Search Results (1,290)

Developing plant-based weed-management tools from allelopathy requires evidence that phytotoxicity is both chemically supported and biologically reproducible. This study examined whether the allelopathic activity of Clitoria ternatea L. varies among leaves, stems, and a leaf + stem mixture, and whether such variation is associated with organ-specific chemical traits. Hydroethanolic extracts were characterized by histochemical, phytochemical, and thin-layer chromatographic analyses and tested in vitro on Lactuca sativa L. at 75, 150, and 300 mg L⁻¹. All matrices contained phenols/tannins, flavonoids, and triterpenes/sterols; however, the leaf extract showed the strongest coumarin signal, the presence of saponins, and the richest TLC pattern. These chemical differences were matched by a clear biological gradient, with inhibitory activity ranked as leaf > leaf + stem > stem. At 300 mg L⁻¹, the leaf extract reduced germination to 71%, radicle length to 10.23 mm, and vigor index to 1372, while increasing mean germination time to 5.78 days and yielding the most negative allelopathic response index (−0.663). Overall, the results identify leaves as the main reservoir of phytotoxic metabolites in C. ternatea and support their prospective use in botanical weed-management research. Full article

Oleanolic acid (OA) is a hydrophobic pentacyclic triterpene widely distributed in the plant kingdom and characterized by broad biological activity, including antioxidant, anti-inflammatory, neuroprotective, renoprotective, and anticancer effects. Increasing evidence suggests, however, that many of these actions are better explained not by single molecular targets, but by OA-dependent modulation of an integrated organelle stress network involving mitochondria, the endoplasmic reticulum (ER), autophagy, mitophagy, and apoptosis. This review critically analyzes the available evidence on the effects of OA on the mitochondria–ER–autophagy–apoptosis axis, with particular emphasis on mechanisms governing the transition between cellular adaptation and cell death. The available literature indicates that, in non-cancer models, OA most commonly lowers reactive oxygen species (ROS), stabilizes mitochondrial function, attenuates the ER stress signature, and promotes adaptive autophagy and mitophagy. In contrast, in many cancer models, OA may enhance mitochondrial dysfunction, lower the threshold for mitochondrial apoptosis, and induce autophagy that can be either protective or cytotoxic depending on the biological context. Overall, the current evidence supports a model in which OA acts as a context-dependent modulator of the organelle stress threshold, shifting the balance of an integrated mitochondria–ER–autophagy–apoptosis network rather than functioning as a uniformly cytoprotective or uniformly proapoptotic compound. At the same time, the literature remains heterogeneous with respect to models, doses, exposure times, and markers used, while poor aqueous solubility and limited bioavailability continue to constrain translation. Future studies should therefore integrate analyses of mitochondria, ER, mitochondria–ER contact sites (MERCS), autophagy, apoptosis, pharmacokinetics, formulation, and safety in order to define the true potential of OA as a modulator of biological stress. Full article

The genus Cirsium (family Asteraceae, subfamily Carduoideae) comprises more than 200 species distributed throughout the temperate regions of the Northern Hemisphere. In recent years, particular scientific interest has focused on Cirsium arvense (L.) Scop. (creeping thistle) and Cirsium vulgare (Savi) Ten. (spear thistle). These species are notable for their high content of secondary metabolites and broad biological activity. However, the available data on their phytochemical composition and biological potential remain fragmented. This information is methodologically diverse and scattered across different scientific disciplines, underscoring the need for systematic analysis. In this study, a comprehensive literature review was conducted. Sources included PubMed, Scopus, Web of Science, Google Scholar, and other online databases. The focus was on phytochemical composition and pharmacological activity. Both species contain a wide range of secondary metabolites. These include phenolic acids (chlorogenic, caffeic, and ferulic acids), flavonoids (luteolin, apigenin, kaempferol, quercetin), triterpenoids (lupeol, taraxerol), and phytosterols. C. vulgare generally has higher levels of chlorogenic acid and flavonoid glycosides. In contrast, C. arvense has a greater abundance of triterpenes and steroidal compounds. Pharmacological studies show antioxidant, antimicrobial, hepatoprotective, anti-inflammatory, and cytotoxic activities for both species. Overall, the available data indicate that C. arvense and C. vulgare are promising sources of biologically active compounds with diverse pharmacological potential. Although there are some limitations regarding standardization and the depth of preclinical and clinical validation, the obtained results confirm their relevance for further pharmacological and phytochemical research. Full article

