The density functional calculation is performed for centrosymmetric（La–Pm） GaO3 rare earth gallates, using a full potential linear augmented plane wave method with the LSDA and LSDA＋U exchange correlation to treat...The density functional calculation is performed for centrosymmetric（La–Pm） GaO3 rare earth gallates, using a full potential linear augmented plane wave method with the LSDA and LSDA＋U exchange correlation to treat highly correlated electrons due to the very localized 4f orbitals of rare earth elements, and explore the influence of U = 0.478 Ry on the magnetic phase stability and the densities of states. LSDA＋U calculation shows that the ferromagnetic（FM） state of RGaO3 is energetically more favorable than the anti-ferromagnetic（AFM） one, except for LaGaO3 where the NM state is the lowest in energy. The energy band gaps of RGaO3 are found to be in the range of 3.8–4.0 eV, indicating the semiconductor character with a large gap.展开更多
Soluble receptor for advanced glycation end products(sRAGE)acts as a decoy sequestering of RAGE ligands,thus preventing the activation of the ligand-RAGE axis linking human diseases.However,the molecular mechanisms un...Soluble receptor for advanced glycation end products(sRAGE)acts as a decoy sequestering of RAGE ligands,thus preventing the activation of the ligand-RAGE axis linking human diseases.However,the molecular mechanisms underlying sRAGE remain unclear.In this study,THP-1 monocytes were cultured in normal glucose(NG,5.5 mmol/L)and high glucose(HG,15 mmol/L)to investigate the effects of diabetesrelevant glucose concentrations on sRAGE and interleukin-1β(IL-1β)secretion.The modulatory effects of epigallocatechin gallate(EGCG)in response to HG challenge were also evaluated.HG enhanced intracellular reactive oxygen species(ROS)generation and RAGE expression.The secretion of sRAGE,including esRAGE and cRAGE,was reduced under HG conditions,together with the downregulation of a disintegrin and metallopeptidase 10(ADAM10)and nuclear factor erythroid 2-related factor 2(Nrf2)nuclear translocation.Mechanistically,the HG effects were counteracted by siRAGE and exacerbated by siNrf2.Chromatin immunoprecipitation results showed that Nrf2 binding to the ADAM10 promoter and HG interfered with this binding.Our data reinforce the notion that RAGE and Nrf2 might be sRAGE-regulating factors.Under HG conditions,the treatment of EGCG reduced ROS generation and RAGE activation.EGCG-stimulated cRAGE release was likely caused by the upregulation of the Nrf2-ADAM10 pathway.EGCG inhibited HG-mediated NLRP3 inflammasome activation at least partly by stimulating sRAGE,thereby reducing IL-1βrelease.展开更多
Dextran-covered poly(D,L-lactide) (PLA) nano-and microparticles were prepared using an emulsion/solvent evaporation (or diffusion) process for the encapsulation of alkyl gallates (AGs).In the first step,a solution of ...Dextran-covered poly(D,L-lactide) (PLA) nano-and microparticles were prepared using an emulsion/solvent evaporation (or diffusion) process for the encapsulation of alkyl gallates (AGs).In the first step,a solution of PLA and AG in ethyl acetate was emulsified to give an aqueous phase containing a hydrophobically modified dextran,which acted as a stabilizer.The second step involved solvent evaporation or diffusion.The emulsification conditions were varied,which allowed for the preparation of nanoand microparticle suspensions covering a wide range of surface-average particle diameters from 0.1 μm (sonication) to 500 μm (stirring with a magnetic bar),with narrow and reproducible size distributions.Continuous microfluidic emulsification in a flow-focusing system led to well-defined microparticles,in the 10-50 μm range.Particles loaded with octyl gallate (OG) and nonyl gallate (NG) were obtained using the three processes,and we showed that the encapsulation efficiency of OG and NG varied significantly depending on the emulsification process.The effect of particle size on the mechanism of in vitro release of encapsulated AGs was investigated.The kinetics of release were controlled either by Fickian diffusion within the solid core or swelling and hydrolytic degradation of the PLA matrix,depending on the pH of the external medium.展开更多
To investigate the anti-α_(s1)-casein allergy mechanism of two tea-derived polyphenols,epigallocatechin(EGC)and epigallocatechin gallate(EGCG),BALB/c mice were sensitized and challenged withα_(s1)-casein and nutriti...To investigate the anti-α_(s1)-casein allergy mechanism of two tea-derived polyphenols,epigallocatechin(EGC)and epigallocatechin gallate(EGCG),BALB/c mice were sensitized and challenged withα_(s1)-casein and nutritional intervention was given by EGC and EGCG during the sensitization provocation phase.The main evaluation indexes used were levels of mast cell proteases,histamine,and specific antibody immunoglobulin E(IgE),as well as cytokine secretion and pathological observation.The results showed that both EGC and EGCG significantly reduced levels of mast cell protease,histamine,specific IgE antibodies,and Th2 cytokines in allergic mice.The histopathology results showed that both EGC and EGCG markedly reduced the degree of lesions in the intestine,thymus,spleen,and lung.The conclusions from this study can provide a theoretical basis for the mechanism by which tea polyphenols regulate food allergens.展开更多
AIM:To evaluate the effect of epigallocatechin gallate(EGCG) in preventing lens opacity and the aggregation of lens αB-crystallin in model rats of diabetes mellitus(DM).METHODS:This experimental study included Wistar...AIM:To evaluate the effect of epigallocatechin gallate(EGCG) in preventing lens opacity and the aggregation of lens αB-crystallin in model rats of diabetes mellitus(DM).METHODS:This experimental study included Wistar rats for DM as in vivo models and divided into 5 groups.The treatment groups were administered EGCG by orally for 20d and were then assessed for their degree of lens opacity with binocular microscope and lens αB-crystallin expression from Western blot analyze.RESULTS:Pearson correlation test and regression analysis on EGCG exposure and final random blood sugar(RBS) obtained a significance level of P<0.05.EGCG exposure can significantly lower RBS with an R~2 of 0.5634(56.34%).The same analysis on EGCG exposure and the degree of lens opacity obtained a significance level of P<0.05 and increased exposure to EGCG can significantly lower the degree of lens opacity with an R~2 of 0.8577(85.77%).Correlation analysis between EGCG and the expression of lens αB-crystallin can be concluded that the higher the EGCG exposure administered,the higher the native lens αB-crystallin expression and the lower the aggregate lens αB-crystallin expression.There was also significant effect in which every 1 mg/kg body weight dose of EGCG can increase the native lens αB-crystallin expression by 0.0063 and decrease the aggregate lens αB-crystallin expression by 0.0076.CONCLUSION:The administration of EGCG at a dose of 300,600,and 1200 mg shows a significant effect on preventing lens opacity and aggregation of αB-crystallin in diabetic rat models and this research could be a biomolecular prevention of cataract.展开更多
