Sophora Flavescens Research Articles

Characterization and anticancer evaluation of zirconia nanoparticles synthesized via green route using sophora flavescens roots extract

The emergence of drug resistance in cancer cells has impeded recent progress in cancer therapy, leading to the investigation of novel anticancer drugs. The fabrication of metal and ZrO2 nanoparticles is a promising path with prospective applications across diverse technological domains. The present study investigates the potential anticancer effects of ZrO2 NPs obtained from the root extract of Sophora flavescens on MCF-7 breast cancer cells. The structural and chemical features of these nanoparticles are analyzed using several techniques such as flow cytometry, SEM, TEM, FTIR, and UV–vis spectroscopy. The examination of XRD and TEM images demonstrates the significant contribution of plant root extract in enhancing the efficiency of nanoparticles, leading to the formation of nearly tetragonal crystal structures with an average size of 8 nm. The MTT experiment verifies the nanoparticles' anticancer activity, which depends on the dosage. The IC50 value of 253 μg/mL indicates the half-maximal inhibitory concentration. The optical microscope reveals an unusual sight: MCF-7 cells appear more spherical and less dense at higher concentrations. This research also investigates the antibacterial properties of ZrO2 nanoparticles against harmful bacteria, particularly those resistant to multiple drugs. The diffusion disk assay indicates that the nanoparticles are active against drug-resistant isolates, with zones of inhibition ranging from 31 to 55 millimeters. Additionally, the researchers noted a positive correlation between nanoparticle concentration and the size of the inhibition zone. Overall, the data indicates the potential of ZrO2 NPs to aid in cancer therapy as well as in combating infections.

Quaternity method for integrated screening, separation, extraction optimization, and bioactivity evaluation of acetylcholinesterase inhibitors from Sophora flavescens Aiton.

Sophora flavescens Aiton (Fabaceae), a ubiquitous plant species in Asia, contains a wide range of pharmacologically active compounds, such as flavonoids, with potential anti-Alzheimer's disease (anti-AD) effects. The objective of the study is to develop a quaternity method for the screening, isolation, extraction optimization, and activity evaluation of acetylcholinesterase (AChE)-inhibiting compounds from S. flavescens to realize high-throughput screening of active substances in traditional Chinese medicine and to provide experimental data for the development of anti-AD drugs. With AChE as the target molecule, affinity ultrafiltration and liquid chromatography-mass spectrometry were applied to screen for potential inhibitors of the enzyme in S. flavescens. Orthogonal array experiments combined with the multi-objective Non-Dominated Sorting Genetic Algorithm III was used for the first time to optimize the process for extracting the active substances. Enzyme inhibition kinetics and molecular docking studies were performed to verify the potential anti-AD effects of the active compounds. Five AChE-inhibiting compounds were identified: kushenol I, kurarinone, sophoraflavanone G, isokurarinone, and kushenol E. These were successfully separated at purities of 72.88%, 98.55%, 96.86%, 96.74%, and 95.84%, respectively, using the n-hexane/ethyl acetate/methanol/water (4.0/5.0/4.0/5.0, v/v/v/v), n-hexane/ethyl acetate/methanol/water (5.0/5.0/6.0/4.0, v/v/v/v), and n-hexane/ethyl acetate/methanol/water (4.9/5.1/5.7/4.3, v/v/v/v) mobile phase systems. Enzyme inhibition kinetics revealed that kushenol E had the best inhibitory effect. This study elucidates the mechanism of action of five active AChE inhibitors in S. flavescens and provides a theoretical basis for the screening and development of anti-AD and other therapeutic drugs.

First Report of Powdery Mildew on Sophora flavescens Caused by Erysiphe diffusa in China.

