Search Results (1,499)

Objective: In this study, the heat shock transcription factor (HSF) gene family in Ganoderma lucidum was systematically characterized. Using genomic and transcriptomic data, we identified HSF family members and investigated their expression patterns under temperature stress and their potential regulatory roles in triterpenoid biosynthesis. Methods: A genome-wide identification of HSF genes in G. lucidum was performed using bioinformatic approaches. A phylogenetic tree was constructed, and conserved motifs, gene structures, and protein tertiary structures were predicted. The relative expression levels of HSF genes and key mevalonate (MVA) pathway enzyme genes were examined by a quantitative real-time reverse transcription polymerase chain reaction (qRT-PCR) in mycelia subjected to temperature stress. Total triterpenoid content in fermented mycelia under temperature stress was determined using the vanillin–glacial acetic acid method. Results: Eight HSF family members (GlHSF1–GlHSF8) were identified in G. lucidum. Phylogenetic analysis revealed that GlHSF proteins were closely related to PoHSF from Pleurotus ostreatus. Transcriptomic analysis showed that HSF genes exhibited relatively high expression levels during the mature stage while being barely expressed during the mycelial stage. Under heat stress (42 °C), most GlHSF genes peaked at 18 h, with GlHSF2 showing the most pronounced response (approximately 13-fold upregulation). Downstream MVA pathway genes, including IDI, PMK, and MVD, were significantly upregulated at 24 h, whereas the upstream rate-limiting enzyme gene HMGR was continuously suppressed. Despite HMGR suppression, total triterpenoid content did not decrease significantly, likely due to the activation of downstream genes. Under cold stress (14 °C), the expression of most GlHSF and MVA pathway genes decreased, accompanied by a significant reduction in total triterpenoid content. Conclusions: The HSF gene family was identified in the G. lucidum genome. Based on expression analysis, GlHSF2 showed the strongest response under heat stress, and its expression peak was correlated with the sequential activation of downstream genes in the MVA pathway. This suggests that GlHSF2 acts as a potential key regulatory node, differentially regulating upstream and downstream MVA pathway genes to influence triterpenoid biosynthesis under heat stress. These findings provide a theoretical basis for future research on the biological functions of GlHSF homeostasis. Full article

Elaeocarpus sylvestris (Lour.) Poir., an evergreen tree native to East and Southeast Asia, has gained increasing scientific attention owing to its broad pharmacological properties. Traditionally used in East Asian medicine to treat inflammation, fever, and infectious diseases, modern research has revealed diverse bioactivities, including potent antioxidant, anti-inflammatory, antiviral, anticancer, antidiabetic, and immunomodulatory effects. This therapeutic potential is primarily attributed to its rich phytochemical composition, particularly polyphenols such as geraniin, 1,2,3,4,6-penta-O-galloyl-β-D-glucose and quercetin. This review particularly focuses on the chemistry of E. sylvestris, summarizing structurally elucidated compounds, including hydrolysable tannins, flavonoids, and triterpenoids, along with recent insights into the structure–activity relationships that underpin these antiviral, antioxidant, and anticancer activities. Recent studies have demonstrated substantial antiviral efficacy of E. sylvestris extracts and isolated compounds against major human pathogens, including herpesviruses, influenza A virus, and SARS-CoV-2, supported by in silico, in vitro, in vivo, and early-phase clinical evaluations. Its cosmeceutical applications, including antioxidant, skin-whitening, and blue-light protective effects, further highlight its multifunctional potential. To our knowledge, this is the first comprehensive review summarizing the phytochemistry, pharmacological activities, therapeutic potential, and cosmeceutical applications of E. sylvestris. Despite these promising findings, challenges remain in elucidating precise molecular mechanisms, pharmacokinetics, and clinical validation. This review identifies current research gaps and future directions necessary to advance E. sylvestris as a scientifically validated natural therapeutic resource. Full article