Seven compounds were isolated from the EtOH extraction of the twig of Carapa guianensis Aubl. (Meliaceae). On the basis of spectroscopic methods, their structures were elucidated as (-)-epicatechin-3-O-(3' , 5'...Seven compounds were isolated from the EtOH extraction of the twig of Carapa guianensis Aubl. (Meliaceae). On the basis of spectroscopic methods, their structures were elucidated as (-)-epicatechin-3-O-(3' , 5'-di-O-methyl) gallate (1), (-)-catechin (2), sciadopitysin (3), cleomiscosin B (4), photogedunin (5), chisocheton compound F (6) and odoratone (7), respectively. Among them compound 1 was a new flavane, compounds 2-7 were firstly obtained from this plant, and compound 5 was assigned the C-13-NMR data for the first time. Compound 7 exhibited strong antifeedant activity against Pieris brassicae, and compound 2 exhibited moderate activity, while the n-BuOH portion showed weak activity.展开更多
Cancer is one of the leading causes of death worldwide.Commonly used cancer treatments,including chemotherapy and radiation therapy,often have side effects and a complete cure is sometimes impossible.Therefore,prevent...Cancer is one of the leading causes of death worldwide.Commonly used cancer treatments,including chemotherapy and radiation therapy,often have side effects and a complete cure is sometimes impossible.Therefore,prevention,suppression,and/or delaying the onset of the disease are important.The onset of gastroenterological cancers is closely associated with an individual's lifestyle.Thus,changing lifestyle,specifically the consumption of fruits and vegetables,can help to protect against the development of gastroenterological cancers.In particular,naturally occurring bioactive compounds,including curcumin,resveratrol,isothiocyanates,(-)-epigallocatechin gallate and sulforaphane,are regarded as promising chemopreventive agents.Hence,regular consumption of these natural bioactive compounds found in foods can contribute to prevention,suppression,and/or delay of gastroenterological cancer development.In this review,we will summarize natural phytochemicals possessing potential antioxidant and/or anti-inflammatory and anti-carcinogenic activities,which are exerted by regulating or targeting specific molecules against gastroenterological cancers,including esophageal,gastric and colon cancers.展开更多
Systematic inflammatory response after spinal cord injury （SCI） is one of the factors leading to lesion development and a profound degree of functional loss. Anti-inflammatory compounds, such as curcumin and epigall...Systematic inflammatory response after spinal cord injury （SCI） is one of the factors leading to lesion development and a profound degree of functional loss. Anti-inflammatory compounds, such as curcumin and epigallocatechin gallate （EGCG） are known for their neuroprotective effects. In this study, we investigated the effect of combined therapy of curcumin and EGCG in a rat model of acute SCI induced by balloon compression. Immediately after SCI, rats received curcumin, EGCG, curcumin ＋ EGCG or saline [daily intraperitoneal doses （curcumin, 6 mg/kg; EGCG 17 mg/kg）] and weekly intramuscular doses （curcumin,60 mg/kg; EGCG 17 mg/kg）] for 28 days. Rats were evaluated using behavioral tests （the Basso, Beattie, and Bresnahan （BBB） open-field locomotor test, flat beam test）. Spinal cord tissue was analyzed using histological methods （Luxol Blue-cresyl violet staining） and mmunohistochemistry （anti-glial fibrillary acidic protein, anti-growth associated protein 43）. Cytokine levels （interleukin-1β, interleukin-4, interleukin-2,interleukin-6, macrophage inflammatory protein 1-alpha, and RANTES） were measured using Luminex assay. Quantitative polymerase chain reaction was performed to determine the relative expression of genes （Sort1, Fgf2, Irf5, Mrc1, Olig2, Casp3, Gap43, Gfap, Vegf, NfκB, Cntf） related to regenerative processes in injured spinal cord. We found that all treatments displayed significant behavioral recovery, with no obvious synergistic effect after combined therapy of curcumin and ECGC. Curcumin and EGCG alone or in combination increased axonal sprouting, decreased glial scar formation, and altered the levels of macrophage inflammatory protein 1-alpha, interleukin-1β, interleukin-4 and interleukin-6 cytokines. These results imply that although the expected synergistic response of this combined therapy was less obvious, aspects of tissue regeneration and immune responses in severe SCI were evident.展开更多
AIM To investigate the effect of epigallocatechin gallate(EGCG) on structural changes of gut microbiota in colorectal carcinogenesis.METHODS An azoxymethane(AOM)/dextran sodium sulfate(DSS)-induced colitis mouse model...AIM To investigate the effect of epigallocatechin gallate(EGCG) on structural changes of gut microbiota in colorectal carcinogenesis.METHODS An azoxymethane(AOM)/dextran sodium sulfate(DSS)-induced colitis mouse model was established. Fortytwo female FVB/N mice were randomly divided into the following three groups: group 1(10 mice, negative control) was treated with vehicle, group 2(16 mice, positive control) was treated with AOM plus vehicle, and group 3(16 mice, EG) was treated with AOM plus EGCG. For aberrant crypt foci(ACF) evaluation, the colons were rapidly took out after sacrifice, rinsed with saline, opened longitudinally, laid flat on a polystyrene board, and fixed with 10% buffered formaldehyde solution before being stained with 0.2% methylene blue in saline. For tumor evaluation, the colon was macroscopically inspected and photographed, then the total number of tumors was enumerated and tumor size measured. For histological examination, the fixed tissues were paraffin-embedded and sectioned at 5 mm thickness. Microbial genomic DNA was extracted from fecal and intestinal content samples using a commercial kit. The V4 hypervariable regions of 16 S r RNA were PCR-amplified with the barcoded fusion primers. Using the best hit classification option, the sequences from each sample were aligned to the RDP 16 S r RNA training set to classify the taxonomic abundance in QIIME. Statistical analyses were then performed.RESULTS Treatment of mice with 1% EGCG caused a significant decrease in the mean number of ACF per mouse, when compared with the model mice treated with AOM/DSS(5.38 ± 4.24 vs 13.13 ± 3.02, P < 0.01). Compared with the positive control group, 1% EGCG treatment dependently decreased tumor load per mouse by 85%(33.96 ± 6.10 vs 2.96 ± 2.86, respectively, P < 0.01). All revealed that EGCG could inhibit colon carcinogenesis by decreasing the number of precancerous lesions as well as solid tumors, with reduced tumor load and delayed histological progression of CRC. During the cancerization, the diversity of gut microbiota increased, potential carcinogenic bacteria such as Bacteroides were enriched, and the abundance of butyrate-producing bacteria(Clostridiaceae, Ruminococcus, etc.) decreased continuously. In contrast, the structure of gut microbiota was relatively stable during the intervention of EGCG on colon carcinogenesis. Enrichment of probiotics(Bifidobacterium, Lactobacillu, etc.) might be a potential mechanism for EGCG's effects on tumor suppression. Via bioinformatics analysis, principal coordinate analysis and cluster analysis of the tumor formation process, we found that the diversity of gut microbiota increased in the tumor model group while that in the EGCG interfered group(EG) remained relatively stable.CONCLUSION Gut microbiota imbalance might be a potential mechanism for the prevention of malignant transformation by EGCG, which is significant for diagnosis, treatment, prognosis evaluation, and prevention of colorectal cancer.展开更多
