Cuspidatum Extract Research Articles

Senescence Rejuvenation through Reduction in Mitochondrial Reactive Oxygen Species Generation by Polygonum cuspidatum Extract: In Vitro Evidence.

Oxidative stress caused by reactive oxygen species (ROS) is one of the major causes of senescence. Strategies to reduce ROS are known to be important factors in reversing senescence, but effective strategies have not been found. In this study, we screened substances commonly used as cosmetic additives to find substances with antioxidant effects. Polygonum cuspidatum (P. cuspidatum) extract significantly reduced ROS levels in senescent cells. A novel mechanism was discovered in which P. cuspidatum extract reduced ROS, a byproduct of inefficient oxidative phosphorylation (OXPHOS), by increasing OXPHOS efficiency. The reduction in ROS by P. cuspidatum extract restored senescence-associated phenotypes and enhanced skin protection. Then, we identified polydatin as the active ingredient of P. cuspidatum extract that exhibited antioxidant effects. Polydatin, which contains stilbenoid polyphenols that act as singlet oxygen scavengers through redox reactions, increased OXPHOS efficiency and subsequently restored senescence-associated phenotypes. In summary, our data confirmed the effects of P. cuspidatum extract on senescence rejuvenation and skin protection through ROS reduction. This novel finding may be used as a treatment in senescence rejuvenation in clinical and cosmetic fields.

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.

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.

The Role of VARVIMAX™ In the Treatment of Chronic Inflammation and Pain in Arthritis and Fibromyalgia

Background: Arthritis and fibromyalgia are chronic inflammatory conditions that cause significant pain and discomfort in affected individuals. Current treatments, such as nonsteroidal anti-inflammatory drugs (NSAIDs), are associated with adverse effects and do not always provide adequate relief. Therefore, there is a need for safe and effective treatments for chronic inflammation and pain in arthritis and fibromyalgia.
 Review of the Literature: This review aims to evaluate the safety and efficacy of VARVIMAX™, a dietary supplement derived from a plant extract, for managing chronic pain in arthritis and fibromyalgia. According to the literature, the prevalence of fibromyalgia and arthritis is still high and even these two conditions occur together. VARVIMAX™ is a dietary supplement derived from a plant extract. VARVIMAX™ contains high levels of anthocyanins, such as Astaxanthins have been shown to possess anti-inflammatory and antioxidant properties. The formulation includes amino acids and flavonoids such as choline L-bitartrate, GABA, L-arginine, black pepper (piperine), docosahexaenoic acid (DHA), eicosapentaenoic acid (EPA), trans-resveratrol 98% (polygonum cuspidatum extract), which all have anti-inflammatory effects and play a significant role in pain management. Studies have shown that these ingredients have been effective in reducing pain, and inflammation, and improving joint function in patients with arthritis, fibromyalgia, and other inflammatory conditions. The most common side effects reported were gastrointestinal symptoms, such as nausea and diarrhea. 
 Conclusion: VARVIMAX™, a dietary supplement derived from a plant extract Ephedra, shows promise as a safe and effective treatment for chronic pain in arthritis and fibromyalgia. It is composed of several anthocyanins, amino acids, and flavonoids that impart it its characteristic anti-inflammatory and antioxidant properties. This results in reducing pain and inflammation, and improving joint function. Further research is needed to establish its long-term safety and efficacy in a wider range of inflammatory conditions.

Isolation and characterization of uric acid-lowering functional components from Polygonum cuspidatum

Polygonum cuspidatum (P. cuspidatum) is an herbaceous perennial plant known as Asian knotweed that is used in Chinese medicine due to its active components. Recent studies of the uric acid-lowering activity of P. cuspidatum extracts have mainly focused on analysis of its crude extract or specific chemical components, with limited research about its uric acid-lowering activity in vivo. In present study, monomeric compounds with higher uric acid-lowering ability were isolated from P. cuspidatum extract by column chromatography and thin-layer chromatography (TLC) and tested in a hyperuricemia mouse model and xanthine oxidase (XOD) inhibition assay in vitro. Structural characterization of the isolated components was performed by nuclear magnetic resonance (NMR) spectroscopy and the potential mechanism of decreasing uric acid was analyzed using untargeted metabolomics. Two main novel compounds were isolated and identified, 1-(4-hydroxy-2-methoxyphenyl)-2-(4-hydroxy-3,5-dimethylphenyl)butane-1,2,3-triol (compound 1) and 1-(4-hydroxy-2-methoxyphenyl)-2-(4-hydroxy-3,5-dimethylphenyl)-3-methylbutane-1,2-diol (compound 2), and compounds 1 was proved more significant inhibitory effect on the activity of XOD (p < 0.01) with inhibition of 49.80%. Metabolomics analysis indicated that the fractions (compound 1 and compound 2) affected hyperuricemic mice mainly through changes in galactose metabolism (p = 5.74E-4) and the effects were closely related to metabolic pathways of organic acid, carbohydrate, and lipid metabolism. These results contribute to providing theoretical support for the utilization of P. cuspidatum as a food and medicinal material, which can increase its use as an alternative treatment for hyperuricemia.

