Search Results (4,718)

The present work reports the bioguided isolation of constituents from the ethanol extract of Holarrhena floribunda stem bark, their identification by UHPLC-ESI-QTOF-MS/MS identification, and the in silico prediction of the pharmacokinetic and toxicity parameters. The crude extract, along with its n-hexane and alkaloid-rich fractions, displayed moderate to good antiplasmodial activity in vitro against chloroquine-sensitive (3D7) and multidrug-resistant (Dd2) strains of Plasmodium falciparum, with IC₅₀ values ranging from 6.54 to 43.54 µg/mL. Seventeen steroidal alkaloids (1–17) were identified in the most active fraction using UHPLC-ESI-QTOF-MS/MS, based on their fragmentation patterns and analysis with the Structural Similarity Network Annotation Platform for Mass Spectrometry (SNAP-MS). Furthermore, bioguided isolation of the ethanol extract yielded twenty-one compounds (3, 5, 10, 14–16, 18–31), whose structures were elucidated by spectroscopic methods. Among them, compounds 5, 14, and 27 showed the highest potency against the two strains of P. falciparum, with IC₅₀ values between 25.97 and 55.78 µM. In addition, the in silico prediction of pharmacokinetic parameters and drug-likeness using the SwissADME web tool indicated that most of the evaluated compounds (1, 3–5, and 14–16) complied with Lipinski’s rule of five. Full article

Erica spiculifolia Salisb. (Balkan heath) is an evergreen shrub growing in the mountain shrublands of Eastern Europe. E. spiculifolia was used as a diuretic, anti-inflammatory, and antioxidant herbal remedy. The present study aims to conduct an evaluation of the phytochemical composition and antitumor activity of the methanol–aqueous extract from E. spiculifolia aerial parts to explore its potential in cancer treatment. Overall, a total of 54 secondary metabolites, including 28 hydroxybenzoic, hydroxycinnamic acids, and phenolic glycosides, and 10 triterpene acids, together with 17 flavonoids, were identified or annotated in the assayed E. spiculifolia extract using liquid chromatography-high-resolution mass spectrometry. The cytotoxic activity of the extract, alongside gallic, protocatechuic, and oleanolic acids as its constituents, was screened against a panel of malignant human cell lines of different origin (LAMA-84, HL-60, MDA-MB-231, MCF-7, and CASKI). The most prominent antiproliferative effect of the studied extract (with IC₅₀ 16.6 μg/mL), matched with the highest tumor selectivity (SI > 120), was observed in the LAMA-84 myeloid cells. These findings were further supported by gallic and oleanolic acid (IC₅₀ 6.2 and 1.7 μg/mL, respectively), accounting for a more distinct cytotoxicity. The strongest selective antineoplastic activity was achieved towards the triple-negative breast carcinoma cell line MDA-MB-231, with an IC₅₀ of 32.5 μg/mL. This study provided compelling evidence for a wide spectrum of E. spiculifolia antitumor activity, indicating its potential as a natural alternative for future therapeutic applications. Full article

Lung cancer is a leading cause of cancer mortality worldwide. Targeted therapies with epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) represent a significant advance in the management of lung cancer. However, their long-term efficacy is often limited by acquired resistance, particularly due to the T790M mutation, highlighting the need for novel EGFR-TKIs. Although compounds derived from Centella asiatica have demonstrated anticancer potential, their role in EGFR inhibition has not yet been reported. In this study, we investigated the inhibitory activity of two primary constituents, asiaticoside and asiatic acid, against wild-type and double-mutant (L858R/T790M) EGFR, as well as the anticancer effects of the more potent compound in lung cancer cells. A kinase activity assay revealed that asiatic acid potently inhibited both wild-type and double-mutant EGFR, whereas asiaticoside showed minimal inhibitory activity. Molecular docking demonstrated that asiatic acid bound to the ATP-binding pocket of both EGFR forms with binding energies superior to those of erlotinib and osimertinib. Treatment with asiatic acid significantly (i) reduced viability of A549 and H1975 cells while remaining non-toxic to BEAS-2B normal lung cells, (ii) enhanced cancer cell apoptosis, (iii) suppressed extracellular signal-regulated kinase (ERK) and protein kinase B (Akt) signaling pathways, and (iv) inhibited EGFR activation in A549 and H1975 cells. These results suggest that asiatic acid is a promising lead compound for anticancer drug development. Full article

