Search Results (51)

In this study, the cosmeceutical potential of a 70% ethanol extract of Rosa lucieae was investigated as a multifunctional bioactive ingredient. The extract was systematically evaluated for its antioxidant, anti-melanogenic, and anti-aging properties, and was comprehensively phytochemically profiled using ultra-high-performance liquid chromatography–quadrupole time-of-flight mass spectrometry. The analysis tentatively identified 21 metabolites, including phenolic acids (gallic acid, ellagic acid, and corilagin), flavonoids (catechin, rutin, quercetin, hyperoside, and quercitrin), and glycosidic derivatives (e.g., phlorizin), several of which are well-documented for their skin-protective effects. Quantitative measurements confirmed high polyphenol and flavonoid contents, correlating with strong radical-scavenging and reducing capacities in α-diphenyl-β-picrylhydrazyl, 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid, as well as ferric ion reducing antioxidant power assays. Moreover, the extract inhibited tyrosinase activity and 3,4-dihydroxyphenylalanine oxidation, thereby suppressing melanin biosynthesis. In addition, marked inhibitory effects against collagenase, elastase, and hyaluronidase were observed; these enzymes are critically involved in extracellular matrix degradation and skin aging. Taken together, these results indicate that the biological activities of R. lucieae are supported by a diverse polyphenol- and flavonoid-rich chemical profile, highlighting the potential of this plant as a natural multifunctional ingredient for cosmeceutical, nutraceutical, functional food, and preventive healthcare applications. Full article

Objectives: Modern lifestyles factors such as digital overload, aging, and poor sleep hygiene have led to increasing cases of sleep disturbances and inflammation-related disorders. These conditions are often associated with oxidative stress and immune dysregulation. Longan flower extract (LFE), traditionally used in East Asian medicine, has shown potential health benefits but remains scientifically underexplored. This study aims to investigate the chemical composition and bioactive effects of LFE on inflammation, oxidative stress, and melatonin biosynthesis in relevant cellular models. Methods: LFE was prepared using ethanol extraction and characterized for its total polyphenols, flavonoids, oligomeric proanthocyanidins (OPCs), and corilagin content via HPLC. Its anti-inflammatory, antioxidant, and neuroregulatory activities were assessed in LPS-stimulated RAW 264.7 macrophages and BV-2 microglial cells. Key assays included quantification of cytokines (TNF-α, IL-6), detection of nitric oxide (NO) and reactive oxygen species (ROS), and measurement of antioxidant enzyme activities (GPx, SOD). Gene expression of melatonin biosynthesis enzymes was evaluated using quantitative PCR. Results: LFE treatment significantly reduced LPS-induced TNF-α, IL-6, NO, and ROS production in both cell models. It enhanced GPx and SOD activity and increased intracellular glutathione levels. Moreover, LFE upregulated the expression of TPH1, DDC, AANAT, and ASMT, genes involved in melatonin biosynthesis, and promoted serotonin secretion. Conclusions: These findings suggest that LFE holds significant potential as a natural therapeutic supplement, particularly for alleviating sleep disturbances, reducing oxidative stress, and modulating inflammatory responses associated with modern lifestyle-related health conditions. Full article

Rosa damascena Mill., widely recognized for its remarkable skincare benefits, is extensively used in the cosmeceutical industry. This study introduces a novel green approach to extract bioactive compounds from R. damascena for cosmeceutical applications while also evaluating its stability in terms of physical, chemical, and biological properties. R. damascena petals were extracted using deionized water instead of organic solvents, using various green extraction methods, including infusion, microwave, ultrasound, pulsed electric field, and micellar extraction. Their chemical composition was analyzed using high-performance liquid chromatography. The extract with the highest concentration of bioactive compounds was further evaluated for its cosmeceutical properties and stability and compared with its individual chemical components. Various factors influencing stability were evaluated, including pH level (5, 7, and 9), temperature (4 °C, 30 °C, and 45 °C), and light exposure. The findings indicate that the extract obtained through microwave-assisted extraction (MAE) contained the highest concentration of bioactive constituents, with corilagin being the most abundant, followed by cyanidin-3,5-O-diglucoside, gallic acid, ellagic acid, L-ascorbic acid, and rutin, respectively. Additionally, MAE exhibited excellent antioxidant, whitening, and anti-skin-aging effects, demonstrating significantly higher activities than both the positive control (L-ascorbic acid for antioxidant effects, kojic acid for anti-tyrosinase effects, and epigallocatechin gallate and oleanolic acid for anti-skin-aging effects) and the individual chemical constituents. However, the physico-chemical and biological stability of MAE was influenced by pH, temperature, and light exposure, and as such, light-protected and controlled temperature (not exceeding 30 °C) is essential to maintain the extract’s efficacy in skincare products, and optimal formulation strategies are strongly recommended to ensure long-term stability. Full article