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.

Chinese medicinal plant Polygonum cuspidatum ameliorates silicosis via suppressing the Wnt/β-catenin pathway

Abstract Polygonum cuspidatum (PC) extract has effect on silica-induced pulmonary fibrosis. This study aimed to explore the anti-pulmonary-fibrosis effects and mechanism of PC. Sprague–Dawley rat model was constructed by inhalation of silicon dioxide suspension through tracheal intubation method. And histopathological examination showed that PC inhibited inflammatory cell infiltration, fibrous and collagen hyperplasia, and protected the normal structure of alveoli. TUNEL assay declared that PC retarded cell apoptosis. Meanwhile, up-regulation of basic fibroblast growth factor, plated-derived growth factor, and TNF-α in silicosis rats was decreased by PC addition. In addition, human fetal lung fibroblasts (HFL-1) cells were stimulated with transforming growth factor-β1 (TGF-β1). PC administration increased the proliferation and invasion of TGF-β1-stimulated HFL-1 cells whereas decreased cell apoptosis. Moreover, western blotting exhibited that PC treatment decreased the expression of α-smooth muscle actin, collagen I, and collagen III in silicosis rats and TGF-β1-stimulated HFL-1 cells. Furthermore, the levels of Wnt/β-catenin pathway proteins were up-regulated in silicosis rats and TGF-β1-stimulated HFL-1 cells, which were weakened by PC treatment. Meanwhile, Wnt3a (an activator of Wnt/β-catenin) addition reversed the effect of PC addition. In conclusion, PC prevents silica-induced fibrosis through inhibiting the Wnt/β-catenin pathway.

Characterization of the chemical constituents and metabolic profile of Polygonum cuspidatum Sieb. et Zucc. in rat plasma, urine, and feces by ultra-high performance liquid chromatography coupled with Quadrupole-Exactive Orbitrap mass spectrometry.

Polygonum cuspidatum Sieb. et Zucc. is a traditional and popular Chinese medicine with a wide spectrum of pharmacological effects such as anti-bacterial, anti-inflammatory, and anti-tumor activities together with other health effects like lowering lipids, preventing diabetes, and regulating the immune system. It is of great significance to explore the complex chemical constituents and metabolic process of Polygonum cuspidatum in vivo to further clarify the effective substances. However, studies on its metabolism in vivo were not comprehensive in previous literature. In this study, ultra-high performance liquid chromatography coupled with Quadrupole-Exactive Orbitrap mass spectrometry was used to comprehensively identify the chemical constituents in Polygonum cuspidatum and further analyze its metabolic profile in rats. Compared with reference substances, various databases, and literature retrieval, 62 compounds were inferred from the Polygonum cuspidatum extract. Furthermore, a total of 119 compounds, including 44 prototype compounds and 75 metabolites, were annotated in rat plasma, urine, and feces. The main metabolic pathways of Polygonum cuspidatum in rats included hydrogenation reduction, hydroxylation, dehydration, methylation, sulfation, and glucuronidation. This is the first systematic study on the chemical constituents of Polygonum cuspidatum and its metabolic profile in vivo, which contributes to finding its bioactive components and seeking its therapeutic targets.

Polygonum cuspidatum Extract (Pc-Ex) Containing Emodin Suppresses Lung Cancer-Induced Cachexia by Suppressing TCF4/TWIST1 Complex-Induced PTHrP Expression.

