Screening and characterization of potential anti-gout components from Polygonum cuspidatum by integration off-line two-dimensional liquid chromatography-mass spectrometry with affinity ultrafiltration and on-line HPLC-ABTS.

Polygonum cuspidatum (P. cuspidatum) is a traditional herbal medicine with a long history and proven efficacy in treating gout. However, due to the complexity of composition and extensive content distribution, the substance basis of its anti-gout effectiveness is still unclear. A strategy was proposed via integrating off-line two-dimensional liquid chromatography (2D-LC) and targeted rapid screening technology based on ultrafiltration-liquid chromatography-mass spectrometry (UF-LC/MS) and on-line high-performance liquid chromatography-2, 2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (HPLC-ABTS) to accomplish high coverage and high throughput screening of anti-gout components from P. cuspidatum. As a result, twenty components were screened from P. cuspidatum extract with both xanthine oxidase (XOD) inhibitory activity and free radical scavenging activity, then were preliminarily identified by high-resolution electrospray ionization-quadrupole-time-of-flight mass spectrometer (ESI-Q-TOF/MS). The screened results were verified by the in vitro assays. Meanwhile, molecular docking further elucidated that the screened bioactive ingredients had favourable binding capabilities with XOD. The performance of this study can achieve high efficiency and high coverage screening of the anti-gout components from P. cuspidatum, which provides methodology and strategy support for the rapid screening of bioactive ingredients from complex medicinal plants.

Surface molecularly imprinted polymers based on magnetic multi-walled carbon nanotubes for the highly selective purification of resveratrol from crude extracts of Vitis vinifera, Arachis hypogaea, and Polygonum cuspidatum.

In this work, surface molecularly imprinted polymers based on magnetic multi-walled carbon nanotubes were prepared for the specific recognition and adsorption of resveratrol. The functionalization of magnetic multi-walled carbon nanotubes and the synthesis process of surface molecularly imprinted polymers were optimized. Characterizations were performed to demonstrate the successful synthesis of the imprinted materials. The imprinted materials showed satisfactory adsorption capacity of resveratrol (45.73 ± 1.72 mg/g) and excellent selectivity (imprinting factor 2.89 ± 0.15). In addition, the imprinted materials were used as adsorbents in molecularly imprinted solid-phase extraction for the purification of resveratrol from crude extracts of some food and medicinal resources, achieving recoveries of 93.69%-95.53% with high purities of 88.37%-92.33%. Moreover, the purified products exhibited extremely strong free radical scavenging activity compared with crude extracts. Overall, this work provided a promising approach for the highly selective purification of resveratrol from natural resources, which would contribute to the application of this valuable compound in the food/nutraceutical fields.

Screening of Key Components for Melanogenesis Inhibition of Polygonum cuspidatum Extract Based on the Spectrum-Effect Relationship and Molecular Docking.

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.

Foliar application of nettle and Japanese knotweed extracts on Vitis vinifera: impact on phenylpropanoid biosynthesis and antioxidant activity during veraison and harvest of cv. Touriga Franca.

BACKGROUND: Plant-based extracts have been recently used as sustainable tools to improve biotic and abiotic stress tolerance and increase grape (Vitis vinifera L.) quality. However, knowledge about the effect of these extracts on secondary metabolism compounds, that are fundamental for grape and wine quality, is still scarce. In this study, a trial was installed in an experimental vineyard with the variety Touriga Franca located at University of Trás-os-Montes e Alto Douro, Baixo Corgo sub-region of the Douro Demarcated Region, Portugal in two growing seasons: 2019 and 2020. The aim was to evaluate the effect of foliar application of nettle (Urtica spp.) extract (NE) and Japanese knotweed (Reynoutria japonica) extract (JKE) on grapevines leaves and berries bioactive compounds contents and antioxidant activity, at veraison and harvest. RESULTS: The application of NE increased the total carotenoids in leaves and the total phenolics content and the antioxidant activity (ferric reducing antioxidant power, FRAP) in berries while JKE increased flavonoids content in leaves and the antioxidant activity (2,2-diphenyl-1-picrylhydrazyl, DPPH) in berries. CONCLUSION: These extracts seem to have a stimulatory effect on grapevine, enhancing bioactive compounds contents and antioxidant capacity and, consequently, the physiological performance of the plant and the quality of the berries. © 2024 Society of Chemical Industry.

Effects of Fermented Polygonum cuspidatum on the Skeletal Muscle Functions.

