Search Results (52)

The Pet-Sang-Kard mixed herbal remedy (PSKMHR) is a traditional Thai medicinal formulation used as an herbal supplement for the treatment of hemorrhoids. This remedy consists of four specific herbal ingredients in the following proportions: 50 parts Cissus quadrangularis L. stems, 15 parts Eclipta prostrata L. aerial parts, 10 parts Rheum sp. rhizome, and 10 parts Boesenbergia rotunda (L.) Mansf. rhizome. This study presents the development, validation, and application of a high-performance liquid chromatography with photodiode array detection (HPLC-PDA) method designed for the simultaneous quantification of 13 key bioactive compounds, including rhaponticin, rhapontigenin, quercitrin, wedelolactone, aloe-emodin, rhein, emodin, chrysophanol, physcion, alpinetin, pinocembrin, pinostrobin, and panduratin A, present in the 70% ethanolic extract of PSKMHR. Method validation was conducted in accordance with Association of Official Analytical Collaboration (AOAC) international guidelines, evaluating parameters such as the specificity, linearity, accuracy, precision, and limit of detection. The results demonstrated exceptional linearity (R > 0.9999), high precision (% RSD < 2), and recovery rates within acceptable limits (98–102%) for all analytes. This developed method was successfully applied to quantify the 13 target compounds in the crude extracts of PSKMHR formulated from 10 market raw material samples, providing a robust analytical framework for quality control of this herbal remedy. Full article

Rhamnus formosana is a creeping evergreen shrub endemic to Taiwan. In traditional medicine, Rhamnaceae plants are used as herbal remedies for conditions such as itching, difficulty urinating, and constipation. This study explores the inhibitory effects of various solvent extracts and bioactive components of R. formosana on α-glucosidase, tyrosinase, acetylcholinesterase (AChE), and antioxidant activity. The 100 °C water extract exhibited strong antioxidant activity in DPPH, ABTS, superoxide, and FRAP assays. The methanol extract demonstrated the highest α-glucosidase inhibitory effect, while the ethanol extract displayed potent AChE inhibition and the acetone extract showed the most potential tyrosinase inhibitory activity among the extracts. Five main biocomponents were isolated and evaluated for their bioactivities. Among them, kaempferol (1) and quercetin (2) exhibited notable antioxidant activity in DPPH and ABTS assays. Particularly, kaempferol (1) performed the best α-glucosidase inhibitory effect, physcion (5) showed the strongest AChE inhibition, and quercetin (2) demonstrated the most potential for tyrosinase inhibitory activity. Further molecular docking studies revealed that there may be stronger binding mechanisms between bioactive components and target enzymes (including α-glucosidase, acetylcholinesterase, and tyrosinase) than the positive control. These findings suggest that bioactive extracts and compounds from the stems of R. formosana may have potential as natural antioxidant, anti-α-glucosidase, anti-AChE, and anti-tyrosinase drug candidates or dietary supplements for the management of oxidative stress-related conditions, including hyperglycemia, pigmentation disorders, and neurodegenerative diseases. Full article

Primary and metastatic tumors of the nervous system represent a diverse group of neoplasms, each characterized by distinct biological features, prognostic outcomes, and therapeutic approaches. Due to their molecular complexity and heterogeneity, nervous system cancers (NSCs) pose significant clinical challenges. For decades, plants and their natural products with established anticancer properties have played a pivotal role in the treatment of various medical conditions, including cancers. Anthraquinone derivatives, a class of tricyclic secondary metabolites, are found in several botanical families, such as Fabaceae, Polygonaceae, Rhamnaceae, and Rubiaceae. In a comprehensive review, recent advancements in the anticancer properties of 1,8-dihydroanthraquinone derivatives—such as emodin, aloe-emodin, hypericin, chrysophanol, rhein, and physcion—were analyzed. These compounds have been studied extensively, both used individually and in combination with other chemotherapeutic agents, using in vitro and in vivo models of nervous system tumors. It was demonstrated that 1,8-dihydroanthraquinone derivatives induce apoptosis and necrosis in cancerous cells, intercalate into DNA, disrupting transcription and replication in rapidly dividing cells, and alter ROS levels, leading to oxidative stress that damages tumor cells. Additionally, they can influence signaling pathways involved in oncogenesis, such as MAPK, PI3K/Akt, or others crucial for the survival and the proliferation of NSC cells. The exploration of 1,8-dihydroanthraquinone derivatives aims to develop novel therapies that could overcome resistance and improve cancer patients’ outcomes. Full article