Metabolic dysfunction-associated fatty liver disease (MAFLD) is the most prevalent chronic liver disease worldwide with complex pathogenesis and no approved specific therapy. Siraitia grosvenorii is a widely used medicinal and edible herb, yet its efficacy and underlying mechanisms against MAFLD remain poorly defined. This study explored the protective effects and potential mechanisms of aqueous extract of Siraitia grosvenorii (AESG) on MAFLD. Based on ultra-high-performance liquid chromatography-linear trap quadrupole orbitrap mass spectrometry (UHPLC-LTQ-Orbitrap-MS) analysis, 38 components in AESG were tentatively assigned, with tetracyclic triterpene saponins being the most abundant. In high-fat diet (HFD)-induced MAFLD mice, AESG significantly attenuated body weight gain, reduced plasma total cholesterol (T-CHO) and low-density lipoprotein cholesterol (LDL-C) levels, and dramatically decreased hepatic triglyceride (TG) accumulation from 0.0141 mmol/g in the model group to 0.0063 mmol/g in the low-dose AESG group, corresponding to a reduction of 55.00%. AESG also alleviated plasma alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activities, and improved hepatocyte steatosis. Furthermore, AESG restored HFD-induced gut dysbiosis by enriching beneficial bacteria including Akkermansia and suppressing harmful bacteria such as Ruminococcus. In free fatty acids (FFA) stimulated HepG2 cells, AESG suppressed de novo lipogenesis via downregulating Fatty Acid Synthase (FASN), Acetyl-CoA Carboxylase (ACC) and Sterol Regulatory Element-Binding Protein 1c (SREBP1c), and enhanced antioxidant capacity via activating the Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2)/Heme Oxygenase 1 (HO-1)/Sirtuin 1 (SIRT1) pathway, thereby attenuating lipid accumulation and oxidative stress. In conclusion, AESG ameliorates MAFLD by inhibiting lipogenesis, improving oxidative stress, and regulating gut microbiota. These findings support Siraitia grosvenorii as a promising natural dietary intervention for MAFLD prevention and adjuvant therapy. Full article

This study evaluated olive leaves from three cultivars (Hojiblanca, Picual, and Arbequina) and olive pomace as complementary sources of bioactive compounds, comparing ultrasound-assisted extraction using organic solvents (UAE) with supercritical CO₂ extraction (SFE). The aim was to determine how the plant matrix and extraction method influence phytochemical composition and functional properties, including antioxidant and antimicrobial activity. The results showed that both factors strongly affected extract composition and bioactivity. UAE favored the recovery of phenolic compounds associated with antioxidant activity, particularly in leaf extracts, while SFE promoted a distinct compositional profile enriched in flavonoids and lipophilic constituents, especially in olive pomace. Multivariate analysis confirmed a clear differentiation between matrices and extraction methods. Leaf extracts from Picual and Arbequina were mainly associated with phenolic compounds linked to antioxidant activity, including luteolin, ethyl vanillin, tyrosol, and isorhamnetin-3-O-glucoside. In contrast, olive pomace extracts were more strongly associated with flavonoids and lipophilic metabolites, such as triterpenes (oleanolic, maslinic, and ursolic acids) and lipid derivatives (oleic acid and lauric isopropanolamide). These compositional differences were reflected in biological activity: UAE extracts showed higher antioxidant activity, whereas SFE extracts, enriched in lipophilic and triterpenic compounds, exhibited stronger antimicrobial effects against Pseudomonas savastanoi and Hanseniaspora sp. Overall, these findings demonstrate that extraction-driven selectivity enables the production of olive-derived extracts with targeted functionalities, with UAE favoring antioxidant-oriented extracts and SFE promoting extracts enriched in lipophilic compounds with antimicrobial potential, particularly from olive pomace. Full article

