Search Results (27)

Phytochemical investigation of the ethyl acetate extract from the aerial parts of Pouzolzia pentandra led to the isolation and identification of fourteen compounds (1–14). These include known compounds such as β-sitosterol (1), bauerenol (2), oleanolic acid (3), 3β-friedelanol (4), kaempferol (5), quercetin (6), 2′,6′-dihydroxy-3′,4′-dimethoxychalcone (7), friedelan-3-one (8), dipterocarpol (9), 3β-hydroxyolean-12-en-28-one 3-p-coumarate (10), daucosterol (11), astilbin (12), 3-methoxy-4-hydroxybenzoic acid (13), and pouzolignan F (14). Among these, compound 14 displayed the most potent inhibitory activity on nitric oxide (NO) production in LPS-stimulated RAW264.7 macrophages, with an IC₅₀ value of 10.54 ± 0.4 µM. Mechanistic studies further revealed that compound 14 significantly suppressed the LPS-induced release of key pro-inflammatory cytokines, tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6). Furthermore, it inhibited the activation of the nuclear factor-kappa B (NF-κB) signaling pathway by preventing the nuclear translocation of its p65 subunit. Molecular docking studies were performed to evaluate the anti-inflammatory potential of compound 14 against cyclooxygenase-2 (COX-2) and phosphodiesterase-4 (PDE4). The compound exhibited binding affinities of −6.138 kcal/mol and −9.361 kcal/mol for COX-2 and PDE4, respectively. Subsequent molecular dynamics (MD) simulations confirmed the formation of a stable complex with the active site of PDE4. Collectively, these integrated in vitro and in silico findings demonstrate that pouzolignan F acts as a multi-target anti-inflammatory agent, likely through the inhibition of inflammatory mediators, cytokines, and the NF-κB pathway. Full article

Pasuchaca (Geranium dielsianum Knuth), a traditional Peruvian medicinal plant from the Geraniaceae family used for diabetes management, was investigated for its antiglycative properties. This study aimed to screen, isolate, and identify the active antiglycative compounds from its aerial parts. By coupling a methylglyoxal (MGO)-HPLC screening assay with high-speed counter-current chromatography (HSCCC), seven dihydroflavonol derivatives were separated and identified from the 80% methanol extract. The compounds were identified as 2,3-dihydromyricetin 3-O-α-rhamnopyranoside (1), (+)-taxifolin 3-O-β-D-xylopyranoside (2), astilbin (6), isoastilbin (8), 3″-acetyl astilbin (9), and 2″-acetyl astilbin (11). Astilbin was identified as the major constituent, with remarkably high contents of 252.41 mg/g in the 80% methanol extract and 541.04 mg/g in the partitioned upper layer fraction. Astilbin demonstrated potent antiglycation activity across all stages of protein glycation (early, middle, late, and whole stages), significantly surpassing the positive control aminoguanidine. Furthermore, the formation of MGO-astilbin adducts was confirmed by LC-ESI-MS, validating its role as an effective MGO scavenger. This report is the first to isolate these phytochemicals from Pasuchaca. The findings establish astilbin as the key antiglycative component of Pasuchaca, substantiating its traditional use and highlighting its potential as a source of functional food ingredients or natural therapeutics for mitigating glycative stress. Full article

Coconut milk is a widely consumed plant-based milk alternative, valued for its creamy texture and functional properties. This study systematically evaluated the fatty acid and phenolic profiles of coconut meat and water at tender and mature stages to inform coconut milk production. Fatty acid analysis revealed that mature coconut meat (MCM) contained 299.7 g/kg total fatty acids, predominantly lauric acid (C12:0, 142.97 g/kg, 48%), myristic acid (C14:0, 57.39 g/kg, 19%), and palmitic acid (C16:0, 29.79 g/kg, 10%), whereas tender coconut meat (TCM) contained 90.87 g/kg total fatty acids. Tender coconut water (TCW) exhibited the highest total phenolic content (TPC) and DPPH radical scavenging activity. UHPLC-Q-Orbitrap-MS identified 1065 phytochemicals, including 96 phenolics, with multivariate analyses showing distinct profiles between tissues and developmental stages. Notably, tender samples contained higher levels of bioactive phenolics, such as catechin, epicatechin, and astilbin. Collectively, these results demonstrate that tissue type and developmental stage jointly shape the nutritional and functional attributes of coconuts. Mature coconut meat provides lipid-rich nutrition for coconut milk, while tender coconut water offers antioxidant-rich bioactivity. Integrating these raw materials can enhance the nutritional and functional properties of coconut milk, enhancing its role as a versatile plant-based alternative for functional food and beverages. Full article