Rambutan peel is a great source of bioactive compounds, the same that, over the years, has been extracted using conventional technologies which have been proven to be harmful to the environment and potentially toxic to human beings. This study aimed to extract the same compounds using a hybridization of ultrasound/microwave extraction. The results were promising, as a total of 378.48 ± 9.19 mg/g of polyphenols were recovered from this procedure, and the most important molecules (geraniin, corilagin, and ellagic acid) were identified, giving this much more relevance. Furthermore, treatment with rambutan peel extract recovered with green technologies significantly reduced cell viability in HCV-infected liver cells. Notably, higher concentrations (4000 and 5000 ppm) led to more pronounced cell death in huh7 cells. The treatment also led to a significant reduction in viral protein and RNA expression in HCV-infected cells. These findings suggest that rambutan peel extract obtained from the combination of ultrasound and microwave extraction, particularly the ellagitannins present, have potential antiviral properties. Further research is needed to explore its mechanism of action and its potential as a therapeutic agent for Hepatitis C. Full article

Background/Objectives: Toxoplasmosis is a zoonotic disease caused by Toxoplasma gondii. The parasite infection in humans continues to rise due to an increasing seroprevalence rate in domestic and wild warm-blooded animals that serve as a major reservoir of the parasite. There are fewer drugs available for the treatment of toxoplasmosis. However, these drugs are limited in efficacy against tachyzoites and bradyzoites. Also, there are clinical side effects and geographical barriers to their use, especially in immunocompromised patients, children, and pregnant women. Tannins, a class of natural products, are known to have antimicrobial properties. However, little is known about the effects of Corilagin (CG) and Punicalagin (PU), which are classified as tannins, on T. gondii growth and their possible mechanism of action in vitro. We hypothesize that CG and PU could inhibit T. gondii growth in vitro and cause mitochondria membrane disruption via oxidative stress. Methods: Here, we investigated the anti-T. gondii activity of the two named tannins using a fluorescent-based reporter assay. Results: The 50% effective concentrations (EC_50s) values for CG and PU that inhibited T. gondii parasites growth in vitro were determined to be 3.09 and 19.33 µM, respectively. Pyrimethamine (PY) was used as a standard control which gave an EC₅₀ value of 0.25 µM. Interestingly, CG and PU were observed to cause high reactive oxygen species (ROS) and mitochondrial superoxide (MitoSOX) production in tachyzoites. This resulted in a strong mitochondria membrane potential (MMP) disruption in T. gondii tachyzoites. Conclusions: Therefore, the possible mechanism(s) of action of CG and PU against T. gondii is associated with the disruption of the mitochondria redox biology. Thus, the high ROS and MitoSOX produced as a result of these compounds created high oxidative stress, leading to mitochondrial dysfunction. Full article

Previous studies have demonstrated corilagin’s inhibitory effects on the growth of various cancer cells. Given the limited research on corilagin’s impact on ovarian cancer, a particularly deadly gynecological malignancy, this study aimed to investigate corilagin’s influence on A2780 ovarian cancer cell apoptosis and its underlying mechanisms. The goal was to evaluate corilagin’s potential as a therapeutic agent for ovarian cancer. The results of the CCK-8 assay showed that corilagin inhibited the proliferation of A2780 ovarian cancer cells while exhibiting lower toxicity to normal ovarian surface epithelial cells (IOSE-80). We found that corilagin significantly altered the A2780 cell cycle, decreasing the proportion of cells in the G₀/G₁ and G₂/M phases and inducing cell cycle arrest in the S phase. At low concentrations, corilagin induced apoptosis in A2780 cells, accompanied by a decline in mitochondrial membrane potential and calcium influx. Transcriptome sequencing analysis identified differentially expressed apoptosis-related genes in corilagin-treated A2780 cells, primarily within the PI3K-AKT pathway. Furthermore, qPCR and Western blot results confirmed the upregulation of p53 and Bax genes and the downregulation of BCL-2. Corilagin also increased the expression of apoptotic factors caspase-9, caspase-3, PUMA, and cytochrome C, indicating its ability to induce apoptosis. Overall, corilagin effectively inhibited A2780 cell proliferation, induced cell cycle arrest, and triggered apoptosis. Its anti-tumor effect in vitro suggests its potential as a therapeutic agent for ovarian cancer A2780, especially through the PI3K/p53 pathway. Full article