Plant extract fermentation is widely employed to enhance the nutritional and pharmaceutical value of functional foods. Polygonum cuspidatum (Pc) contains flavonoids, anthraquinones, and stilbenes, imparting protective effects against inflammatory diseases, cancer, diabetes, and cardiovascular diseases. However, the effects of fermented Pc on skeletal muscle strength remain unexplored. In this study, we generated fermented Pc using a complex of microorganisms containing Lactobacillus spp. (McPc) and assessed its effects on muscle strength and motor function in mice. Compared to unfermented Pc water extract, elevated levels of emodin and resveratrol were noted in McPc. This was identified and quantified using UPLC-QTOF/MS and HPLC techniques. Gene expression profiling through RNA-seq and quantitative RT-PCR revealed that McPc administration upregulated the expression of genes associated with antioxidants, glycolysis, oxidative phosphorylation, fatty acid oxidation, and mitochondrial biogenesis in cultured C2C12 myotubes and the gastrocnemius muscle in mice. McPc significantly improved skeletal muscle strength, motor coordination, and traction force in mice subjected to sciatic neurectomy and high-fat diet (HFD). McPc administration exhibited more pronounced improvement of obesity, hyperglycemia, fatty liver, and hyperlipidemia in HFD mice compared to control group. These findings support the notion that emodin and resveratrol-enriched McPc may offer health benefits for addressing skeletal muscle weakness.

Preliminary study on molecular mechanism of COVID-19 intervention by Polygonum cuspidatum through computer bioinformatics.

To explore the mechanism of action of Polygonum cuspidatum in intervening in coronavirus disease 2019 using a network pharmacology approach and to preliminarily elucidate its mechanism. The active ingredients and action targets of P cuspidatum were classified and summarized using computer virtual technology and molecular informatics methods. The active ingredients and relevant target information of P cuspidatum were identified using the TCM Systematic Pharmacology Database and Analysis Platform, the TCM Integrated Pharmacology Research Platform v2.0, and the SwissTarget database. The GENECARDS database was used to search for COVID-19 targets. The STRING database was analyzed and combined with Cytoscape 3.7.1 software to construct a protein interaction network map to screen the core targets. Kyoto Encyclopedia of Genes and Genomes pathway enrichment analysis was then performed. The core compound, polydatin, was selected and the core targets were analyzed by computer virtual docking using software such as discovery studio autodock tool. In vitro cell models were constructed to experimentally validate the activity of the core compound, polydatin. By computer screening, we identified 9 active ingredients and their corresponding 286 targets from P cuspidatum. A search of the GENECARDS database for COVID-19 yielded 303 core targets. By mapping the active ingredient targets to the disease targets, 27 overlapping targets could be extracted as potential targets for the treatment of COVID-19 with P cuspidatum. In addition, the enrichment analysis of Kyoto Encyclopedia of Genes and Genomes pathway on core targets showed that the coronavirus disease, MAPK signaling pathway, NF kappa B signaling pathway, and other signaling pathways were highly enriched. Combined with the degree-high target analysis in the protein interaction network, it was found to be mainly concentrated in the NF-kappaB (NF-κB) signaling pathway, indicating that the NF-κB signaling pathway may be an important pathway for P cuspidatum intervention. In vitro assays showed no effect of 0.1 to 10 µM polydatin on cell viability, but an inhibitory effect on the transcriptional activity of NF-κB-RE. Molecular docking showed stable covalent bonding of polydatin molecules with Il-1ß protein at residue leu-26, TNF protein ser-60, residue gly-121, and residue ile-258 of ICAM-1 protein, indicating a stable docking result. The treatment of COVID-19 with P cuspidatum is characterized by multi-component, multi-target, and multi-pathway, which can exert a complex network of regulatory effects through the interaction between different targets, providing a new idea and basis for further exploration of the mechanism of action of P cuspidatum in the treatment of COVID-19.

Exploiting exotic pathogens as mycoherbicides against invasive alien weeds: Japanese knotweed as a case study.

Plant species have been introduced increasingly into non-native ranges, where many have become exotic weeds with adverse impacts on native ecosystems, as well as on farming and other livelihoods. In biological control, the classical or inoculative approach is the one most commonly used for the management of invasive alien weeds and is based on the use of co-evolved natural enemies from the native range to control the invasive weed. Typically, the inundative or mycoherbicide approach targets problematic weeds using local plant pathogens that, in the case of introduced species, have 'jumped' onto the exotic host. The leaf-spot fungus, Mycosphaerella polygoni-cuspidati, co-evolved with its host, Reynoutria (Fallopia) japonica (Japanese knotweed), in Japan and has a unique history of being investigated both as a classical biological control agent and a mycoherbicide against this highly invasive weed in the United Kingdom and North America. Here, we highlight our research on M. polygoni-cuspidati as part of a biological control programme for Japanese knotweed and review the potential of mycoherbicides using exotic pathogens for the management of invasive alien weeds. © 2023 The Authors. Pest Management Science published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.

