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Ellagitannins (ETs), characterized by their diversity and chemical complexity, belong to the class of hydrolysable tannins that, via hydrolysis under acidic or alkaline conditions, can yield ellagic acid (EA). They are mostly found as a part of extractives in angiosperms. As known antioxidants and chelators, EA and EA derivatives are drawing an increasing interest towards extensive technical and biomedical applications. The latter ones include possible antibacterial, antifungal, antiviral, anti-inflammatory, hepato- and cardioprotective, chemopreventive, neuroprotective, anti-diabetic, gastroprotective, antihyperlipidemic, and antidepressant-like activities, among others. EA’s synthesis and production challenges prompt further research on new methods and alternative sources. Conventional and prospective methods and raw materials for the production of EA and its derivatives are reviewed. Among the potential sources of EA, the residues and industrial streams of the pulp industry have been highlighted and considered as an alluring alternative in terms of commercial exploitation.

To overcome natural skin barrier, deliver ellagic acid (EA) to the dermis, and promote its anti-ageing efficacy, oligomeric hyaluronic acid (HA) modified EA-loaded liposomes (EA-HA-L) were constructed via self-synthesized different molecular weights of HA linked cholesterol (HA-Chol), and then the effect of HA molecular weight on the skin permeability of EA was explored to clarify the optimal molecular weight of HA with best transdermal delivery effectiveness. Finally, a series of in vitro and in vivo experiments were conducted to survey the transdermal mechanism, skin irritation, antioxidant, anti-photo ageing and antiwrinkle effects of EA-loaded liposomes modified with the optimal molecular weight of HA. The results showed that EA-HA-L had less than 200 nm particle size and high encapsulation efficiency. Among them, 5 kDa of oligomeric HA-modified liposomes (EA-HA5k-L) maximized the skin penetration and retention of EA and promoted the distribution width of EA in the skin far beyond the thickness of the epidermal layer, indicating its good ability to deliver EA to the dermis. EA-HA5k-L displayed uniformly sized nanosphere morphology and slow-release behavior in neutral and acidic environments that simulated skin. The transdermal mechanism of EA-HA5k-L was proven to be related to the loosening of the stratum corneum, reduction of calcium adhesion proteins, and recognition of CD44 receptor. EA-HA5k-L had no irritant effect on the chicken embryo chorioallantoic membrane, with an irritant index close to 0.9% NaCl. EA-HA5k-L not only improved the clearance rate of EA on DPPH and hydroxyl radicals but also elevated its inhibition effect on elastase. Significantly, compared to free EA and EA-loaded liposomes without oligomeric HA modification (EA-L), EA-HA5k-L significantly increased the cellular uptake of EA through receptor-mediated endocytosis, and effectively blocked the increase in metalloproteinase-1 (MMP-1) content and decrease in type I collagen content induced by UVB in human dermal fibroblasts (HDFs), demonstrating better anti-photo ageing effectiveness. Moreover, EA-HA5k-L upregulated the relative expression of the elastin gene and three types of type I collagen gene (col1a1a, col1a1b, and col1a2) in zebrafish, and its expression promotion rates in col1a1b, col1a2 and elastin were remarkably higher than those of free EA, EA-L, and acetyl hexapeptide-8 as positive control. Conclusively, EA-HA5k-L ameliorated the anti-ageing effectiveness of EA due to the successful transdermal delivery and efficient cellular uptake, and 5 kDa of oligomeric HA-modified liposomes may be a promising transdermal delivery carrier to overcome skin barrier and upgrade the application prospects of EA in anti-skin ageing.

The current chemotherapy treatments for liver cancer have shown limited effectiveness. Therefore, there is an urgent need to develop new drugs to combat this disease more effectively. This study reports synthesis of cobalt oxide nanoparticles coated with glucose, and conjugated with Ellagic acid. Physicochemical characterization of Co 3 O 4 @Glu-Ellagic acid nanoparticles was done using FT-IR, XRD, SEM, TEM, TGA, EDS-mapping, DLS, and zeta potential analyses, and the investigation of their anticancer potential on liver cancer cell lines involved the use of MTT, flow cytometry, and cell cycle analysis. The synthesized nanoparticles were somewhat spherical, arranged in a relatively cluster-shaped form, and were 33–46 nm in diameter. The zeta potential and particle hydrodynamic size were − 5.43 and 169 nm, respectively and had no elemental impurity. Also, the synthesized particles had proper thermal stability at temperatures below 100 °C. Treating cancer cells with the nanoparticles considerably increased ROS levels by 2.6 folds. Compared to normal human cells, Co 3 O 4 @Glu-Ellagic acid nanoparticles showed significantly higher toxicity for liver cancer and the 50% inhibitory concentration was 94 and 187 µg/mL for the cancer and normal cells, respectively. Co 3 O 4 @Glu-Ellagic acid increased cell apoptosis, from 0.87 to 9.24%, and the cells were mainly arrested at the G0/G1 and G2/M phases. Overall, the present work indicated that Co 3 O 4 @Glu-Ellagic acid has antiproliferative effects on liver cancer cells through an increased oxidative stress level, inhibition of cell cycle, and apoptosis induction.