Sophora flavescens (Fabaceae) is a deciduous subshrub which has been used in Chinese popular medicine for a long history (He et al. 2015). In June 2023, severe powdery mildew symptoms were observed on wild S. flavescens plants on Longwen hill of Guizhou Normal University, Guiyang, China. The incidence was approximately 80% among 100 S. flavescens plants observed. Almost all leaves were infected. Mycelia occurred on both adaxial and abaxial leaf surfaces, petioles, and stems, forming small-to-large patches. Hyphae were hyaline, 5 to 7 μm wide. Hyphal appressoria were solitary. Conidiophores were erect, straight to somewhat flexuous, and 45 to 120 µm long (n = 50). Foot cells were subcylindrical to slightly curved, followed by 2 to 3 shorter cells. Conidia formed singly, were ovoid to cylindrical, 26 to 42 × 12 to18 µm (n = 50). Based on these morphological characteristics, the powdery mildew fungus was tentatively identified as Erysiphe diffusa (Braun and Cook 2012). To confirm the identification, the ribosomal DNA internal transcribed spacer (ITS) and the ribosomal large subunit (LSU) region were amplified and sequenced using primer pairs ITS1/ITS4 (White et al. 1990) and NL1/NL4 (Ziemiecki et al. 1990), respectively. The obtained 647-bp ITS sequence (GenBank accession no. PP130131) displayed 100% identity with the ITS sequences of E. diffusa. The obtained 618-bp LSU sequence (GenBank accession no. PP693303) displayed 100% identity with the ITS sequences of E. diffusa (MT325922 and MT628019) and E. manihoticola (MT106658 and MT106660). Using a phylogenetic tree based on the combined ITS-LSU data, the isolate was grouped in a clade with the E. diffusa strain (GenBank accession no. LC777871). To fulfill Koch's postulates, leaves of three healthy potted S. flavescens plants were inoculated by gently pressing with diseased leaves. Non-inoculated plants were used as controls. All plants were incubated in a greenhouse at 25 ± 2°C, 80% relative humidity. After 15 days, typical powdery mildew symptoms were observed on the inoculated plants, whereas no symptoms were found on the control plants. The reisolated fungus from the inoculated S. flavescens was morphologically identical to that on naturally diseased plants, and the ITS sequence of the reisolated fungus showed 100% identity with PP130131. As the causal fungus of soybean powdery mildew, E. diffusa is known to infect papaya and other legumes, including Lens culinaris and Mimosa caesalpiniifolia (Attanayake et al. 2009; Luz et al. 2019). Particularly, E. diffusa has been previously reported to infect S. flavescens in the United Kingdom (Jones and Baker 2007; Bradshaw et al. 2023), but this is the first report of S. flavescens powdery mildew caused by E. diffusa in China. This work further expands the geographical range of E. diffusa-infected S. flavescens plants.

Unraveling the Pharmacological Intricacies of Kurarinone in Osteoporosis: Insights from a Network Pharmacology Approach

Background Kurarinone, a compound derived from Sophora flavescens, has been widely studied for its anti-inflammatory properties, as well as its potential in treating autoimmune encephalomyelitis and inflammation-related musculoskeletal diseases. However, the specific molecular mechanisms by which Kurarinone affects osteoporosis are still not fully understood. Objectives To explore the potential pharmacological targets and molecular mechanisms underlying the therapeutic effects of Kurarinone on osteoporosis. Materials and Methods To confirm the impact of Kurarinone on osteoporosis, network pharmacology techniques were used to analyze the mechanisms of Kurarinone on osteoporosis. Molecular docking was performed to examine the binding of Kurarinone to key targets involved in osteoporosis. Then, we conducted TRAcP staining, quantitative polymerase chain reaction (q-PCR), and Western blot experiments to validate the results. Results Utilizing network pharmacology approaches coupled with docking analysis, our investigation revealed that Kurarinone was involved in the osteoclast differentiation and MAPK signaling pathways. According to in vitro experiments, Kurarinone was found to inhibit osteoclast formation through the p38/MAPK pathway. Conclusion This study suggests that Kurarinone may treat osteoporosis by inhibiting MAPK phosphorylation and inhibiting osteoclast formation.

Natural Prenylflavonoids from Sophora flavescens Root Bark against Multidrug-Resistant Methicillin-Sensitive Staphylococcus aureus Targeting the Membrane Permeability.