Polygonum Cuspidatum Alcohol Extract Exerts Analgesic Effects via the MAPK/ERK Signaling Pathway.

Objective: Traditional Chinese medicine Polygonum cuspidatum (PC) has significant effects on reducing pain. In this study, we investigated the analgesic effects of the alcohol extract of PC on three types of inflammatory pain and explored its mechanism. Methods: Potential targets for the analgesic effects of the main active components of PC alcohol extract were screened by network pharmacology and molecular docking. Three different inflammatory pain mouse models (acetic acid twisting, formalin foot swelling, and xylene ear swelling) were used to study the analgesic effects of PC. The expression of latent signaling pathways in L4-6 spinal cord tissues in formalin foot swelling mice was evaluated using real-time qPCR (RT-qPCR), Western blot (WB), and immunohistochemistry (IHC) analyses. Results: Network pharmacology analysis shows that PC analgesic mechanism is related to the MAPK/ERK signaling pathway. The five main active components of PC have good docking ability with JNK and p38. PC alcohol extract significantly reduced the pain behavior and alleviated inflammatory reactions in three mouse models, inhibited the mRNA and protein phosphorylation levels of JNK, ERK, p38, and CREB in spinal cord tissues. Conclusion: PC alcohol extract can inhibit inflammation and alleviate pain, which is related to its inhibition of the MAPK/ERK signaling pathway in spinal cord. Thus, PC alcohol extract is a promising candidate for pain treatment.

Fallopia japonica and Fallopia × bohemica extracts cause ultrastructural and biochemical changes in root tips of radish seedlings.

Japanese knotweed (Fallopia japonica) and Bohemian knotweed (Fallopia × bohemica) are invasive plants that use allelopathy as an additional mechanism for colonization of the new habitat. Allelochemicals affect the growth of roots of neighboring plants. In the present study, we analyze the early changes associated with the inhibited root growth of radish seedlings exposed to aqueous extracts of knotweed rhizomes for 3 days. Here, we show that cells in the root cap treated with the knotweed extracts exhibited reduced cell length and displayed several ultrastructural changes, including the increased abundance of dilated ER cisternae filled with electron-dense material (ER bodies) and the accumulation of dense inclusions. Moreover, mitochondrial damage was exhibited in the root cap and the meristem zone compared to the non-treated radish seedlings. Furthermore, malfunction of the intracellular redox balance system was detected as the increased total antioxidative capacity. We also detected increased metacaspase-like proteolytic activities and, in the case of 10% extract of F. japonica, increased caspase-like proteolytic activities. These ultrastructural and biochemical effects could be the reason for the more than 60% shorter root length of treated radish seedlings compared to controls.

Deposition is a phosphorus source for Fallopia japonica during early-stage primary succession.

Phosphorus is a key plant nutrient linked to plant growth during the early stages of primary succession in volcanic soils. Available phosphorus is thought to include soil and atmospheric phosphorus, but it is not well understood. Here, we focused on deposition as a potential phosphorus source. We evaluated the contribution of deposition to phosphorus uptake and growth in Fallopia japonica, a key pioneer species of primary succession. When we experimented with growing F. japonica under field conditions, F. japonica not covered by a roof absorbed more phosphorus than that covered by the roof, suggesting the influence of total (dry + wet) deposition. Furthermore, we tested the effects of deposition by treating F. japonica seedlings with wet deposition or distilled water in six volcanic soils. Plants that received the wet deposition treatment exhibited higher phosphorus contents and growth rates than those treated with distilled water. The phosphorus from wet deposition and the phosphorus from soil contributed nearly equally to F. japonica development. Our findings suggest that F. japonica grows during primary succession and builds up the phosphorus cycle by absorbing a trace amount of phosphorus from deposition and volcanic soils.

[Site-directed mutagenesis enhances the activity of benzylidene acetone synthase of polyketide synthase from Polygonum cuspidatum].