Background/Objectives: Ampelopsis grossedentata, a novel food resource (vine tea), is a therapeutically valuable species wherein all parts exhibit bioactive potential. The therapeutic value and health benefits of A. grossedentata are rooted in its metabolomic profile, yet the metabolites in its various parts remain incompletely characterized. In this study, the tissue-specific biochemical properties and metabolic profiles of A. grossedentata were systematically characterized to identify the optimal tissue type for harvesting, with the goal of maximizing the production of bioactive compounds. Methods: The biochemical properties of various A. grossedentata tissues were assessed using a spectrophotometer, and their metabolic profiles were characterized through LC-MS/MS-based untargeted metabolomics. Results: The results demonstrate that, compared with the stems and roots, the tender leaves and floral tissues contained a higher TFC and TPC, correlating with superior antioxidant activity (DPPH, ABTS, and FRAP). A metabolic analysis revealed that the tender leaves accumulated multiple bioactive flavonoids beyond dihydromyricetin, including naringenin 7-O-beta-D-glucoside, (-)-epigallocatechin, tricetin, and cyanidin 3-O-sophoroside. The floral tissues displayed a comparable antioxidant capacity and dihydromyricetin level to the leaves, as well as unique compounds, such as leucodelphinidin, naringenin, epicatechin, dihydroquercetin, astilbin, and myricitrin. A metabolomic analysis further demonstrated a high accumulation of L-glutamine and L-glutamic acid in the floral tissues, potentially contributing to the characteristic umami flavor profile of vine tea made from A. grossedentata flowers. Conclusions:A. grossedentata flowers could be considered a promising raw material for developing novel functional foods and premium herbal tea products, as they possess superior antioxidant activity and abundant flavonoids and amino acids. Full article

Kujingcha (KJC) is a widely consumed substitute tea due to its unique flavor quality and health benefits. However, the biochemical basis for the formation of KJC’s unique flavor quality and health benefits remain unclear. In this study, using Camellia sinensis green tea and its processed fresh leaves as a control, we systematically analyzed the non-volatile and volatile components in KJC and its processed fresh leaves. The results indicate that high levels of flavonoids and water-soluble sugars, and low levels of amino acids and water-soluble proteins, are important biochemical foundations for the formation of taste quality in KJC. High aldehyde, alkene and heterocyclics contents contribute significantly to the aroma of KJC, among which heterocyclics are the key components for the formation of KJC’s rich pan-fried bean-like aroma. Flavonoids such as neohesperidin, hyperoside, rutin, astilbin and morin are important components for the formation of KJC’s health benefits. Full article

Psoriasis, a chronic inflammatory skin disorder, is driven by dysregulated immune responses and keratinocyte dysfunction. Here, we explore the therapeutic potential of Astilbin (AST), a flavonoid with potent anti-inflammatory properties, in modulating ferroptosis and the cyclic GMP-AMP synthase (cGAS)-stimulator of interferon genes (STING) pathway in IL-17-stimulated HaCaT keratinocytes. Our psoriatic cell model recapitulated key pathological features, including hyperproliferation, membrane integrity loss, mitochondrial dysfunction, and heightened oxidative stress, alongside elevated proinflammatory cytokine levels. Ferroptosis-related biomarkers were significantly altered, with increased malondialdehyde (MDA) accumulation, reduced glutathione (GSH) levels, iron overload (Fe²⁺), and enhanced lipid peroxidation (detected via C11-BODIPY). Mechanistically, mitochondrial damage triggered cytoplasmic leakage of mitochondrial DNA (mtDNA), activating the cGAS-STING pathway, as evidenced by upregulated pathway-associated protein expression. AST intervention effectively mitigated these pathological changes by suppressing ferroptosis and modulating cGAS-STING signaling. These findings reveal a dual-pathway regulatory mechanism, positioning AST as a promising therapeutic candidate for psoriasis. By elucidating the interplay between ferroptosis and the cGAS-STING pathway, this study provides new insights into psoriatic inflammation and offers a rationale for targeting these pathways in therapeutic strategies. Full article