The overuse of antibiotics in animal farming and aquaculture has led to multidrug-resistant methicillin-sensitive Staphylococcus aureus (MR-MSSA) becoming a common pathogen in foodborne diseases. Sophora flavescens Ait. serves as a traditional plant antibacterial agent and functional food ingredient. A total of 30 compounds (1-30) were isolated from the root bark of S. flavescens, consisting of 20 new compounds (1-20). In the biological activity assay, compound 1 demonstrated a remarkable inhibitory effect on MR-MSSA, with an MIC of 2 μg/mL. Furthermore, 1 was found to rapidly eliminate bacteria, inhibit biofilm growth, and exhibit exceptionally low cytotoxicity. Mechanistic studies have revealed that 1 possesses an enhanced membrane-targeting ability, binding to the bacterial cell membrane components phosphatidylglycerol (PG), phosphatidylethanolamine (PE), and cardiolipin (CL). This disruption of bacterial cell membrane integrity increases intracellular reactive oxygen species, protein and DNA leakage, reduced bacterial metabolism, and ultimately bacterial death. In summary, these findings suggest that compound 1 holds promise as a lead compound against MR-MSSA.

Adsorption properties of cellulose-derived hydrogel and magnetic hydrogels from Sophora flavescens on Cu2+ and Congo red

This study synthesized a robust, magnetically responsive hydrogel from Sophora flavescens-modified cellulose and chitosan, employing Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), thermogravimetric analysis (TGA and DTG), and scanning electron microscopy (SEM) to confirm the preservation of cellulose's intrinsic properties and the hydrogel's remarkable elasticity, toughness, and porosity. These hydrogels integrate cellulose's structural backbone with functional moieties from chitosan, enhancing adsorption capabilities for Cu2+ ions and Congo red (CR) dye. Kinetic and thermodynamic analyses reveal that adsorption is spontaneous and endothermic, following a pseudo-second-order model and the Freundlich isotherm. Notably, Cu2+ adsorption capacity increases with pH, while CR adsorption initially decreases before rising, demonstrating the hydrogels' potential as effective, sustainable adsorbents for removing pollutants from water.

Prenylated Flavonoids in Sophora flavescens: A Systematic Review of Their Phytochemistry and Pharmacology.

Sophora flavescens has been widely used in traditional Chinese medicine for over 1700 years. This plant is known for its heat-clearing, damp-drying, insecticidal, and diuretic properties. Phytochemical research has identified prenylated flavonoids as a unique class of bioactive compounds in S. flavescens. Recent pharmacological studies reveal that the prenylated flavonoids from S. flavescens (PFS) exhibit potent antitumor, anti-inflammatory, and glycolipid metabolism-regulating activities, offering significant therapeutic benefits for various diseases. However, the pharmacokinetics and toxicological profiles of PFS have not been systematically studied. Despite the diverse biological effects of prenylated flavonoid compounds against similar diseases, their structure-activity relationship is not yet fully understood. This review aims to summarize the latest findings regarding the chemical composition, drug metabolism, pharmacological properties, toxicity, and structure-activity relationship of prenylated flavonoids from S. flavescens. It seeks to highlight their potential for clinical use and suggest directions for future related studies.

Clinical Efficacy of Microwave Combined with Sophora flavescens Gel in Treating HPV Infection Complicated with Chronic Cervicitis and its Influence on Vaginal Microecology of Patients

Objective: To analyze the effect of microwave combined with Sophora flavescens gel in patients with HPV infection and chronic cervicitis (CC). Methods: From May 2022 to May 2023, 65 patients with HPV infection complicated with CC were randomly selected and divided into group A (31 cases, microwave) and group B (34 cases, microwave + Sophora flavescens gel) by numerical numbering envelope method, and the effects of the two groups were compared. Results: The positive rate of vaginal microenvironment factors, inflammatory factor indexes, immune function indexes, and HPV-DNA viral load in group B were better than those in group A in the following month after treatment (P < 0.05). Conclusion: Combined use of microwave and Sophora flavescens gel in patients with HPV infection and CC can better improve the vaginal microenvironment and inflammatory reaction, boost the body’s immune function, and reduce HPV-DNA viral load.