There has been no chemical analysis of the fruit of medicinal plant Jatropha podagrica until now. The current study aimed to qualitatively and quantitatively analyze the J. podagrica fruit using a high-resolution LC-MS strategy, i.e., library-comparison ultra-high-performance liquid chromatography-Quadrupole-Orbitrap-tandem mass spectrometry. The strategy putatively identified 46 compounds from fresh fruit. During the putative identification, 10 isomers (e.g., (vitexin vs. isovitexin) were completely distinguished from each other. Thereafter, all 46 compounds were simultaneously quantified using authentic standard comparison method. Finally, they were also subjected to the 2,2′-azino bis (3-ethylbenzothiazolin-6-sulfonic acid radical (ABTS^+•)-scavenging assay to characterize their relative antioxidant capacities. Their antioxidant capacities were thus multiplied by chemical contents to calculate their antioxidant contribution values, respectively. Corilagin, gallic acid, ellagic acid, and phillygenin exhibited the highest antioxidant contribution percentages and thereby were suggested as the four top antioxidant contributors. The four are recommended to build up a quality-markers (Q-markers) system of J. podagrica fruits. All these findings can help to develop J. podagrica fruits as a potential resource of natural medicine. Full article

Acute lung injury (ALI) and its severe manifestation, acute respiratory distress syndrome (ARDS), are characterized by uncontrolled inflammatory responses, neutrophil activation and infiltration, damage to the alveolar capillary membrane, and diffuse alveolar injury. Neutrophil extracellular traps (NETs), formed by activated neutrophils, contribute significantly to various inflammatory disorders and can lead to tissue damage and organ dysfunction. Corilagin, a compound found in Phyllanthus urinaria, possesses antioxidative and anti-inflammatory properties. In this study, we investigated the protective effects and underlying mechanisms of corilagin in hydrochloric acid (HCl)/lipopolysaccharide (LPS)-induced lung injury. Mice received intraperitoneal administration of corilagin (2.5, 5, or 10 mg/kg) or an equal volume of saline 30 min after intratracheal HCl/LPS administration. After 20 h, lung tissues were collected for analysis. Corilagin treatment significantly mitigated lung injury, as evidenced by reduced inflammatory cell infiltration, decreased production of proinflammatory cytokines, and alleviated oxidative stress. Furthermore, corilagin treatment suppressed neutrophil elastase expression, reduced NET formation, and inhibited the expression of ERK, p38, AKT, STAT3, and NOX2. Our findings suggest that corilagin inhibits NET formation and protects against HCl/LPS-induced ALI in mice by modulating the STAT3 and NOX2 signaling pathways. Full article

The use of diversified raw materials and various extractant types is justified because the varied chemical composition of extracts obtained via extraction determines their biological activity. Therefore, the objective of this study was (i) to characterize the chemical profile of two types of bearberry extracts (70% ethanolic and water) and (ii) to investigate the biological activity of the analyzed extracts through an assessment of their possible proapoptotic effects on glioma cell lines. The HPLC-UV analysis of individual compounds was performed for the determination of the phytochemical profile of the bearberry extracts, and their total phenolic content (TPC) and total flavonoid content (TFC) were determined spectrophotometrically. The induction of apoptosis, autophagy, and necrosis in anaplastic astrocytoma MOGGCCM and human glioblastoma LN229 cell lines were investigated. The results indicated that the ethanolic (Et) and aqueous (Aq) extracts had different chemical profiles. The TPC in the Et was ca. 60% higher than in the Aq. Similarly, the TFC and methylarbutin (mARB) concentrations were significantly higher in the Et. On the other hand, the concentration of hydroquinone (HQ) was ca. 70% and that of corilagin (COR) was ca. 100% higher in the Aq. In turn, the presence of ursolic acid (UA) and oleanolic acid (OA) was confirmed solely in the Et. In contrast to Aq, Et demonstrated high proapoptotic activity. At the concentration of 2 µL/mL, the level of apoptosis varied between 14.7% and 26% in the case of the MOGGCCM cells and between 12.3% and 33.3% in the case of the LN229 cell line. The knowledge and information obtained in this study indicate a need for further research on the anticancer effect of the studied bearberry phytochemicals on the MOGGCCM and LN229 cell lines and for the elucidation of their molecular anticancer mechanisms. Full article

