPH and ABTS, respectively, at 1 mg/mL. The extract also displayed significant ferric reducing power, with a concentration of 1.087 ± 0.026 mg ascorbic acid equivalents per mg of dry extract. Furthermore, a strong positive correlation (p < 0.0001) between the antioxidant activity, the polyphenol and the flavonoid contents. Regarding anticancer activity, the SCJ strain extract demonstrated significant anticancer activity against TNBC MDA-MB-468 cancer cells, with an inhibition percentage of 62.76 ± 0.62%, 62.67 ± 0.93%, and 58.07 ± 4.82% at 25, 50, and 100 µg/mL of the extract, respectively. The HPLC-UV/vis analysis revealed nine phenolic compounds: gallic acid, sinapic acid, p-coumaric acid, cinnamic acid, trans-fereulic acid, syringic acid, chloroqenic acid, ellagic acid, epicatechin. Streptomyces coeruleofuscus SCJ showed promise for drug discovery, exhibiting antioxidant and anticancer effects.

Native corn (Zea mays L., cv. ‘Elotes Occidentales’) polyphenols extract reduced total cholesterol and triglycerides levels, and decreased lipid accumulation in mice fed a high-fat diet

Obesity is a complex disease with numerous molecular and metabolic implications that could be prevented through proper diet and lifestyle. Native corn is a promissory underutilized plant species containing bioactive compounds that could reduce the impact of obesity. This research aimed to characterize and evaluate the anti-obesogenic effect of a polyphenols-rich extract of native corn (‘Elotes Occidentales’) in HFD-fed mice. The powdered extract was administered using gelatins to C57BL/6 J mice randomly divided into four groups (n:8/group) for 13 weeks: standard diet (SD) group, HFD group, HFD+200 mg extract/kg body weight (BW), and HFD+400 mg extract/kg BW/day. Ellagic acid, chlorogenic acid, rutin, and kaempferol were the most abundant phenolics (2022.44–4028.43 µg/g). Among the HFD groups, the highest dose of the extracts promoted the lowest BW gain, and fasting triglycerides and cholesterol levels. Moreover, the HFD+400 mg/kg BW group showed the lowest epididymal and subcutaneous adipose tissue weight and adipocytes’ diameter and area between the HFD-treated animals. The extract administration prevented hepatic lipid accumulation. Rutin demonstrated the highest in silico binding affinity with proteins from the AMPK pathway (ACACA, SIRT1, and SREBP1) (-6.70 to −8.70 kcal/mol). Results indicated beneficial effects in alleviating obesity-associated parameters in vivo due to bioactive compounds from native maize extracts.

Phytochemical characterization and biomedical potential of Iris kashmiriana flower extracts: a promising source of natural antioxidants and cytotoxic agents.

Iris kashmiriana belongs to the family Iridaceae and is an important endemic medicinal plant of Kashmir. The current study was designed to determine the phytoconstituents, antioxidant, and cytotoxic potential of ethyl acetate (IRK-ETH) and methanol (IRK-MTH) extracts of Iris kashmiriana flowers. IRK-MTH extract demonstrated maximum radical scavenging activity in DPPH, ABTS, and Superoxide anion radical antioxidant assays with IC50 values of 73.15μg/ml, 79.05μg/ml, and 86.52μg/ml respectively. IRK-ETH and IRK-MTH extracts possessed phenolic (70.9 and 208.5 mgGAE/gdw) and flavonoid (487.7 and 40.55mgRE/gdw) contents respectively. In MTT assay IRK-ETH demonstrated the highest cytotoxicity towards the MCF-7 cell line with a GI50 value of 49.13μg/ml. Phase contrast and fluorescence microscopic studies in MCF-7 cells revealed that IRK-ETH extract caused condensation of chromatin, rounding of cells, and nuclear condensation in cells which shows the apoptotic potential of the extract. GCMS analysis for phytochemical characterization revealed the presence of 9 compounds in both extracts which have been reported to possess antibacterial, cytotoxic, and anti-oxidant activities. HPLC analysis confirmed the presence of different polyphenols in both extracts with IRK-MTH extract having maximum polyphenols like epicatechin, rutin, quercetin, vanillic acid, sinapic acid, caffeic acid, chlorogenic acid and ellagic acid. These findings suggest that the flowers of Iris kashmiriana possess very good antioxidant and cytotoxic potential owing to its rich phytoconstituents.

