Sinensis Walker Research Articles

Development of an Ultrasensitive Competitive Double-Enzyme Cascade Fluorescence Signal Amplification Method for Factor XIa Inhibitor Screening.

Coagulation factor XIa (FXIa) is associated with a low risk of bleeding and has been identified as an effective and safe target for the development of novel anticoagulant drugs. In this study, we established an ultrasensitive competitive dual-enzyme cascade signal amplification method for the quantitative analysis and screening of FXIa inhibitors. Due to the specific recognition of FXIa's active site by the aptamer AptE40, the AptE40-QDs-EK recognition probe modified with enterokinase (EK) and the aptamer AptE40, was attached to the MNPs-FXIa capture probe. When FXIa inhibitor was present, it competed with AptE40 for binding to FXIa, resulting in the detachment of AptE40-QDs-EK from MNPs-FXIa. After magnetic separation, the enterokinase of AptE40-QDs-EK in the supernatant hydrolyzed N-terminal hexapeptide of trypsinogen, leading to the production of a large amount of trypsin as part of the first-stage signal cascade amplification. Next, trypsin could hydrolyze the hexameric arginine peptide (RRRRRR, R6), leading to the dissociation of RQDs from the R6-RQDs signal probe; this resulted in a dramatic increase in the fluorescence intensity of the supernatant as the second-stage signal cascade was amplified. The feasibility of the method was investigated using the FXIa inhibitor aptamer FELIAP as a positive model drug. Furthermore, the method was applied to screen the FXIa inhibitors in Eupolyphaga sinensis Walker. Two fractions with more active anticoagulated ingredients were successfully identified and validated via the conventional method, and the results were consistent. The established method provides a key technique for the sensitive detection, high-throughput analysis, and screening of the FXIa inhibitors.

A highly sensitive and specific fluorescent probe for thrombin detection and high-throughput screening of thrombin inhibitors in complex matrices

Thrombin plays a critical role in hemostasis and hemolysis, and is a significant biomarker for blood-related diseases. Detection and inhibitors screening of thrombin are essential in medical research. In this study, we developed a fluorescent sensor based on the interaction between quantum dots (QDs) and fibrinogen (Fib) for thrombin detection and its inhibitors screening. Upon the presence of thrombin, the fibrinogen of soluble QDs-Fib were converted into insoluble fibrin precipitate, causing a change of fluorescence intensity in the supernatant. Under optimized conditions, our method exhibited an excellent linearity (R2 ≥0.99) over the range of 2∼100 U/L with a limit of detection (LOD) as low as 0.29 U/L. Moreover, we employed this method to screen for thrombin inhibitors using dabigatran as an exemplary direct thrombin inhibitor (DTI), even at concentrations as low as 1 nM. Finally, the established method was successfully used to screen thrombin inhibitors in 23 different extracts from Eupolyphaga sinensis walker. The method provided not only a sensitive, specific and high throughput assay for the detection of thrombin activity in biological samples, but also a reliable strategy for the screening of thrombin inhibitors in complex matrices.

Comparative analysis of the nutritional composition and volatile compounds in male and female adults, nymphs, and molts of Eupolyphaga sinensis Walker.

Female adult Eupolyphaga sinensis Walker (FAESW) has traditionally been a food source in Southeast Asian countries such as China and India, due to its rich nutritional content. However, the nutritional value of male adults (MAESW) and its molts (MESW) has hardly been reported. Therefore, this study aims to explore the potential application of MAESW and MESW in food by investigating and comparing their nutritional composition (i.e., protein, amino acids, fatty acids, and essential elements) with traditional sources of nutrition. The protein content of MAESW and MESW was 66.10±0.49% and 59.86±6.07%, respectively, and the highest energy content (462.26±1.28kcal/100g) was observed for MAESW. Eight essential amino acids were determined, of which the males and MESW were found to have higher contents than those of FAESW (p<0.05). Oleic and linoleic acid contents were higher in the adults than nymphs. Moreover, MESW was predominant in calcium (6770.84mg/kg), whereas MAESW was rich in iron (556.12mg/kg). Likened to chicken, the protein, amino acid, fatty acid, and mineral contents of ESW were higher. The volatiles of ESW were related to hexaldehyde, benzaldehyde, acetic acid, and butyric acid. This study provides a better understanding of the chemical composition of ESWs during their growth cycle and helps optimize information on edible insects, promoting their use as a potential food source for humans. As a kind of edible insect, the utilization of adult male Eupolyphaga sinensis Walker (ESW) and its molt is very low at present. Therefore, this study examined the nutrients and volatile substances of ESW (at different growth stages) and molt, which provided a theoretical basis for the subsequent development and utilization of ESW.