Oxymatrine attenuates sepsis-induced inflammation and organ injury via inhibition of HMGB1/RAGE/NF-κB signaling pathway.

Sepsis is a life-threatening organ dysfunction that endangers patient lives and is caused by an imbalance in the host defense against infection. Sepsis continues to be a significant cause of morbidity and mortality in critically sick patients. Oxymatrine (OMT), a quinolizidine alkaloid derived from the traditional Chinese herb Sophora flavescens Aiton, has been shown to have anti-inflammatory effects on a number of inflammatory illnesses according to research. In this study, we aimed to evaluate the therapeutic effects of OMT on sepsis and explore the underlying mechanisms. We differentiated THP-1 cells into THP-1 macrophages and studied the anti-inflammatory mechanism of OMT in a lipopolysaccharide (LPS)-induced THP-1 macrophage sepsis model. Activation of the receptor for advanced glycation end products (RAGE), as well as NF-κB, was assessed by Western blot analysis and immunofluorescence staining. ELISA was used to measure the levels of inflammatory factors. We found that OMT significantly inhibited HMGB1-mediated RAGE/NF-κB activation and downstream inflammatory cytokine production in response to LPS stimulation. Finally, an in vivo experiment was performed on septic mice to further study the effect of OMT on injured organs. The animal experiments showed that OMT significantly inhibited HMGB1-mediated RAGE/NF-κB activation, protected against the inflammatory response and organ injury induced by CLP, and prolonged the survival rate of septic mice. Herein, we provide evidence that OMT exerts a significant therapeutic effect on sepsis by inhibiting the HMGB1/RAGE/NF-κB signaling pathway.

Nanoparticles of Various Herbal Drugs Extract Produce Anticancer Activity: Review

The global burden of cancer disease is steadily increasing, and because of the symptoms of chemotherapy, there is a great deal of interest in herbal treatment. Herbal products appear to be innocuous and at that time they can meddle with malignancy treatment. An enormous volume of clinical examinations has detailed that the helpful impacts of natural herbal products on the endurance, insusceptible regulation, and Quality of life (QOL) of malignant growth patients. Herbal drugs can deflect chemotherapy from executing malignancy cells certain herbal products improve the impact of chemotherapy. Nanoparticles of herbal drugs are used to target the drug in a specific site which results better efficacy and better bioavailability than any other formulations. The investigation of nanoparticles on herbal drugs to treat cancer, for example. Sesquiterpenoid from Tussilagofarfara, oligopeptides from Perillafrutescens, Oxymatrine from Sophora Flavescens, Curcumin from curcuma longa, vincristine from Catharanthusroseus, Berberine from Berberis vulgaris, Quercetin from Cuscutachinensis, Paclitaxel from Taxusbrevifolia, Camptothein from camptotheca acuminate, Catechins from camellia sinesis etc. In summary, this review emphasizes how important herbal nanoparticles are to boosting the effectiveness of cancer treatment. Through clarifying the limitations of chemotherapy and highlighting the advantages of novel herbal nanoparticle formulations, this study adds to the current conversation on complementary and alternative methods to cancer treatment.

Beneficial effects of oxymatrine from Sophora flavescens on alleviating Ulcerative colitis by improving inflammation and ferroptosis