Anti-tumor effects of ellagic acid and mesenchymal stem cell-conditioned medium on breast cancer cells on the 3D printed PCL/agarose scaffolds

Numerous investigations have demonstrated that natural bioactive compounds, such as flavonoids, exhibit synergistic effects with anticancer agents utilized in clinical practice. Stem cell therapies play a critical role in the domain of oncology; nevertheless, conflicting results have surfaced regarding the potential pro-cancer or anti-cancer characteristics of mesenchymal stem cells. The primary aim of the current investigation was to examine the anticancer efficacy of ellagic acid (EA) alone or in combination with adipose tissue stem cells derived conditioned medium (ADSCs-CM) on human breast cancer cells. In order to overcome the potential effects of two-dimensional (2D) culture, a three-dimensional (3D) printed polycaprolactone (PCL)/agarose scaffold is utilized to evaluate cancer cell behavior. More recently it was reported this scaffold had open and interconnected pores, as well as good water absorption and mechanical properties. Assessment of MCF-7 cancer cell viability was conducted through MTT assay, flow cytometry, cell cycle assay, and quantitative real-time PCR within a 3D cell culture framework. The outcomes revealed a reduction in cancer cell viability across all treatment cohorts in comparison to the control group. Particularly noteworthy was the significantly enhanced effect of the EA and CM combination relative to each component administered individually. Flow cytometry assessment using annexin V/PI staining indicated a decrease in cancer cells, particularly evident in the combination-treated group. Furthermore, the mRNA expression levels of BAX, BCL2, vascular endothelial growth factor (VEGF), and caspase 3 genes were consistent with pathways associated with apoptosis. Consequently, the synergistic anti-proliferative impact of EA in conjunction with ADSCs-CM on MCF-7 cells has been substantiated. These findings have two important implications for breast cancer research; highlight the utility of the PCL/agarose scaffold as a cancer model and suggest new avenues for the development of adjuvant anticancer therapeutic approaches.

Integrating network pharmacology and experimental verification to explore the pharmacological mechanisms of Guanxin Shutong capsule in treating heart failure.

The Guanxin Shutong capsule (GXST), a traditional Chinese medicine, is commonly used for treating cardiovascular disease, it has shown efficacy in improving symptoms and enhancing the quality of life for patients with heart failure (HF). However, the specific mechanism of action of GXST in HF remains unclear. In this study, we employed a comprehensive approach combining network pharmacology, molecular dynamics (MD) simulations, and in vitro validations to investigate the potential targets and molecular mechanisms of GXST against HF. We collected active ingredients and target genes of GXST, as well as related genes of HF, from multiple public databases. Using bioinformatics analysis, we constructed networks of ingredients-disease-targets and performed functional annotations of the core targets. MD simulations were conducted to verify the binding between the core protein-ligand complexes. In vitro evaluations, including cell proliferation, apoptosis, and protein expression in human umbilical vein endothelial cells (HUVECs) and H9C2 cells were treated with GXST, were performed for pharmacodynamics evaluation. Network analysis revealed 320 intersection genes and 74 active ingredients in the Herbs-ingredients-target genes-disease network. We identified key active ingredients and target genes that overlapped. The KEGG pathways of the intersection genes were primarily enriched in the PI3K-Akt signaling pathway and apoptosis. The protein-protein interaction network highlighted proteins such as AKT1, VEGFR2, and eNOS. MD simulations confirmed stable docking and lower binding energy between 4 identified ingredients (kaempferol, quercetin, (2R)-5,7-dihydroxy-2-(4-hydroxyphenyl) chroman-4-one, and ellagic acid) and their respective core proteins (VEGFR2, eNOS, and AKT). In vitro experiments demonstrated the protective effects of GXST against H2O2-induced apoptosis in both HUVECs and H9C2 cells. Notably, consistent with the in silico predictions, GXST effectively activates the VEGFR2/AKT/eNOS signaling pathways in HUVECs. This study provides insights into the underlying mechanism of GXST's therapeutic effects in heart failure. The involvement of the VEGFR2/AKT/eNOS signaling pathways suggests their importance in further elucidating and applying GXST in the clinical treatment of heart failure.

Assessing a "Least-Concern" Red List Tree Species from Madagascar Used in Traditional Medicine: Morella spathulata (Myricaceae) Phyto-Compounds and Anti-Inflammatory Properties.