Oyamel forest, Abies religiosa (Kunth) Schltdl. et Cham., is a high-mountain ecosystem that contains abundant biodiversity, contributes to supporting traditional medicine, and represents a reservoir of medicinal plants. Despite this medicinal relevance, the potential of the flora of the Mexican Oyamel forest from Santuario del Agua Presa Corral de Piedra (SAPCP), Mexico, has been scarcely studied. This review focused on identifying the flora of the SAPCP which has been reported as medicinal resource in the literature through the recovery of ethnomedicinal uses and their proven pharmacological effects. In addition, phytochemical reports of the SAPCP medicinal flora and their pharmacological activities were integrated and analyzed to estimate their medicinal potential. The results showed that the SAPCP forest represents an important source of medicinal plants, with 39% of the total species reporting at least one ethnomedicinal use belonging to different taxonomic families, but mainly included Asteraceae, Lamiaceae, Rosaceae, and Solanaceae. The most commonly observed ethnomedicinal uses among all the species were against inflammation, infections, diarrhea, and diabetes, while antioxidant, antidiabetic, and anti-inflammatory effects were predominantly proven as pharmacological effects. The phytochemical results revealed a great diversity of secondary metabolites, although flavonoids, phenolic acids, and triterpenes were observed in a major number of species, many of which have been proven to exert anti-inflammatory, antidiabetic, and antibacterial effects through several action mechanisms. In conclusion, these results highlight the importance of sustainable management and the conservation of forest species, as they provide a reservoir of medicinal species that produce bioactive metabolites. Full article

Loquat (Eriobotrya japonica Lindl.) is a subtropical evergreen fruit tree that accumulates abundant bioactive triterpene compounds with diverse pharmaceutical activities. Its leaves have been used in traditional Chinese medicine for over 1000 years. Methyl jasmonate (MeJA) is a conserved elicitor that stimulates plant secondary metabolism. However, the regulatory mechanisms of terpenoid biosynthesis after MeJA treatment in loquat callus remain largely unknown. In this study, we employed an integrated targeted metabolomic and transcriptomic approach to investigate the effect of exogenous MeJA on terpenoid biosynthesis in loquat callus. In total, 131 terpenoid compounds were detected, including 112 triterpenes, six triterpene saponins, seven diterpenoids, three sesquiterpenoids and three monoterpenoids. After MeJA treatment, a total of 55 and 33 differential metabolites (DEMs) were identified at 24 h and 48 h, respectively. Most DEMs were triterpene compounds, displaying increased accumulation. Among them, ursolic acid showed the highest accumulation at 24 h, and betulinic acid was most abundant at 48 h. Meanwhile, transcriptome analysis showed significant upregulation of terpenoid biosynthesis genes, including EjFPSs, EjSQEs, EjOSC2 and EjCYP716A2, as well as genes related to jasmonic acid (JA)-mediated signaling and JA-responsive genes in loquat callus treated with MeJA. Overall, these results provide a deeper understanding of the mechanism of terpenoid accumulation in loquat callus induced by MeJA and establish a theoretical basis for utilizing plant cell culture techniques to achieve production of the valuable terpenoid metabolites that are applied in the functional food and pharmacological industries. Full article

This review examines the historical development, ethnopharmacology, traditional applications, phytochemistry, and pharmacological attributes of Atractylodis Rhizoma (AR). Data were collected from a range of electronic databases, academic libraries, and classical literature. In China, AR is highly valued for its medicinal properties. Research has identified 327 compounds, including sesquiterpenes, triterpenes, flavonoids, and phenolics, which contribute to its diverse pharmacological activities, such as antimicrobial, anti-inflammatory, antioxidant, hepatoprotective, and neuroprotective effects. AR is particularly effective in treating modern gastrointestinal disorders and influenza. As a traditional herb with a rich historical background, AR exhibits significant therapeutic potential. This review aims to correlate its active components with its primary therapeutic effects and highlight existing research gaps. Current studies primarily focus on extraction methods and pharmacodynamics. Future research should employ multi-omics and molecular biology techniques to further elucidate active components and their targets, while also addressing the challenge of low bioavailability. Full article