Ethnopharmacological relevanceSophora flavescens is often used in traditional Chinese medicine for skin issues, diarrhea, and vaginal itching (Plant names have been checked with http://www.the/plant/list.org on Feb 22nd, 2024). Oxymatrine (OY), a major bioactive compound from Sophora flavescens, is commonly used in China to treat ulcerative colitis, but its mechanisms are still unclear. Aim of the studyRecent studies have found that the crosstalk between ferroptosis and inflammation is an important mechanism in the pathogenesis of UC. The aim of this study was to investigate the potential underlying mechanisms of OY treatment on DSS-induced ulcerative colitis, specifically focusing on the processes of ferroptosis and inflammation. Materials and methodsBioinformatics methods were used to identify key targets of OY for ferroptosis and inflammation in ulcerative colitis, based on GEO data and FerrDb database. Then, 4% DSS solution was used to induce UC model. OY’s impact on morphological changes was assessed using colon views, Hematoxylin and eosin (HE) staining, and transmission electron microscopy (TEM). Ferroptosis phenotype index and inflammations factors were detected by ELISA or chem-bio detection kits.The screen out hub related genes about ferroptosis and inflammation were verified by RT-PCR, immunohistochemistry (IHC), and western blotting (WB) respectively. ResultsBioinformatics results show that there are 16 key target genes involved in ferroptosis and inflammation interaction of OY treatment for UC, such as IL6, NOS2, IDO1, SOCS1, and DUOX. The results of animal experiments show that OY could depress inflammatory factors (IL-1β, IL-6, TNF-α, HMGB1, and NLRP3) and reduce iron deposition (Fe2+, GSH). Additionally, OY suppressed the hub genes or proteins expression involved in ferroptosis and inflammation, including IL-1β, IL-6, NOS2, HIF1A, IDO1, TIMP1, and DUOX2. ConclusionThis present study combines bioinformatics, molecular biology, and animal experimental research evidently demonstrated that OY attenuates UC by improving ferroptosis and inflammation, mainly target to the expression of IL-1β, IL-6, NOS2, HIF1A, IDO1, TIMP1, and DUOX2.

Sophoraflavanone G Inhibits RANKL-Induced Osteoclastogenesis via MAPK/NF-κB Signaling Pathway.

Osteoporosis is a common chronic bone metabolism disorder characterized by decreased bone mass and reduced bone density in the bone tissue. Osteoporosis can lead to increased fragility of the skeleton, making it prone to brittle fractures. Osteoclasts are macrophage-like cells derived from hematopoietic stem cells, and their excessive activity in bone resorption leads to lower bone formation than absorption during bone remodeling, which is one of the important factors inducing osteoporosis. Therefore, how to inhibit osteoclast formation and reducing bone loss is an important direction for treating osteoporosis. Sophoraflavanone G, derived from Sophora flavescens Alt and Rhizoma Drynariae, is a flavonoid compound with various biological activities. However, there have been few studies on osteoporosis and osteoclasts so far. Therefore, we hypothesize that genistein G can inhibit osteoclast differentiation, alleviate bone loss phenomenon, and conduct in vitro and in vivo experiments for research and verification purposes.

Metabolic Profiling for Unveiling Mechanisms of Kushenol F against Imiquimod-Induced Psoriasis with UHPLC/MS Analysis.

Psoriasis is a common chronic immune-mediated inflammatory skin disorder. Sophora flavescens Alt. (S. flavescens) has been widely acknowledged in the prevention and treatment of psoriasis. Kushenol F (KSCF) is a natural isopentenyl flavonoid extracted from the root of S. flavescens. We aimed to investigate the effect and mechanism of KSCF on imiquimod (IMQ)-induced psoriasis-like skin lesions in mice. A mouse model of psoriasis was induced with 5% IMQ for 5 days, and the mice were given KSCF dermally for 5 days. Changes in skin morphology, the psoriasis area, the severity index (PASI), and inflammatory factors of psoriasis-like skin lesions were evaluated. Metabolites in the psoriasis-like skin lesions were analyzed with ultra-high-performance liquid chromatography/mass spectrometry followed by a multivariate statistical analysis to identify the differential metabolites and metabolic pathway. The results of the present study confirmed that KSCF significantly reduced PASI scores, epidermal thickening, and epidermal cell proliferation and differentiation. KSCF also reduced the levels of interleukin (IL)-1β, IL-6, IL-8, IL-17A, IL-22, IL-23, and tumor necrosis factor (TNF)-α in the injured skin tissues while increasing IL-10 content. KSCF significantly regulated metabolites in the skin samples, and a total of 161 significant metabolites were identified. These differential metabolites involved sphingolipid and linoleic acid metabolism and steroid hormone biosynthesis. Collectively, KSCF inhibited the inflammatory response to prevent IMQ-induced psoriasis-like skin lesions in mice by call-backing the levels of 161 endogenous metabolites and affecting their related metabolic pathways. KSCF has the potential to be developed as a topical drug for treating psoriasis symptoms.