AIM:To analyze the antiviral mechanism of Epigallocatechin gallate(EGCG)against hepatitis B virus(HBV) replication.METHODS:In this research,the HBV-replicating cell line HepG2.117 was used to investigate the antiviral...AIM:To analyze the antiviral mechanism of Epigallocatechin gallate(EGCG)against hepatitis B virus(HBV) replication.METHODS:In this research,the HBV-replicating cell line HepG2.117 was used to investigate the antiviral mechanism of EGCG.Cytotoxicity of EGCG was analyzed by 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay.Hepatitis B virus e antigen(HBeAg)and hepatitis B virus surface antigen(HBsAg)in the supernatant were detected by enzyme-linked immunosorbent assay.Precore mRNA and pregenomic RNA(pgRNA) levels were determined by semi-quantitative reverse transcription polymerase chain reaction(PCR)assay.The effect of EGCG on HBV core promoter activity was measured by dual luciferase reporter assay.HBV covalently closed circular DNA and replicative intermediates of DNA were quantified by real-time PCR assay.RESULTS:When HepG2.117 cells were grown in the presence of EGCG,the expression of HBeAg was suppressed,however,the expression of HBsAg was not affected.HBV precore mRNA level was also downregulated by EGCG,while the transcription of precore mRNA was not impaired.The synthesis of both HBV covalently closed circular DNA and replicative intermediates of DNA were reduced by EGCG treatment to a similar extent,however,HBV pgRNA transcripted from chromosome-integrated HBV genome was not affected by EGCG treatment,indicating that EGCG targets only replicative intermediates of DNA synthesis.CONCLUSION:In HepG2.117 cells,EGCG inhibits HBV replication by impairing HBV replicative intermediates of DNA synthesis and such inhibition results in reduced production of HBV covalently closed circular DNA.展开更多
Objective:Our aim was to test the hypothesis that fatty acid synthase(FASN)expression contributes to radioresistance of nasopharyngeal carcinoma(NPC)cells and that inhibiting FASN enhances radiosensitivity.Methods:Tar...Objective:Our aim was to test the hypothesis that fatty acid synthase(FASN)expression contributes to radioresistance of nasopharyngeal carcinoma(NPC)cells and that inhibiting FASN enhances radiosensitivity.Methods:Targeting FASN using epigallocatechin gallate(EGCG)or RNA interference in NPC cell lines that overexpress endogenous FASN was performed to determine their effects on cellular response to radiationin vitro using MTT and colony formation assays,andin vivo using xenograft animal models.Western blot,immunohistochemistry,real-time PCR arrays,and real-time RT-PCR were used to determine the relationship between FASN and frizzled class receptor 10(FZD10)expression.FZD10 knockdown and overexpression were used to determine its role in mediating FASN function in cellular response to radiation.Immunohistochemical staining was used to determine FASN and FZD10 expressions in human NPC tissues,followed by analysis of their association with the overall survival of patients.Results:FASN knockdown or inhibition significantly enhanced radiosensitivity of NPC cells,bothin vitro andin vivo.There was a positive association between FASN and FZD10 expression in NPC cell lines grown as monolayers or xenografts,as well as human tissues.FASN knockdown reduced FZD10 expression,and rescue of FZD10 expression abolished FASN knockdown-induced enhancement of radiosensitivity.FASN and FZD10 were both negatively associated with overall survival of NPC patients.Conclusions:FASN contributes to radioresistance,possiblyvia FZD10 in NPC cells.Both FZD10 and FASN expressions were associated with poor outcomes of NPC patients.EGCG may sensitize radioresistance by inhibiting FASN and may possibly be developed as a radiosensitizer for better treatment of NPCs.展开更多
Flavonoids,secondary plant products which could be essential for normal physiology in humans and animals,may be the vitamins of the next century.Flavonoids belong to the polyphenols and possess antioxidative,anti-infl...Flavonoids,secondary plant products which could be essential for normal physiology in humans and animals,may be the vitamins of the next century.Flavonoids belong to the polyphenols and possess antioxidative,anti-inflammatory,antimutagenic and anticarcinogenic properties.Among the various flavonoid species,tea flavonoids such as apigenin (from camomile) and epigallocatechin gallate (EGCG from green tea) can be used for the prevention of intestinal neoplasia,especially for adenoma and cancer prevention in the gastrointestinal tract.Numerous experimental studies with molecular and biological end points support the therapeutic efficacy of bioflavonoids.Clinical studies with cohorts and case-control trials suggest that flavonoids are effective in tertiary bioprevention but,as yet,there are no controlled randomized clinical trials.Flavonoids can inhibit inflammatory pathways and could be useful for chronic inflammatory bowel diseases.Flavonoid deficiency syndromes could be therapeutic targets in the future.展开更多
Objective: To investigate the effect of Red Peony 801 (propyl gallate,PrG) on cyclooxygenase (COX) activity in murine peritoneal macrophages. Methods: A screening model for COX inhibitors in vitro based on murine peri...Objective: To investigate the effect of Red Peony 801 (propyl gallate,PrG) on cyclooxygenase (COX) activity in murine peritoneal macrophages. Methods: A screening model for COX inhibitors in vitro based on murine peritoneal macrophages was used. COX-1 activity was reflected by the level of 6-ketoprostaglandin F1α(6-keto-PGF1α) in supernatants of cultured macrophages which were stimulated with calcium ionophore A23187 for a short-term, while COX-2 activity was reflected by the level of prostaglandin E2 (PGE2) in supernatants of cultured macrophages which were stimulated with lipopolysaccharide (LPS) for a long-term. Results: PrG did not affect A23187-induced, COX-1-derived 6-keto-PGF1α synthesis at the concentrations of 1×10-5, 5×10-6 mol/L (P>0.05), but enhanced 6-keto-PGF1α synthesis at the concentrations of 1×10-6, 5×10-7, 1×10-7 mol/L (P<0.01) in vitro, and showed a good dose-dependent manner. It inhibited LPS-induced, COX-2-derived PGE2 synthesis at the concentrations of 1×10-5,1×10-6 mol/L (P< 0. 05). Conclusion: Within the range of 1×10-5 to 1×10-7 mol/L, PrG activated COX-1 at lower concentrations and inhibited COX-2 at higher concentrations in murine peritoneal macrophages.展开更多
The fresh leaves of China green tea, Camellia sinensis, were collected from Fuyang, Zhejiang Province, China, in April. The tea polyphenols was extracted by four different methods （homogenized with distilled water at...The fresh leaves of China green tea, Camellia sinensis, were collected from Fuyang, Zhejiang Province, China, in April. The tea polyphenols was extracted by four different methods （homogenized with distilled water at room temperature, homogenized with 0.3% citric acid （w/v） at room temperature, 5- min boiling and homogenized with distilled water at room temperature, homogenized with 85℃ distilled water）, and after preserving at room temperature, the change of the Epigallocatechin gallate （EGCG） contents of the extracts was investigated. Results indicated that the EGCG content of homogenate extracted with 85℃ distilled water was the highest before the extract was preserved, followed by that of the extract homogenized with 0.3% citric acid at room temperature. During preservation, EGCG content changed obviously. The EGCG contents of homogenates extracted with distilled water at room temperature and 85℃ distilled water declined quickly and separately reduced to 21.52% and 54.6% of their initial contents after preservation for 12 h. The EGCG contents extracted by 0.3% citric acid （w/v） solvent at room temperature and 5- min boiling/homogenized with distilled water at room temperature declined relatively slowly ,and separately reduced to 76.9% and 85.16% of their initial contents after preservation for 12 h. It was also found that the citric acid can prevent the degradation of EGCG and the extract solution color is light green展开更多
