Macrophages undergo dynamic transitions between M1 and M2 states,exerting profound influences on both inflammatory and regenerative processes.The biocompatible and wound-healing properties of decellularized amniotic m...Macrophages undergo dynamic transitions between M1 and M2 states,exerting profound influences on both inflammatory and regenerative processes.The biocompatible and wound-healing properties of decellularized amniotic membrane(d AM)make it a subject of exploration for its potential impact on the anti-inflammatory response of macrophages.Experimental findings unequivocally demonstrate that d AM promotes anti-inflammatory M2 polarization of macrophage,with its cytokine-rich content posited as a potential mediator.The application of RNA sequencing unveils differential gene expression,implicating the hypoxia inducible factor-1α(HIF-1α)signaling pathway in this intricate interplay.Subsequent investigation further demonstrates that d AM facilitates anti-inflammatory M2 polarization of macrophage through the upregulation of epidermal growth factor(EGF),which,in turn,activates the phosphatidylinositol 3-kinase(PI3K)/protein kinase B(AKT)pathway and stabilizes HIF-1α.This cascade results in a noteworthy augmentation of anti-inflammatory gene expression.This study significantly contributes to advancing our comprehension of d AM's immunomodulatory role in tissue repair,thereby suggesting promising therapeutic potential.展开更多
Respiratory syncytial virus(RSV)is a ubiquitous respiratory virus that affects individuals of all ages;however,there is a notable lack of targeted treatments.RSV infection is associated with a range of respiratory sym...Respiratory syncytial virus(RSV)is a ubiquitous respiratory virus that affects individuals of all ages;however,there is a notable lack of targeted treatments.RSV infection is associated with a range of respiratory symptoms,including bronchiolitis and pneumonia.Baicalin(BA)exhibits significant therapeutic effects against RSV infection through mechanisms of viral inhibition and anti-inflammatory action.Nonetheless,the clinical application of BA is constrained by its low solubility and bioavailability.In this study,we prepared BA nanodrugs(BA NDs)with enhanced water solubility utilizing the supramolecular self-assembled strategy,and we further conducted a comparative analysis of this pharmacological activity between free drugs and NDs of BA.Both in vitro and in vivo results demonstrated that BA NDs significantly enhanced the dual effects of viral inhibition and inflammation relief compared to free BA,attributed to prolonged lung retention,improved cellular uptake,and increased targeting affinity.Our study confirms that the nanosizing strategy,a straightforward approach to enhance drug solubility,can also increase biological activity compared to free drugs with the same content,thereby providing a potential ND for RSV treatment.This correlation analysis between the existing forms of drugs and their biological activity offers a novel perspective for research on the active ingredients of traditional Chinese medicine.展开更多
Silica gel column chromatography(CC),Sephadex LH-20 CC and high performance liquid chromatography(HPLC)were used to study the chemical constituents of the fruits of the medicine-food plant Rubus idaeus Linnaeus.A new ...Silica gel column chromatography(CC),Sephadex LH-20 CC and high performance liquid chromatography(HPLC)were used to study the chemical constituents of the fruits of the medicine-food plant Rubus idaeus Linnaeus.A new tetrahydrogenated naphthol syringic acid ester,named rubusnolicester(1),two new phenolic glycoside derivatives,4-chloro-2,6-dimethoxylphenol-1-O-β-D-glucopyranoside(2)and salicylic acid-2-O-(6'-O-acetyl)-β-D-glucopyranoside(3),together with one known salicylic acid glycoside derivative(4)and three known flavonoids derivatives(5~7),were isolated.Their structures were elucidated by HRESI-MS,NMR spectroscopy,and a comparison of optical rotation(OR).Compounds 1~7 were evaluated the inhibitory activities against the nitric oxide(NO)production induced by lipopolysaccharide(LPS)in mouse macrophage RAW264.7 cells in vitro.Compound 1 exhibited inhibitory effect with the IC50 value of(12.28±1.25)μmol/L.展开更多