A dual-column tandem mode was used to establish the fingerprints of Sarcandrae herb from different origins, and their chemical compositions were characterized by UPLC-Q-TOF-MS/MS, which provided an experimental basis for the establishment of a rapid and efficient method for the overall quality control of Sarcandrae herba. For the first time, nine common components were identified from the Sarcandrae herba herbs of 24 origins, which were neochlorogenic acid, chlorogenic acid, 4-caffeoylquinic acid, eleutheroside B1, quercetin-3-O-β-D-glucuronide, neoastilbin, astilbin, isofraxidin, and rosmarinic acid, respectively. A total of 92 compounds were identified by liquid mass spectrometry. The quality of the Sarcandrae herb from 24 origins was analyzed by similarity evaluation, principal component analysis, and cluster analysis, and the chemical components of Sarcandrae herba were identified by UPLC-Q-TOF-MS/MS. The results showed that the overall analysis based on fingerprinting and mass spectrometry could differentiate the origins of the herbs. Full article

Purpose: This study aimed to clarify the protective effect of astilbin (AST) on radiation-induced pulmonary fibrosis (RIPF) and explore its underlying molecular mechanism, focusing on non-coding RNAs. Methods: Mouse lung epithelial cells (MLE-12 and TC-1) and C57BL/6J mice were used to establish in vitro radiation injury models and in vivo RIPF models, respectively. Cell viability, apoptosis, the epithelial-to-mesenchymal transition (EMT), and fibrosis-related markers were assessed using cell-counting kit-8 assays, Western blotting, immunohistochemistry, and histological staining. High-throughput sequencing identified differentially expressed circRNAs. The mechanistic studies included RNA-FISH, a dual-luciferase reporter assay, an RNA immunoprecipitation (RIP) assay, and loss-of-function experiments. Results: AST significantly alleviated radiation-induced apoptosis and EMT in vitro, as well as RIPF in vivo. AST treatment reduced collagen deposition, fibrosis-related protein expression, and EMT marker changes. High-throughput sequencing revealed that AST upregulated circPRKCE, a non-coding RNA that functions through a ceRNA mechanism by binding to miR-15b-5p, thereby promoting Smad7 expression and suppressing the TGF-β/Smad7 pathway. Knockdown of circPRKCE abolished AST’s protective effects, confirming its pivotal role in mediating AST’s anti-fibrotic activity. Conclusions: This study demonstrates that Astilbin alleviates radiation-induced pulmonary fibrosis via circPRKCE targeting the TGF-β/Smad7 pathway to inhibit EMT, suggesting AST as a potential therapeutic agent for managing this severe complication of radiotherapy. Full article

Exploiting by-products from the oenological industry to extract antioxidant chemicals is a shared goal that combines the need to reduce the wine sector’s environmental impact with the need to improve the availability of these biomolecules, according to a circular economy approach. Natural deep eutectic solvents (NaDES) have recently captured researchers’ interest as a safer and more environmentally friendly alternative to traditional solvents due to their effectiveness, low toxicity, and stability. In this work, we set out to investigate several NaDES for the extraction of phenolic chemicals from local monovarietal grape pomace resulting from different vinification procedures (including both red and rosé vinification of Negroamaro and Primitivo grapes; rosé vinification of Susumaniello grapes and white vinification of Chardonnay, Fiano and Malvasia bianca grapes), with the additional goal of generalizing the use of NaDES to extract chemicals of interest from organisms selected from the wide plant biodiversity. Three binary choline chloride-based NaDES (DES-Lac, DES-Tar, and DES-Gly, with lactic acid, tartaric acid, and glycerol as hydrogen bond donors, respectively) were compared to ethanol as a conventional solvent, and the extracts were evaluated using HPLC/MS and colorimetric techniques. The results revealed that each NaDES produces a substantially higher total phenolic yield than ethanol (up to 127.8 mg/g DW from Primitivo rosé grape pomace). DES-Lac and DES-Tar were more effective for anthocyanins extraction; the most abundant compound was malvidin 3-O-glucoside (highest extraction yield with DES-Lac from Susumaniello pomace: 29.4 mg/g DW). Regarding phenolic compounds, DES-Gly was the most effective NaDES producing results comparable to ethanol. Unexpectedly, Chardonnay pomace has the greatest content of astilbin. In most cases, grape pomace extracts obtained by rosé and white vinification provided the maximum yield. As a result, NaDES have emerged as a viable alternative to traditional organic solvent extraction techniques, allowing for higher (or equal) yields while significantly lowering costs, hazards, and environmental impact. Full article