Polygonum cuspidatum polyketide synthase 1 (PcPKS1) has the catalytic activity of chalcone synthase (CHS) and benzylidene acetone synthase (BAS), which can catalyze the production of polyketides naringenin chalcone and benzylidene acetone, and then catalyze the synthesis of flavonoids or benzylidene acetone. In this study, three amino acid sites (Thr133, Ser134, Ser33) that may affect the function of PcPKS1 were identified by analyzing the sequences of PcPKS1, the BAS from Rheum palmatum and the CHS from Arabidopsis thaliana, as well as the conformation of the catalytic site of the enzyme. Molecular modification of PcPKS1 was carried out by site-directed mutagenesis, and two mutants were successfully obtained. The in vitro enzymatic reactions were carried out, and the differences in activity were detected by high performance liquid chromatography (HPLC). Finally, mutants T133LS134A and S339V with bifunctional activity were obtained. In addition to bifunctional activities of BAS and CHS, the modified PcPKS1 had much higher BAS activity than that of the wild type PcPKS1 under the conditions of pH 7.0 and pH 9.0, respectively. It provides a theoretical basis for future use of PcPKS1 in genetic engineering to regulate the biosynthesis of flavonoids and raspberry ketones.

Fallopia japonica Root Extract Ameliorates Ovalbumin-Induced Airway Inflammation in a CARAS Mouse Model by Modulating the IL-33/TSLP/NF-κB Signaling Pathway.

Fallopia japonica (Asian knotweed) is a medicinal herb traditionally used to treat inflammation, among other conditions. However, the effects of F. japonica root extract (FJE) on airway inflammation associated with combined allergic rhinitis and asthma (CARAS) and the related mechanisms have not been investigated. This study examined the effect of FJE against CARAS in an ovalbumin (OVA)-induced CARAS mouse model. Six-week-old male BALB/c mice were randomly segregated into six groups. Mice were sensitized intraperitoneally with OVA on days 1, 8, and 15, and administered saline, Dexamethasone (1.5 mg/kg), or FJE (50, 100, or 200 mg/kg) once a day for 16 days. Nasal symptoms, inflammatory cells, OVA-specific immunoglobulins, cytokine production, mast cell activation, and nasal histopathology were assessed. Administration of FJE down-regulated OVA-specific IgE and up-regulated OVA-specific IgG2a in serum. FJE reduced the production of T helper (Th) type 2 cytokines, and the Th1 cytokine levels were enhanced in nasal and bronchoalveolar lavage fluid. Moreover, FJE positively regulated allergic responses by reducing the accumulation of inflammatory cells, improving nasal and lung histopathological characteristics, and inhibiting inflammation-associated cytokines. FJE positively modulated the IL-33/TSLP/NF-B signaling pathway, which is involved in regulating inflammatory cells, immunoglobulin levels, and pro-inflammatory cytokines at the molecular level.

Exploring the inhibition mechanism of interleukin-1-beta in gouty arthritis by polygonum cuspidatum using network pharmacology and molecular docking: A review.

Polygonum cuspidatum (Huzhang, HZ) is one of the commonly used traditional Chinese medicines for treating gouty arthritis (GA), but the specific mechanism is not clear. This study employed network pharmacology and molecular docking techniques to examine the molecular mechanisms underlying the therapeutic effects of HZ on GA. The network pharmacology approach, including active ingredient and target screening, drug-compound-target-disease network construction, protein-protein interaction (PPI) networks, enrichment analysis, and molecular docking, was used to explore the mechanism of HZ against GA. Ten active ingredients of HZ were predicted to interact with 191 targets, 14 of which interact with GA targets. Network pharmacology showed that quercetin, physovenine, luteolin, and beta-sitosterol are the core components of HZ, and IL (interleukin)-1ß, IL-6, and tumor necrosis factor (TNF) are the core therapeutic targets. The mechanism of HZ in GA treatment was shown to be related to the IL-17 signaling pathway, NOD-like receptor signaling pathway, and Toll-like receptor signaling pathway, and is involved in the inflammatory response, positive regulation of gene expression, cellular response to lipopolysaccharide, and other biological processes. Molecular docking showed that all four core compounds had good binding properties to IL-1ß, with luteolin and beta-sitosterol showing better docking results than anakinra, suggesting that they could be used as natural IL-1ß inhibitors in further experimental studies. The mechanism of action of HZ against GA has multi-target and multi-pathway characteristics, which provides an important theoretical basis for the study of the active ingredients of HZ as natural IL-1ß inhibitors.

Evaluation of the Biological Properties of an Optimized Extract of Polygonum cuspidatum Using Ultrasonic-Assisted Extraction.