Eight sesquiterpenes were isolated from Ainsliaea glabra.Among them,a new guaianolide sesquiterpenoid,named ainsglaolide A(1),and seven known sesquiterpenoids 2~8 were identified.Compound 1 was a novel guaianolide ses...Eight sesquiterpenes were isolated from Ainsliaea glabra.Among them,a new guaianolide sesquiterpenoid,named ainsglaolide A(1),and seven known sesquiterpenoids 2~8 were identified.Compound 1 was a novel guaianolide sesquiterpenoid featuring a rare six-membered lactone ring formed between C-4 and C-15.The new compound structure was elucidated by HRESI-MS and NMR spectroscopy,as well as electrostatic circular dichroism(ECD)calculations were used to further confirm the absolute of 1.Anti-inflammatory activity tests were conducted on the separated compounds,indicating that compound 1 had significant inhibitory effect on NLRP3 inflammasome with an IC_(50) value of 1.86μmol/L.展开更多
Artemisia dracunculus L.,or tarragon,is a perennial herb from the Asteraceae family that is extensively cultivated for its aromatic leaves,which are valued for its preventative and therapeutic properties in both cooke...Artemisia dracunculus L.,or tarragon,is a perennial herb from the Asteraceae family that is extensively cultivated for its aromatic leaves,which are valued for its preventative and therapeutic properties in both cookery and traditional medicine.This study aims to investigate the antibacterial,antioxidant,and anti-inflammatory properties of A.dracunculus(tarragon)essential oil(ADEO),with estragole(57.23%)identified as the major compound through gas chromatography-mass spectrometry(GC-MS)analysis.ADEO exhibited varying degrees of antibacterial activity,with Escherichia coli showing higher resistance inhibition zone(IZ)=14.7±0.58 mm,minimum (inhibitory concentration(MIC)=2%and minimum bactericidal concentration(MBC)=4%),while Bacillus subtilis(IZ=24.05±2.11 mm and MIC=MBC=0.125%)and Staphylococcus aureus(IZ=18.69±1.45 mm,MIC=0.0612%and MBC=0.125%)were more sensitive to its actions.Antioxidant ability was assessed using 1,1-diphenyl-2-picrylhydrazil(DPPH),2,2′-azinobis(3-ethylbenzothiazoline-6-sulfonic acid)(ABTS),xanthine oxidase inhibition,and beta-carotene bleaching assays.ADEO showed remarkable antiradical effect on DPPH(IC_(50)=127.05±3.47μg/mL)and ABTS radical(IC_(50)=89.60±8.73μg/mL)as well as significant inhibition of xanthine oxidase(IC_(50)=47.9±2.04μg/mL)and lipid peroxidation(IC_(50)=231.63±5.21μg/mL).ADEO also showed significant anti-inflammatory activity by inhibiting the enzymesCOX-1(IC_(50)=59.2±2.43μg/mL),Cyclo-oxygenase-2(COX-2)(IC_(50)=74.68±1.34μg/mL)and 5-lipooxygense(5-LOX)(IC_(50)=93.18±1.87μg/mL),which are involved in the inflammatory pathway.These findings suggest that ADEO,with its high estragole content,holds promising potential as a natural antibacterial,antioxidant,and anti-inflammatory agent for preventive and therapeutic applications.Further research is needed to explore its safety and efficacy in clinical settings.展开更多
Background:The root of Desmodium gangeticum,a key component of“Dashamoola,”is a significant Ayurveda remedy for inflammatory conditions.Due to the less availability of D.gangeticum in Sri Lanka,indigenous physicians...Background:The root of Desmodium gangeticum,a key component of“Dashamoola,”is a significant Ayurveda remedy for inflammatory conditions.Due to the less availability of D.gangeticum in Sri Lanka,indigenous physicians often substitute Alysicarpus vaginalis root without scientific validation.Further,no comparative study has been conducted on the whole plants of these species.This research is focused on comparing the aqueous extracts of roots and whole plants of A.vaginalis and D.gangeticum for anti-inflammatory activity,acute toxicity,and to quantify major phytochemicals.Methods:Freeze-dried aqueous extracts were prepared and assessed for anti-inflammatory potency using the egg albumin denaturation assay,heat-induced red blood cell membrane stabilization assay,and nitric oxide assay.Acute toxicity was evaluated using the zebrafish embryo assay,and major phytochemicals,were quantitatively screened.Results:In egg albumin denaturation assay,D.gangeticum whole plant(IC_(50)107.89±0.71μg/mL)and root(IC_(50)210.37±0.39μg/mL)exhibited superior anti-inflammatory potency compared to diclofenac sodium(IC_(50)826.04±0.27μg/mL)and A.vaginalis(whole plant IC_(50)1,336μg/mL,root IC_(50)3,162.28μg/mL).In red blood cell membrane stabilization assay,D.gangeticum(whole plant IC_(50)47.86±0.52μg/mL,root IC_(50)331.13±0.83μg/mL)showed the highest activity.Quercetin(IC_(50)285.01μg/mL)was the most potent,with D.gangeticum(IC_(50)2,080.03μg/mL)and A.vaginalis(IC_(50)7,183.87μg/mL)showing weaker inhibition in the nitric oxide assay.Regarding toxicity,lower toxicity showed for D.gangeticum(LC502,570.39μg/mL)compared to A.vaginalis(LC501,348.96μg/mL).In phytochemical analysis,phenols,flavonoids,tannins,alkaloids and saponins were quantified.Statistical analysis revealed significant differences between effects of all extracts and reference drugs(P<0.05).Conclusion:Comparative analysis revealed,D.gangeticum has higher anti-inflammatory activity and lower toxicity than A.vaginalis,suggesting its suitability over A.vaginalis in Sri Lankan practices.展开更多