Psoriasis is a chronic inflammatory disease that affects around 2–3% of the world’s population. The treatment for this autoimmune disease still remains centered around conventional methods using synthetic substances, even though more recent advancements focus on biological therapies. Given the numerous side effects of such treatments, current research involves plant extracts and constituents that could prove useful in treating psoriasis. The aim of this narrative review is to highlight the most known representatives belonging to classes of natural compounds such as polyphenols (e.g., astilbin, curcumin, hesperidin, luteolin, proanthocyanidins, and resveratrol), alkaloids (e.g., berberine, capsaicin, and colchicine), coumarins (psoralen and 8-methoxypsoralen), and terpenoids (e.g., celastrol, centelloids, and ursolic acid), along with plants used in traditional medicine that could present therapeutic potential in psoriasis. The paper also provides an overview of these compounds’ mechanisms of action and current inclusion in clinical studies, as well as an investigation into their potential incorporation in various nanotechnological systems, such as lipid-based nanocarriers or polymeric nanomaterials, that may optimize their efficacy during treatment. Full article

The outbreak of SARS-CoV-2, also known as the COVID-19 pandemic, is still a critical risk factor for both human life and the global economy. Although, several promising therapies have been introduced in the literature to inhibit SARS-CoV-2, most of them are synthetic drugs that may have some adverse effects on the human body. Therefore, the main objective of this study was to carry out an in-silico investigation into the medicinal properties of Petiveria alliacea L. (P. alliacea L.)-mediated phytocompounds for the treatment of SARS-CoV-2 infections since phytochemicals have fewer adverse effects compared to synthetic drugs. To explore potential phytocompounds from P. alliacea L. as candidate drug molecules, we selected the infection-causing main protease (Mpro) of SARS-CoV-2 as the receptor protein. The molecular docking analysis of these receptor proteins with the different phytocompounds of P. alliacea L. was performed using AutoDock Vina. Then, we selected the three top-ranked phytocompounds (myricitrin, engeletin, and astilbin) as the candidate drug molecules based on their highest binding affinity scores of −8.9, −8.7 and −8.3 (Kcal/mol), respectively. Then, a 100 ns molecular dynamics (MD) simulation study was performed for their complexes with Mpro using YASARA software, computed RMSD, RMSF, PCA, DCCM, MM/PBSA, and free energy landscape (FEL), and found their almost stable binding performance. In addition, biological activity, ADME/T, DFT, and drug-likeness analyses exhibited the suitable pharmacokinetics properties of the selected phytocompounds. Therefore, the results of this study might be a useful resource for formulating a safe treatment plan for SARS-CoV-2 infections after experimental validation in wet-lab and clinical trials. Full article

Aluminum (Al) affects the yield of forest trees in acidic soils. The oil tea plant (Camellia drupifera Lour.) has high Al tolerance, with abundant phenolic compounds in its leaves, especially flavonoid compounds. The role of these flavonoids in the Al resistance of oil tea plants is unclear. In this metabolomic study of C. drupifera under Al stress, ultra-pressure liquid chromatography coupled with tandem mass spectrometry (UPLC-MS/MS) was utilized to identify metabolites, while principal component analysis, cluster analysis, and orthogonal partial least squares discriminant analysis were applied to analyze the data on the flavonoid metabolites. The leaf morphology of C. drupifera revealed significant damage by excess aluminum ions under each treatment compared with the control group. Under Al stress at 2 mmol/L (GZ2) and 4 mmol/L (GZ4), the total flavonoid content in C. drupifera leaves reached 24.37 and 35.64 mg/g, respectively, which are significantly higher than the levels measured in the control group (CK) (p < 0.01). In addition, we identified 25 upregulated and 5 downregulated metabolites in the GZ2 vs. CK comparison and 31 upregulated and 7 downregulated flavonoid metabolites in GZ4 vs. CK. The results demonstrate that different levels of Al stress had a significant influence on the metabolite profile of C. drupifera. It was found that the abundance of the 24 differential flavonoid metabolites was gradually elevated with increasing concentrations of Al stress, including catechin, epicatechin, naringenin-7-glucoside, astilbin, taxifolin, miquelianin, quercitrin, and quercimeritrin. Moreover, the most significant increase in antioxidant activity (about 30%) was observed in C. drupifera precultured in leaf extracts containing 7.5 and 15 μg/mL of active flavonoids. The qRT-PCR results showed that the expression levels of key genes involved in the synthesis of flavonoids were consistent with the accumulation trends of flavonoids under different concentrations of Al. Therefore, our results demonstrate the key role of flavonoid compounds in the oil tea plant C. drupifera in response to Al stress, which suggests that flavonoid metabolites in C. drupifera, as well as other aluminum-tolerant plants, may help with detoxifying aluminum. Full article