Morella spathulata (Myricaceae family) is a common plant from Madagascar and is present on the IUCN Red List of threatened species classified at the 'least concern' level, used by the local population to treat numerous illnesses and pain. Despite its frequent use, comprehensive phytochemical and pharmacological research on the species is limited. This study evaluated the antioxidant, analgesic, and anti-inflammatory properties, as well as the toxicity of methanol extracts from the leaves (MS_L) and bark (MS_B) of M. spathulata. The research involved the analysis of nutritional traits such as sugars, organic acids, vitamin C, polyphenolic content (TPC) and the main phytochemicals by HPLC analysis. Antioxidant capacity was assessed through DPPH and FRAP assays. Analgesic and anti-inflammatory activities were evaluated using acetic acid-induced writhing and carrageenan-induced paw oedema tests in mice. The results showed a high content of phenolic and bioactive components in the leaf and bark extracts, associated with antioxidant, analgesic and anti-inflammatory properties. The interaction of key compounds such as ferulic acid and ellagic acid with proteins involved in pH regulation and immune modulation provides clues to the mechanisms underlying the therapeutic effects. However, conservation efforts are crucial due to habitat loss and illegal logging, and further studies are needed to fully explore the plant's therapeutic potential.

Regulation Progression on Ellagic Acid Improving Poultry Production Performance by Regulating Redox Homeostasis, Inflammatory Response, and Cell Apoptosis.

It has been approximately 2000 years since the medicinal homologous theory, which primarily holds that food has the same therapeutic value as medicine in order to improve the health of both humans and animals. In recent years, this theory has also been proposed to be used in poultry breeding. Ellagic acid (EA), a natural compound primarily extracted from medicinal homologous foods such as raspberries and pomegranates, is reported to have incomparable advantages in improving the production performance and disease resistance of poultry due to its pharmacological properties, which regulate the processes of redox homeostasis, inflammatory response, and cell apoptotic death. However, the application and research of EA in poultry production are still in the initial stage, and the potential mechanisms of its biological functions affecting animal health have not been clearly identified, which requires more attention worldwide. This mini-review collects the latest 10-year achievements of research on the effects of EA on poultry health, aiming to promote the practical application of EA in maintaining animal health and formulating corresponding targeted strategies.

Wuzi-Yanzong-Wan Prevents the Defect of Cell-Cell Junctions between Sertoli-Germ Cells by Up-Regulating the Expression of TAp73.

The TAp73 gene is an anti-cancer gene that also affects the junction between Sertoli and germ cells. Inhibition of this gene causes infertility in male mice. Our previous research proved that Wuzi-Yanzong-Wan (WZYZW) can protect spermatogenesis and maturation by preventing TAp73 inhibition. This study aimed to investigate the effect of drug-containing serum of WZYZW on the defect of cell-cell junctions in the Sertoli-germ cells co-culture system in vitro. LC-HRMS was used to analyze the content of active ingredients in WZYZWmedicated serum. Then, primary extraction and co-culture of germ cells and Sertoli cells were carried out. Co-cultured cells were added with PFT-α to induce the TAp73 inhibition model, with WZYZW-medicated serum at 2.5%, 5%, and 10% treated in parallel. Sloughing of germ cells from Sertoli cells was calculated. Transmission electron microscopy (TEM), Immunofluorescence, qRT-PCR, and western blot methods were employed. The drug-containing serum of WZYZW contained schisandrin, hyperoside, geniposidic acid, ellagic acid, and quercetin. Using TEM assay, we observed restoration of the desmosomelike (Des), tight junctions (TJ), and basal ectoplasmic specialization (ES) structure following WZYZW treatment. WZYZW caused inhibition of peptidase and protease inhibitors (tissue inhibitor of metalloproteinase-1 (TIMP1), Serpina3n) by immunofluorescence analysis. Western blot and qRT-PCR analysis revealed that WZYZW was able to ameliorate the expressions of peptidase and protease inhibitors and cell adhesion factors, such as TAp73, TIMP1, Serpina3n, Desmocollin-3, N-cadherin, and Nectin-2. WZYZW-medicated serum could prevent the defect of cell-cell junctions between Sertoli-germ cells co-culture system in vitro by up-regulating the expression of TAp73.

Role of Molecular Packing in Solvent-Mediated Ellagic Acid·Phenazine Co-Crystals Toward Biological Activity Enhancement and Rational Drug Design

Role of Molecular Packing in Solvent-Mediated Ellagic Acid·Phenazine Co-Crystals Toward Biological Activity Enhancement and Rational Drug Design

Bio-functional properties of Jilungin (Terminalia canescens).