At present, the characteristics of key enzyme genes in the upstream pathway for triterpenoid saponin biosynthesis in P. grandiflorum, as well as their expression patterns over the growth duration, have not been systematically analyzed. This study, at the whole-genome level, conducts the first bioinformatics and expression analyses of the SS and SE gene families in P. grandiflorum. Four PgSS and seven PgSE genes were identified and distributed across six chromosomes. Members within the same subfamily exhibited highly conserved sequences and structures, while distinct structural divergence was observed between different subfamilies. Phylogenetic analysis showed that PgSS and PgSE genes were closely related to those of dicotyledons such as Panax ginseng and Polygala tenuifolia, suggesting high evolutionary conservation. Promoter analysis revealed abundant light- and hormone-responsive elements and MYB/MYC binding sites, indicating regulation by multiple signals. Protein secondary structures were dominated by the Alpha helix and were structurally stable. Quantitative real-time polymerase chain reaction (qPCR) demonstrated that expression levels of PgSS and PgSE in one-year-old Platycodonis Radix were significantly higher than in perennial Platycodonis Radix, especially for the PgSE family. This study characterized the basic biological features and growth-stage-dependent expression patterns of the SS and SE gene families in P. grandiflorum. The results identify key candidate genes and molecular targets for regulating triterpenoid saponin biosynthesis, and provide data supporting quality improvement and active metabolite research in this medicinal plant. Full article

Leaves of Actinidia chinensis Planch. var. deliciosa (A.Chev.) A.Chev. (A. deliciosa) represent agro-industrial byproducts with potential for valorization. The present study evaluated the metabolomics profiling, cytotoxicity, genotoxicity, and antigenotoxicity of the methanolic extract of A. deliciosa leaves. The metabolomics profiling was determined using an untargeted metabolomic approach employing UPLC-HRMS. Cytotoxicity, genotoxicity, and antigenotoxicity were assessed in Chinese hamster ovary K1 (CHO-K1) cells using the in vitro cytokinesis-block micronucleus (CBMN) assay. The metabolic profile of A. deliciosa leaf extracts revealed the presence of three major classes of secondary/specialized metabolites: proanthocyanidins, flavonols, and triterpenoid saponins. Medium-polar metabolites were monomeric fla-van-3-ols, such as (+)-catechin and (−)-epicatechin, oligomeric procyanidins and prodelphinidins, and flavonols. Certain glycosylated flavonols and their derivatives, such as myricetin, quercetin, and kaempferol. Low-polarity metabolites were characterized by low-polarity triterpenoids such as maslinic, corosolic, oleanolic, and ursolic acids. At concentrations of 37.5, 75, and 150 µg/mL, the extract did not significantly increase micronuclei frequency compared to untreated control cells, indicating an absence of genotoxic potential. Moreover, co-treatment of CHO-K1 cells with the extract and mitomycin C (MMC) at 0.025 µg/mL resulted in a significant reduction in micronuclei formation induced by MMC at concentrations of 75 and 150 µg/mL, suggesting antigenotoxic activity likely associated with the phytochemical constituents presented in the extract. Full article

Natural products from plants have played an important role in cancer and neurodegenerative diseases. In this context, the root bark of Maytenus chiapensis (Celastraceae) was investigated to examine its chemical constituents and potential biological activities. Chromatographic separation of the root bark extract yielded a new Diels–Alder adduct (morenine) formed by a triterpenophenolic moiety derived from tingenone and a bicyclic guaiane-type sesquiterpene linked through a 1,4-dioxane bridge. In addition, eight previously reported Diels–Alder adducts—retusonine and cheiloclines A–D and F–H—were isolated, together with their biosynthetic precursors, the quinone-methide triterpenoids (QMTs) pristimerin and tingenone. Structural elucidation was achieved through detailed 1D and 2D NMR spectroscopic analyses. The adducts were tested for cytotoxicity against six cancer cell lines (A549, SW1573, MIA PaCa-2, T-47D, HeLa, and WiDr cell lines), showing moderate-to-low activity compared with their precursors. Continuous live cell imaging identified apoptosis and vacuole formation as the main modes of action of pristimerin in SW1573 cells. Moreover, acetylcholinesterase inhibition assays revealed that cheiloclines B–D, F, and H exhibited up to 50% inhibition. These findings reinforce the potential of Celastraceae species as a source of unique and complex compounds and enhance our understanding of their therapeutic potential. 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