Thymus serpyllum L.,often known as wild thyme,has been used since ancient times due to its multifaceted culinary and medicinal attributes.It is usually utilized in folk medicine to manage different health issues.This ...Thymus serpyllum L.,often known as wild thyme,has been used since ancient times due to its multifaceted culinary and medicinal attributes.It is usually utilized in folk medicine to manage different health issues.This work aimed to investigate the chemical composition and biological characteristics of T.serpyllum essential oil(EO),including its antimicrobial,antioxidant,and anti-inflammatory capabilities.Moreover,we have prompted an in-silico simulation to reveal the underlying mode of action of these properties.The chemical characterization of T.serpyllum(EO)by Gas Chromatography-Mass Spectrometry(GC-MS)indicated sabinene(17.33%),terpinen-4-ol(11.73%),phellandral(13.18%),and thymol(10.54%)as main components.The antimicrobial screening utilized the disc-diffusion technique,MIC,and MBC assays.The disc-diffusion test’s results revealed significant anti-Candida activity and notable antibacterial efficacy.The MIC and MBC tests showed that T.serpyllum EO effectively stops bacterial growth,including Gram-positive and Gram-negative strains and Candida strains.The tolerance level ratio demonstrated that this EO exhibits bactericidal and fungicidal effects on all tested bacteria and Candida strains.Also,T.serpyllum EO presented effective inhibitory activity against the 5-lipoxygenase(5-LOX)enzyme(IC50=744.19±0.1µg/mL)(p<0.05).It also effectively affected FRAP,β-carotene,DPPH,and ABTS radicals.In light of these findings,T.serpyllum holds promise for diverse applications across pharmaceuticals,nutraceuticals,and the food industry.However,further research and collaboration between traditional knowledge and modern medicine are crucial to fully realizing its potential benefits in these fields.展开更多
Gallstone disease(cholelithiasis)is a common gastrointestinal(GI)disorder characterized by the accumulation of hardened bile constituents,often leading to complications such as cholecystitis,cholangitis,and pancreatit...Gallstone disease(cholelithiasis)is a common gastrointestinal(GI)disorder characterized by the accumulation of hardened bile constituents,often leading to complications such as cholecystitis,cholangitis,and pancreatitis.Most gallstones are cholesterol-based and form due to bile supersaturation,gallbladder dysm-otility,and inflammation.Current treatment options–such as ursodeoxycholic acid,laparoscopic cholecystectomy,and dietary modifications–have limitations including invasiveness,prolonged duration,side effects,and recurrence risk.Melatonin,a hormone secreted by the pineal gland,has gained attention for its antioxidant and anti-inflammatory properties,as well as its regulatory effects on lipid metabolism and gallbladder motility.Experimental studies suggest that melatonin reduces biliary cholesterol,suppresses oxidative stress,and restores gallbladder muscle function,thereby preventing gallstone formation.It is also present in bile and shown to enhance cholesterol conversion into bile acids and inhibit intestinal cholesterol absorption.Beyond gallstone prevention,melatonin demonstrates protective effects against GI malignancies,including hepatocellular carcinoma and cholangiocarcinoma,by regulating mitochondrial function,inhibiting glycolysis,and modulating apoptosis.With a strong safety profile and minimal side effects,melatonin may serve as a promising adjunct or alternative for gallstone management,particularly in patients unfit for surgery.Further clin-ical research is warranted to validate its therapeutic role.展开更多