Hydroxyanthracene derivatives (HADs) are plant substances produced by a variety of plant species, including different Aloe, Rheum, and Rhamnus species and Cassia senna. These plants are often used in food supplements to improve bowel function. However, recently, the European Commission prohibited a number of HADs due to toxicological concerns. These HADs included aloin (aloin A and aloin B), aloe-emodin, emodin, and danthron. Most of the currently available analytical methods are restricted to the analysis of only these compounds and do not include other HADs. In this view, a multi-analyte method could be useful for both regulatory analysis and dietary intake studies. To this end, such a method, employing liquid chromatography–tandem mass spectrometry and targeting 16 different HADs, was developed and validated in this study. Limits of quantification were in the range from 0.025 mg kg⁻¹ to 1 mg kg⁻¹. The recovery of the method was within the acceptable range of 80% to 120%, with the exception of physcion. Repeatability varied from 0.5% to 11.6%, and the range for within-laboratory reproducibility was from 3.4% to 16.3%. The expanded measurement uncertainty was below 50% for all HADs. Subsequently, 24 commercial samples of food supplements and herbal infusions sourced in Belgium were analyzed. The results indicated that although the industry put a great effort into minimizing the amount of aloin and danthron present in food supplements, more than half of the products still exceeded the maximum tolerated levels suggested for aloe-emodin and emodin. Full article

Polygonum cuspidatum, an important medicinal plant, often experiences shading from surrounding vegetation during its growth phase, raising questions about the impact of such conditions on the functionality of arbuscular mycorrhizal fungi. This study investigated the effects of an arbuscular mycorrhizal fungus (Funneliformis mosseae) on the growth, leaf gas exchange, and concentrations of active ingredient concentrations in leaves and roots of P. cuspidatum under shading (with a 72% shading rate) conditions. A nine-week shading intervention significantly suppressed root colonization by F. mosseae and the formation of soil mycorrhizal mycelium. Shading significantly inhibited the above-ground growth performance, biomass production, leaf photosynthetic rate, transpiration rate, stomatal conductance, and intercellular CO₂ concentration, while F. mosseae significantly increased these variables in the absence of shading. Plant height, leaf biomass, stem biomass, leaf photosynthetic rate, transpiration rate, and stomatal conductance were all decreased by F. mosseae when the plants were shaded. The shading treatment also significantly diminished the concentrations of active components measured in both leaves and roots. Under no-shading conditions, F. mosseae significantly boosted the concentrations of polydatin, resveratrol, aloe-emodin, emodin, chrysophanol, and physcion in roots, as well as the concentrations of polydatin and chrysophanol in leaves. Conversely, in the presence of shading, F. mosseae distinctly reduced these active ingredient levels in roots, followed by an increase in leaf polydatin and chrysophanol concentrations. In summary, shading substantially impaired the mycorrhizal benefits on plant growth, leaf gas exchange, and root active ingredients in P. cuspidatum, highlighting the importance of sufficient light to maximize mycorrhizal contributions. Full article

Alzheimer’s disease (AD) is the most predominant cause of dementia, considered a progressive decline in cognitive function that ultimately leads to death. AD has posed a substantial challenge in the records of medical science over the past century, representing a predominant etiology of dementia with a high prevalence rate. Neuroinflammation is a common characteristic of various central nervous system (CNS) pathologies like AD, primarily mediated by specialized brain immune and inflammatory cells, such as astrocytes and microglia. The present study aims to elucidate the potential mechanism of physcion that mitigates LPS-induced gliosis and assesses oxidative stress in mice. Physcion reduced the reactivity of Iba-1- and GFAP-positive cells and decreased the level of inflammatory cytokines like TNF-α and IL-1β. Physcion also reversed the effect of LPS-induced oxidative stress by upregulating the expression of Nrf2 and HO-1. Moreover, physcion treatment reversed LPS-induced synaptic disorder by increasing the level of presynaptic protein SNAP-23 and postsynaptic protein PSD-95. Our findings may provide a contemporary theoretical framework for clinical investigations aimed at examining the pathogenic mechanisms and therapeutic approaches for neuroinflammation and AD. Full article