Alternating Low and High Temperatures Increases the Hatching Rate of Eupolyphaga sinensis (Blattaria: Polyphagidae) Eggs

The hatching rates and developmental durations of Eupolyphaga sinensis Walker eggs were studied under variable combinations of low temperatures (5 °C and 10 °C) and high temperatures (25 °C and 30 °C). Our findings were intended to provide new evidence on the effect of temperature on the hatching of insect eggs. The results showed that both low temperatures and high temperatures significantly affected the hatching rate and time of E. sinensis eggs. Further analysis revealed a significant interactive effect between low temperatures and high temperatures. The 5 °C + 30 °C treatment achieved the highest egg hatching rate (77.33%) and the shortest hatching time (44.11 ± 1.55 d), which was significant compared with three other temperature treatments. The effects of high temperatures treatments on the hatching rate and the hatching time were more significant than that in the low temperature treatments. Hatching began earlier at 5 °C + 30 °C and 10 °C+30 °C temperatures, and single-day hatching first increased rapidly before declining afterwards within a short period. Comparatively, the hatching of eggs under the (5 °C+25 °C) and (10 °C+25 °C) temperatures was initially significantly delayed, including the peak single-day hatching rate. Under these treatments, the hatching rate tended to be gradual in terms of the temporal dynamics without showing any prominent peak. These results showed that low and high temperatures significantly affect the hatching rates of E. sinensis eggs. This study provided basis for the large-scale breeding of E. sinensis.

The water-soluble TF3 component from Eupolyphaga sinensis Walker promotes tibial fracture healing in rats by promoting osteoblast proliferation and angiogenesis

ObjectiveTo determine the active components of Eupolyphaga sinensis Walker (Tu Bie Chong) and explore the mechanisms underlying its fracture-healing ability. MethodsA modified Einhorn method was used to develop a rat tibial fracture model. Progression of bone healing was assessed using radiological methods. Safranin O/fast green and CD31 immunohistochemical staining were performed to evaluate the growth of bone cells and angiogenesis at the fracture site. Methylthiazoletetrazolium blue and wound healing assays were used to analyze cell viability and migration. The Transwell assay was used to explore the invasion capacity of the cells. Tubule formation assays were used to assess the angiogenesis capacity of human vascular endothelial cells (HUVECs). qRT-PCR was used to evaluate the changes in gene transcription levels. ResultsTu Bie Chong fraction 3 (TF3) significantly shortened the fracture healing time in model rats. X-ray results showed that on day 14, fracture healing in the TF3 treatment group was significantly better than that in the control group (P = .0086). Tissue staining showed that cartilage growth and the number of H-shaped blood vessels at the fracture site of the TF3 treatment group were better than those of the control group. In vitro, TF3 significantly promoted the proliferation and wound healing of MC3T3-E1s and HUVECs (all P < .01). Transwell assays showed that TF3 promoted the migration of HUVECs, but inhibited the migration of MC3T3-E1 cells. Tubule formation experiments confirmed that TF3 markedly promoted the ability of vascular endothelial cells to form microtubules. Gene expression analysis revealed that TF3 significantly promoted the expression of VEGFA, SPOCD1, NGF, and NGFR in HUVECs. In MC3T3-E1 cells, the transcript levels of RUNX2 and COL2A1 were significantly elevated following TF3 treatment. ConclusionTF3 promotes fracture healing by promoting bone regeneration associated with the RUNX2 pathway and angiogenesis associated with the VEGFA pathway.