Objective:To investigate the anti-inflammatory,antioxidant,and goblet cell-stimulating effects of a suspension of Ophiopogon japonicus(L.f.)Ker Gawl.(O.japonicus,Mai Dong)extract combined with hyaluronic acid(HA)in th...Objective:To investigate the anti-inflammatory,antioxidant,and goblet cell-stimulating effects of a suspension of Ophiopogon japonicus(L.f.)Ker Gawl.(O.japonicus,Mai Dong)extract combined with hyaluronic acid(HA)in the mouse model with dry eye disease(DED).Methods:A DED mouse model was induced using benzalkonium chloride(BAK),followed by treatment with O.japonicus extract-containing eye drops at varying concentrations.Experimental groups included a normal control,a DED model control,a positive control,and an O.japonicus extract-treated group.Corneal fluorescein staining and tear break-up time(TBUT)were used to assess tear film stability and ocular surface integrity.Enzyme-linked immunosorbent assay(ELISA)measured inflammatory factor levels in corneal and conjunctival tissues,whereas Western blot(WB)analyzed key antioxidant and inflammatory markers,including nuclear factor erythroid 2-related factor(2Nrf2)and heme oxygenase 1(HO-1).Periodic acid-schiff(PAS)staining and immunofluorescence were used to evaluate goblet cell density and mucin secretion.Results:O.japonicus extract significantly improved corneal damage,reduced fluorescein staining scores,prolonged TBUT,and increased tear secretion.It downregulated inflammatory markers,including interleukin-8(IL-8),interleukin-1β(IL-1β),and interferon-g(IFN-γ)while upregulating Nrf2,HO-1,and the interleukin-13(IL-13)/IFN-γ ratio,alleviating oxidative stress and inflammation.PAS staining showed increased conjunctival goblet cell density and restored mucin secretion,enhancing tear film stability.Conclusion:O.japonicus extract demonstrated significant anti-inflammatory,antioxidant,and goblet cell-stimulating effects in a DED model,with good biocompatibility and promising therapeutic potential.Future research should optimize extraction processes and validate their efficacy and safety in clinical settings.展开更多
Five new flavan-4-ol glycosides jixueqiosides A-E(1-5)and two new flavan glycosides jixueqiosides F and G(6 and 7),along with twelve known flavan-4-ol glycosides(8-19),were isolated from the roots of Pronephrium penan...Five new flavan-4-ol glycosides jixueqiosides A-E(1-5)and two new flavan glycosides jixueqiosides F and G(6 and 7),along with twelve known flavan-4-ol glycosides(8-19),were isolated from the roots of Pronephrium penangianum.Comprehensive spectral analyses,X-ray single-crystal diffraction,and theoretical electronic circular dichroism(ECD)calculations established structures and absolute configurations.A single crystal structure of flavan-4-ol glycoside(14)was reported for the first time,while the characteristic ECD and NMR data for all isolated flavan-4-ol glycosides(1-5,8-19)were analyzed,establishing a set of empirical rules.Activity screening of these isolates showed that 8 and 9 could inhibit the proliferation of MDA-MB-231 and MCF-7 cells with IC50 values of 7.93±2.85μmol·L^(-1)and 5.87±1.58μmol·L^(-1)(MDA-MB-231),and 2.21±1.38μmol·L^(-1)and 3.52±1.55μmol·L^(-1)(MCF-7),respectively.Western blotting and flow cytometry analyses demonstrated that 8 and 9 dose-dependently induced apoptosis in MDA-MB-231 cells by up-regulating BAX,activating caspase-3 and down-regulating BCL-2.Additionally,compound 8 affected autophagy-related proteins,increasing the ratio of LC3-II/LC3-I and Beclin-1 levels to inhibit MDA-MB-231 cell proliferation.Moreover,anti-inflammatory studies indicated that 2,3,7,13,14,and 18 moderately inhibited tumor necrosis factor-α(TNF-α),interleukin-6(IL-6),and nitric oxide(NO)release.展开更多
Gentianopsis barbata(G.barbata)represents a significant plant species with considerable ornamental and medicinal value in China.This investigation sought to elucidate the primary constituents within the plant and inve...Gentianopsis barbata(G.barbata)represents a significant plant species with considerable ornamental and medicinal value in China.This investigation sought to elucidate the primary constituents within the plant and investigate their pharmacological properties.Fifty triterpenoids(1-50),including nine previously undescribed compounds(1,2,7,10,20,28,29,37,and 41)were isolated and characterized from the whole plants of G.barbata.Notably,compounds 1 and 2 exhibited the novel 3,4;9,10-diseco-24-homo-cycloartane triterpenoid skeleton.The isolated triterpenoids demonstrated substantial anti-inflammatory activity through inhibition of tumor necrosis factorα(TNF-α)and interleukin-6(IL-6)cytokine secretion in LPS-induced RAW264.7 macrophages,and hepatoprotective effects by preventing tertbutyl hydroperoxide(t-BHP)-induced oxidative injury in HepG2 cells.These results demonstrate both the presence of diverse triterpenoids in G.barbata and their therapeutic potential for inflammatory and hepatic conditions,providing scientific evidence supporting the clinical application of this traditional Mongolian medicinal plant.展开更多