The purpose of this study was to examine the free radical scavenging and antioxidant activities of ellagic acid (EA) and ellagic acid peracetate (EAPA) by measuring their reactions with the radicals, 2,2-diphenyl-1-picrylhydrazyl and galvinoxyl using EPR spectroscopy. We have also evaluated the influence of EA and EAPA on the ROS production in L-6 myoblasts and rat liver microsomal lipid peroxidation catalyzed by NADPH. The results obtained clearly indicated that EA has tremendous ability to scavenge free radicals, even at concentration of 1 µM. Interestingly even in the absence of esterase, EAPA, the acetylated product of EA, was also found to be a good scavenger but at a relatively slower rate. Kinetic studies revealed that both EA and EAPA have ability to scavenge free radicals at the concentrations of 1 µM over extended periods of time. In cellular systems, EA and EAPA were found to have similar potentials for the inhibition of ROS production in L-6 myoblasts and NADPH-dependent catalyzed microsomal lipid peroxidation.

Breast cancer is one of the leading causes of death in women worldwide, highlighting the crucial need for novel and effective treatments. In this study, we look at the ability of four natural compounds i.e. Berberine, Curcumin, Withaferin A, and Ellagic Acid to target important breast cancer biomarkers such as B-cell lymphoma 2 (BCL-2), programmed death-ligand 1 (PDL-1), cyclin-dependent kinase 4/6 (CDK4/6) and fibroblast growth factor receptor (FGFR). These indicators have important roles in tumor development, survival, immune response, and cell cycle control, making them potential targets for future cancer treatments. Our study employs a variety of techniques, including pharmacokinetic profiling (ADME), molecular docking, and molecular dynamics simulations, to determine how successful these drugs could be in therapy. The pharmacokinetic investigation found that Berberine and Ellagic Acid stand out due to their high absorption and solubility, implying that they could be suitable for clinical application. When we ran docking simulations, we discovered substantial connections between these chemicals and the target proteins. Additionally, Berberine has a binding affinity of − 9.3 kcal/mol for BCL-2, indicating that it can impair the protein’s cancer cell-protective activities. Ellagic Acid, on the other hand, has an even higher binding affinity for PDL-1 of − 9.8 kcal/mol, showing that it may be able to increase immune responses against tumors. Molecular dynamics simulations over 100 ns demonstrated the stability of these protein–ligand complexes. Interestingly, Ellagic Acid was found to be more structurally stable than Berberine throughout these simulations. We found consistent interactions between the chemicals and key residues in the target proteins. For example, Ellagic Acid (CID: 5281855) established persistent linkages with LYS43, ASP163, and VAL27, whereas Berberine (CID: 2353) interacted with VAL27, ALA41, and LEU152 throughout the simulation. In conclusion, the combination of good pharmacokinetics, robust interactions with cancer biomarkers, and stable complexes makes Berberine and Ellagic Acid interesting candidates for further investigation as natural inhibitors in breast cancer treatment. These findings establish the framework for future research into novel and inventive techniques to effectively combating breast cancer.

Naturally occurring compounds are considered as attractive candidates for cancer treatment and prevention. Quercetin and ellagic acid are naturally occurring flavonoids abundantly seen in several fruits and vegetables. In the present study, we evaluate and compare antitumor efficacies of quercetin and ellagic acid in animal models and cancer cell lines in a comprehensive manner. We found that quercetin induced cytotoxicity in leukemic cells in a dose-dependent manner, while ellagic acid showed only limited toxicity. Besides leukemic cells, quercetin also induced cytotoxicity in breast cancer cells, however, its effect on normal cells was limited or none. Further, quercetin caused S phase arrest during cell cycle progression in tested cancer cells. Quercetin induced tumor regression in mice at a concentration 3-fold lower than ellagic acid. Importantly, administration of quercetin lead to ~5 fold increase in the life span in tumor bearing mice compared to that of untreated controls. Further, we found that quercetin interacts with DNA directly and could be one of the mechanisms for inducing apoptosis in both, cancer cell lines and tumor tissues by activating the intrinsic pathway. Thus, our data suggests that quercetin can be further explored for its potential to be used in cancer therapeutics and combination therapy.

Ellagic acid (EA) is a natural polyphenol found in various fruits, nuts, and mushrooms. It exhibits a variety of biological activities, including potent antioxidant, anti-inflammatory, anti-obesity, and neuroprotective properties. EA exerts hepatoprotective effects through multiple mechanisms, including (1) scavenging reactive oxygen species (ROS) and enhancing endogenous antioxidant defenses (e.g., by activating Nrf2/ARE), (2) modulating inflammatory signaling pathways (e.g., inhibiting NF-κB, TNF-α, and IL-6), and (3) regulating apoptosis (e.g., downregulating the Bax/Bcl-2 ratio) and fibrosis (e.g., inhibiting TGF-β/Smad signaling). Despite its promising preclinical efficacy, the clinical applicability of EA is currently limited by its poor bioavailability. This could potentially be overcome by advanced delivery systems or by directly administering its active microbial metabolites, known as urolithins. EA and its derivatives also modulate the gut microbiota, promoting the growth of beneficial species and reducing gut permeability and hepatic inflammation. Preliminary clinical trials and other emerging evidence suggest that EA may reduce liver inflammation, oxidative stress, and metabolic dysregulation. However, more extensive human studies are needed to confirm its efficacy and safety in managing liver disease. This review highlights the therapeutic potential of EA in the treatment of liver diseases, particularly metabolic-dysfunction-associated steatotic liver disease (MASLD).