Antifungal Effects of Fermented Sophora flavescens and Eleutherococcus sessiliflorus Extract

In this study, a microbial strain was isolated from humus soil to ferment Sophora flavescens and Eleutherococcus sessiliflorus extracts. The isolated microbial was identified as the Bacillus genus by 16S rRNA sequence analysis. The fermented plant extracts exhibited antifungal effects against four types plant pathogen, P. carotorum, B. cinerea, C. fructicola Sau-3, and C. gloeosporioides, according to incubation time. In particular, the fermented plant extracts showed the most activity for Colletotrichum genus in inhibiting mycelium growth. Metabolite changes in fermented S. flavescens and E. sessiliflorus extracts were confirmed through LC-Q-TOF/MS. Flavonoid and peptide derivatives were improved in fermented S. flavescens and E. sessiliflorus extracts compared to their unfermented counterparts. This study suggested that isolated Bacillus microbial fermentation could be a valuable tool in improving the bioactivity of S. flavescens and E. sessiliflorus extracts, with the potential to form more environmentally friendly antifungal agents.

A review on the pharmacology, pharmacokinetics and toxicity of sophocarpine.

Sophocarpine is a natural compound that belongs to the quinolizidine alkaloid family, and has a long history of use and widespread distribution in traditional Chinese herbal medicines such as Sophora alopecuroides L., Sophora flavescens Ait., and Sophora subprostrata. This article aims to summarize the pharmacology, pharmacokinetics, and toxicity of sophocarpine, evaluate its potential pharmacological effects in various diseases, and propose the necessity for further research and evaluation to promote its clinical application. A large number of studies have shown that it has anti-inflammatory, analgesic, antiviral, antiparasitic, anticancer, endocrine regulatory, and organ-protective effects as it modulates various signaling pathways, such as the NF-κB, MAPK, PI3K/AKT, and AMPK pathways. The distribution of sophocarpine in the body conforms to a two-compartment model, and sophocarpine can be detected in various tissues with a relatively short half-life. Although the pharmacological effects of sophocarpine have been confirmed, toxicity and safety assessments and reports on molecular mechanisms of its pharmacological actions have been limited. Given its significant pharmacological effects and potential clinical value, further research and evaluation are needed to promote the clinical application of sophocarpine.

Liquid Chromatography/Tandem Mass Spectrometry Analysis of Sophora flavescens Aiton and Protective Effects against Alcohol-Induced Liver Injury and Oxidative Stress in Mice.

In this study, we investigated the hepatoprotective effects of an ethanol extract of Sophora flavescens Aiton (ESF) on an alcohol-induced liver disease mouse model. Alcoholic liver disease (ALD) was caused by the administration of ethanol to male C57/BL6 mice who were given a Lieber-DeCarli liquid diet, including ethanol. The alcoholic fatty liver disease mice were orally administered ESF (100 and 200 mg/kg bw/day) or silymarin (50 mg/kg bw/day), which served as a positive control every day for 16 days. The findings suggest that ESF enhances hepatoprotective benefits by significantly decreasing serum levels of aspartate transaminase (AST) and alanine transaminase (ALT), markers for liver injury. Furthermore, ESF alleviated the accumulation of triglyceride (TG) and total cholesterol (TC), increased serum levels of superoxide dismutase (SOD) and glutathione (GSH), and improved serum alcohol dehydrogenase (ADH) activity in the alcoholic fatty liver disease mice model. Cells and organisms rely on the Kelch-like ECH-associated protein 1- Nuclear factor erythroid 2-related factor 2 (Keap1-Nrf2) system as a critical defensive mechanism in response to oxidative stress. Therefore, Nrf2 plays an important role in ALD antioxidant responses, and its level is decreased by increased reactive oxidation stress (ROS) in the liver. ESF increased Nrf2, which was decreased in ethanol-damaged livers. Additionally, four polyphenol compounds were identified through a qualitative analysis of the ESF using LC-MS/MS. This study confirmed ESF's antioxidative and hangover-elimination effects and suggested the possibility of using Sophora flavescens Aiton (SF) to treat ALD.