Chemical isotope labeling-assisted liquid chromatography-mass spectrometry enables sensitive and accurate determination of dipeptides and tripeptides in complex biological samples

Small peptides have attracted increasing attention for their unique features and diverse biological functions. Achieving rapid separation and accurate quantification, however, remains a challenge because of their low abundance and the co-existence of numerous structural isomers. In this study, we developed a novel approach using isotope chemical labeling for ultrasensitive determination of di/tripeptides in biological samples. We successfully synthesized a novel derivatization reagent, 4-(2-(ethoxymethylene)-3-oxobutanamido)-N,N,N-trimethylbenzenaminium iodide (EOTMBA) as well as its deuterium-labeled isotope reagent (d3-EOTMBA). A total of 97 small peptides, including 89 dipeptides and 8 tripeptides, could be completely derivatized in methanol within 1.5 h at 60 °C. After EOTMBA labeling, analysis of these di/tripeptides were achieved within 22 min by LC-MS/MS analysis. The method demonstrated 86.3 %–113 % accuracy and the limit of quantification ranged from 0.25 fmol/L to 5 nmol/L. Using this method, we achieved ultrasensitive and accurate quantification of di/tripeptides in 147 plasma, 49 urine and 46 bile samples obtained from healthy individuals and patients with biliary tract diseases. The identified differential di/tripeptide biomarker panels showed promising diagnostic performance for patients with biliary tract cancer with area under the receiver operating curve values from 0.870 to 0.996. Furthermore, this method was successfully applied to quantify di/tripeptides in the extract of an animal-derived traditional Chinese medicine, Eupolyphaga sinensis Walker. These findings highlight the possible application of the analytical method in clinics and for the purposes of quality control of traditional Chinese medicines.

Active peptides from Eupolyphaga sinensis walker attenuates experimental hyperlipidemia by regulating the gut microbiota and biomarkers in rats with dyslipidemia

Eupolyphaga sinensis Walker (ESW) is a traditional Chinese medicine formulation used to treat hyperlipidemia. However, the hypolipidemic effect of the active peptides from E. sinensis Walker (APE) is incompletely understood. We studied the hypolipidemic effect of APE and explored the impact of APE on the gut microbiota (GM) in rats suffering from hyperlipidemia. APE was prepared by enzymatic digestion, and its structure was characterized using various methods. The anti-hyperlipidemic activity of APE was assessed using a high-fat diet (HFD)-induced model in zebrafish and rats. In rats, HFD administration caused abnormalities of lipid metabolism and disturbances of the GM and amino acid (AA) profile in plasma. The abundance of bacteria of the phyla Firmicutes and Bacteroides was increased significantly (p < 0.05), and the relative abundance of Lactobacillus species and Clostridium species was decreased significantly (p < 0.05). HFD therapy affected the levels of 12 AAs in vivo: 10 AAs showed increased levels and two AAs had decreased levels (p < 0.05). Similar results were demonstrated in an experiment on fecal microbiota transplantation. APE treatment dose-dependently decreased lipid factors and liver damage (p < 0.05). Sequencing of the 16 S rRNA gene indicated that APE improved the intestinal-flora structure of rats with HL markedly, and increased the relative abundance of Lactobacillus species and Clostridium species. Metabolomics analysis indicated that APE could alter the levels of 10 AAs affected by HFD consumption. Spearman correlation analysis revealed that gamma-aminobutyric acid (GABA) could be a crucial metabolite, and Lactobacillus species and Clostridium species might be important bacteria for the action of APE against hyperlipidemia. We speculate that APE exhibited an anti-hyperlipidemic effect by regulating GABA synthesis in the presence of Lactobacillus species and Clostridium species.