The leaves of Engelhardia roxburghiana Wall (LERW) has been used as sweet tea in China throughout history. In this study, the ethanol extract of LERW (E-LERW) was prepared and the compositions were identified by HPLC-MS/MS. It indicates that astilbin was the predominant component in E-LERW. In addition, E-LERW was abundant in polyphenols. Compared to astilbin, E-LERW presented much more powerful antioxidant activity. The E-LERW also had stronger affinity with α-glucosidase and exerted more vigorous inhibitory effect on the enzyme. Alloxan-induced diabetic mice had significantly elevated glucose and lipid levels. Treatment with E-LERW at the medium dose (M) of 300 mg/kg could reduce the levels of glucose, TG, TC, and LDL by 16.64%, 12.87%, 32.70%, and 22.99%, respectively. In addition, E-LERW (M) decreased food intake, water intake, and excretion by 27.29%, 36.15%, and 30.93%, respectively. Moreover, E-LERW (M) therapy increased the mouse weight and insulin secretion by 25.30% and 494.52%. With respect to the astilbin control, E-LERW was more efficient in reducing the food and drink consumption and protecting pancreatic islet and body organs from alloxan-induced damage. The study demonstrates that E-LERW may be a promising functional ingredient for the adjuvant therapy of diabetes. Full article

Astilbin (AST), isoastilbin (ISO), and engeletin (ENG) are the main flavonoids in Rhizoma Smilacis Glabrae (RSG) and have many biological activities. In this study, the adsorption kinetics of AST, ISO, and ENG on HPD-300 resin was investigated and their adsorption processes conformed to a pseudo-second-order kinetics equation. The fitting curves of the intraparticle diffusion model showed three linear stages and did not pass through the origin, meaning the adsorption process of the three flavonoids was controlled by boundary layer diffusion and intraparticle diffusion. Their adsorption isotherms were also constructed and could be well-fitted by the Langmuir equation. A low temperature was favorable for their adsorption. The relative adsorption capacity of ENG was significantly higher than those of the other two compounds, indicating that the substitution pattern on ring B has an important impact on the adsorption of flavonoids with resin. The separation process was optimized by dynamic adsorption/desorption experiments. After separation, the purities of AST, ISO, and ENG increased from 5.55%, 1.22%, and 0.45% to 27.46%, 6.14%, and 2.27%, respectively, and all the recoveries exceeded 75%. After that, the three compounds were further separated by preparative HPLC and silica gel chromatography. In the final product, the purities of AST, ISO, and ENG could reach above 98%. Full article

Taxifolin is known to have multiple biological functions. It has been widely used as a multifunctional food additive, and consequently, the global demand for taxifolin is increasing. The main method for taxifolin production is an extraction from larch wood, but the global resources of larch are limited. Astilbin, taxifolin-3-o-rhamnoside, is abundant in many plants and much more readily available, meaning taxifolin can be obtained by deglycosylation of astilbin. In this study, a fungal strain, Aspergillus fumigatus SQH4, was isolated from an enrichment culture of Smilax glabra rhizome to achieve the deglycosylation reaction. A culture of SQH4, adjusted to pH 6.5, with 5 g/L astilbin achieved a yield of taxifolin of 91.3% after biotransformation for 14 h at 35 °C. These findings offer an alternative method for the production of taxifolin. Full article