BACKGROUND Epigallocatechin gallate(EGCG)is a polyhydroxy phenolic compound extracted from tea and its antitumor effect has received widespread attention.We explored the inhibitory effect of EGCG on dimethylhydrazine(...BACKGROUND Epigallocatechin gallate(EGCG)is a polyhydroxy phenolic compound extracted from tea and its antitumor effect has received widespread attention.We explored the inhibitory effect of EGCG on dimethylhydrazine(DMH)-induced colorectal cancer(CRC)using a rat model,predicted the interaction between EGCG and CRC target genes using a database,and explained the EGCG associated target pathways and mechanisms in CRC.AIM To understand the inhibitory mechanisms of EGCG on CRC cell proliferation and identify its pharmacological targets by network pharmacology analysis.METHODS DMH(40 mg/kg,s.c.,twice weekly for eight weeks)was used to induce CRC in rats.After model establishment,the rats were administered with EGCG(50,100,or 200 mg/kg,p.o.,once daily for eight weeks)and killed 12 and 20 wk after the start of the experiment.Formation of aberrant crypt foci and tumor was studied by histological analysis.Using network pharmacology analysis,candidate and collective targets of EGCG and CRC were identified,and Gene ontology(GO)and Kyoto Encyclopedia of Genes and Genomes analyses were used to predict the pathways altered by EGCG.RESULTS At week 12,high-dose EGCG treatment significantly reduced the tumor formation rate,total number of tumors,cancerous and non-cancerous tumors,tumor volume,ascites formation,and aberrant crypt foci count.At week 20,all three doses of EGCG were effective.Seventy-eight collective targets of EGCG and CRC were identified,of which 28 genes were dysregulated in CRC.Kyoto Encyclopedia of Genes and Genomes and GO analyses showed that the dysregulated genes were enriched in hsa05210(CRC),hsa04115(p53 signaling pathway),and hsa04151(PI3K-Akt signaling pathway),GO:0043124(negative regulation of I-kappaB kinase/NF-kappaB signaling pathway),GO:0043409(negative regulation of mitogen-activated protein kinase cascade),and GO:2001244(positive regulation of intrinsic apoptotic signaling pathway)respectively.CONCLUSION EGCG inhibits the formation of DMH-induced CRC by regulating key pathways involved in tumorigenesis.展开更多
Although herbal medicines(HMs)are widely used in the prevention and treatment of obesity and obesity-associated disorders,the key constituents exhibiting anti-obesity activity and their molecular mechanisms are poorly...Although herbal medicines(HMs)are widely used in the prevention and treatment of obesity and obesity-associated disorders,the key constituents exhibiting anti-obesity activity and their molecular mechanisms are poorly understood.Recently,we assessed the inhibitory potentials of several HMs against human pancreatic lipase(hPL,a key therapeutic target for human obesity),among which the root-extract of Rhodiola crenulata(ERC)showed the most potent anti-hPL activity.In this study,we adopted an integrated strategy,involving bioactivity-guided fractionation techniques,chemical profiling,and biochemical assays,to identify the key anti-hPL constituents in ERC.Nine ERC fractions(retention time=12.5e35 min),obtained using reverse-phase liquid chromatography,showed strong anti-hPL activity,while the major constituents in these bioactive fractions were subsequently identified using liquid chromatography-quadrupole time-of-flight mass spectrometry(LC-Q-TOF-MS/MS).Among the identified ERC constituents,1,2,3,4,6-penta-O-galloyl-β-D-glucopyranose(PGG)and catechin gallate(CG)showed the most potent anti-hPL activity,with pIC50 values of 7.59±0.03 and 7.68±0.23,respectively.Further investigations revealed that PGG and CG potently inhibited hPL in a non-competitive manner,with inhibition constant(Ki)values of 0.012 and 0.082 mM,respectively.Collectively,our integrative analyses enabled us to efficiently identify and characterize the key anti-obesity constituents in ERC,as well as to elucidate their anti-hPL mechanisms.These findings provide convincing evidence in support of the anti-obesity and lipid-lowering properties of ERC.展开更多
Thermosetting polyurethanes are widely used in various fields owing to their excellent elasticity,strength and solvent resistance.Three environmental friendly propyl gallate-based self-healing polyurethanes were prepa...Thermosetting polyurethanes are widely used in various fields owing to their excellent elasticity,strength and solvent resistance.Three environmental friendly propyl gallate-based self-healing polyurethanes were prepared from polyurethane prepolymers with varying isocyanate content.The thermal stabilities of the polyurethanes were tested using thermogravimetric analysis.Their self-healing and mechanical properties were analyzed using a universal testing machine and dynamic thermomechanical analysis.The polyurethanes were found with high self-healing ability and excellent mechanical properties due to the absence of phenolic carbamate.These qualities improved with increased isocyanate content and the prolonged selfhealing time.We found,therefore,that the propyl gallate-based polyurethane has potential for use in industrial applications as self-healing materials.展开更多
AIM：To compare the potential protective effects of epigallocatechin gallate（EGCG） and ellagic acid（EA） in an experimental cataract model.●METHODS：Twenty-eight Spraque-Dawley rat pups were assigned into four gro...AIM：To compare the potential protective effects of epigallocatechin gallate（EGCG） and ellagic acid（EA） in an experimental cataract model.●METHODS：Twenty-eight Spraque-Dawley rat pups were assigned into four groups.All the rats,except for those in the control group,were injected subcutaneously sodium selenite to induce experimental cataract on the postpartum ninth day,and between 10 th and 14 th days.Rats in the sham,EGCG,and EA groups were intraperitoneally administered 50 mg/（kg·d） saline solution,50 mg/（kg·d） EGCG and 200 mg/（kg·d） EA,respectively.The reduced glutathione（GSH） and malondialdehyde（MDA） levels,total antioxidant status（TAS） and total oxidant status（TOS） in lens supernatants were measured.RESULTS：The mean cataract gradings in EGCG and EA groups were found to be significantly lower than that in sham group（P〈0.001）.The mean GSH levels and TASs in EGCG and EA groups were significantly higher than that in sham group while mean MDA levels and TOSs in EGCG and EA groups were significantly lower than that in the sham group（P〈0.001）.CONCLUSION：EGCG and EA have protective effects on cataract development via the inhibition of oxidative stress.展开更多
文摘The density functional calculation is performed for centrosymmetric（La–Pm） GaO3 rare earth gallates, using a full potential linear augmented plane wave method with the LSDA and LSDA＋U exchange correlation to treat highly correlated electrons due to the very localized 4f orbitals of rare earth elements, and explore the influence of U = 0.478 Ry on the magnetic phase stability and the densities of states. LSDA＋U calculation shows that the ferromagnetic（FM） state of RGaO3 is energetically more favorable than the anti-ferromagnetic（AFM） one, except for LaGaO3 where the NM state is the lowest in energy. The energy band gaps of RGaO3 are found to be in the range of 3.8–4.0 eV, indicating the semiconductor character with a large gap.