Cachexia, which is characterised by the wasting of fat and skeletal muscles, is the most common risk factor for increased mortality rates among patients with advanced lung cancer. PTHLH (parathyroid hormone-like hormone) is reported to be involved in the pathogenesis of cancer cachexia. However, the molecular mechanisms underlying the regulation of PTHLH expression and the inhibitors of PTHLH have not yet been identified. The PTHLH mRNA levels were measured using quantitative real-time polymerase chain reaction, while the PTHrP (parathyroid hormone-related protein) expression levels were measured using Western blotting and enzyme-linked immunosorbent assay. The interaction between TCF4 (Transcription Factor 4) and TWIST1 and the binding of the TCF4–TWIST1 complex to the PTHLH promoter were analysed using co-immunoprecipitation and chromatin immunoprecipitation. The results of the mammalian two-hybrid luciferase assay revealed that emodin inhibited TCF4–TWIST1 interaction. The effects of Polygonum cuspidatum extract (Pc-Ex), which contains emodin, on cachexia were investigated in vivo using A549 tumour-bearing mice. Ectopic expression of TCF4 upregulated PTHLH expression. Conversely, TCF4 knockdown downregulated PTHLH expression in lung cancer cells. The expression of PTHLH was upregulated in cells ectopically co-expressing TCF4 and TWIST1 when compared with that in cells expressing TCF4 or TWIST1 alone. Emodin inhibited the interaction between TCF4 and TWIST1 and consequently suppressed the TCF4/TWIST1 complex-induced upregulated mRNA and protein levels of PTHLH and PTHrP. Meanwhile, emodin-containing Pc-Ex significantly alleviated skeletal muscle atrophy and downregulated fat browning-related genes in A549 tumour-bearing mice. Emodin-containing Pc-Ex exerted therapeutic effects on lung cancer-associated cachexia by inhibiting TCF4/TWIST1 complex-induced PTHrP expression.

Polygonum cuspidatum Extract Exerts Antihyperlipidemic Effects by Regulation of PI3K/AKT/FOXO3 Signaling Pathway

Polygonum cuspidatum (PC) has been reported to exert a potent antihyperlipidemic effect. However, its mechanisms of action and active ingredients remain elusive and require further research. In this study, we first conducted in vivo experiments to validate that Polygonum cuspidatum extract (PCE) could ameliorate the blood lipid level in hyperlipidemia model rats. Then, ultrahigh performance liquid chromatography coupled with Q-Exactive MS/MS (UPLC-QE-MS/MS) was applied to verify its 12 main active ingredients. The pharmacophore matching model was employed to predict the target point of the active ingredient, and 27 overlapping genes were identified via database and literature mining. String online database and Cytoscape software were utilized to construct a Protein-Protein Interaction (PPI) network, followed by function annotation analysis and pathway enrichment analysis. The results showed that the PI3K/AKT signaling pathway and its downstream FOXO3/ERα factors were significantly enriched. Furthermore, in vitro experiments were performed to determine the lipid content and oxidative stress (OS) indicators in OA-induced HepG2 cells, and immunofluorescence and western blotting analysis were carried out to analyze the effects of PCE on related proteins. Our experimental results show that the mechanism of antihyperlipidemic action of PCE is related to the activation of the PI3K/AKT signaling pathway and its downstream FOXO3/ERα factors, and polydatin and resveratrol are the main active ingredients in PCE that exert antihyperlipidemic effects.

Application of β-glucosidase Immobilized on Chitosan microspheres in Degradation of Polydatin in Polygonum cuspidatum

Resveratrol in Polygonum cuspidatum is a β-glycoside, which can be hydrolyzed to resveratrol by β-glucosidase. it is an efficient production process to degrade polydatin from Polygonum cuspidatum extract by immobilized β-glucosidase. It is of great significance to explore suitable immobilization conditions to improve the catalytic efficiency and reusability of β-glucosidase for polydatin degradation and cost reduction. In this paper, the recombinant Escherichia coli bgl2238, which was screened and constructed from corn soil of Heilongjiang Province in the early laboratory, was immobilized by chitosan adsorption and glutaraldehyde crosslinking. The preparation conditions and immobilization process of bgl2238 were determined by single factor method: the optimal crosslinking time was 1 h, the optimal crosslinking temperature was 20 °C, the recovery rate of enzyme activity of bgl2238 was 87 %, and the enzyme activity was 859.65 mU/g. The optimum temperature of the immobilized bgl2238 is 50 °C, which is 6 °C higher than that of the free bgl2238, and the temperature stability and pH stability are improved. After six consecutive hydrolysis of Polygonum cuspidatum, the degradation rate of polydatin is still over 70 %, which proves that the immobilized bgl2238 has good reusability. This will be helpful to evaluate the application prospect of β - glucosidase immobilized in this system and determine the best conditions for its production.