Polygonum cuspidatum (PC) extract has been listed in the “Catalog of Used Cosmetic Ingredients (2021 Edition)”, which can inhibit melanogenesis, thus exerting a whitening effect, and has been widely used in cosmetics. However, there are currently no quality standards for PC extract used in cosmetics, and the bioactive components associated with anti-melanogenesis remain unclear. In view of this, the present study was the first to investigate the spectrum-effect relationship between fingerprints of PC extract and melanogenesis inhibition. Ten batches of PC extract fingerprints were established by HPLC. Pearson’s correlation analysis, gray correlation analysis (GRA) and orthogonal partial least squares regression analysis (OPLSR) were used to screen out resveratrol, emodin and physcion as the main whitening active ingredients using the inhibition of tyrosinase in B16F10 cells as the pharmacological index. Then, the melanogenesis inhibitory effects of the above three components were verified by tyrosinase inhibition and a melanin content assay in B16F10 cells. The interaction between small molecules and proteins was investigated by the molecular docking method, and it was confirmed by quantitative real-time PCR (qRT-PCR) that resveratrol, emodin and physcion significantly down-regulated the transcript levels of melanogenesis-related factors. In conclusion, this study established a general model combining HPLC fingerprinting and melanogenesis inhibition and also analyzed the spectrum–effect relationship of PC extract, which provided theoretical support for the quality control of PC extract in whitening cosmetics. Full article

Physcion can induce plant resistance to disease, and is registered to control powdery mildew by spraying in China. Seed coating is a widely applied precision method for pest prevention and control. To explore its potential in disease control and yield increase by seed coating, mixtures containing physcion and commonly used fungicides were designed and applied in a field trial. Greenhouse experiments screened the optimal concentration of physcion for seed coating an found it to be 1:50, with excellent promotion of plant growth and powdery mildew control. In field trials, seeds coated with a combinations of physcion with validamycin and pyrimidine nucleotide (2#) at 1:50 exhibited the highest emergence rate, tillering number, control effect of wheat powdery mildew, enzyme activity of ascorbate peroxidase (APX), glutathione reductase (GR), and peroxidase (POD), photosynthetic pigment content, and yield. These results provide an effective approach to wheat disease control and yield increase in wheat fields, and can lay the basis for reasonable application of physcion in Huang-huai-hai plain in China. Full article

Breast cancer (BC) is the most common malignancy among women worldwide. In recent years, significant progress has been made in BC therapy. However, serious side effects resulting from the use of standard chemotherapeutic drugs, as well as the phenomenon of multidrug resistance (MDR), limit the effectiveness of approved therapies. Advanced research in the BC area is necessary to create more effective and safer forms of therapy to improve the outlook for individuals diagnosed with this aggressive neoplasm. For decades, plants and natural products with anticancer properties have been successfully utilized in treating various medical conditions. Anthraquinone derivatives are tricyclic secondary metabolites of natural origin that have been identified in plants, lichens, and fungi. They represent a few botanical families, e.g., Rhamnaceae, Rubiaceae, Fabaceae, Polygonaceae, and others. The review comprehensively covers and analyzes the most recent advances in the anticancer activity of 1,8-dihydroanthraquinone derivatives (emodin, aloe-emodin, hypericin, chrysophanol, rhein, and physcion) applied both individually, or in combination with other chemotherapeutic agents, in in vitro and in vivo BC models. The application of nanoparticles for in vitro and in vivo evidence in the context of 1,8-dihydroanthraquinone derivatives was also described. Full article