文摘Soluble receptor for advanced glycation end products(sRAGE)acts as a decoy sequestering of RAGE ligands,thus preventing the activation of the ligand-RAGE axis linking human diseases.However,the molecular mechanisms underlying sRAGE remain unclear.In this study,THP-1 monocytes were cultured in normal glucose(NG,5.5 mmol/L)and high glucose(HG,15 mmol/L)to investigate the effects of diabetesrelevant glucose concentrations on sRAGE and interleukin-1β(IL-1β)secretion.The modulatory effects of epigallocatechin gallate(EGCG)in response to HG challenge were also evaluated.HG enhanced intracellular reactive oxygen species(ROS)generation and RAGE expression.The secretion of sRAGE,including esRAGE and cRAGE,was reduced under HG conditions,together with the downregulation of a disintegrin and metallopeptidase 10(ADAM10)and nuclear factor erythroid 2-related factor 2(Nrf2)nuclear translocation.Mechanistically,the HG effects were counteracted by siRAGE and exacerbated by siNrf2.Chromatin immunoprecipitation results showed that Nrf2 binding to the ADAM10 promoter and HG interfered with this binding.Our data reinforce the notion that RAGE and Nrf2 might be sRAGE-regulating factors.Under HG conditions,the treatment of EGCG reduced ROS generation and RAGE activation.EGCG-stimulated cRAGE release was likely caused by the upregulation of the Nrf2-ADAM10 pathway.EGCG inhibited HG-mediated NLRP3 inflammasome activation at least partly by stimulating sRAGE,thereby reducing IL-1βrelease.
文摘Dextran-covered poly(D,L-lactide) (PLA) nano-and microparticles were prepared using an emulsion/solvent evaporation (or diffusion) process for the encapsulation of alkyl gallates (AGs).In the first step,a solution of PLA and AG in ethyl acetate was emulsified to give an aqueous phase containing a hydrophobically modified dextran,which acted as a stabilizer.The second step involved solvent evaporation or diffusion.The emulsification conditions were varied,which allowed for the preparation of nanoand microparticle suspensions covering a wide range of surface-average particle diameters from 0.1 μm (sonication) to 500 μm (stirring with a magnetic bar),with narrow and reproducible size distributions.Continuous microfluidic emulsification in a flow-focusing system led to well-defined microparticles,in the 10-50 μm range.Particles loaded with octyl gallate (OG) and nonyl gallate (NG) were obtained using the three processes,and we showed that the encapsulation efficiency of OG and NG varied significantly depending on the emulsification process.The effect of particle size on the mechanism of in vitro release of encapsulated AGs was investigated.The kinetics of release were controlled either by Fickian diffusion within the solid core or swelling and hydrolytic degradation of the PLA matrix,depending on the pH of the external medium.
基金supported by the National Key Research and Development Program of China(2019YFC1605002)the National Natural Science Foundation of China(31872886)。
文摘To investigate the anti-α_(s1)-casein allergy mechanism of two tea-derived polyphenols,epigallocatechin(EGC)and epigallocatechin gallate(EGCG),BALB/c mice were sensitized and challenged withα_(s1)-casein and nutritional intervention was given by EGC and EGCG during the sensitization provocation phase.The main evaluation indexes used were levels of mast cell proteases,histamine,and specific antibody immunoglobulin E(IgE),as well as cytokine secretion and pathological observation.The results showed that both EGC and EGCG significantly reduced levels of mast cell protease,histamine,specific IgE antibodies,and Th2 cytokines in allergic mice.The histopathology results showed that both EGC and EGCG markedly reduced the degree of lesions in the intestine,thymus,spleen,and lung.The conclusions from this study can provide a theoretical basis for the mechanism by which tea polyphenols regulate food allergens.
文摘AIM:To evaluate the effect of epigallocatechin gallate(EGCG) in preventing lens opacity and the aggregation of lens αB-crystallin in model rats of diabetes mellitus(DM).METHODS:This experimental study included Wistar rats for DM as in vivo models and divided into 5 groups.The treatment groups were administered EGCG by orally for 20d and were then assessed for their degree of lens opacity with binocular microscope and lens αB-crystallin expression from Western blot analyze.RESULTS:Pearson correlation test and regression analysis on EGCG exposure and final random blood sugar(RBS) obtained a significance level of P<0.05.EGCG exposure can significantly lower RBS with an R~2 of 0.5634(56.34%).The same analysis on EGCG exposure and the degree of lens opacity obtained a significance level of P<0.05 and increased exposure to EGCG can significantly lower the degree of lens opacity with an R~2 of 0.8577(85.77%).Correlation analysis between EGCG and the expression of lens αB-crystallin can be concluded that the higher the EGCG exposure administered,the higher the native lens αB-crystallin expression and the lower the aggregate lens αB-crystallin expression.There was also significant effect in which every 1 mg/kg body weight dose of EGCG can increase the native lens αB-crystallin expression by 0.0063 and decrease the aggregate lens αB-crystallin expression by 0.0076.CONCLUSION:The administration of EGCG at a dose of 300,600,and 1200 mg shows a significant effect on preventing lens opacity and aggregation of αB-crystallin in diabetic rat models and this research could be a biomolecular prevention of cataract.
文摘Seven compounds were isolated from the EtOH extraction of the twig of Carapa guianensis Aubl. (Meliaceae). On the basis of spectroscopic methods, their structures were elucidated as (-)-epicatechin-3-O-(3' , 5'-di-O-methyl) gallate (1), (-)-catechin (2), sciadopitysin (3), cleomiscosin B (4), photogedunin (5), chisocheton compound F (6) and odoratone (7), respectively. Among them compound 1 was a new flavane, compounds 2-7 were firstly obtained from this plant, and compound 5 was assigned the C-13-NMR data for the first time. Compound 7 exhibited strong antifeedant activity against Pieris brassicae, and compound 2 exhibited moderate activity, while the n-BuOH portion showed weak activity.