The custard apple (CA) is a noble fruit in tropical regions worldwide. It has attracted a growing interest due to its organoleptic properties and nutritional value. With the expansion of international trade, both its cultivation and consumption have grown significantly in recent years. Previous researchers have sporadically investigated its nutritional composition and health benefits; however, existing information on its processing and utilization is highly fragmented and lacks a comprehensive overview of its constituents, biological activities, and potential applications. This review is a detailed summary of the nutritional and bioactive properties, safety evaluations, and potential applications of CA. Following PRISMA guidelines, peer-reviewed studies published between 2000 and 2025 were systematically searched in PubMed, Scopus, ResearchGate, and Web of Science. Inclusion criteria comprised studies reporting on nutritional composition, phytochemicals, bioactivities, health promotion, and applications of CA. In addition to primary nutrients like carbohydrates, protein, fatty acids, vitamins, and minerals, CA also contains a multitude of bioactive compounds, mainly including phenols, flavonoids, terpenoids, acetogenins, and alkaloids, which are attributed to a range of health benefits, such as antioxidant, anti-microbial, anti-tumor, blood sugar regulation, and cognitive function improvement. However, more clinical and toxicological profiles remain underexplored, and future research should focus on standardized extraction, safety evaluation, and translational applications. Additionally, the challenges and future perspectives in industrial applications are discussed, which are expected to offer comprehensive information for the utilization of CA. Full article

Jefea lantanifolia (S. Schauer) Strother is traditionally used in Hidalgo, Mexico, to manage type 2 diabetes (T2D). The aerial parts are prepared as an infusion and consumed throughout the day. This study conducted a 2 h acute experiment under both fasting and postprandial conditions to evaluate the effects of the aqueous infusion (AE), the ethanol–water extract (EWE), and their isolated constituents in hyperglycemic rats. Structures were established using conventional spectroscopic methods. The absolute configuration was determined by optical rotation and calculated electronic circular dichroism (ECD) methods. Phytochemical analysis led to the isolation of six compounds: luteolin (1); 2β-hydroxy-dimerostemma brasiolide-1-O-(3-hydroxymethacrylate) (2); homoplantaginin (3); cynarin (4); luteolin-7-O-glucoside (5); and nepitrin (6). The extract was deemed safe at a dose of 2 g/kg b. w. in acute toxicity assays. In vivo experiments showed significant reductions in blood glucose levels during fasting, with compounds 2 and 3 achieving reductions of 42% and 40%, respectively, compared to 51% with glibenclamide. Postprandially, all treatments demonstrated effective glucose-lowering activity, particularly compound 3 and the EWE. These findings support the traditional use of J. lantanifolia and highlight its phytochemicals as promising candidates for further pharmacological investigation. Long-term studies and high-dose evaluations are warranted to validate therapeutic potential and establish safety profiles. Full article

Camellia oleifera, a member of the Theaceae family and belonging to the Camellia Linn species, is a plant utilized for edible oil production and medicinal value. Its fruit is abundant in various bioactive compounds, including triterpene saponins, flavonoids, lignans, fatty acids, sterols, polysaccharides, and numerous other chemical constituents. Among these, triterpene saponins and flavonoids serve as the primary active ingredients. The pharmacological effects of C. oleifera fruits are diverse, encompassing anti-tumor properties, cardiovascular and cerebrovascular protection, anti-inflammatory, antioxidant activity, lipid-lowering capability, anti-fungal property, and neuroprotective function. In recent years, this area has garnered significant attention from scholars both domestically and internationally. This article reviews the chemical constituents and pharmacological effects of C. oleifera fruits, aiming to provide a comprehensive reference for further research and development. Additionally, it offers a scientific foundation and innovative insights for clinical applications and the identification of relevant bioactive components. Full article