Untargeted and Targeted Metabolomics Reveal the Active Peptide of Eupolyphaga sinensis Walker against Hyperlipidemia by Modulating Imbalance in Amino Acid Metabolism.

The active peptide (APE) of Eupolyphaga sinensis Walker, which is prepared by bioenzymatic digestion, has significant antihyperlipidemic effects in vivo, but its mechanism of action on hyperlipidemia is not clear. Recent studies on amino acid metabolism suggested a possible link between it and hyperlipidemia. In this study, we first characterized the composition of APE using various methods. Then, the therapeutic effects of APE on hyperlipidemic rats were evaluated, including lipid levels, the inflammatory response, and oxidative stress. Finally, the metabolism-regulating mechanisms of APE on hyperlipidemic rats were analyzed using untargeted and targeted metabolomic approaches. The results showed that APE significantly reduced the accumulation of fat, oxidative stress levels, and serum pro-inflammatory cytokine levels. Untargeted metabolomic analysis showed that the mechanism of the hypolipidemic effect of APE was mainly related to tryptophan metabolism, phenylalanine metabolism, arginine biosynthesis, and purine metabolism. Amino-acid-targeted metabolomic analysis showed that significant differences in the levels of eight amino acids occurred after APE treatment. Among them, the expression of tryptophan, alanine, glutamate, threonine, valine, and phenylalanine was upregulated, and that of arginine and proline was downregulated in APE-treated rats. In addition, APE significantly downregulated the mRNA expression of SREBP-1, SREBP-2, and HMGCR. Taking these points together, we hypothesize that APE ameliorates hyperlipidemia by modulating amino acid metabolism in the metabolome of the serum and feces, mediating the SREBP/HMGCR signaling pathway, and reducing oxidative stress and inflammation levels.

Enhancing NKT cell-mediated immunity against hepatocellular carcinoma: Role of XYXD in promoting primary bile acid synthesis and improving gut microbiota

Ethnopharmacological relevance‘Xiayuxue decoction’ (XYXD) is a traditional Chinese medicine compound, composing of three natural medicines: Rheum officinale Baill., Prunus persica (L.) Batsch and Eupolyphaga sinensis Walker. It is derived from the famous traditional Chinese medical classics ‘Jingui Yaolue’ and has been used for thousands of years. In the Guidelines for the Diagnosis and Treatment of Primary liver Cancer issued by China's Health Commission, XYXD was applied in the treatment of primary liver cancer. Aim of the studyTo clarify the pharmacodynamic material basis and mechanism of XYXD in the treatment of hepatocellular carcinoma (HCC). Materials and methodsFirstly, the active components of XYXD and its distribution in vivo were identified by Ultraperformance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS). Then, the effective components and mechanism of XYXD against HCC were explored by network pharmacology combined with cell experiments in vitro. Furthermore, the anti-HCC effect of XYXD was determined by animal experiments in vivo. Metagenomic sequencing was used to detect its effect in gut microbiota, and targeted metabolism was used to detect the changes of bile acids in the liver. Finally, the related targets of NKT cell immune function activation were detected by RT-qPCR and Elisa. ResultsA total of 113 active ingredients in XYXD were identified, and the distribution of active ingredients in blood, liver, tumor, cecum, intestinal contents and feces was clarified. The circulation process and active ingredient group of XYXD were preliminarily clarified. In addition, we found five anti-HCC active ingredients in XYXD through network pharmacology combined with cell experiments in vitro, among which aloe emodin had the most significant effect, and predicted the potential mechanism of XYXD against HCC through NKT cell pathway. Moreover, the inhibitory effect of XYXD on liver tumor growth was clarified by animal experiments in vivo. The mechanism was mainly to promote the production of bile salt hydrolase (BSH) by increasing the abundance of Bacteroides and Lactobacillus, BSH converts conjugated bile acids into primary bile acids, and reduces the conversion of primary bile acids to secondary bile acids by reducing the abundance of Eubacterium, thereby increasing the content of primary bile acids. Primary bile acids trigger NKT cells in the liver to produce interferon-γ to exert anti-HCC immune effects. ConclusionThis study found that the traditional Chinese herbal formula XYXD can trigger the immune effect of NKT cells against HCC by regulating the interaction between gut microbiota and bile acids.