Plants and plant extracts are a relevant source of bioactive compounds widely employed as functional foods. In the Mediterranean area, the shrub Sarcopoterium spinosum is traditionally used as an herbal medicine for weight loss and a diabetes treatment. Inflammation is a protective mechanism involved in the development of many pathological conditions, including cardiovascular diseases. The present study aimed to investigate in vitro the antioxidant and cytoprotective properties of an ethanolic extract from S. spinosum fruits (SEE) in a cellular model of endothelium dysfunction. Corilagin and quercetin are two polyphenols abundant in SEE and were tested for comparison. The exposure of HECV cells for 24 h to 30 µM hydrogen peroxide (H₂O₂) lead to an oxidative stress condition. When HECV cells were treated with 10 µg/mL of SEE or single compounds after or before the oxidative insult, the results showed their ability to (i) decrease the reactive oxygen species (ROS) production quantified using fluorometric analysis and the lipid peroxidation measured with a spectrophotometric assay; (ii) rescue both the glutathione reduced to oxidized (GSH/GSSG) ratio and nitric oxide impair and the protein denaturation; and (iii) accelerate the wound repair measured using a T-scratch assay. Taken together, our findings indicate that the ethanolic extract from S. spinosum fruits could be a potential candidate for nutraceutical application. Full article

Dietary fruits and vegetables play a vital role as food and drugs and are the main sources of antioxidant defences against degenerative diseases, such as brain dysfunctions, cardiovascular diseases, immune system deteriorations, and cancers, brought on by oxidative damage. Phyllanthus emblica is a significant herbal remedy used in conventional medicine to recover lost strength and power. In this research, the potential value of Phyllanthus emblica as a food and drug is researched. The total phenolic, total flavonoid, and total tannin contents as well as the nutritional value, vitamin C, vitamin E, and mineral contents of different organs of P. emblica were evaluated. The antioxidant and antimicrobial activities of extracts and fractions of different organs of P. emblica were determined. A total of eleven flavonoids, simple phenolic, tannin-related phenolic, and tannin molecules were isolated from a hydroalcoholic extract of the leaves and fruits. The structures were identified by spectroscopic data and comparison with the literature values as gallic acid (1), naringenin 7-O-(6″-O-galloyl)-β-D-glucopyranoside (2), 3,3′-di-O-methyl ellagic acid-4′-O-β-d-glucopyranoside (3), 1-O-galloyl glycerol (4), 1,6-di-O-galloyl-β-d-glucopyranoside (5), flavogallonic acid bislactone (6), corilagin (7), ethyl gallate (8), urolithin M5 (9), (E)-p-coumaroyl-1-O-β-d-glucopyranoside (10), and 1,2,4,6-tetra-O-galloyl-β-d-glucopyranoside (11). Among them, compounds 3 and 10 are first isolated from the plant. Molecular docking was performed to investigate the comparative interactions between positive controls (galantamine and donepezil) and selected compounds utilizing acetylcholinesterase (4EY7) as a target receptor. Results exhibited the potency of these compounds against the target receptor. In summary, P. emblica has a wealth of minerals, vitamins C and E, and polyphenolic phytochemicals that may work together to treat infectious disease, prevent and/or treat oxidative-damage-related illnesses including Alzheimer’s disease. Full article

Cascalote pods are an important source of phenolic compounds, mainly recovered using solvent extraction methods. To find a sustainable alternative to these methods, this study aimed to evaluate solid-state fermentation (SSF) in order to enhance the extractability of total phenolic compounds (TPC) with antioxidant activity (AA) from cascalote pods. Aspergillus niger GH1 was selected based on the amount of TPC released and AA measured (ABTS, DPPH, FRAP) in a short period of time. Moreover, moisture, temperature, inoculum size, and mineral composition were evaluated. The largest amount of TPC released was 124.17 mg/gdw (g of dry weight) after 12 h of culture, which significantly correlated with the AA (Pearson’s R = 0.94). Moisture and KH₂PO₄ concentration were the main influencing factors of TPC release. Treatment 6 (1 × 10⁷ spores/gdw, 30 °C, 60% moisture, mineral composition (g/L): KH₂PO₄, 1.52; NaNO₃, 7.65; and MgSO₄, 1.52) was selected due to the highest values of both TPC and AA. SSF-assisted extraction allowed for an increase of 118% and 93% in TPC and AA values, respectively. Corilagin, lagerstannin, geraniin, and ellagic acid were the main phenolic compounds identified by RP-HPLC-ESI-MS in the cascalote extracts. The results obtained demonstrate the feasibility of SSF-assisted extraction as a biotechnological alternative for the recovery of important bioactive molecules from this underutilized material. Full article