基金Supported by Grants from the Next-Generation BioGreen 21 Program (Plant Molecular Breeding Center,No. PJ008187),Rural Development Administrationthe Leap Research Program(2010-0029233)World Class University Program (GrantR31-2008-00-10056-0) through the National Research Foundation of Korea funded by the Ministry of Education,Science and Technology,South Korea
文摘Cancer is one of the leading causes of death worldwide.Commonly used cancer treatments,including chemotherapy and radiation therapy,often have side effects and a complete cure is sometimes impossible.Therefore,prevention,suppression,and/or delaying the onset of the disease are important.The onset of gastroenterological cancers is closely associated with an individual's lifestyle.Thus,changing lifestyle,specifically the consumption of fruits and vegetables,can help to protect against the development of gastroenterological cancers.In particular,naturally occurring bioactive compounds,including curcumin,resveratrol,isothiocyanates,(-)-epigallocatechin gallate and sulforaphane,are regarded as promising chemopreventive agents.Hence,regular consumption of these natural bioactive compounds found in foods can contribute to prevention,suppression,and/or delay of gastroenterological cancer development.In this review,we will summarize natural phytochemicals possessing potential antioxidant and/or anti-inflammatory and anti-carcinogenic activities,which are exerted by regulating or targeting specific molecules against gastroenterological cancers,including esophageal,gastric and colon cancers.
基金supported by the grant GACR(Grant Agency of the Czech Republic)P304/12/G069the Ministry of Education,Youth and Sports under the project“Centre of Reconstructive Neuroscience”,registration number CZ.02.1.01/0.0./0.0/15_003/0000419project Inter Action LTAUSA17120
文摘Systematic inflammatory response after spinal cord injury （SCI） is one of the factors leading to lesion development and a profound degree of functional loss. Anti-inflammatory compounds, such as curcumin and epigallocatechin gallate （EGCG） are known for their neuroprotective effects. In this study, we investigated the effect of combined therapy of curcumin and EGCG in a rat model of acute SCI induced by balloon compression. Immediately after SCI, rats received curcumin, EGCG, curcumin ＋ EGCG or saline [daily intraperitoneal doses （curcumin, 6 mg/kg; EGCG 17 mg/kg）] and weekly intramuscular doses （curcumin,60 mg/kg; EGCG 17 mg/kg）] for 28 days. Rats were evaluated using behavioral tests （the Basso, Beattie, and Bresnahan （BBB） open-field locomotor test, flat beam test）. Spinal cord tissue was analyzed using histological methods （Luxol Blue-cresyl violet staining） and mmunohistochemistry （anti-glial fibrillary acidic protein, anti-growth associated protein 43）. Cytokine levels （interleukin-1β, interleukin-4, interleukin-2,interleukin-6, macrophage inflammatory protein 1-alpha, and RANTES） were measured using Luminex assay. Quantitative polymerase chain reaction was performed to determine the relative expression of genes （Sort1, Fgf2, Irf5, Mrc1, Olig2, Casp3, Gap43, Gfap, Vegf, NfκB, Cntf） related to regenerative processes in injured spinal cord. We found that all treatments displayed significant behavioral recovery, with no obvious synergistic effect after combined therapy of curcumin and ECGC. Curcumin and EGCG alone or in combination increased axonal sprouting, decreased glial scar formation, and altered the levels of macrophage inflammatory protein 1-alpha, interleukin-1β, interleukin-4 and interleukin-6 cytokines. These results imply that although the expected synergistic response of this combined therapy was less obvious, aspects of tissue regeneration and immune responses in severe SCI were evident.
基金Supported by Natural Science Foundation of Minhang District of Shanghai,No.2012MHZ001
文摘AIM To investigate the effect of epigallocatechin gallate(EGCG) on structural changes of gut microbiota in colorectal carcinogenesis.METHODS An azoxymethane(AOM)/dextran sodium sulfate(DSS)-induced colitis mouse model was established. Fortytwo female FVB/N mice were randomly divided into the following three groups: group 1(10 mice, negative control) was treated with vehicle, group 2(16 mice, positive control) was treated with AOM plus vehicle, and group 3(16 mice, EG) was treated with AOM plus EGCG. For aberrant crypt foci(ACF) evaluation, the colons were rapidly took out after sacrifice, rinsed with saline, opened longitudinally, laid flat on a polystyrene board, and fixed with 10% buffered formaldehyde solution before being stained with 0.2% methylene blue in saline. For tumor evaluation, the colon was macroscopically inspected and photographed, then the total number of tumors was enumerated and tumor size measured. For histological examination, the fixed tissues were paraffin-embedded and sectioned at 5 mm thickness. Microbial genomic DNA was extracted from fecal and intestinal content samples using a commercial kit. The V4 hypervariable regions of 16 S r RNA were PCR-amplified with the barcoded fusion primers. Using the best hit classification option, the sequences from each sample were aligned to the RDP 16 S r RNA training set to classify the taxonomic abundance in QIIME. Statistical analyses were then performed.RESULTS Treatment of mice with 1% EGCG caused a significant decrease in the mean number of ACF per mouse, when compared with the model mice treated with AOM/DSS(5.38 ± 4.24 vs 13.13 ± 3.02, P < 0.01). Compared with the positive control group, 1% EGCG treatment dependently decreased tumor load per mouse by 85%(33.96 ± 6.10 vs 2.96 ± 2.86, respectively, P < 0.01). All revealed that EGCG could inhibit colon carcinogenesis by decreasing the number of precancerous lesions as well as solid tumors, with reduced tumor load and delayed histological progression of CRC. During the cancerization, the diversity of gut microbiota increased, potential carcinogenic bacteria such as Bacteroides were enriched, and the abundance of butyrate-producing bacteria(Clostridiaceae, Ruminococcus, etc.) decreased continuously. In contrast, the structure of gut microbiota was relatively stable during the intervention of EGCG on colon carcinogenesis. Enrichment of probiotics(Bifidobacterium, Lactobacillu, etc.) might be a potential mechanism for EGCG's effects on tumor suppression. Via bioinformatics analysis, principal coordinate analysis and cluster analysis of the tumor formation process, we found that the diversity of gut microbiota increased in the tumor model group while that in the EGCG interfered group(EG) remained relatively stable.CONCLUSION Gut microbiota imbalance might be a potential mechanism for the prevention of malignant transformation by EGCG, which is significant for diagnosis, treatment, prognosis evaluation, and prevention of colorectal cancer.