Ginsenoside Rd, a protopanaxadiol (PPD)-type tetracyclic triterpenoid saponin, has emerged as a promising bioactive constituent for multitarget therapeutic interventions. However, its natural abundance in the source plant is extremely low, making direct extraction both costly and inefficient. This review systematically summarizes the latest research progress on regioselective biotransformation strategies for Rd production since 2022. Furthermore, it comprehensively reviews recent advances in the diverse pharmacological activities of Rd. Beyond its well-recognized neuroprotective effects against neurological disorders including Alzheimer’s disease and Parkinson’s disease, we also highlight its antitumor activity and multitarget protective effects in liver diseases. This review provides a theoretical basis for developing Rd as a high-value nutraceutical and therapeutic candidate for systemic health. Full article

Geopropolis, a complex natural product composed of propolis, wax, plant resins, and soil produced by Meliponine (stingless) bees, has traditionally been used for its therapeutic properties. Its chemically diverse composition and broad biological activities have recently attracted growing scientific interest. In this study, we characterized the physicochemical and immunomodulatory properties of a hydroalcoholic extract of geopropolis (HEG) from Melipona quadrifasciata (Mandaçaia). Physicochemical characteristics were determined by measuring moisture, ash, and wax content, and its bioactive constituents were identified by GC–MS. THP-1-derived macrophages were exposed to increasing HEG concentrations to assess cytotoxicity, and two sublethal doses were selected for immunomodulatory assays with or without LPS stimulation. Cytokine and chemokine secretion were quantified by CBA, and the expression of key immunoregulatory and angiogenic genes was evaluated by RT-qPCR. Chemical profiling revealed a high wax content and a predominance of di- and triterpenoids, largely derived from coniferous sources. In mccrophages stimulated with LPS, HEG at 31.25 and 62.50 µg/mL significantly reduced the secretion of pro-inflammatory mediators (IL-6, CCL2, CCL5, CXCL9, and CXCL10) while preserving cell viability. In unstimulated macrophages, HEG upregulated the expression of genes VEGFA and TGFB1 as well as the protein CXCL8, all of them associated with angiogenesis and tissue repair. These findings demonstrate that M. quadrifasciata geopropolis extract modulates macrophage activity, promoting a shift toward a reparative phenotype that integrates inflammatory resolution with pro-healing effects. These results underscore its pharmacological potential as a terpenoid-rich natural product with complementary anti-inflammatory and regenerative activities. Full article

Natural deep eutectic solvents (NADESs) have emerged as promising green alternatives to conventional solvents for the extraction of bioactive compounds from plant materials. In this study, eight natural deep eutectic solvents were synthesized and evaluated for their efficiency in extracting betulin from birch bark. Extraction yield was assessed using high-performance liquid chromatography with ultraviolet detection. Among the tested systems, N3 (choline chloride and urea in a 1:1 molar) and N4 (choline chloride and fructose in a 1:1 molar) were the most effective, yielding 101.26 ± 0.03 and 243.32 ± 0.26 mg betulin per gram of dry extract, respectively. Fourier transform infrared spectroscopy analysis confirmed the structural similarity of the N4 extract to pure betulin. In addition to increased extraction performance, the N4 extract demonstrated the greatest antioxidant activity (DPPH (1,1-diphenyl-2-picrylhydrazyl): 63% and ABTS (2,2′-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid)): 97% inhibition) and total phenolic content (12.12 mg GAE/g extract), and betulin yield was strongly correlated with total phenolic content (TPC) and antioxidant activity (FRAP (ferric ion reducing antioxidant power), DPPH, and ABTS), indicating the preservation of bioactivity. These findings underscore the potential of NADESs as sustainable solvents for the extraction of bioactive compounds from birch bark, supporting greener extraction technologies for biomass valorization and natural product processing. Full article