This study investigates the phytochemical composition and biological activity of eight Thymus species distributed in Bulgaria, with a focus on taxa from section Hyphodromi. High-performance liquid chromatography (HPLC) and gas chromatography–mass spectrometry (GC–MS) were used to characterize the methanolic (MeOH) and diethyl ether (Et₂O) extracts, respectively. MeOH extracts revealed high concentrations of phenolic acids, particularly rosmarinic acid, salicylic acid, and flavonoid glycosides, with T. atticus, T. jalasianus, and T. leucotrichus showing the most diverse profiles. Et₂O extracts were dominated by triterpenic acids (ursolic and oleanolic) and monoterpenes such as thymol and carvacrol, especially in T. zygioides and T. leucotrichus. All MeOH extracts exhibited significant antioxidant activity in the DPPH assay (IC₅₀ < 50 µg/mL), with T. jalasianus and T. atticus demonstrating the strongest effects. Radical scavenging potential generally followed the trend of total phenolic content. Moderate acetylcholinesterase-inhibitory activity was observed only in T. zygioides and T. leucotrichus. The study reports for the first time data on the biological activity and metabolic composition of extracts from endemic and rare species and from the species of Bulgarian origin. The results provide new data on the phytochemical composition and in vitro antioxidant and acetylcholinesterase-inhibitory activities of selected Thymus species, contributing to the characterization of their overall in vitro biochemical profiles. Full article

This study evaluated the effects of the dietary administration of a glycosylated form of active vitamin D (calcitriol, 1,25(OH)₂D₃) combined with ursolic acid (UA) and oleanolic acid (OA) triterpenes on sow health and productivity. Twenty-four third-parity Landrace × Large White sows were allocated at day 108 of gestation into three groups: a control group receiving 1800 IU/kg of vitamin D₃, and two treatment groups receiving the control diet supplemented with either 0.64 µg/kg (ACTD1) or 0.96 µg/kg (ACTD2) of glycosylated 1,25(OH)₂D₃ plus 140 or 210 µg/kg of UA + OA (4:1 ratio), respectively. Diets were administered from late gestation through the end of lactation. Farrowing duration, sow body weight, backfat thickness, and litter growth were recorded. Blood samples collected at key physiological stages were analyzed for pro-inflammatory cytokines, mineral homeostasis, endocrine markers, and serum proteome. Farrowing time was reduced in both treatment groups compared with the control (p < 0.05). Treated sows exhibited lower backfat thickness at the end of lactation and improved litter weights at farrowing, after cross-fostering, and at weaning (p < 0.05). Plasma pro-inflammatory cytokines (TNF-α, IL-1α, and IL-1β) were reduced at the end of lactation in ACTD1 and ACTD2 sows, with TNF-α and IL-1β already decreased after farrowing (p < 0.05). Treated sows also displayed decreased plasma parathormone concentrations at the end of lactation, along with increased circulating 1,25(OH)₂D₃ and calcium concentrations after farrowing and at lactation end (p < 0.05), while plasma phosphate levels remained unchanged. Proteomic analysis supported the systemic availability of the supplemented compounds and their involvement in metabolic and inflammatory pathways rather than calcium transport or vitamin D binding mechanisms. Overall, this nutritional strategy influenced the immune modulation while maintaining mineral homeostasis via modest endocrine adaptations. Larger-scale trials are warranted to confirm these results and to evaluate their practical applicability under commercial production conditions. Full article