This research provides a comprehensive evaluation of the phytochemical composition, antioxidant potential, and biological properties of four plant species with longstanding use in ethnobotanical traditions: Calendula officinalis, Mentha × piperita, Urtica dioica, and Juglans regia. Plant extracts were obtained using a range of solvent systems and subsequently analyzed for their content of total polyphenols, flavonoids, and phenolic acids. Ultra-high-performance liquid chromatography coupled with mass spectrometry (UHPLC-MS) enabled the accurate identification and quantification of major polyphenolic constituents. The antioxidant capacity was assessed through a series of in vitro assays, and elemental analysis was conducted to determine microelement content. To evaluate potential ecological implications, acute toxicity was tested using Daphnia magna, while phytotoxic effects were also examined. The results demonstrate pronounced antioxidant activity along with notable biocidal and soil-enhancing properties. These findings underscore the potential of such plant-based formulations as sustainable alternatives to conventional agrochemicals and highlight the relevance of integrating traditional botanical knowledge with modern strategies for enhancing soil quality, crop performance, and environmental sustainability. Full article

The development of advanced photocatalysts that are efficient, recyclable and sustainable represents a significant challenge in the face of the growing presence of persistent organic contaminants in industrial wastewaters. This paper presents a novel approach based on the design of new heterostructures synthesized from BiOI and magnetic materials, using not only synthetic magnetite, but also magnetic compounds extracted from mine tailings, transforming environmental liabilities in active supporting materials through valorization strategies in line with the circular economy. Through precise control of composition, it was established that a proportion of 6% by mass of the magnetic phase allows the formation of a heterostructure that is highly photocatalytically efficient. These compounds were evaluated using caffeic acid, an organic contaminant of agroindustrial origin, as a target compound. Experiments were carried out under simulated solar radiation for 120 min. Among the materials synthesized, the BiOI/MMA heterostructure, derived from industrial tailing A, displayed an outstanding photodegradation efficiency of over 89.4 ± 0.25%, attributed to an effective separation of photoinduced charges, a broad active surface and a synergic interface interaction between its constituent phases. Furthermore, BiOI/MMA exhibited excellent structural stability and magnetic recovery capacity, which allowed for its reuse through two consecutive cycles without any significant losses to its photocatalytic performance. Thus, this study constitutes a significant contribution to the design of functional photocatalysts derived from industrial tailings, thus promoting clean, technological solutions for the treatment of wastewater and reinforcing the link between environmental remediation and circular economy. Full article

The rising incidence of cancer and the limitations of current therapeutic strategies underscore the urgent need to identify novel bioactive compounds for antitumor drug development. Cyanobacteria are widespread Gram-negative, photoautotrophic prokaryotes that have been recognized as an important source of biologically active secondary metabolites with vast potential for application in the fields of pharmaceutics. The aim of the present study was to analyze the phytochemical composition, antioxidant, and antitumor activities of low-temperature (LT) and high-temperature (HT) aqueous extracts of the cyanobacterium Chroococcus sp. R-10. Extracts were prepared and analyzed for phytochemical composition using UPLC-DAD, and antioxidant activity was tested via multiple assays. Antiproliferative effects were evaluated on human tumor cell lines, and the effects on cell cycle progression studied using flow cytometry. Fluorescence microscopy was employed to examine extract-induced cytomorphological changes in the treated cancer cells. UPLC-DAD analyses showed very similar chromatographic profiles of the extracts and identified glycogen as their main constituent. Both extracts displayed concentration-dependent antioxidant activity, with notable radical scavenging and ferric-reducing capacity. LT extract demonstrated higher phenolic content and antioxidant capacity. Both extracts reduced cell viability, particularly in MCF-7 and MDA-MB-231 breast carcinoma cell lines. Flow cytometry and fluorescent microscopy analyses revealed that the suppressed proliferative activity of the cancer cells was associated with a retardation of cell cycle progression and apoptosis induction. This study identifies Chroococcus sp. R-10 as a promising source of phytochemical compounds with pharmaceutical relevance and provides a rationale for further investigations to identify the primary bioactive constituents and elucidate their mechanisms of anticancer action. Full article