Phytochemicals are natural compounds found in plants that have potential health benefits such as antioxidants, anti-inflammatory and anti-cancer properties, and immune reinforcement. Polygonum cuspidatum Sieb. et Zucc. is a source rich in resveratrol, traditionally consumed as an infusion. In this study, P. cuspidatum root extraction conditions were optimized to increase antioxidant capacity (DPPH, ABTS+), extraction yield, resveratrol concentration, and total polyphenolic compounds (TPC) via ultrasonic-assisted extraction using a Box-Behnken design (BBD). The biological activities of the optimized extract and the infusion were compared. The optimized extract was obtained using a solvent/root powder ratio of 4, 60% ethanol concentration, and 60% ultrasonic power. The optimized extract showed higher biological activities than the infusion. The optimized extract contained 16.6 mg mL-1 resveratrol, high antioxidant activities (135.1 µg TE mL-1 for DPPH, and 230.4 µg TE mL-1 for ABTS+), TPC (33.2 mg GAE mL-1), and extraction yield of 12.4%. The EC50 value (effective concentration 50) of the optimized extract was 0.194 µg mL-1, which revealed high cytotoxic activity against the Caco-2 cell line. The optimized extract could be used to develop functional beverages with high antioxidant capacity, antioxidants for edible oils, functional foods, and cosmetics.

Discovery of the potential neuraminidase inhibitors from Polygonum cuspidatum by ultrafiltration combined with mass spectrometry guided by molecular docking.

Neuraminidase is an important target in the treatment of the influenza A virus. Screening natural neuraminidase inhibitors from medicinal plants is crucial for drug research. This study proposed a rapid strategy for identifying neuraminidase inhibitors from different crude extracts (Polygonum cuspidatum, Cortex Fraxini, and Herba Siegesbeckiae) using ultrafiltration combined with mass spectrometry guided by molecular docking. Firstly, the main component library of the three herbs was established, followed by molecular docking between the components and neuraminidase. Only the crude extracts with numbers of potential neuraminidase inhibitors identified by molecular docking were selected for ultrafiltration. This guided approach reduced experimental blindness and improved efficiency. The results of molecular docking indicated that the compounds in Polygonum cuspidatum demonstrated good binding affinity with neuraminidase. Subsequently, ultrafiltration-mass spectrometry was employed to screen for neuraminidase inhibitors in Polygonum cuspidatum. A total of five compounds were fished out, and they were identified as trans-polydatin, cis-polydatin, emodin-1-O-ß-D-glucoside, emodin-8-O-ß-D-glucoside, and emodin. The enzyme inhibitory assay showed that they all had neuraminidase inhibitory effects. In addition, the key residues of the interaction between neuraminidase and fished compounds were predicted. In all, this study could provide a strategy for the rapid screening of the potential enzyme inhibitors from medicinal herbs.

Assessing the relative impacts and economic costs of Japanese knotweed management methods.

Sustainable land management encompasses a range of activity that balance land use requirements with wider conservation and ecosystem impact considerations. Perennial invasive alien plants (IAPs), such as Japanese knotweed, cause severe ecological and socio-economic impacts, and methods to control their spread also come at a cost. Synthetic herbicides are generally viewed as less sustainable and more ecologically damaging than alternative approaches. Here we used a comparative Life Cycle Assessment to evaluate the sustainability of herbicide-based management approaches and physical alternatives, using a large-scale Japanese knotweed field study as a model IAP system. Glyphosate-based methods elicited the lowest environmental impacts and economic costs during production. Geomembrane covering and integrated physiochemical methods were the costliest and imposed the greatest impacts. We discuss the costs and benefits of chemical and physical approaches for the sustainable management of invaded land and question how sustainable environmental stewardship is defined for the control of IAPs.

Ultra-high performance liquid chromatography-quadrupole/time-of-flight mass spectrometry-based lipidomics reveals key lipid molecules as potential therapeutic targets of Polygonum cuspidatum against hyperlipidemia in a hamster model.