Selective separation of structurally similar alkaloids by graphene oxide membranes

Matrine (MT) and oxymatrine (OMT) are alkaloids coexisting in Sophora flavescens, and they have similar structure but different clinical applications. Graphene oxide (GO) membranes with different oxidation degrees were used to explore the separation mechanism of MT and OMT. When the ratios of O-C=O and C=O groups remained basically unchanged, the higher C-OH content and the lower C-O-C content on the GO nanosheets provided higher O/C ratios, more negative Zeta potentials, stronger hydrophilicity, rougher surface, and larger interlayer spacing of the GO membranes. With the increases in the O/C ratio, the rejection rates for MT and OMT exhibited opposite trends, and it was considered that a competitive relationship between MT and OMT on the membrane converted from hydrophilic interaction to electrostatic interaction. Within the separation channels limited by the GO nanosheets, the tertiary amine in the alkaloid catalyzed C-O-C group ring opening and formed C-OH or O-C=O groups. As the C-OH content of the original GO membranes increased, the stability during alkaloid separation was improved. The GO-5 membrane showed stable separation ability within 72 h, and the separation factor of MT and OMT almost doubled during the secondary membrane process. This study provides new insight into the application of membrane technology for the separation of similar molecules of pharmacodynamic substances in traditional Chinese medicine.

Radix Sophorae Flavescentis of Sophora flavescens Aiton inhibits LPS-induced macrophage pro-inflammatory response via regulating CFHR2 expression

Ethnopharmacological relevanceLong-term chronic inflammation often leads to chronic diseases. Although Sophora flavescens has been shown to have anti-inflammatory properties, its detailed molecular mechanism is still unknown. Aim of studyThis study investigated the effect of Radix Sophorae Flavescentis on the LPS-induced inflammatory response in macrophages. Materials and methodsLPS was used to induce the peritoneal macrophages to simulate the inflammatory environment in vitro. Different concentrations of Radix Sophorae Flavescentis-containing (medicated) serum were used for intervention. The peritoneal macrophages were identified by using hematoxylin-eosin and immunofluorescence staining. ELISA was used to measure the TNF-α and IL-6 expression to determine the concentration of LPS. ELISA and Western blot (WB) were used to detect the PGE2 and CFHR2 expression in each group, respectively. The lentiviral vector for interference and overexpression of the CFHR2 gene was constructed, packaged, and transfected into LPS-induced macrophages. The transfection efficiency was verified by WB. Then, ELISA was used to detect the TNF-α, PGE2, and IL-6 expression. WB was used to detect the CFHR2, iNOS, COX-2, TLR2, TLR4, IFN-γ, STAT1, and p-STAT1 expression. ResultsThe primary isolated cells were identified as macrophages. The LPS-treated macrophages exhibited significantly higher expression of PGE2 and CFHR2, and the inflammatory factors TNF-α and IL-6, as well as iNOS, COX-2, TLR2, TLR4, IFN-γ, STAT1, and p-STAT1 expression compared with the control group (P < 0.05). The TNF-α, PGE2, and IL-6 levels, as well as CFHR2, iNOS, COX-2, TLR2, TLR4, IFN-γ, STAT1, and p-STAT1 expression were considerably lower in the LPS-induced+10% medicated-serum group, LPS-induced+20% medicated-serum group, and shCFHR interference group compared with the LPS group (P < 0.05). ConclusionRadix Sophorae Flavescentis might mediate CFHR2 expression and play an important role in inhibiting the LPS-induced pro-inflammatory response of macrophages. Radix Sophorae Flavescentis could be a potential treatment for LPS-induced related inflammatory diseases.

Mechanism of Sophorae Flavescentis Radix against ovarian cancer via new pharmacology, molecular docking, and experimental verification.