Background/Objectives: Natural products, especially plant metabolites, play a crucial role in drug development and are widely used in medicine, cosmetics, and nutrition. The present review aims to provide a comprehensive overview of the pharmacological profile of Glycyrrhizin (GL), with a specific focus on its molecular targets. Methods: Scientific literature was thoroughly retrieved from reputable databases, including Scopus, Web of Science, and PubMed, up to 30 July 2025. The keywords “glycyrrhizin” and “glycyrrhizic acid” were used to identify relevant references, with a focus on pharmacological applications. Studies on synthetic analogs, non-English publications, non-pharmacological applications, and GL containing crude extracts were largely excluded. Results: Glycyrrhizin, the major bioactive constituent of Glycyrrhiza glabra, exhibits diverse pharmacological activities, including anti-inflammatory, antiviral, hepatoprotective, antitumor, neuroprotective, and immunomodulatory effects. These actions are primarily mediated through the inhibition of high-mobility group box 1 (HMGB1) and the modulation of key signaling pathways, including nuclear factor kappa B (NF-κB), mitogen-activated protein kinase (MAPK), phosphoinositide 3-kinase/protein kinase B (PI3K/Akt), and various cytokine networks. As a result of its therapeutic potential, GL-based formulations, including Stronger Neo-Minophagen C, and GL-rich extracts of G. glabra are commercially available as pharmaceutical preparations and food additives. Conclusions: Despite its therapeutic potential, the clinical application of GL is limited by poor oral bioavailability, metabolic variability, and adverse effects such as pseudoaldosteronism. Hence, careful consideration of pharmacokinetics and safety is essential for translating its therapeutic potential into clinical practice. Full article

Lavender species are economically valuable plants, widely cultivated for their essential oils (EOs), which include sesquiterpenes. The sesquiterpenes caryophyllene and cadinol are major constituents, contributing woody and balsamic notes. However, the specific enzymes catalyzing their formation in lavender have not been elucidated. This study reports the comprehensive functional and structural characterization of two pivotal sesquiterpene synthases from Lavandula angustifolia (lavender): caryophyllene synthase (CARS) and cadinol synthase (CADS). Mutation experiments were performed based on molecular docking predictions, revealing that negatively charged residues interact electrostatically with magnesium ions (Mg²⁺). Both deletion of 1–226 and 1–228 (∆1–226 and ∆1–228) display activity levels equivalent to their corresponding wild-type proteins, while deletions at positions 522–548 and 529–555 significantly enhanced enzyme activity. Additionally, the highest expression levels of CARS were in the flowers under white light for 8 h, while CADS exhibited peak expression in the leaves under white light for 12 h. These findings deepen our understanding of the regulatory mechanisms involved in sesquiterpene biosynthesis in lavender and provide insights for genetic engineering strategies aimed at enhancing EO production. Such advances could also inform the development of cosmetic, personal care, and medicinal products. Full article

Tomato leaves, typically discarded during harvest, are a rich yet underutilized source of bioactive compounds. This study aimed to valorize tomato leaves by optimizing the extraction of their phenolic compounds using a water-based method and response surface methodology. The optimal conditions, notably heating a mixture of 1:50 solid-to-liquid ratio at 71 °C for 29 min, yielded the most total phenolic content and antioxidant activity. The biological activities of the lyophilized tomato leaf extract (TLE) were then assessed. TLE showed dose-dependent antimicrobial activity against Escherichia coli and Candida albicans, but neither against Pseudomonas aeruginosa nor Staphylococcus aureus. In addition, it demonstrated moderate cytotoxicity against MCF-7 breast cancer cells with an IC₅₀ value of 114.5 µg/mL. Interestingly, the extract significantly reduced intracellular reactive oxygen species levels in RAW 264.7 macrophages, supporting its anti-inflammatory potential. LC-MS analysis identified rutin (45.21%), 4-hydroxycoumarin (13.60%), and α-tomatine (12.37%) as the major chemical constituents in TLE, suggesting contributing effects behind the observed bioactivities. These results support the potential of tomato leaf extract as an eco-friendly source for functional ingredients, transforming agricultural waste through green extraction into valuable applications for nutraceuticals and sustainable product development. Full article