Polygonum cuspidatum, an important medicinal plant, is rich in resveratrol and polydatin, but it frequently suffers from drought stress in the nursery stage, which inhibits the plant’s growth, active components concentrations, and the price of rhizome in the later stage. The purpose of this study was to analyze how exogenous 100 mM melatonin (MT) (an indole heterocyclic compound) affected biomass production, water potential, gas exchange, antioxidant enzyme activities, active components levels, and resveratrol synthase (RS) gene expression of P. cuspidatum seedlings growing under well-watered and drought stress conditions. The 12-week drought treatment negatively affected the shoot and root biomass, leaf water potential, and leaf gas exchange parameters (photosynthetic rate, stomatal conductance, and transpiration rate), whereas the application of exogenous MT significantly increased these variables of stressed and non-stressed seedlings, accompanied by higher increases in the biomass, photosynthetic rate, and stomatal conductance under drought versus well-watered conditions. Drought treatment raised the activities of superoxide dismutase, peroxidase, and catalase in the leaves, while the MT application increased the activities of the three antioxidant enzymes regardless of soil moistures. Drought treatment reduced root chrysophanol, emodin, physcion, and resveratrol levels, while it dramatically promoted root polydatin levels. At the same time, the application of exogenous MT significantly increased the levels of the five active components, regardless of soil moistures, with the exception of no change in the emodin under well-watered conditions. The MT treatment also up-regulated the relative expression of PcRS under both soil moistures, along with a significantly positive correlation between the relative expression of PcRS and resveratrol levels. In conclusion, exogenous MT can be employed as a biostimulant to enhance plant growth, leaf gas exchange, antioxidant enzyme activities, and active components of P. cuspidatum under drought stress conditions, which provides a reference for drought-resistant cultivation of P. cuspidatum. Full article

Endophytic fungi are a highly unpredictable group of microorganisms that can create a diverse range of secondary metabolites with biological activity. These metabolites enhance the host’s ability to tolerate stress caused by various factors, such as disease, insects, pathogens, and herbivores. The secondary metabolites produced by endophytic fungi may have potential applications in agriculture, pharmacy, and medicine. The purpose of this study was to examine the anti-acetylcholinesterase activity of secondary metabolites extracted from endophytic fungi. Aspergillus versicolor SB5 was one of the many endophytic fungi isolated from Juncus rigidus and identified genetically with accession number ON872302. Our study utilized fermentation and microbial cultivation techniques to obtain secondary metabolites. During the course of our investigation, we isolated a compound called Physcion (C1) from the endophytic fungus Aspergillus versicolor SB5. We subsequently identified that C1 possesses inhibitory activity against COX-2 and LOX-1, with IC50 values of 43.10 and 17.54 µg/mL, respectively, making it an effective anti-inflammatory agent. Moreover, we found that C1 also exhibited potent anticholinesterase activity (86.9 ± 1.21%). In addition to these promising therapeutic properties, our experiments demonstrated that C1 possesses strong antioxidant capacity, as evidenced by its ability to scavenge DPPH, ABTS, O2 radicals, and NO and inhibit lipid peroxidation. To further investigate the molecular mechanisms underlying C1 pharmacological properties, we employed SwissADME web tools to predict the compound’s ADME-related physicochemical properties and used Molecular Operating Environment and PyMOL for molecular docking studies. Full article

Over the past decade, methicillin-resistant Staphylococcus aureus (MRSA) has become a major source of biofilm formation and a major contributor to antimicrobial resistance. The genes that govern biofilm formation are regulated by a signaling mechanism called the quorum-sensing system. There is a need for new molecules to treat the infections caused by dangerous pathogens like MRSA. The current study focused on an alternative approach using juglone derivatives from Reynoutria japonica as quorum quenchers. Ten bioactive compounds from this plant, i.e., 2-methoxy-6-acetyl-7-methyljuglone, emodin, emodin 8-o-b glucoside, polydatin, resveratrol, physcion, citreorosein, quercetin, hyperoside, and coumarin were taken as ligands and docked with accessory gene regulator proteins A, B, and C and the signal transduction protein TRAP. The best ligand was selected based on docking score, ADMET properties, and the Lipinski rule. Considering all these parameters, resveratrol displayed all required drug-like properties with a docking score of −8.9 against accessory gene regulator protein C. To further assess the effectiveness of resveratrol, it was compared with the commercially available antibiotic drug penicillin. A comparison of all drug-like characteristics showed that resveratrol was superior to penicillin in many aspects. Penicillin showed a binding affinity of −6.7 while resveratrol had a score of −8.9 during docking. This was followed by molecular dynamic simulations wherein inhibitors in complexes with target proteins showed stability inside the active site during the 100 ns simulations. Structural changes due to ligand movement inside the cavity were measured in the protein targets, but they remained static due to hydrogen bonds. The results showed acceptable pharmacokinetic properties for resveratrol as compared to penicillin. Thus, we concluded that resveratrol has protective effects against Staphylococcus aureus infections and that it suppresses the quorum-sensing ability of this bacterium by targeting its infectious proteins. Full article