Rambutan (Nephelium lappaceum L.) is a tropical fruit that is originally from Southeast Asia and it was introduced to Mexico in the 1960s; the fruit’s peel is known to possess ellagitannins such as ellagic acid which give the peel great biological activity; solid-state fermentation has been used to obtain said compounds and rambutan peel can be used as a fermentation support/substrate; this work aims to obtain, identify and quantify ellagic acid obtained via SSF with a strain of yeast. The water-absorption index and the support’s maximum moisture were determined. To determine the ideal conditions for ellagic acid accumulation, a Box–Behnken 3^k experimental design was applied using variables such as temperature, moisture and inoculum. The maximum accumulation time of ellagic acid via solid-state fermentation was determined to be 48 h with ideal conditions of 30 °C, 60% moisture and 1.5 × 10⁷ cells/g using S. cerevisiae, and high-performance liquid chromatography was used to identify ellagic acid, geraniin and corilagin as the most abundant compounds. The maximum recovery of ellagic acid was 458 ± 44.6 mg/g. HPLC/ESI/MS analysis at 48 h fermentation showed biodegradation of geraniin and corilagin due to ellagic acid. Mexican rambutan peel has been demonstrated to be a suitable substrate for SSF. Full article

Ludwigia octovalvis (Jacq.) P.H. Raven is widely used in traditional medicine for different illnesses, including diabetes and hypertension. However, its impact on lipotoxicity and metabolic syndrome in vivo has not been addressed. Therefore, the aim of this study was to evaluate the effects of this plant on the metabolic syndrome parameters in a C57BL6J mouse hypercaloric diet model. L. octovalvis hydroalcoholic extract and its ethyl acetate fraction (25 mg/kg/day) were used for sub-chronic assessment (10 weeks). Additionally, four subfractions (25 mg/kg) were evaluated in the postprandial triglyceridemia test in healthy C57BL6J mice. The hydroalcoholic extract and ethyl acetate fraction significantly decreased body weight gain (−6.9 g and −1.5 g), fasting glycemia (−46.1 and −31.2 mg/dL), systolic (−26.0 and −22.5 mmHg) and diastolic (−8.1 and 16.2 mmHg) blood pressure, free fatty acid concentration (−13.8 and −8.0 μg/mL) and insulin-resistance (measured by TyG index, −0.207 and −0.18), compared to the negative control. A postprandial triglyceridemia test showed that the effects in the sub-chronic model are due, at least in part, to improvement in this parameter. L. octovalvis treatments, particularly the hydroalcoholic extract, improve MS alterations and decrease free fatty acid concentration. These effects are possibly due to high contents of corilagin and ellagic acid. Full article

This research sought to optimize the microwave-assisted extraction of Chatuphalathika as an herbal recipe maximizing the active compounds and the antioxidant activity by the Box–Behnken design. Three factors—microwave power, time, and cycle—were varied. Eight responses—extraction yield, total phenolic content, gallic acid content, corilagin content, chebulagic acid, chebulinic acid, IC₅₀ from DPPH assay, and IC₅₀ from FRAP assay—were monitored. Furthermore, cytotoxicity was evaluated to ensure the safety of the extract. After that, the optimized extract was compressed into tablets. The results showed that the optimal condition of the microwave-assisted extraction gave the simultaneous maximum extraction yield, total phenolic content, and antioxidant activity with a microwave power of 450 W for 30 s and 3 cycles. The extract obtained from the optimal condition exhibited a good safety profile although a concentration of 5 mg/mL was used. The optimized tablets were achieved when a compression force of 1500 psi and magnesium stearate of 1% were applied, and no sodium starch glycolate was added. In conclusion, the optimal green extraction method could be used for the extraction of the Chatuphalathika. Furthermore, the fabrication of Chatuphalathika tablets was successful, as the tablets had low friability with a short disintegration time. Full article