Background/Objectives: Thrombin, a serine protease central to coagulation and platelet activation, remains an important target for the development of safer and more effective antithrombotic agents. Naturally derived pentacyclic triterpenoids, such as betulinic acid and its acetylated derivatives, 3β-acetoxybetulinic acid, exhibit promising antiplatelet aggregation activity in validated in vitro and ex vivo assays; however, the molecular determinants underlying their direct thrombin inhibition remain unexplored. Results: Docking and MM/GBSA analyses revealed that Baa exhibits the strongest binding affinity (ΔG = −29.58 ± 2.97 kcal/mol), exceeding those of Ba (−20.94 ± 5.81 kcal/mol) and Asp (−18.87 ± 4.18 kcal/mol). Baa forms a highly persistent hydrogen bond with Trp96 (95.5% occupancy) and extensive hydrophobic contacts with Trp215, Leu99, Ile174, and Tyr60A residues defining thrombin’s aryl-binding pocket. MD trajectories demonstrated that Baa binding reduced solvent-accessible surface area (SASA) and residue fluctuations, indicating enhanced structural compaction and stability. In contrast, Ba exhibited weaker, transient hydrogen bonding, while Asp bound primarily near the catalytic triad. The triterpenes exhibit limited oral bioavailability, free PAINS alerts, favourable permeability and metabolic stability. Conclusions: Acetylation at C-3 (acetoxy substitution) substantially enhances thrombin binding via cooperative hydrogen bonding and van der Waals stabilisation, explaining the superior experimental inhibitory potency of Baa. These findings provide a mechanistic framework for structure-guided optimisation of triterpenoid-based thrombin inhibitors and support their further experimental development. Methods: In this study, molecular docking, molecular dynamics (MD) simulations (400 ns), and MM/GBSA free energy analyses were employed to elucidate the binding mechanisms of 3β-acetoxybetulinic acid (Baa), betulinic acid (Ba), and aspirin (Asp) within the thrombin receptor active site. The simulations were explicitly grounded in previously reported chromogenic antithrombin assays and platelet aggregation studies and were designed to mechanistically rationalise the experimentally observed inhibitory potency. Full article

Background/Objectives: Commiphora gileadensis (Balm of Gilead) is an aromatic medicinal plant with a history of traditional use in ancient and Arabic medicine. It has been used traditionally to treat inflammation, infections, and wounds. Despite its long-standing cultural and economic importance, modern pharmacological validation requires a comprehensive synthesis of current scientific data. This review aims to provide a thorough comparative summary of the phytochemical composition and biological activities of its diverse products. Methods: An updated literature search was conducted using databases such as ScienceDirect, PubMed, Scopus, and Google Scholar, covering publications from approximately 2000 to 2025. The review included English-language peer-reviewed articles, books, and reports providing phytochemical analyses or biological evaluations. Data were manually extracted and categorized by plant parts (resin, leaves, bark, stems), major constituents, and specific pharmacological activities. Results: The review identified ten diverse chemical groups, mainly terpenoids (mono-, sesqui-, di-, and triterpenes) and flavonoids. Other remarkable classes included phenolic acids, phytosterols, lignans, coumarins, and fatty acids. However, the essential oil chemical profile is highly variable, influenced by geographical origin and preparation technique. Pharmacological studies demonstrated a wide spectrum of bioactivities, in particular antioxidant, anti-inflammatory, antimicrobial, anticancer, antidiabetic, and wound-healing properties. Toxicological studies classified the plant as generally non-toxic; however, there is a notable lack of clinical and pharmacokinetic data. Conclusions:C. gileadensis possesses a rich and diverse secondary metabolite profile, validating its traditional ethnobotanical applications. Future research should prioritize pre-clinical and clinical trials to establish its safety, bioavailability, and metabolic fate for its successful integration into modern medicine. Full article