Polygonum cuspidatum is a homology of traditional medicine and functional food widely distributed around the world. Our previous study on the hyperlipidemic animal model demonstrated that Polygonum cuspidatum was effective in ameliorating hyperlipidemia, which is characterized by lipid disorders. Herein, the regulatory effect of Polygonum cuspidatum on lipid metabolism needs to be known if its hypolipidemic mechanism is desired to clarify. In this study, an ultra-high performance liquid chromatography-quadrupole/time-of-flight mass spectrometry-based lipidomic strategy was first applied to investigate the lipidomic patterns of high-fat diet-induced hyperlipidemic hamsters when treated with Polygonum cuspidatum. The results showed that Polygonum cuspidatum improved the lipidomic profile of hyperlipidemia. A total of 65 differential lipids related to the hypolipidemic effect of Polygonum cuspidatum were screened out and identified, and these differential lipids covered various categories, such as phosphatidylcholines, phosphatidylethanolamines, triacylglycerols, sphingomyelins and so on. Orally administrated Polygonum cuspidatum restored these differential lipids back to normal or nearly normal levels. This study adopted lipidomics to reveal the key lipid molecules as potential therapeutic targets of Polygonum cuspidatum against hyperlipidemia, which would provide a scientific basis for its clinical application.

Advances for pharmacological activities of Polygonum cuspidatum - A review.

CONTEXT: Polygonum cuspidatum Sieb. et Zucc (Polygonaceae), the root of which is included in the Chinese Pharmcopoeia under the name 'Huzhang', has a long history as a medicinal plant and vegetable. Polygonum cuspidatum has been used in traditional Chinese medicine for the treatment of inflammation, hyperlipemia, etc. OBJECTIVE: This article reviews the pharmacological action and the clinical applications of Polygonum cuspidatum and its extracts, whether in vivo or in vitro. We also summarized the main phytochemical constituents and pharmacokinetics of Polygonum cuspidatum and its extracts. METHODS: The data were retrieved from major medical databases, such as CNKI, PubMed, and SinoMed, from 2014 to 2022. Polygonum cuspidatum, pharmacology, toxicity, clinical application, and pharmacokinetics were used as keywords. RESULTS: The rhizomes, leaves, and flowers of Polygonum cuspidatum have different phytochemical constituents. The plant contains flavonoids, anthraquinones, and stilbenes. Polygonum cuspidatum and the extracts have anti-inflammatory, antioxidation, anticancer, heart protection, and other pharmacological effects. It is used in the clinics to treat dizziness, headaches, traumatic injuries, and water and fire burns. CONCLUSIONS: Polygonum cuspidatum has the potential to treat many diseases, such as arthritis, ulcerative colitis, asthma, and cardiac hypertrophy. It has a broad range of medicinal applications, but mainly focused on root medication; its aerial parts should receive more attention. Pharmacokinetics also need to be further investigated.

Inhibition of Colorectal Cancer Cell Proliferation by Treatment with Itadori Leaf Extract.

Treatment with itadori extract inhibited the growth of mouse colon cancer cells (Colon-26) in mice. In addition, it induced DNA fragmentation and caspase 3/7 activation in Colon-26 cells, suggesting potent induction of apoptosis. Itadori extracts are rich in neochlorogenic acid and rutin and also contain quercetin and piceatannol. These polyphenols are thought to be involved in the observed DNA fragmentation and caspase 3/7 activation in colon cancer cells and may thus have anticancer effects. There is hence scope for development of the leaf of itadori, which currently has only a few known uses, as a novel anti-tumor therapeutic.

Preparation of Solid Dispersion of Polygonum Cuspidatum Extract by Hot Melt Extrusion to Enhance Oral Bioavailability of Resveratrol.

The aim of this study was to improve the solubility, bioavailability, and stability of resveratrol (RES-SD) Solid Dispersion in Polygonum cuspidatum extract (PCE) by hot melt extrusion (HME). In addition, the role of the auxiliary substances in PCE was also studied. The solid dispersion of Polygonum cuspidatum extract was prepared by hot-melt extrusion. The optimum formula was selected by single factor design and orthogonal test. The optimum formula was barrel temperature 140 °C, screw rotation speed 40 rpm/min, and the ratio of Polygonum cuspidatum extract to HPMCAS was 1:2. The dissolution test showed that PCE-SD increased the dissolution of RES from 46.75 ± 0.47% to 130.06 ± 0.12%. The pharmacokinetics curve of rats showed that PCE-SD increased AUC0-t of RES from 111,471.22 ± 11.4% to 160,458.968 ± 15.7%, indicating an approximately 1.44-fold increase in absorption. In addition, the rotation speed of PCE-SD screw is less than that of RES-SD screw. The bioavailability of PCE-SD was slightly better than that of RES-SD. PCE-SD is more hygroscopic than RES-SD. PCE-SD increased the solubility and oral bioavailability of RES. The auxiliary substances in Polygonum cuspidatum extract have influence on its preparation technology, stability, and bioavailability.