Monitoring Thosea sinensis Walker in Tea Plantations Based on UAV Multi-Spectral Image

Thosea sinensis Walker (TSW) rapidly spreads and severely damages the tea plants. Therefore, finding a reliable operational method for identifying the TSW-damaged areas via remote sensing has been a focus of a research community. Such methods also enable us to calculate the precise application of pesticides and prevent the subsequent spread of the pests. In this work, based on the unmanned aerial vehicle (UAV) platform, five band images of multispectral red-edge camera were obtained and used for monitoring the TSW in tea plantations. By combining the minimum redundancy maximum relevance (mRMR) with the selected spectral features, a comprehensive spectral selection strategy was proposed. Then, based on the selected spectral features, three classic machine learning algorithms, including random forest (RF), support vector machine (SVM), and k-nearest neighbors (KNN) were used to construct the pest monitoring model and were evaluated and compared. The results showed that the strategy proposed in this work obtained ideal monitoring accuracy by only using the combination of a few optimized features (2 or 4). In order to differentiate the healthy and TSW-damaged areas (2-class model), the monitoring accuracies of all the three models were computed, which were above 96%. The RF model used the least number of features, including only SAVI and Bandred. In order to further discriminate the pest incidence levels (3-class model), the monitoring accuracies of all the three models were computed, which were above 80%, among which the RF algorithm based on SAVI, Bandred, VARI_green, and Bandred_edge features achieve the highest accuracy (OAA of 87%, and Kappa of 0.79). Considering the computational cost and model accuracy, this work recommends the RF model based on a few optimal feature combinations to monitor and distinguish the severity of TSW in tea plantations. According to the UAV remote sensing mapping results, the TSW infestation exhibited an aggregated distribution pattern. The spatial information of occurrence and severity can offer effective guidance for precise control of the pest. In addition, the relevant methods provide a reference for monitoring other leaf-eating pests, effectively improving the management level of plant protection in tea plantations, and guaranting the yield and quality of tea plantations.

Extraction and characterization of chitosan from Eupolyphaga sinensis Walker and its application in the preparation of electrospinning nanofiber membranes

Due to its capabilities for wound healing, antimicrobial defense, hemostasis, and biodegradation, chitosan has seen increased use in biomedical disciplines in recent years. In the meantime, efforts have been made to develop and use insect chitosan as a source to address the seasonal, irritating, and regional shortcomings of traditional shrimp and crab chitosan. In this study, a new type of insect chitosan (DCS) was first extracted from Eupolyphaga sinensis Walker by a low-temperature intermittent method and was compared with commercially available pharmaceutical chitosan (CS). Firstly, the degree of deacetylation and molecular weight of DCS were determined, and DCS was characterized by FT-IR, 1H NMR, XRD, and TGA-DTG. On this basis, DCS was mixed with PVA and PEO to create a novel electrospun nanofiber membrane. The air permeability, antibacterial properties, and biocompatibility of the nanofiber membrane were evaluated, as well as the membrane's shape, structure, and mechanical characteristics. Finally, the activity of nanofiber membranes in promoting wound healing was verified with a rat full-thickness skin defect model, hoping to provide a reference for the development of new drug delivery carriers and wound dressings.