Gastroprotective and Healing Effects of Polygonum cuspidatum Root on Experimentally Induced Gastric Ulcers in Rats.

Polygonum cuspidatum is widely used as food and medicine in Korea, China, and Japan. Its major bioactive components, resveratrol and emodin, reportedly protect against gastric lesions. We therefore aimed to investigate: (1) the gastroprotective effects of P. cuspidatum roots in hydrochloric acid/ethanol (HCl/EtOH)- and indomethacin-induced acute gastric ulcer rat models; (2) the healing effects in an acetic acid-induced ulcer model; and (3) potential mechanisms by measuring gastric acid secretion-related parameters in a pyloric ligation-induced ulcer model, and by measuring antioxidant enzyme and prostaglandin E2 levels in the gastric tissue of HCl/EtOH-treated rats. Oral administration of P. cuspidatum extract (PCE) at doses of 100 and 300 mg/kg significantly decreased HCl/EtOH- and indomethacin-induced gastric lesions. PCE at 300 mg/kg significantly reduced gastric lesions in acetic acid-induced ulcers. PCE increased superoxide dismutase (SOD) activity and glutathione (GSH) and prostaglandin E2 levels in gastric tissue, whereas it did not alter gastric acid secretion-related parameters. Our findings indicate that PCE has gastroprotective effects against HCl/EtOH and non-steroidal anti-inflammatory drugs (NSAIDs) and promotes healing of acetic acid-induced ulcers. These gastric mucosal protection and ulcer healing effects are associated with antioxidant effects and the augmentation of prostaglandin E2 and suggest that P. cuspidatum might be a promising preventive and therapeutic agent for treating gastric ulcers.

Fabrication of three-dimensional porous cellulose microsphere bioreactor for biotransformation of polydatin to resveratrol from Polygonum cuspidatum Siebold & Zucc

In this study, in order to bio-transform polydatin to resveratrol from Polygonum cuspidatum extract, a 3D-porous structured cellulose microsphere (CMs) immobilized with β-glucosidase acted as a micro-bioreactor. To successfully immobilize β-glucosidase, CMs was treated with epoxidation to attach three different functional amion groups, and finally combined with β-glucosidase. CMs provided large surface area (32.0 m²/g) and many sites for immobilization of β-glucosidase and chemical modification. The porosity of CMs was 90 % and its density was about 1.00 g/m3. According to SEM images, the 3D-porous structure was obviously found and the result of FTIR proved the successful modification of amino groups. The crystal structure of CMs was changed from crystalline cellulose I-β to crystalline cellulose II during the sol-gel method. In the biotransformation tests of the Polygonum cuspidatum extracts, the conversion rate of polydatin reached 93.06 %, and after conversion, the concentration of resveratrol was two times higher than the original Polygonum cuspidatum extract. In addition, the cellulose microsphere micro-bioreactor also possessed good reusability, which could maintain 89.2 % activity after being repeatedly operated 8 times. Therefore, this cellulose microsphere micro-bioreactor can be successfully used to produce resveratrol from polydatin, and this micro-bioreactor may also have the potential to convert other plant glycosides into aglycones. Moreover, because of their good biocompatibility, the 3D porous cellulose microspheres can also be used for immobilization of other enzymes to prepare efficient bioreactors.

Antioxidant and Anti-Obesity Activities of Polygonum cuspidatum Extract through Alleviation of Lipid Accumulation on 3T3-L1 Adipocytes.

Natural products are widely used due to their various biological activities which include antiinflammatory, antioxidant, and anti-obesity effects. In this study, we determined the antioxidative and anti-obesity effects of Polygonum cuspidatum 50% ethanol extract (PEE). The antioxidative effect of PEE was evaluated using its radical scavenging activity, total phenolic content, and reducing power. The anti-obesity effect of PEE was investigated using 3T3-L1 adipocytes. The antioxidative activity of PEE was progressively increased in various concentrations, mainly due to the presence of phenolic compounds. PEE also alleviated lipid accumulation on 3T3-L1 adipocytes and downregulated the mRNA and protein production of adipogenesis-related (SREBP-1c, PPARγ, C/EBPα) and lipogenesis-related (aP2, FAS, ACC) markers. Furthermore, we found that the inhibitory effect on lipid accumulation via PEE was caused by the alleviation of NF-κB, p38 MAPK, ERK1/2, and JNK at the protein level. Taken together, our results imply that PEE is a potential antioxidant that can prevent obesityassociated disorders.