Two unusual sesquiterpenoids,irpexlactones A(1)and B(2),were isolated from cultures of the basidiomycete Irpex lacteus.Their structures were established by means of spectroscopic methods,the single crystal X-ray diffr...Two unusual sesquiterpenoids,irpexlactones A(1)and B(2),were isolated from cultures of the basidiomycete Irpex lacteus.Their structures were established by means of spectroscopic methods,the single crystal X-ray diffraction,as well as electronic circular dichroism(ECD)calculations.They possess a novel carbon skeleton with a 5/6/3-fused ring system that may derive from tremulane type sesquiterpenoids with ring-rearrangement.Both compounds show significant inhibitory activities against nitric oxide production with half maximal inhibitory concentration(IC50)values of 2.2 and 1.4μmol/L,respectively.Their anti-inflammatory effects were further evaluated by enzyme-linked immunosorbent assay(ELISA)and Western blot.展开更多
Five meroterpenoids,rhodonoids K-M(1-2),daurichromene E(3),and grifolins A-B(4-5),together with seven known compounds(6-12),were isolated from Rhododendron anthopogonoides.The chemical structures of these compounds we...Five meroterpenoids,rhodonoids K-M(1-2),daurichromene E(3),and grifolins A-B(4-5),together with seven known compounds(6-12),were isolated from Rhododendron anthopogonoides.The chemical structures of these compounds were elucidated through comprehensive analysis of high-resolution electrospray ionization mass spectrometry(HR-ESI-MS),ultraviolet(UV),infrared spectroscopy(IR),and nuclear magnetic resonance(NMR)data.Their absolute configurations were determined by comparing experimental electronic circular dichroism(ECD)spectra with computed values.Notably,compounds 1 and 3 demonstrated significant inhibitory effects on lipopolysaccharide(LPS)-induced inflammation in RAW264.7 cells.These compounds markedly suppressed the mRNA expressions of inflammatory factors,including interleukin(IL)-1β,IL-6,and tumor necrosis factor-α(TNF-α)while also down-regulating the protein expressions of inducible nitric oxide synthase(iNOS)and cyclooxygenase-2(COX-2).展开更多
Objective To investigate the protective effects of morusin on lipopolysaccharide(LPS)-induced acute liver injury in mice and its underlying mechanisms.Methods Thirty-two male specific pathogen-free(SPF)C57BL/6J mice w...Objective To investigate the protective effects of morusin on lipopolysaccharide(LPS)-induced acute liver injury in mice and its underlying mechanisms.Methods Thirty-two male specific pathogen-free(SPF)C57BL/6J mice were randomly divided into four groups(n=8 per group):control,LPS,low-dose morusin(morusin-L,10 mg/kg),and high-dose morusin(morusin-H,20 mg/kg)groups.The mice in each group were administered the corresponding drugs or normal saline via continuous gavage daily for 16 consecutive days.Except for control group,which received an equal volume of normal saline,other groups were intraperitoneally injected with LPS(5 mg/kg)2 h after the last gavage to establish the acute liver injury model.Serum and liver tissues were collected for subsequent analysis 6 h after LPS injection.The activities of alanine aminotransferase(ALT)and aspartate aminotransferase(AST)in serum were detected with biochemical methods.The levels of tumor necrosis factor(TNF)-α,interleukin(IL)-6,and IL-1βin serum were measured by enzyme-linked immunosorbent assay(ELISA).Hepatic pathological changes were evaluated by hematoxylin-eosin(HE)staining.The 16S ribosomal RNA(16S rRNA)sequencing was performed to assess the composition of intestinal flora,linear discriminant analysis effect size(LEfSe)was applied for multi-level species discrimination,and Spearman’s correlation analysis was performed.The liver tissues of mice with acute liver injury were analyzed by RNA sequencing(RNA-seq)technology to identify differentially expressed genes(DEGs),and then enrichment analysis of the Kyoto Encyclopedia of Genes and Genomes(KEGG)pathway was conducted.The expression levels of selected genes was validated by quantitative reverse transcription polymerase chain reaction(qRT-PCR),while immunohistochemistry(IHC)was performed to examine the expression levels of IL-6,myeloid differentiation primary response 88(MYD88),and toll-like receptor 2(TLR2).Results Morusin significantly reduced the serum levels of ALT,AST,and inflammatory factors(TNF-α,IL-6,and