Jilungin (Terminalia canescens) is a native Australian plant and the Indigenous "Nyul Nyul" people of the Kimberleyregion of Western Australia use its leaves to make herbal tea. Due to the rise in the popularity of drinking Jilungin tea among the consumers in Australia and internationally, it is important to study the nutritional and health-beneficial properties as well as safety of Jilungin leaves. This study aims to determine the nutritional composition, anti-nutritional factors, antimicrobial and antidiabetic properties of Jilungin leaves. Also, the phytochemical profiling using UHPLC-MS/MS (Ultra-performance liquid chromatographymass spectrometry) and antioxidant activity of Jilungin methanolic extracts and herbal infusion were investigated. The safety of the leaves and infusion was also investigated by using in vitro mammalian cell lines (Caco2, HT29, and HepG2) through cell viability assays. The leaves are rich in dietary fiber (43.9%) and linoleic acid (30.4% of total fatty acids). Phytochemical profiling revealed ellagic acid, geraniin, pedunculagin, and punicalagin as the major bioactive compounds. The results also demonstrated that Jilungin has strong antioxidant and antidiabetic activities. A significant (p<0.01) strong positive correlation was observed between the high antioxidant activity of Jilungin infusion with the major bioactive compounds. Jilungin extracts (50mg/mL) exhibited strong antimicrobial activity against Staphylococcus aureus and Bacillus cereus. Its infusion and methanolic extract were safe on the studied cell lines (Caco-2, HT29, and HepG2) at higher concentrations of 66.6 and 98mg/mL, respectively. Therefore, Jilungin teas or infusions could be a safe and effective way to promote health and well-being. PRACTICAL APPLICATION: Jilungin tea is very popular among consumers in Australia and is gaining popularity worldwide. The current study will increase knowledge on the nutritional aspects and safety of the Jilungin use.

Exploring health beneficial effects of poisonous mushroom Paxillus involutus Batsch Fr.

In the present study, phenolic and flavonoid composition and biological properties of methanolic extract of wild growing Paxillus involutus collected in Serbia have been investigated. Ellagic acid was the most abundant phenolic compound (34.92 µg g−1), followed by 5-O-caffeoylquinic acid (4.51 µg g−1), whereas isoorientin was the most abundant flavonoid (3.42 µg g−1). P. involutus turned out to be a rich source of phenolic compounds (74.67 mg GAE g−1 d.w.), whereas total flavonoid content was significantly lower (4.05 mg QE g−1 d.w.). As for the various investigated biological activities, methanolic extract exerted high level of antioxidant, antimicrobial and antibiofilm activities. The highest antioxidative potential was measured by TAC (350 TE mg g−1 d.w.), whereas evaluation of antimicrobial properties showed selective antimicrobial potential toward tested pathogenic microorganisms, with resistant strain of E. coli being the most susceptible to the activity of the extract (MIC 0.08 mg mL−1, MBC 0.16 mg mL−1). Furthermore, methanolic extract of P. involutus demonstrated genotoxicity, severe hemolysis effects and selective cytotoxicity against colon cancer cells. From the obtained data, it may be concluded that investigated mushroom albeit being toxic for human consumption, may be considered as a source of highly bioactive components with potential application in drug development.

Binder‐free 3D printed polyurethane/Bi‐MOFs composites for photocatalytic degradation of rhodamine‐ B

The modularization of metal‐organic‐frameworks (MOFs) powders is a crucial to bringing out the excellent properties of MOFs to industrial applications in water treatment, gas adsorption/separation and catalytic fields. To improve their practical application and recyclability, we propose a hybrid composite of biocompatible MOFs decorated on self‐supported three‐dimensional (3D) printed polyurethane acrylate (PUA) for wastewater treatment. In this study, we select Bi‐based MOFs with good visible‐light response and chemical stability as photocatalysts, two MOFs, bismuth gallate (Bi‐GA) and bismuth ellagic acid (Bi‐EA), are loaded into the mesh‐like PUA template by in‐situ growth method. And then, these two composites, PUA/Bi‐GA and PUA/Bi‐EA are used for the photocatalytic treatment of Rhodamine‐B (RhB) dye. The results demonstrate that PUA/Bi‐EA could reach the highest removal rate of 98.08% under acidic conditions in 4 hours. The excellent performance should be attributed to unique structure that endow their high adsorption capacity for dyes, further, the adsorbed dye as a sensitizer enhances the utilization of sun‐light. This study provides a new composite for advanced photocatalytic water treatment and other environmental purification.