The study aims to elucidate the pharmacological mechanisms of Sophorae Flavescentis Radix (SFR, Kushen) against ovarian cancer (OV) by employing an integrated approach that encompasses network pharmacology, molecular docking, and experimental validation. The effective components and potential targets of SFR were identified through screening the Traditional Chinese Medicine Systems Pharmacology (TSMSP) public database using network pharmacology. Core anti-OV targets were pinpointed using protein-protein interaction (PPI) networks. Datasets from The Cancer Genome Atlas (TCGA), the Human Protein Atlas (HPA), and Gene Expression Profiling Interactive Analysis (GEPIA) were used to investigate the mRNA and protein expressions of critical target genes in both normal and cancerous ovarian tissues, alongside their relationship to overall ovarian survival. Functional and pathway enrichment assessments of putative targets were carried out with Gene Ontology (GO) and the Kyoto Encyclopedia of Genes and Genomes (KEGG). The assessment of stable binding effects was conducted through molecular docking with quercetin, luteolin, and formononetin, and validated by anti-OV cell activity. The investigation identified 22 active SFR components yielding 152 potential targets following the intersection with known OV targets. Analysis of PPI network highlighted 13 crucial target genes, including tumor necrosis factor (TNF) and interleukin-1A (IL-1A). GO enrichment analysis covered 703 biological activities, 72 cellular components, and 144 chemical functions. The KEGG enrichment analysis suggested that anti-cancer effects of SFR are mediated by the TNF, interleukin-17 (IL-17), and AGE-RAGE signaling pathways. Molecular docking demonstrated that TNF and IL-1A were stable and strong binding to quercetin, luteolin, and formononetin, indicating that these stable structures significantly inhibited A2780 OV cell viability. This study demonstrated the ability of TNF and IL-1A combined with quercetin, luteolin, and formononetin to decrease the activity of OV cells, suggesting potential therapeutic effect against OV.

A fluorescence method based on malachite green/aptamer for detection of ochratoxin A in traditional Chinese medicines

A label-free fluorescence method based on malachite green/aptamer was developed for the detection of ochratoxin A(OTA) in traditional Chinese medicines. Malachite green itself exhibits weak fluorescence. Upon interaction with the aptamer specific to OTA, the G-quadruplex structure of the aptamer provides a protective microenvironment for malachite green, which significantly enhances its fluorescence signal. After OTA is added, preferential binding occurs between the aptamer and OTA, and malachite green will be released from the aptamer, which weakens the fluorescence signal. According to this principle, this paper established a fluorescence method with the aptamer of OTA as the recognition element and malachite green as the fluorescent probe for the detection of OTA in traditional Chinese medicines. The key experimental factors such as the concentrations of metal ions, aptamer, and malachite green were optimized to improve the performance of the method. OTA was detected under the optimal experimental conditions, and the results showed that with the increase in OTA concentration, the fluorescence signal gradually weakened. Within the range of 20-1 000 nmol·L~(-1), the OTA concentration was linearly correlated with the fluorescence signal ratio ΔF/F(ΔF=F_0-F, where F_0 is the fluorescence signal of aptamer/malachite green, and F is the fluorescence signal of OTA/aptamer/malachite green), with R~2 of 0.995. The limit of detection of the established method was 7.1 nmol·L~(-1). Furthermore, three substances structurally similar to OTA and two mycotoxins that may coexist with OTA were selected for experiments, which aimed to examine the cross-reactivity and specificity of the established method. The cross-reactivity experiments demonstrated that the interferers did not significantly affect the fluorescence signal of the detection system. The specificity experiments revealed that when mycotoxins were mixed with OTA, the fluorescence signal generated by the mixture closely resembled that of OTA itself. The results indicated that even in the presence of interferents, the established method remained unaffected and demonstrated excellent specificity. Additionally, this method exhibited remarkable reproducibility and stability. In the case of simple centrifugation and dilution of traditional Chinese medicine samples(Puerariae Lobatae Radix, Sophorae Flavescentis Radix, and Periplocae Cortex), the OTA detection method was applicable, with recovery rates ranging from 91.5% to 121.3%. Notably, this approach does not need complex pretreatment of traditional Chinese medicines while offering simple operation, low detection costs, and short detection time. Furthermore, by incorporating aptamers into the quality evaluation of traditional Chinese medicines, this method expands the application scope of aptamers.