Background/Objectives: Cancer has been associated with significant morbidity and mortality worldwide, particularly related to chemotherapy resistance. Therefore, it is essential to investigate alternative sources of non-toxic antitumor compounds. The cactus Lophocereus marginatus is native to Mexico and is commonly used to treat gastrointestinal infections and diabetes in traditional medicine. Methods: The in vitro antitumor activity of L. marginatus extract fractions against murine L5178Y-R lymphoma cells was evaluated. The crude extract and its solvent-derived fractions were evaluated for cytotoxicity, selectivity, and hemolytic activity. Results: The crude extract exhibited an IC₅₀ of 9.09 μg/mL, demonstrating a high selectivity index (SI: 330.03), with no hemolytic activity observed at 1000 μg/mL. The LM-HP, LM-CP, and LM-MP partitions showed varying IC₅₀ values (6.74, 7.93, and 45.38 μg/mL, respectively) and selectivity indices of 445.1, 378.31, and 66.1, respectively. Only LM-HP induced hemolysis at 200 μg/mL. The most promising fraction, CP-F8, exhibited an IC₅₀ of 11.2 μg/mL, high selectivity index (354.29), and antioxidant activity, without hemolytic effects. Phytochemical analysis of CP-F8 identified phenolic compounds, triterpenes, and sterols, which are known for their anti-cancer and anti-inflammatory properties. In vivo tests showed no significant liver damage or changes in body weight, indicating the safety of CP-F8. Conclusions: These results suggest that CP-F8 is a promising antitumor candidate with selective cytotoxicity and minimal toxicity to normal cells. Full article

In the intensive livestock farming industry, weaned piglets are highly prone to renal injury triggered by weaning stress, pathogen infection, and antibiotic abuse. This injury induces metabolic disorders and immunosuppression, severely restricting production efficiency. As a natural pentacyclic triterpene, betulinic acid (BA) exhibits notable biological activities, particularly in anti-inflammatory and antioxidant activities. However, its preventive potential against renal injury in piglets and the underlying mechanisms remain unclear. In this study, BA was administered as a long-term dietary pretreatment prior to lipopolysaccharide (LPS) challenge to evaluate its protective role in a preventive model of renal inflammatory injury in weaned piglets. BA pretreatment significantly mitigated pathological lesions, including renal tubular epithelial cell shedding and interstitial congestion, reduced the renal index, and decreased the concentrations of renal injury markers and serum UREA. In addition, BA pretreatment mitigated the renal oxidative stress and inflammatory injury induced by LPS in piglets. Molecular analyses showed that BA pretreatment was associated with decreased expression of key markers involved in apoptosis, necroptosis, and pyroptosis in renal tissue. Furthermore, protein–protein interaction analysis suggested potential associations between the HMGB1/TLR4/NF-κB signaling pathway and PANoptosis-related processes, providing exploratory and hypothesis-generating support for the proposed regulatory network. Collectively, these findings suggest that dietary BA pretreatment exerts a preventive effect against LPS-induced renal inflammatory injury in weaned piglets, potentially through modulation of HMGB1/TLR4/NF-κB-associated PANoptosis-related pathways, providing a theoretical basis for its application in livestock production. Full article

The increasing antimicrobial resistance of T. pyogenes, one of the principal pathogens associated with endometritis, presents a formidable challenge in veterinary medicine. Astragaloside IV (AS-IV) is a triterpene saponin compound isolated from the traditional Chinese medicine Astragalus membranaceus. While recognized as the primary bioactive constituent of Astragalus membranaceus with diverse pharmacological properties, its potential to counteract T. pyogenes-induced endometritis has yet to be elucidated. In the current study, T. pyogenes infection models were successfully established in both mouse uteri and cultured goat endometrial epithelial cells (gEECs). Integrating histopathology, molecular biology and transcriptomic technology, this study characterized the multifaceted biological effects of AS-IV. Transcriptomic analysis indicates that the regulatory effects of AS-IV on T. pyogenes-induced infection are primarily associated with the enrichment of signaling pathways related to inflammation, apoptosis, and oxidative stress. Subsequent validation demonstrated that AS-IV treatment effectively alleviated T. pyogenes-induced endometrial damage by suppressing inflammation, apoptosis, and oxidative stress. These effects were mediated through Nrf2 and its downstream target HO-1, a mechanism further confirmed by the loss of protection upon Nrf2 inhibition. In summary, AS-IV protects the endometrium against T. pyogenes-induced inflammatory and oxidative damage by activating the Nrf2/HO-1 signaling pathway. Full article