Burgeoning antibiotic resistance in Pseudomonas aeruginosa has necessitated the development of anti pathogenic agents that can quench acylhomoserine lactone (AHL) mediated QS with least risk of resistance. This study explores the anti quorum sensing potential of T. chebula Retz. and identification of probable compounds(s) showing anti QS activity and the mechanism of attenuation of P. aeruginosa PAO1 virulence factors. Methanol extract of T. chebula Retz. fruit showed anti QS activity using Agrobacterium tumefaciens A136. Bioactive fraction (F7), obtained by fractionation of methanol extract using Sephadex LH20, showed significant reduction (p<0.001) in QS regulated production of extracellular virulence factors in P. aeruginosa PAO1. Biofilm formation and alginate were significantly (p<0.05) reduced with enhanced (20%) susceptibility to tobramycin. Real Time PCR of F7 treated P. aeruginosa showed down regulation of autoinducer synthase (lasI and rhlI) and their cognate receptor (lasR and rhlR) genes by 89, 90, 90 and 93%, respectively. Electrospray Ionization Mass Spectrometry also showed 90 and 64% reduction in the production of 3-oxo-C(12)HSL and C(4)HSL after treatment. Decrease in AHLs as one of the mechanisms of quorum quenching by F7 was supported by the reversal of inhibited swarming motility in F7-treated P. aeruginosa PAO1 on addition of C(4)HSL. F7 also showed antagonistic activity against 3-oxo-C(12)HSL-dependent QS in E. coli bioreporter. C. elegans fed on F7-treated P. aeruginosa showed enhanced survival with LT50 increasing from 24 to 72 h. LC-ESI-MS of F7 revealed the presence of ellagic acid derivatives responsible for anti QS activity in T. chebula extract. This is the first report on anti QS activity of T. chebula fruit linked to EADs which down regulate the expression of lasIR and rhlIR genes with concomitant decrease in AHLs in P. aeruginosa PAO1 causing attenuation of its virulence factors and enhanced sensitivity of its biofilm towards tobramycin.

Ellagic acid (EA) is a naturally occurring polyphenolic compound endowed with strong antioxidant and anticancer properties that is present in high quantity in a variety of berries, pomegranates, and dried fruits. The antitumor activity of EA has been mostly attributed to direct antiproliferative and apoptotic effects. Moreover, EA can inhibit tumour cell migration, extra-cellular matrix invasion and angiogenesis, all processes that are crucial for tumour infiltrative behaviour and the metastatic process. In addition, EA may increase tumour sensitivity to chemotherapy and radiotherapy. The aim of this review is to summarize the in vitro and in vivo experimental evidence supporting the anticancer activity of pure EA, its metabolites, and EA-containing fruit juice or extracts in a variety of solid tumour models. The EA oral administration as supportive therapy to standard chemotherapy has been recently evaluated in small clinical studies with colorectal or prostate cancer patients. Novel formulations with improved solubility and bioavailability are expected to fully develop the therapeutic potential of EA derivatives in the near future.

This study investigates the antimalarial potential of extracts and compounds from various plants used in traditional Korean medicine, in response to the increasing resistance of Plasmodium falciparum to standard treatments such as chloroquine and artemisinin. The antimalarial activity screening was conducted on 151 extracts, identifying the top seven candidates, including Geranium thunbergii (50% ethanol and 100% methanol extract), Reynoutria japonica, Amomum villosum (hot water and 50% ethanol extract), Cinnamomum zeylanicum, and Platycodon grandiflorum. Among these, G. thunbergii was identified as the top priority for further analysis due to its high antimalarial activity and high yield of bioactive compounds. The plant extracts were fractionated using ethyl acetate, chloroform, and hot water, and their efficacy against P. falciparum was evaluated through IC50 determination and microscopic analysis. The compounds evaluated included ellagic acid, gallic acid, afzelin, quercetin, and protocatechuic acid. Among the tested compounds, ellagic acid showed the most potent antimalarial activity with an IC50 of 1.60 ± 0.09 µM, followed by gallic acid (39.43 ± 1.48 µM) and afzelin (52.77 ± 1.84 µM). In contrast, quercetin (116.8 ± 3.78 µM) and protocatechuic acid (1.23 ± 0.02 mM) exhibited minimal antimalarial effects. Giemsa staining was employed to visualize parasite morphology and confirmed that ellagic acid is effective in inhibiting growth at the late trophozoite stage. These findings suggest that ellagic acid could serve as a promising lead compound for developing a novel antimalarial agent. This study highlights the importance of exploring plant-based compounds as alternative strategies against drug-resistant malaria. Further investigation into the mechanisms underlying the antimalarial activity of these compounds is necessary to fully validate their therapeutic potential.