The composition of an ethanol extract from the roots of Rumex tianschanicus Losinsk of the Trans-Ili Alatau wild flora was studied in order to determine its antiulcer activity. The phytochemical composition of the anthraquinone–flavonoid complex from (AFC) R. tianschanicus revealed the presence of numerous polyphenolic compounds, the most abundant of which are anthraquinones (1.77%), flavonoids (6.95%), and tannins (13.39%). The use of column chromatography (CC) and thin-layer chromatography (TLC) in conjunction with UV, IR, NMR spectroscopy, and mass spectrometry data allowed the researchers to isolate and identify the major components of the anthraquinone–flavonoid complex’s polyphenol fraction: physcion, chrysophanol, emodin, isorhamnetin, quercetin, and myricetin. The gastroprotective effect of the polyphenolic fraction of the anthraquinone–flavonoid complex (AFC) of R. tianschanicus roots was examined in an experimental model of rat gastric ulcer induced by indomethacin. The preventive and therapeutic effect of the anthraquinone–flavonoid complex at a dose of 100 mg/kg was analyzed using intragastric administration per day for 1 to 10 days, followed by a histological examination of stomach tissues. It has been demonstrated that prophylactic and prolonged use of the AFC R. tianschanicus in laboratory animals resulted in significantly less pronounced hemodynamic and desquamative changes in the epithelium of gastric tissues. The acquired results thus offer fresh insight into the anthraquinone and flavonoid metabolite component composition of R. tianschanicus roots, and they imply that the examined extract can be used to develop herbal medicines with antiulcer activity. Full article

In the search for crop protectants, amino acid ester conjugates have been widely investigated as potential antifungal agents. In this study, a series of rhein–amino acid ester conjugates were designed and synthesized in good yields, and their structures were confirmed by ¹H-NMR, ¹³C-NMR and HRMS. The bioassay results revealed that most of the conjugates exhibited potent inhibitory activity against R. solani and S. sclerotiorum. In particular, conjugate 3c had the highest antifungal activity against R. solani with an EC₅₀ value of 0.125 mM. For S. sclerotiorum, conjugate 3m showed the highest antifungal activity with an EC₅₀ value of 0.114 mM. Satisfactorily, conjugate 3c exhibited better protective effects than that of the positive control, physcion, against powdery mildew in wheat. This research supports the role of rhein–amino acid ester conjugates as potential antifungal agents for plant fungal diseases. Full article

Psoriasis is a chronic, immune-mediated inflammatory skin disorder. Rheum palmatum L. is a common traditional medicinal herb with anti-inflammatory and immunomodulatory activities. This study aimed to investigate the anti-psoriatic effects of the ethanolic extract from R. palmatum L. (RPE) and its chemical constituents, as well as the mechanisms underlying their therapeutic significance. An imiquimod (IMQ)-induced psoriasis-like mouse model was used to examine the anti-psoriatic effect of RPE in vivo. Network pharmacological analysis was performed to investigate the potential targets and related pathways of the RPE components, including rhein, emodin, chrysophanol, aloe-emodin, and physcion. The anti-inflammatory effects and underlying mechanisms of these components were examined using in vitro models. Topical application of RPE alleviated psoriasis-like symptoms and reduced levels of inflammatory cytokines and proliferation markers in the skin. Network pharmacological analysis revealed that RPE components target 20 genes that are linked to psoriasis-related pathways, such as IL-17, MAPK, and TNF signaling pathways. Among the five components of RPE, rhein and emodin showed inhibitory effects on TNF-α and IL-17 production in EL-4 cells, attenuated the production of CXCL8, CXCL10, CCL20, and MMP9, and reduced proliferation in HaCaT cells. Chrysophanol, aloe-emodin, and physcion were less effective than rhein and emodin in suppressing inflammatory responses and keratinocyte proliferation. The effects of these compounds might occur through the inhibition of the ERK, STAT3, and NF-κB signaling pathways. This study suggested the anti-psoriatic effect of RPE, with rhein and emodin as the main contributors that regulate multiple signaling pathways. Full article