Rapid population growth and accelerating urbanization are intensifying the demand for construction materials, particularly concrete, which is predominantly produced with Portland cement and natural aggregates. This reliance imposes substantial environmental burdens through resource depletion and greenhouse gas emissions. Within the framework of sustainable construction, recycled aggregates and industrial by-products such as fly ash, slags, crushed glass, and other secondary raw materials have emerged as viable substitutes in concrete production. At the same time, three-dimensional concrete printing (3DCP) offers opportunities to optimize material use and minimize waste, yet it requires tailored mix designs with controlled rheological and mechanical performance. This review synthesizes current knowledge on the use of recycled construction and demolition waste, industrial by-products, and geopolymers in concrete mixtures for 3D printing applications. Particular attention is given to pozzolanic activity, particle size effects, mechanical strength, rheology, thermal conductivity, and fire resistance of recycled-based composites. The environmental assessment is considered through life-cycle analysis (LCA), emphasizing carbon footprint reduction strategies enabled by recycled constituents and low-clinker formulations. The analysis demonstrates that recycled-based 3D printable concretes can maintain or enhance structural performance while mix-level (cradle-to-gate, A1–A3) LCAs of printable mixes report CO₂ reductions typically in the range of ~20–50% depending on clinker substitution and recycled constituents—with up to ~48% for fine recycled aggregates when accompanied by cement reduction and up to ~62% for mixes with recycled concrete powder, subject to preserved printability. This work highlights both opportunities and challenges, outlining pathways for advancing durable, energy-efficient, and environmentally responsible 3D-printed construction materials. Full article

Background: Shentong Zhuyu Decoction (STZYD) is a traditional Chinese medicine formula that has shown promise in alleviating neuropathic pain (NPP), yet its central mechanisms remain unclear. Methods: We investigated the STZYD effects on NPP using network pharmacology, in vivo assays, and analytical chemistry, focusing on molecular pathways and GABAergic neuronal modulation. Results: Network pharmacology revealed 254 potential STZYD targets enriched in calcium signaling and GABAergic synapse pathways, especially the NMDAR-2B/CaMKII/CREB axis. High-dose STZYD (1.25 g·mL⁻¹) and ifenprodil (6 mg·kg⁻¹) reversed hyperalgesia and anxiety-like behaviors in spared nerve injury (SNI) mice, and microdialysis showed that STZYD and ifenprodil reduced the glutamate, D-serine, aspartate, glycine, and gamma-aminobutyric acid levels in the interpeduncular nucleus (IPN). Immunofluorescence and fiber photometry showed reduced c-Fos expression and suppressed GCaMP signals in IPN GABAergic neurons, with chemogenetic experiments confirming their role in pain modulation. Multimodal molecular biology experiments demonstrated that STZYD and ifenprodil significantly downregulated the GluN2B, p-CaMKII, and p-CREB expressions within the IPN. We identified 145 constituents in STZYD through high-resolution mass spectrometry analysis, among which 40 were absorbed into plasma and 7 were able to cross the blood–brain barrier and accumulate in the IPN. Molecular docking revealed the strong binding of licoricesaponin K2 and senkyunolide F to NMDAR-2B. Conclusions: STZYD exerts dose-dependent antinociceptive effects by modulating IPN GABAergic neuronal activity through the inhibition of the NMDAR-2B-mediated CaMKII/CREB pathway. Full article

The genus Lavandula represents one of the most valuable aromatic and medicinal plants, holding significant economic importance in the pharmaceutical, food, perfumery, and cosmetics industries. Among them, L. multifida is a traditionally used medicinal plant in the Mediterranean region. This work provides a comprehensive review of L. multifida, focusing on its traditional uses, phytochemistry, and pharmacological properties. Unlike conventional lavenders, its essential oil is dominated by phenolic monoterpenes, principally carvacrol, alongside significant concentrations of β-bisabolene, 1,8-cineole, and camphor. This distinct phytochemical profile is further complemented by a rich range of non-volatile constituents, including flavonoids, phenolic acids, and triterpenoids. Pharmacological investigations have validated its broad-spectrum antimicrobial activity, demonstrating efficacy against multidrug-resistant bacterial strains and fungal pathogens through mechanisms such as membrane disruption, metabolic interference, and quorum sensing inhibition. Furthermore, the species exhibits significant antioxidant and anti-inflammatory properties, mediated primarily through radical scavenging, cyclooxygenase inhibition, and cytokine modulation. Owing to its distinct chemistry, specific traditional uses for respiratory and digestive ailments, limited endemic habitat, and underexplored status, L. multifida presents a promising candidate for future research with high potential for novel drug discovery, particularly in antiparasitic and respiratory therapies. This review concludes by identifying key research priorities for L. multifida, including a detailed analysis of its non-volatile compounds, mechanistic elucidation, toxicological assessments, and standardization of extracts. Addressing these gaps is essential to validate its traditional applications and advance its development into evidence-based phytomedicines, adjuvant therapies, and natural agrochemicals. Full article