基金Supported by National Technology and Science Key Project (2008ZX10002-010)the Important National Science and Technology Specific Projects(2009ZX09301-014)
文摘AIM:To analyze the antiviral mechanism of Epigallocatechin gallate(EGCG)against hepatitis B virus(HBV) replication.METHODS:In this research,the HBV-replicating cell line HepG2.117 was used to investigate the antiviral mechanism of EGCG.Cytotoxicity of EGCG was analyzed by 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay.Hepatitis B virus e antigen(HBeAg)and hepatitis B virus surface antigen(HBsAg)in the supernatant were detected by enzyme-linked immunosorbent assay.Precore mRNA and pregenomic RNA(pgRNA) levels were determined by semi-quantitative reverse transcription polymerase chain reaction(PCR)assay.The effect of EGCG on HBV core promoter activity was measured by dual luciferase reporter assay.HBV covalently closed circular DNA and replicative intermediates of DNA were quantified by real-time PCR assay.RESULTS:When HepG2.117 cells were grown in the presence of EGCG,the expression of HBeAg was suppressed,however,the expression of HBsAg was not affected.HBV precore mRNA level was also downregulated by EGCG,while the transcription of precore mRNA was not impaired.The synthesis of both HBV covalently closed circular DNA and replicative intermediates of DNA were reduced by EGCG treatment to a similar extent,however,HBV pgRNA transcripted from chromosome-integrated HBV genome was not affected by EGCG treatment,indicating that EGCG targets only replicative intermediates of DNA synthesis.CONCLUSION:In HepG2.117 cells,EGCG inhibits HBV replication by impairing HBV replicative intermediates of DNA synthesis and such inhibition results in reduced production of HBV covalently closed circular DNA.
基金This work was supported by grants from the National Natural Science Foundation of China(Grant Nos.81572588,81872147)Shantou University Medical College Clinical Trial Uplift Program(Grant No.201423)+4 种基金the Medical Scientific Research Foundation of Guangdong Province,China(Grant No.B2018222)the Traditional Chinese Medicine Research Project from Traditional Chinese Medicine Bureau of Guangdong Province(Grant No.20191182)the Youth Research Grant from Shantou University Medical College Cancer Hospital(Grant No.2018A001,2018A008)the key Project of Science and Technology of Shantou[Grant No.(2018)37]and the Natural Science Foundation of Guangdong Province of China(Grant No.2020A1515010094).
文摘Objective:Our aim was to test the hypothesis that fatty acid synthase(FASN)expression contributes to radioresistance of nasopharyngeal carcinoma(NPC)cells and that inhibiting FASN enhances radiosensitivity.Methods:Targeting FASN using epigallocatechin gallate(EGCG)or RNA interference in NPC cell lines that overexpress endogenous FASN was performed to determine their effects on cellular response to radiationin vitro using MTT and colony formation assays,andin vivo using xenograft animal models.Western blot,immunohistochemistry,real-time PCR arrays,and real-time RT-PCR were used to determine the relationship between FASN and frizzled class receptor 10(FZD10)expression.FZD10 knockdown and overexpression were used to determine its role in mediating FASN function in cellular response to radiation.Immunohistochemical staining was used to determine FASN and FZD10 expressions in human NPC tissues,followed by analysis of their association with the overall survival of patients.Results:FASN knockdown or inhibition significantly enhanced radiosensitivity of NPC cells,bothin vitro andin vivo.There was a positive association between FASN and FZD10 expression in NPC cell lines grown as monolayers or xenografts,as well as human tissues.FASN knockdown reduced FZD10 expression,and rescue of FZD10 expression abolished FASN knockdown-induced enhancement of radiosensitivity.FASN and FZD10 were both negatively associated with overall survival of NPC patients.Conclusions:FASN contributes to radioresistance,possiblyvia FZD10 in NPC cells.Both FZD10 and FASN expressions were associated with poor outcomes of NPC patients.EGCG may sensitize radioresistance by inhibiting FASN and may possibly be developed as a radiosensitizer for better treatment of NPCs.
基金Supported by A Grant of the University of Dresden from the Department of Clinical Pharmacology
文摘Flavonoids,secondary plant products which could be essential for normal physiology in humans and animals,may be the vitamins of the next century.Flavonoids belong to the polyphenols and possess antioxidative,anti-inflammatory,antimutagenic and anticarcinogenic properties.Among the various flavonoid species,tea flavonoids such as apigenin (from camomile) and epigallocatechin gallate (EGCG from green tea) can be used for the prevention of intestinal neoplasia,especially for adenoma and cancer prevention in the gastrointestinal tract.Numerous experimental studies with molecular and biological end points support the therapeutic efficacy of bioflavonoids.Clinical studies with cohorts and case-control trials suggest that flavonoids are effective in tertiary bioprevention but,as yet,there are no controlled randomized clinical trials.Flavonoids can inhibit inflammatory pathways and could be useful for chronic inflammatory bowel diseases.Flavonoid deficiency syndromes could be therapeutic targets in the future.
文摘Objective: To investigate the effect of Red Peony 801 (propyl gallate,PrG) on cyclooxygenase (COX) activity in murine peritoneal macrophages. Methods: A screening model for COX inhibitors in vitro based on murine peritoneal macrophages was used. COX-1 activity was reflected by the level of 6-ketoprostaglandin F1α(6-keto-PGF1α) in supernatants of cultured macrophages which were stimulated with calcium ionophore A23187 for a short-term, while COX-2 activity was reflected by the level of prostaglandin E2 (PGE2) in supernatants of cultured macrophages which were stimulated with lipopolysaccharide (LPS) for a long-term. Results: PrG did not affect A23187-induced, COX-1-derived 6-keto-PGF1α synthesis at the concentrations of 1×10-5, 5×10-6 mol/L (P>0.05), but enhanced 6-keto-PGF1α synthesis at the concentrations of 1×10-6, 5×10-7, 1×10-7 mol/L (P<0.01) in vitro, and showed a good dose-dependent manner. It inhibited LPS-induced, COX-2-derived PGE2 synthesis at the concentrations of 1×10-5,1×10-6 mol/L (P< 0. 05). Conclusion: Within the range of 1×10-5 to 1×10-7 mol/L, PrG activated COX-1 at lower concentrations and inhibited COX-2 at higher concentrations in murine peritoneal macrophages.
文摘The fresh leaves of China green tea, Camellia sinensis, were collected from Fuyang, Zhejiang Province, China, in April. The tea polyphenols was extracted by four different methods （homogenized with distilled water at room temperature, homogenized with 0.3% citric acid （w/v） at room temperature, 5- min boiling and homogenized with distilled water at room temperature, homogenized with 85℃ distilled water）, and after preserving at room temperature, the change of the Epigallocatechin gallate （EGCG） contents of the extracts was investigated. Results indicated that the EGCG content of homogenate extracted with 85℃ distilled water was the highest before the extract was preserved, followed by that of the extract homogenized with 0.3% citric acid at room temperature. During preservation, EGCG content changed obviously. The EGCG contents of homogenates extracted with distilled water at room temperature and 85℃ distilled water declined quickly and separately reduced to 21.52% and 54.6% of their initial contents after preservation for 12 h. The EGCG contents extracted by 0.3% citric acid （w/v） solvent at room temperature and 5- min boiling/homogenized with distilled water at room temperature declined relatively slowly ,and separately reduced to 76.9% and 85.16% of their initial contents after preservation for 12 h. It was also found that the citric acid can prevent the degradation of EGCG and the extract solution color is light green
基金Supported by Nursing Advantage Discipline Construction Project Foundation of Jiangsu Province University,No.2019YSHL107Nanjing Medical Science and Technique Development Foundation,No.NWQR-201705.