Processed Meat and Polyphenols: Opportunities, Advantages, and Difficulties

Abstract Currently, processed meats appear increasingly as a nonhealthy food because of their content of fat, salt, nitrite, and particularly in red meat, for the heme-iron concerning oxidant effect and radicals formation in human gut. Polygonum cuspidatum and rosemary extract has been tested to counteract these effects and experiments were carried out to add polyphenols into whole meat cuts with the aims to improve their healthiness. The addition of these extracts can reduce the oxidation-reduction potential of products, increasing the antioxidant power. Nevertheless, a low percentage of polyphenols were found in the products because of the process effects and an interaction with the ascorbate residue was observed. In addition, some drawbacks were a decrease in of yield and a worsening of some sensorial properties when large amount of extract was added. The balance between the improvement of the wholesomeness content and the acceptability of products is the challenge the current research have to overcome.

Processed Meat and Polyphenols: Opportunities, Advantages, and Difficulties.

Currently, processed meats appear increasingly as a nonhealthy food because of their content of fat, salt, nitrite, and particularly in red meat, for the heme-iron concerning oxidant effect and radicals formation in human gut. Polygonum cuspidatum and rosemary extract has been tested to counteract these effects and experiments were carried out to add polyphenols into whole meat cuts with the aims to improve their healthiness. The addition of these extracts can reduce the oxidation-reduction potential of products, increasing the antioxidant power. Nevertheless, a low percentage of polyphenols were found in the products because of the process effects and an interaction with the ascorbate residue was observed. In addition, some drawbacks were a decrease in of yield and a worsening of some sensorial properties when large amount of extract was added. The balance between the improvement of the wholesomeness content and the acceptability of products is the challenge the current research have to overcome.

Polygonum cuspidatum extract attenuates fructose-induced liver lipid accumulation through inhibiting Keap1 and activating Nrf2 antioxidant pathway

BackgroundPolygonum cuspidatum has been used in traditional Chinese medicine to treat liver disorders associated with oxidative stress, inflammation and lipid accumulation for centuries in patients. PurposeThe aim of this study was to examine whether P. cuspidatum extract (PCE) prevented against fructose-induced liver lipid accumulation via regulating Kelch-like ECH-associated protein 1 (Keap1)/nuclear factor erythroid 2-related factor 2 (Nrf2) pathway. MethodPCE was administered orally to male Sprague-Dawley rats given 10% fructose drinking water for 6 weeks at 80 and 160 mg/kg once daily for 11 weeks. ResultsPCE significantly alleviated liver lipid accumulation in fructose-fed rats with metabolic syndrome. It also inhibited Keap1, activated Nrf2 antioxidant pathway, resulting in the suppression of oxidative stress, evidenced by reducing hydrogen peroxide (H2O2), malondialdehyde (MDA) and hydroxy radical (OH•) levels, and increasing glutathione (GSH)/oxidized glutathione (GSSG) ratio as well as superoxidase dismutase (SOD) and catalase (CAT) activity in the liver of fructose-fed rats. Additionally, PCE up-regulated peroxisome proliferator activated receptor-α (PPAR-α), and down-regulated sterol regulatory element binging protein 1 (SREBP-1), fatty acid synthetase (FAS) and stearoyl-CoA desaturase-1 (SCD-1) in this animal model, being consistent with its reduction of triglyceride (TG) levels. ConclusionThese results demonstrate that PCE reduces oxidative stress, and prevent lipid accumulation in the liver of fructose-fed rats possibly by targeting the Keap1/Nrf2 pathway. PCE may be a promising therapeutic strategy for fructose-associated liver lipid accumulation.

Capability of polygonum cuspidatum extract in inhibiting AGEs and preventing diabetes.