IL-1β)(P<0.05,P<0.01,or P<0.001),while alleviating the hepatic pathological damage in mice.Based on efficacy comparisons,morusin-H group was selected for subsequent microbiome and transcriptome analyses.Microbiome analysis revealed that morusin-H effectively mitigated LPS-induced gut dysbiosis and restored the Firmicutes/Bacteroidota balance(P<0.01).At the genus level,morusin-H significantly reduced the abundances of norank_f_Muribaculaceae,Desulfovibrio,Parabacteroides,and Muribaculum(P<0.05,P<0.01,or P<0.001).At the phylum,family,and genus levels,our findings indicated that morusin-H treatment caused a significant decrease in the abundance of Desulfobacterota,Desulfovibrionaceae,and Desulfovibrio(P<0.01).Importantly,the abundance of Desulfovibrio was positively correlated with the levels of ALT,AST,TNF-α,IL-1β,and IL-6.Transcriptomic and molecular analyses showed that the therapeutic mechanism of morusin-H involved suppression of the IL-17/TNF signaling pathways and downregulating the mRNA levels of Tlr2,Tlr3,Myd88,Il6,and Cxcl10(P<0.05 or P<0.001),as well as the protein levels of key inflammatory mediators(IL-6,MYD88,and TLR2)(P<0.001).Conclusion Morusin demonstrates protective effects against LPS-induced acute liver injury,likely through modulation of gut microbiota and suppression of pro-inflammatory factor expression.These findings indicate that morusin exerts its effects through the"microbiota-inflammation-liver"axis,providing a theoretical basis for its use as a multi-target plant-based drug in the treatment of metabolic inflammation-related liver diseases.展开更多
AIM:To assess and rank the efficacy of various nonsteroidal anti-inflammatory drugs(NSAIDs)in preventing postoperative macular edema(PME)after cataract surgery.METHODS:A comprehensive search was conducted across PubMe...AIM:To assess and rank the efficacy of various nonsteroidal anti-inflammatory drugs(NSAIDs)in preventing postoperative macular edema(PME)after cataract surgery.METHODS:A comprehensive search was conducted across PubMed,Embase,Cochrane Library,and Web of Science databases.Randomized controlled trials(RCTs)comparing different NSAIDs and control treatments for the prevention of PME were included.Data from the studies were synthesized using the“gemtc”package in R.Risk of bias was assessed with the Cochrane RoB 2 tool,and heterogeneity was evaluated using the global I2 statistic.Surface under the cumulative ranking curve(SUCRA)values were calculated for each treatment.RESULTS:Of 132 identified records,9 RCTs met the inclusion criteria.The Network Meta-analysis indicated that nepafenac had the highest efficacy in preventing PME,followed by artificial tear substitute,ketorolac,diclofenac,and bromfenac.The league table comparisons and rankograms corroborated these findings,with nepafenac consistently ranking highest.Heterogeneity analysis yielded high I2 values,indicating substantial variability across studies.CONCLUSION:This Network Meta-analysis suggests that nepafenac is the most effective NSAID for preventing PME following cataract surgery.Given the substantial heterogeneity observed,further high-quality RCTs are required to confirm these findings and explore the sources of variability.Clinicians should consider these results when selecting NSAIDs for PME prophylaxis in cataract surgery patients.展开更多
In continuation of research aimed at identifying anti-inflammatory agents from natural sesquiterpenoids,an activity-guided fractionation approach utilizing lipopolysaccharide(LPS)-mediated RAW264.7 cells was employed ...In continuation of research aimed at identifying anti-inflammatory agents from natural sesquiterpenoids,an activity-guided fractionation approach utilizing lipopolysaccharide(LPS)-mediated RAW264.7 cells was employed to investigate chemical constituents from Inula Britannica(I.britannica).Seven novel sesquiterpenoid dimers inulabritanoids A−G(1−7)and two novel sesquiterpenoid monomers inulabritanoids H(8)and I(9)were isolated from I.britannica together with eighteen known compounds(10−27).The structural elucidation was accomplished through comprehensive analysis of 1D and 2D nuclear magnetic resonance(NMR),high-resolution mass spectrometry(HR-MS),and electronic circular dichroism(ECD)spectra,complemented by quantum chemical calculations.Compounds 1,2,12,16,19,and 26 demonstrated inhibitory effects on NO production,with IC50 values of 3.65,5.48,3.29,6.91,3.12,and 5.67μmol·L^(−1),respectively.Mechanistic studies revealed that compound 1 inhibited IκB kinaseβ(IKKβ)phosphorylation,thereby blocking nuclear factorκB(NF-κB)nuclear translocation,and activated the kelch-like ECH-associated protein 1(Keap1)/nuclear factor erythroid 2-related factor 2(Nrf2)signal pathway,leading to decreased expression of NADPH oxidase 2(NOX-2),inducible nitric oxide synthase(iNOS),tumor necrosis factorα(TNF-α),interleukin-6(IL-6),monocyte chemotactic protein-1(MCP-1),IL-1β,and IL-1αand increased expression of NAD(P)H:quinone oxidoreductase 1(NQO-1)and heme oxygenase-1(HO-1),thus exhibiting anti-inflammatory effects in vitro.These results indicate that dimeric sesquiterpenoids may serve as promising candidates for anti-inflammatory drug development.展开更多