A Polysaccharide From Eupolyphaga sinensis Walker With Anti-HBV Activities In Vitro and In Vivo

Hepatitis B virus (HBV) infection remains a major global threat to human health worldwide. Recently, the Chinese medicines with antiviral properties and low toxicity have been a concern. In our previous study, Eupolyphaga sinensis Walker polysaccharide (ESPS) has been isolated and characterized, while its antiviral effect on HBV remained unclear. The anti-HBV activity of ESPS and its regulatory pathway were investigated in vitro and in vivo. The results showed that ESPS significantly inhibited the production of HBsAg, HBeAg, and HBV DNA in the supernatants of HepG2.2.15 in a dose-dependent manner; HBV RNA and core protein expression were also decreased by ESPS. The in vivo studies using HBV transgenic mice further revealed that ESPS (20 and 40 mg/kg/2 days) significantly reduced the levels HBsAg, HBeAg, and HBV DNA in the serum, as well as HBV DNA and HBV RNA in mice liver. In addition, ESPS activated the Toll-like receptor 4 (TLR4) pathway; elevated levels of IFN-β, TNF-α, and IL-6 in the serum were observed, indicating that the anti-HBV effect of ESPS was achieved by potentiating innate immunity function. In conclusion, our study shows that ESPS is a potential anti-HBV ingredient and is of great value in the development of new anti-HBV drugs.

A periodic review of chemical and pharmacological profiles of Tubiechong as insect Chinese medicine.

Tubiechong, in Chinese medicine, denotes the dried female insects of Eupolyphaga sinensis Walker (ESW) or Polyphaga plancyi Bolivar (PPB). As a traditional insect-type, in medicine, it has been historically utilized to treat bruises, fractures, amenorrhea, postpartum blood stasis, lumps and relieving pain. We herein have performed a systematic survey involving the chemical and biological studies in the past decades to reveal the value of such insect resources for their development and clinical utilization. Chemical studies indicated that Tubiechong generated many active compounds, including proteins, amino acids, peptides, fatty acids, alkaloids, nucleosides, polysaccharides, fat-soluble vitamins and mineral elements. Tubiechong or its extract has a wide range of activities including anticoagulation and anti-thrombosis, anti-tumor, antioxidant, immune regulation, blood lipid regulation and hepatoprotection. Finally, a periodic mini-review was conducted to summarize such chemical and pharmacological profiles of Tubiechong medicine. The active peptides in Tubiechong are majorly focused in this review and introduced as one important aspect since there is much literature and huge investigative interest in it. Traditional medical use of the insect was also stressed in this review associating with its disease-eliminating actions by promoting blood circulation or eliminating tissue-swelling pains, which might play important roles in anticancer practices or investigation. In accordance with the modern pharmacological progress, Tubiechong and its extracts indeed exerted antitumor actions through multiple pathways, such as interfering with tumor biological behaviors (growth, apoptosis, invasion, metastasis and angiogenesis), and regulating host immune function. To some extent, this knowledge would provide a basis for further research and application of Tubiechong medicine.

Huoxuezhitong capsule ameliorates MIA-induced osteoarthritis of rats through suppressing PI3K/ Akt/ NF-κB pathway

Huoxuezhitong capsule (HXZT, activating blood circulation and relieving pain capsule), has been applied for osteoarthritis since 1974. It consists of Angelica sinensis (Oliv.) Diels, Panax notoginseng (Burkill) F. H. Chen ex C. H., Boswellia sacra, Borneol, Eupolyphaga sinensis Walker, Pyritum. However, the direct effects of HXZT on osteoarthritis and the underlying mechanisms were poorly understood. In this study, we aimed to explore the analgesia effect of HXZT on MIA-induced osteoarthritis rat and the underlying mechanisms. The analgesia and anti-inflammatory effect of HXZT on osteoarthritis in vivo were tested by the arthritis model rats induced by monosodium iodoacetate (MIA).. Mechanistic studies confirmed that HXZT could inhibit the activation of NF-κB and down-regulate the mRNA expression of related inflammatory factors in LPS-induced RAW264.7 and ATDC5 cells. Furtherly, in LPS-induced RAW264.7 cells, HXZT could suppress NF-κB via inhibiting PI3K/Akt pathway. Taken together, HXZT capsule could ameliorate MIA-induced osteoarthritis of rats through suppressing PI3K/ Akt/ NF-κB pathway.