文摘BACKGROUND Epigallocatechin gallate(EGCG)is a polyhydroxy phenolic compound extracted from tea and its antitumor effect has received widespread attention.We explored the inhibitory effect of EGCG on dimethylhydrazine(DMH)-induced colorectal cancer(CRC)using a rat model,predicted the interaction between EGCG and CRC target genes using a database,and explained the EGCG associated target pathways and mechanisms in CRC.AIM To understand the inhibitory mechanisms of EGCG on CRC cell proliferation and identify its pharmacological targets by network pharmacology analysis.METHODS DMH(40 mg/kg,s.c.,twice weekly for eight weeks)was used to induce CRC in rats.After model establishment,the rats were administered with EGCG(50,100,or 200 mg/kg,p.o.,once daily for eight weeks)and killed 12 and 20 wk after the start of the experiment.Formation of aberrant crypt foci and tumor was studied by histological analysis.Using network pharmacology analysis,candidate and collective targets of EGCG and CRC were identified,and Gene ontology(GO)and Kyoto Encyclopedia of Genes and Genomes analyses were used to predict the pathways altered by EGCG.RESULTS At week 12,high-dose EGCG treatment significantly reduced the tumor formation rate,total number of tumors,cancerous and non-cancerous tumors,tumor volume,ascites formation,and aberrant crypt foci count.At week 20,all three doses of EGCG were effective.Seventy-eight collective targets of EGCG and CRC were identified,of which 28 genes were dysregulated in CRC.Kyoto Encyclopedia of Genes and Genomes and GO analyses showed that the dysregulated genes were enriched in hsa05210(CRC),hsa04115(p53 signaling pathway),and hsa04151(PI3K-Akt signaling pathway),GO:0043124(negative regulation of I-kappaB kinase/NF-kappaB signaling pathway),GO:0043409(negative regulation of mitogen-activated protein kinase cascade),and GO:2001244(positive regulation of intrinsic apoptotic signaling pathway)respectively.CONCLUSION EGCG inhibits the formation of DMH-induced CRC by regulating key pathways involved in tumorigenesis.
基金supported by the National Natural Science Foundation of China(Grant Nos.:82160739,81922070,81973286,and 81973393)Sailing Special Project of Shanghai Rising-Star Program(Grant No.:22YF1441500)+6 种基金Program for Innovative Leading Talents of Qinghai Province(2018&2019)Innovation Team and Talents Cultivation Program of National Administration of Traditional Chinese Medicine(Grant No.:ZYYCXTD-D-202004)Shanghai Science and Technology Innovation Action Plans(Grant Nos.:20S21901500 and 20S21900900)supported by the Shanghai Science and Technology CommitteeProject of the National Multidisciplinary Innovation Team of Traditional Chinese Medicine supported by the National Administration of Traditional Chinese MedicineKey R&D and Transformation Science and Technology Cooperation Project of Qinghai Province(Grant No.:2019-HZ-819)Basic Public Welfare Research Program of Zhejiang Province(Grant No.:LGF22H280012).
文摘Although herbal medicines(HMs)are widely used in the prevention and treatment of obesity and obesity-associated disorders,the key constituents exhibiting anti-obesity activity and their molecular mechanisms are poorly understood.Recently,we assessed the inhibitory potentials of several HMs against human pancreatic lipase(hPL,a key therapeutic target for human obesity),among which the root-extract of Rhodiola crenulata(ERC)showed the most potent anti-hPL activity.In this study,we adopted an integrated strategy,involving bioactivity-guided fractionation techniques,chemical profiling,and biochemical assays,to identify the key anti-hPL constituents in ERC.Nine ERC fractions(retention time=12.5e35 min),obtained using reverse-phase liquid chromatography,showed strong anti-hPL activity,while the major constituents in these bioactive fractions were subsequently identified using liquid chromatography-quadrupole time-of-flight mass spectrometry(LC-Q-TOF-MS/MS).Among the identified ERC constituents,1,2,3,4,6-penta-O-galloyl-β-D-glucopyranose(PGG)and catechin gallate(CG)showed the most potent anti-hPL activity,with pIC50 values of 7.59±0.03 and 7.68±0.23,respectively.Further investigations revealed that PGG and CG potently inhibited hPL in a non-competitive manner,with inhibition constant(Ki)values of 0.012 and 0.082 mM,respectively.Collectively,our integrative analyses enabled us to efficiently identify and characterize the key anti-obesity constituents in ERC,as well as to elucidate their anti-hPL mechanisms.These findings provide convincing evidence in support of the anti-obesity and lipid-lowering properties of ERC.
基金supported by the National Natural Science Foundation of China.(Grand No.31570563)Jiangsu Province Biomass Energy and Materials Laboratory,China(Grant No.JSBEM-S-201807)Fundamental Research Funds of Chinese academy of forestry(CAFYBB2017MB017).
文摘Thermosetting polyurethanes are widely used in various fields owing to their excellent elasticity,strength and solvent resistance.Three environmental friendly propyl gallate-based self-healing polyurethanes were prepared from polyurethane prepolymers with varying isocyanate content.The thermal stabilities of the polyurethanes were tested using thermogravimetric analysis.Their self-healing and mechanical properties were analyzed using a universal testing machine and dynamic thermomechanical analysis.The polyurethanes were found with high self-healing ability and excellent mechanical properties due to the absence of phenolic carbamate.These qualities improved with increased isocyanate content and the prolonged selfhealing time.We found,therefore,that the propyl gallate-based polyurethane has potential for use in industrial applications as self-healing materials.
基金Funded by an unrestricted grant from Firat University Scientific Research Unit
文摘AIM：To compare the potential protective effects of epigallocatechin gallate（EGCG） and ellagic acid（EA） in an experimental cataract model.●METHODS：Twenty-eight Spraque-Dawley rat pups were assigned into four groups.All the rats,except for those in the control group,were injected subcutaneously sodium selenite to induce experimental cataract on the postpartum ninth day,and between 10 th and 14 th days.Rats in the sham,EGCG,and EA groups were intraperitoneally administered 50 mg/（kg·d） saline solution,50 mg/（kg·d） EGCG and 200 mg/（kg·d） EA,respectively.The reduced glutathione（GSH） and malondialdehyde（MDA） levels,total antioxidant status（TAS） and total oxidant status（TOS） in lens supernatants were measured.RESULTS：The mean cataract gradings in EGCG and EA groups were found to be significantly lower than that in sham group（P〈0.001）.The mean GSH levels and TASs in EGCG and EA groups were significantly higher than that in sham group while mean MDA levels and TOSs in EGCG and EA groups were significantly lower than that in the sham group（P〈0.001）.CONCLUSION：EGCG and EA have protective effects on cataract development via the inhibition of oxidative stress.