[Objectives]To observe the effects of chloramphenicol prednisone liniment on anti-inflammatory and anti-pruritic responses and skin barrier function in an acute eczema mouse model and explore its potential underlying ...[Objectives]To observe the effects of chloramphenicol prednisone liniment on anti-inflammatory and anti-pruritic responses and skin barrier function in an acute eczema mouse model and explore its potential underlying mechanism.[Methods]Twenty-four female SPF-grade ICR mice were randomly and equally assigned to three groups:the blank control group,the acute eczema group,and the chloramphenicol prednisone liniment group according to the random number table method,with 8 mice per group.Except for the blank control group,the acute eczema model was established by applying 2,4-dinitrochlorobenzene(DNCB)to the right dorsal area.On day 10(d10),0.1 mL of normal saline was administered to the modeling site in both the blank control group and the acute eczema group,whereas chloramphenicol prednisone liniment was applied to the positive drug group.Medication was applied twice daily in all three groups for a total duration of 14 d.Sixty minutes following the final administration of the drug,the development of eczema in mice was visually assessed,and the severity of skin lesions was scored.Trans-epidermal water loss(TEWL)was measured using a multifunctional skin tester.Experiments inducing and alleviating pruritus were performed to compare the frequency of mice licking their bodies,the latency period before pruritus onset,and the duration of pruritus episodes.Levels of histamine and substance P(SP)in the lesion tissues were quantified using enzyme-linked immunosorbent assay(ELISA).[Results]Compared to the acute eczema group,the chloramphenicol prednisone liniment group exhibited a prolonged latency period of pruritus,an increased inhibition rate,and a shortened duration of pruritus.Additionally,there was a significant reduction in the frequency of mice licking their bodies,as well as in six eczema severity indicators:redness and swelling,scratch marks,papules,blisters,exudation or erosion at the lesion site,and the degree of skin swelling.Furthermore,levels of TEWL,histamine,and SP were also significantly decreased(P<0.05).[Conclusions]Chloramphenicol prednisone liniment exhibits anti-inflammatory and anti-pruritic properties.Its mechanism of action may involve the inhibition of mast cell activation within the lesion tissues of eczema model mice,thereby reducing the release of histamine and other active substances.This process alleviates inflammatory damage associated with eczema and contributes to the restoration of skin barrier function.展开更多
This work aims to compare the chemical composition and anti-inflammatory effects on RAW264.7 macrophages of Keemun black tea stems and leaves.A total of 50 volatile compounds were identified in tea stems and leaves,an...This work aims to compare the chemical composition and anti-inflammatory effects on RAW264.7 macrophages of Keemun black tea stems and leaves.A total of 50 volatile compounds were identified in tea stems and leaves,and aldehydes,alcohols,and esters were the main volatile compound categories.There were 11 key volatile compounds,including geraniol,benzeneacetaldehyde,methyl salicylate,linalool,etc.contributed to distinguishing the tea stems from the tea leaves.In the quantitative and liquid chromatography-mass spectrometry(LC-MS)-based metabolomics analysis,higher contents of amino acids,monosaccharides,and quinic acids were found in stems than those in leaves.Inversely,higher contents of tea pigments,flavan-3-ols,gallic acid,purine alkaloids,and flavonol glycosides were present in tea leaves than in stems.LC-MS-based metabolomics also revealed that organic acids were the most critical non-volatile compounds responsible for the differences between tea stems and leaves.Furthermore,tea stems had better inhibiting effects of pro-inflammatory cytokines(interleukin(IL)-1βand IL-6)in lipopolysaccharide-challenged RAW264.7 macrophages than tea leaves,while no significant differences exist between leaves and stems for inhibiting the secretion of tumor necrosis factorα(TNF-α)and NO.In conclusion,our results support using Keemun black tea stems as a novel source of anti-inflammatory compounds.展开更多