Characterization of a polysaccharide from Eupolyphaga sinensis walker and its effective antitumor activity via lymphocyte activation

A polysaccharide (ESPS) purified from Eupolyphaga sinensis Walker by ion exchange chromatography and gel chromatography was investigated, including its structure characterization and antitumor activity. The results showed that ESPS was composed of rhamnose, fucose, arabinose, xylose, glucose, and galactose in a molar ratio of 7.4: 3.1: 13.9: 9.3: 39.7: 26.5, with the mean weight (Mw) of 2.14 × 104Da; the main chain of ESPS was mainly composed of → 4) - α - D - Glcp - (1 → and → 3) - β - D - Galp - (1 →, and the side chains were connected to the main chain through the O-6 atom of glucose and O-4 and O-6 atom of galactose. In addition, ESPS promoted the lymphocyte proliferation and inhibited liver cancer cells growth through enhancing lymphocyte activity in vitro, mainly NK cells. Moreover, ESPS markedly stimulated immunity in H22-bearing mice by increasing the spleen and thymus indices and effectively inhibited H22 cell growth in vivo. These data indicated that ESPS was a polysaccharide component possessing high anti-hepatocellular carcinoma activity, representing a potential immunotherapy candidate for the treatment of liver cancer.

Polypeptides extracted from Eupolyphaga sinensis walker via enzymic digestion alleviate UV radiation-induced skin photoaging

The traditional medicine-Eupolyphaga sinensis walker is a rich source of functional proteins and peptides. In this study, Eupolyphaga sinensis walker were identified to include fifteen amino acids, of which hydrophobic amino acids accounted for 46.7%. Eupolyphaga sinensis walker polypeptides (EPs) were extracted by sequentially hydrolyzing with pepsin and trypsin. EPs could effectively scavenge 1,1-diphenyl-2-picrylhydrazyl radical (DPPH·), superoxide anion radical (O2−), and hydroxyl radical (OH-), and reduce ferric solution in vitro. EPs also enhanced the activities of Ssuperoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPH-Px), increased the contents of hydroxyproline (HYP), and reduced the content of Malondialdehyde (MDA) in photoaged mice skin. Histological study confirmed that EPs improved UV irradiation-induced damage of skin texture and morphology. Therefore, the extracted EPs are effective antioxidants and can serve as powerful treatment for skin photoaging.

Sophora flavescens Containing-QYJD Formula Activates Nrf2 Anti-Oxidant Response, Blocks Cellular Transformation and Protects Against DSS-Induced Colitis in Mouse Model.

Qu-Yu-Jie-Du decoction (QYJD) is a commercially available traditional Chinese medicine (TCM). It is an aqueous extract of a Chinese herbal formula primarily consisting of eight TCM herbs: Taraxacum campylodes G.E.Haglund, Coix lacryma-jobi L., Smilax glabra Roxb., Sanguisorba officinalis L, Styphnolobium japonicum (L.) Schott, Prunus persica (L.) Batsch, Sophora flavescens Aiton, and Eupolyphaga sinensis Walker. Matrine and oxymatrine are two of the major phytochemical constituents of QYJD.Inflammation and oxidative stress are strongly associated with colon carcinogenesis. Colorectal cancer (CRC) is the third most common type of cancer. Therefore, cancer chemopreventive agents targeting CRC are urgently needed. This study was conducted to investigate the potential anticancer effects and the underlying mechanisms of QYJD and its active constituents, matrine and oxymatrine, in human colon cancer HT29 cells and in a dextran sulfate sodium (DSS)-induced colitis mouse model. QYJD and matrine effectively inhibited the proliferation and anchorage-independent growth of HT29 cells in a dose-dependent manner. QYJD and matrine also induced an Nrf2-mediated anti-oxidant response element-luciferase activity and upregulated the Nrf2-mediated anti-oxidative stress genes HO-1 and NQO1 at both the mRNA and protein levels. In the DSS-induced colitis mouse model, QYJD reduced the disease activity index (DAI) and alleviated colonic shortening. Elevated Nrf2 and HO-1 mRNA levels were also observed in QYJD-treated mice. These findings showed that QYJD could elicit anti-inflammatory and anti-oxidative stress response in vitro in a cell line and in vivo in a DSS-induced colitis mouse model. These responses may contribute to the overall anticolon cancer effect of QYJD.