Traditional Chinese prescriptions are characterized by complex chemical constituents and wide variations in constituent content, which pose a substantial challenge to their comprehensive characterization. As a classic traditional Chinese prescription known for its heat-clearing and detoxifying properties, Huangqintang Decoction (HQD) is composed of Scutellariae Radix, Paeoniae Radix Rubra, Glycyrrhizae Radix et Rhizoma, and Jujubae Fructus. In this study, we developed an off-line two-dimensional liquid chromatography that addressed the limitations of traditional analysis of unfractionated extracts, such as restricted peak capacity, which often obscured trace components. By coupling with ultra-high performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOF/MS), this study successfully performed rapid identification or characterization of the complete chemical profile of HQD. Notably, beyond high-throughput identification, this approach leveraged characteristic fragment ions and reversed-phase chromatographic behaviors to differentiate some isomers of flavonoid glycosides and triterpenoid saponins, demonstrating its depth in structural identification. Flavonoid glycoside isomers were distinguished by diagnostic neutral losses, while flavanones and chalcones were characterized by retro-Diels–Alder (RDA) and β-rearrangement, respectively. Isomers of triterpenoid saponins were inferred from aglycone-specific pathways alongside RDA cleavages. Ultimately, a total of 192 compounds were identified, including 88 flavonoids, 80 triterpenoids, 7 monoterpene glycosides, 3 fatty acid amides, 3 phenylethanoid glycosides, 4 coumarins, 3 saccharides, 1 organic acid, and 3 others. This study demonstrated that the off-line two-dimensional liquid chromatography analysis strategy significantly enhanced chromatographic resolution and expanded the coverage of trace components. It presented an effective strategy for comprehensive compound identification in complex traditional Chinese medicine prescriptions. Full article

Ganoderma mushrooms produce bioactive metabolites with therapeutic potential, yet their tissue-level distribution is not well characterized. This study quantified triterpenoids, β-glucans, and phenolics across six anatomical sections of fruiting bodies from five wild Ganoderma species. Twenty-six triterpenoids were identified. Laccate species showed thicker context tissue enriched in ganoderic and lucidenic acids, resembling the chemotype of G. lucidum. Matte species displayed greater triterpenoid diversity, including elfvingic, applanoxidic, and ganoderenic analogues. Maximum contents reached 3.5% triterpenoids, 34.3% β-glucans, 20.8 mg TE·g⁻¹ (ABTS), 175.2 µmol Fe²⁺·g⁻¹ (FRAP), and 23.5 mg GAE·g⁻¹ phenolics. Triterpenoids and phenolics were highest in outer cap tissues, while β-glucans predominated in context layers. These patterns reflect functional tissue roles and developmental variation. The tissue distribution of metabolites in wild Ganoderma presented here identifies surface tissues as a major source of triterpenoids and phenolics, and internal tissues as a source of β-glucans. These traits represent selection targets for extraction and selective breeding to produce strains with thicker context tissue and higher triterpenoid and β-glucan yields. Full article

The effects of static magnetic field (SMF) treatment on the solid-state culture of Sanghuangporus vaninii (SV) were investigated to enhance metabolite production and bioactivity. SMF parameters including intensity, exposure duration, and temperature were optimized, and treatment at 4 mT for 2 h per day produced the most pronounced effects, increasing total flavonoid (TFC), polyphenol (TPC), and triterpenoid (TTC) contents by 61–438% compared with the control. Ultrasonic extraction and semi-preparative chromatography enabled the isolation of three key compounds: D-(+)-trehalose (1), 5,7-dihydroxy-3,4′-dimethoxyflavone (2), and pinolenic acid (3), all of which were elevated following SMF treatment. Importantly, SMF exposure was associated with enhanced inhibitory activities against enzymes relevant to chronic metabolic disorders. The overall inhibitory activities against α-amylase, α-glucosidase, pancreatic lipase, and xanthine oxidase increased by 6–28% compared with the control, reaching a maximum inhibition of 97.60 ± 0.17%. Preliminary in vitro screening at 100 μg/mL showed that compounds 1 and 2 inhibited both α-amylase and α-glucosidase, whereas compound 3 selectively inhibited pancreatic lipase. Subsequent IC₅₀ analysis confirmed that compound 2 under SMF treatment exhibited inhibitory activity comparable to acarbose against α-amylase (45.62 μg/mL vs. 52.18 μg/mL) and α-glucosidase (38.74 μg/mL vs. 35.42 μg/mL). In addition, compound 3 showed moderate inhibition of pancreatic lipase with an IC₅₀ value of 42.15 μg/mL. These findings suggest that SMF treatment may enhance metabolite production and in vitro enzyme inhibitory activity in S. vaninii. However, these results are limited to in vitro assays, and further studies including cellular and in vivo validation, toxicity assessment, and pharmacokinetic evaluation, are required before any therapeutic or industrial applications can be considered. Full article