Diabetes is a metabolic disorder disease associated with advanced glycation end products (AGEs) and protein glycation. The effect of polygonum cuspidatum extract (PE) on AGEs and Nε‐(Carboxymethyl)‐L‐lysine formation, protein glycation, and diabetes was investigated. Six primary phenolics in a range of 12.36 mg/g for ellagic acid to 0.01 mg/g for piceid were determined in PE. In an intermediate‐moisture‐foods model, inhibition rate of PE was as high as 54.2% for AGEs and 78.9% for CML under aw 0.75. The protein glycation was also inhibited by PE. In a diabetic rat model, the levels of blood glucose, serum malondialdehyde, cholesterol, triglycerides, and low‐density lipoproteins were effectively reduced by PE treatment. The antioxidation capacity (T‐AOC) and superoxide dismutase (SOD) activity were also mediated by PE. Additionally, the activates of liver function‐related enzymes including alkaline phosphatase (ALP), glutamate pyruvate transaminase (GPT), and glutamate oxaloacetate transaminase (GOT) in diabetic rat were improved by PE.

Autophagy and apoptotic machinery caused by Polygonumcuspidatum extract in cisplatin‑resistant human oral cancer CAR cells.

Polygonum cuspidatum (Hu Zhang) is a traditional Chinese medicine (TCM) and has been revealed to exert anticancer, anti‑angiogenesis, anti‑human immunodeficiency virus (HIV), anti‑hepatitis B virus, anti‑microbial, anti‑inflammatory, and neuro‑protective bio‑activities. However, the effect of P. cuspidatum extract (PCE) on drug‑resistant human oral cancer cells regarding cell death is not fully understood yet. The present study was undertaken to explore the induction of autophagic and apoptotic cell death and to investigate their underlying molecular mechanisms in PCE‑treated cisplatin‑resistant human oral cancer CAR cells. Our results revealed that PCE was determined via HPLC analytic method, and it was revealed that resveratrol may be a major compound in PCE. The data also demonstrated that PCE reduced CAR cell viability in a concentration‑ and time‑dependent response via an MTT assay. PCE had an extremely low toxicity in human normal gingival fibroblasts (HGF). Autophagic and apoptotic cell death was found after PCE treatment by morphological determination. PCE was revealed to induce autophagy as determined using acridine orange (AO), LC3‑GFP, monodansylcadaverine (MDC) and LysoTracker Red staining in CAR cells. In addition, PCE was revealed to induce apoptosis in CAR cells via 4',6‑diamidino‑2‑phenylindole (DAPI)/terminal deoxynucleotidyl transferase dUTP nick‑end labeling (TUNEL) double staining. PCE significantly stimulated caspase‑9 and ‑3 activities as revealed using caspase activity assays. PCE markedly increased the protein levels of Atg5, Atg7, Atg12, Beclin‑1, LC3, Bax and cleaved caspase‑3, while it decreased the protein expression of Bcl‑2 in CAR cells as determined by western blotting. In conclusion, our findings are the first to suggest that PCE may be potentially efficacious for the treatment of cisplatin‑resistant human oral cancer.

α-Glucosidase immobilization on functionalized Fe3O4 magnetic nanoparticles for screening of enzyme inhibitors

Magnetic nanoparticles (MNPs) are widely used for the immobilization of enzyme owing to the unique properties such as good biocompatibility and rapid separation. Herein, we used Fe3O4 magnetic nanoparticles (Fe3O4 MNPs) as the carrier core with (3-aminopropyl)triethoxysilane (APTES) modification by our approach, in which α-glucosidase was stereoscopically immobilized on the surface of Fe3O4 MNPs via covalent binding. The result of immobilization was characterized by scanning electron microscope (SEM) and fourier transform-infrared spectroscopy (FT-IR). Then we optimized some key parameters of the immobilization reaction, including the ratio of MNPs to enzyme, GA concentration, crosslinking time and immobilization time. Moreover, under the optimal conditions, pH tolerance, thermo stability and reusability of the immobilized enzyme were investigated and compared with the free one. In order to evaluate the change of the affinity of the enzyme to its specific substrate after immobilization, the Michaelis-Menten constant (Km) was also studied. Finally, the immobilized α-glucosidase combining with high performance liquid chromatography-tandem mass spectrometry technique (HPLC-MS/MS) was applied to screen and identify eight inhibitors from Polygonum cuspidatum extract. These results indicated that the established method had the broad prospects for biotechnological applications.