Eupolyphaga sinensis Walker Ethanol Extract Suppresses Cell Growth and Invasion in Human Breast Cancer Cells.

To examine the antiproliferation and anti-invasion of Eupolyphaga sinensis Walker 70% ethanol extract (ESWE) on breast cancer and elucidate the underlying signaling mechanisms. MTT and colony formation assays were used to investigate the effect of ESWE on proliferation of breast cancer cells in vitro. The xenograft mouse tumor model was used to determine the effect of ESWE on breast cancer in vivo. To investigate the underlying molecular mechanisms, we used western blotting to analyze the expression of ERK1/2, CXCR4, matrix metalloproteinase 2 (MMP2), and MMP9 pretreated with ESWE. The stromal cell-derived factor (SDF)-1α-induced migration and invasion potential of breast cancer cells were examined by wound-healing assays and Matrigel invasion chamber assays. ESWE effectively inhibited the proliferation of MDA-MB-435s and MDA-MB-231 cells and exhibited antitumor effects in an MDA-MB-231 xenograft mice model. Furthermore, ESWE suppressed the activity of ERK1/2, a key molecule of MAPK signaling. We also observed that ESWE treatment led to downregulation of CXCR4 expression as well as greatly reduced MMP2 and MMP9. ESWE affected CXCR4 expression partially through the modulation of autocrine vascular endothelial growth factor. However, suppression of CXCR4 expression was the result of downregulation of mRNA expression. Inhibition of CXCR4 expression by ESWE further correlated with the suppression of SDF-1α-induced migration and invasion in breast cancer cells. ESWE exerted its antiproliferation and antiinvasion by regulating MAPK signaling and related metastasis factorsand thus could be a useful therapeutic candidate for breast cancer intervention.

Eupolyphaga sinensis Walker screened by cell membrane chromatography and its inhibition on Hek293/EGFR cells by modulating the EGFR signaling pathway

Eupolyphaga sinensis Walker screened by cell membrane chromatography and its inhibition on Hek293/EGFR cells by modulating the EGFR signaling pathway

Eupolyphaga sinensis Walker demonstrates angiogenic activity and inhibits A549 cell growth by targeting the KDR signaling pathway.

Eupolyphaga sinensis Walker has been reported to have anticoagulation, antithrombotic, liver protective and antitumor effects. In the present study, the inhibitory effects on proliferation of A549 human non‑small cell lung cancer cells and the underlying mechanisms were examined. Firstly, three solvents, 70% ethanol, distilled water and 95% ethanol, were used to extract Eupolyphaga sinensis Walker. The MTT assay results demonstrated that the 70% ethanol extract more potently reduced the growth of A549 cells and it was therefore adopted in the subsequent experiments. Eupolyphaga sinensis Walker 70% ethanol extract significantly inhibited A549 cell migration in a time‑ and dose‑dependent manner and inhibited human umbilical vein endothelial cell proliferation, migration and tube formation. Furthermore, Eupolyphaga sinensis Walker 70% ethanol extract effectively inhibited blood vessel formation in the established tissue model for angiogenesis. In addition, Eupolyphaga sinensis Walker 70% ethanol extract was demonstrated to inhibit the autophosphorylation of KDR, and downregulate the subsequent activation of AKT and extracellular signal regulated kinase (ERK)1/2 in A549 cells. In conclusion, these findings demonstrated that the antitumor mechanism of Eupolyphaga sinensis Walker 70% ethanol extract was through inhibiting angiogenesis. It functioned by interrupting the autophosphorylation of KDR and subsequently, AKT and ERK1/2.