For decades, the pharmacological identity of Panax ginseng has been primarily attributed to triterpenoid saponins known as ginsenosides. However, accumulating evidence indicates that ginseng also contains a structurally distinct lipid–protein complex, termed gintonin, enriched in lysophosphatidic acid (LPA) species. Unlike ginsenosides, which predominantly exert modulatory effects on membrane dynamics and intracellular kinase pathways, gintonin directly activates LPA G protein-coupled receptors (GPCRs), thereby inducing rapid phospholipase C (PLC) activation and intracellular Ca²⁺ mobilization. Biochemical analyses have identified major LPA species within the gintonin fraction, including C16:0, C18:0, and C18:1, stabilized within a proteinaceous matrix that may influence receptor engagement kinetics. Pharmacological studies demonstrate that gintonin preferentially activates LPA₁ and LPA₃ receptor subtypes, triggering downstream signaling cascades involving MAPK, PI3K/Akt, and Rho pathways. These receptor-mediated effects occur on a rapid temporal scale, distinguishing gintonin from the slower transcriptional and kinase-modulating actions of ginsenosides. In this review, we synthesize current evidence regarding the chemical architecture, receptor pharmacology, and signaling dynamics of gintonin and propose a dual signaling framework in which steroid-like saponins and lipid GPCR ligands represent complementary molecular axes within P. ginseng. Recognition of this layered signaling organization refines the molecular understanding of ginseng biology and highlights gintonin as a unique plant-derived GPCR ligand system. Full article

The aim of this study was to evaluate the potential of selected agri-food by-products—apple pomace extract from Malus domestica cv. ‘Grochówka’ and Roman chamomile (Chamaemelum nobile L.) hydrolate—as functional, sustainable ingredients for cosmetic applications. The work focused on their chemical composition, biological activity, formulation performance, and in vivo effects on skin condition. Volatile compounds, phenolic acids, and triterpenoids were analyzed by GC–MS, while total phenolic content, antioxidant capacity, and enzyme inhibitory activity were evaluated in vitro. An oil-in-water emulsion containing the by-products was formulated and, in a 14-day split-face study, assessed for its effects on skin hydration, elasticity, inflammation, sensitivity, pore visibility, and melanin index. Biochemical analyses have shown that chamomile hydrolate is characterized by very low antioxidant activity (DPPH 5.0 ± 1.25%, FRAP 0%) and weak protease inhibition (9.70 ± 1.84%). In contrast, apple extract contained a significant amount of polyphenols (23.94 ± 0.3 mg GAE/g) and showed strong antioxidant properties (DPPH 79.4 ± 2.12%, FRAP 70.56 ± 2.23%; IC₅₀ = 21.5 ± 0.196 mg/mL), which confirms the dominant role of phenolic compounds in its biological activity. This extract also demonstrated significant protease inhibition (60.88 ± 2.35%; IC₅₀ = 15.02 ± 0.47 mg/mL), while its lipase inhibition activity was moderate (10%), which may be beneficial from a cosmetic perspective. The obtained results indicate that apple extract is a valuable raw material with multifaceted biological potential. Overall, the results demonstrate that apple pomace extract and chamomile hydrolate can be effectively valorized as bioactive cosmetic ingredients, supporting both skin health benefits and circular economy principles in sustainable cosmetic formulation. Full article

Glioblastoma is the most aggressive primary malignant tumor of the central nervous system in adults, with a poor prognosis and high resistance to conventional therapies. Platinum drugs like cisplatin are effective but limited by systemic toxicity, poor blood–brain barrier penetration, and resistance. Natural compounds are increasingly studied for their anticancer potential and ability to enhance existing therapies. Based on this rationale, we designed Pt(IV)Ac-GA, a novel platinum(IV) complex obtained by conjugating cisplatin with ganoderic acid A, a triterpenoid from Ganoderma lucidum known for anticancer and immunomodulatory effects. The compound was synthesized, structurally characterized, and showed high stability and favorable pharmacokinetics. In vitro, Pt(IV)Ac-GA strongly reduced the viability of U251 and T98G glioblastoma cells while sparing normal astrocytes. It triggered apoptosis, cell cycle arrest, impaired migration, and increased sensitivity to ferroptosis and mitochondrial dysfunction. These results highlight Pt(IV)Ac-GA as a promising candidate to overcome current limitations in glioblastoma treatment. Full article