Chondroitin sulfate(CS)is one of the main bioactive compounds in animal cartilage.In this study,the antiinflammatory activity of sturgeon-derived chondroitin sulfate(SCS)was evaluated in the dextran sulfate sodium(DSS...Chondroitin sulfate(CS)is one of the main bioactive compounds in animal cartilage.In this study,the antiinflammatory activity of sturgeon-derived chondroitin sulfate(SCS)was evaluated in the dextran sulfate sodium(DSS)-induced BALB/c mice model.Orally administration of SCS significantly alleviated the DSSinduced colitis symptoms,including the reduction of crypt depth,inhibition of the abnormal crypt foci formation,down-regulation of the proinflammatory biomarkers(NO,interleukin(IL)-6,IL-1βand tumor necrosis factor-α)and up-regulation of the anti-inflammatory biomarkers(IL-10 and IL-4).The gut microbiota analysis revealed that SCS alters the intestinal microbiota composition in colitis mice,especially the increase of the relative abundance of Ruminococcaceae and Lachnospiraceae.This alternation further induced primary bile acids convert into secondary bile acids.With SCS administration,the levels of deoxycholic acid(DCA)and litho cholic acid(LCA)were increased by 1.5-and 2.5-fold,respectively.The stimulated secretion of DCA and LCA showed further activation of the NF-κB signaling pathway,thereby suppressing the inflammatory response and attenuating inflammatory bowel disease(IBD)in mice.This study provided a valuable strategy for colitis prevention and treatment with sturgeon cartilage by-products.展开更多
Scarring poses a significant challenge in wound healing,especially for chronic wounds like those linked to diabetes.This study developed a dual drug-loaded core-shell fiber scaffold(PSPC)containing curcumin(Cur)in the...Scarring poses a significant challenge in wound healing,especially for chronic wounds like those linked to diabetes.This study developed a dual drug-loaded core-shell fiber scaffold(PSPC)containing curcumin(Cur)in the shell and salvianolic acid B(SAB)in the core via electrospinning to address this challenging issue through synergistic anti-inflammatory and anti-fibrosis efficacy.The PSPC scaffold presented favorable tensile properties(3.78±0.29 MPa of tensile strength and 337.64%±32.07%of elongation at break)and suture retention(2.71±0.17 N).In vitro experiments confirmed that this scaffold was biocompatible,supporting cell adhesion and proliferation.Additionally,it also scavenged excessive intracellular reactive oxygen species(ROS)and promoted macrophage polarization towards the regenerative M2 phenotype.In vivo studies using a mouse diabetic wound model showed that the PSPC scaffold effectively mitigated inflammatory responses,promoted neoangiogenesis,and facilitated epidermal formation and re-epithelialization.More importantly,the scaffold also modulated collagen synthesis,decreased the collagen type I/III ratio,supported the functional regeneration of hair follicles,sebaceous glands,and other skin appendages,then ultimately achieved the goal of chronic diabetic wound healing and scar reduction.The developed dual drug-loaded fiber scaffold integrating anti-inflammatory and anti-fibrosis presents a promising strategy for the anti-scarring treatment of chronic wounds.展开更多
基金supported by the National Natural Science Foundation of China(No.82302772)Guizhou Basic Research Project(No.ZK[2023]General 201)partially supported by Wuhan Kangchuang Biotechnology Co.,Ltd。
文摘Macrophages undergo dynamic transitions between M1 and M2 states,exerting profound influences on both inflammatory and regenerative processes.The biocompatible and wound-healing properties of decellularized amniotic membrane(d AM)make it a subject of exploration for its potential impact on the anti-inflammatory response of macrophages.Experimental findings unequivocally demonstrate that d AM promotes anti-inflammatory M2 polarization of macrophage,with its cytokine-rich content posited as a potential mediator.The application of RNA sequencing unveils differential gene expression,implicating the hypoxia inducible factor-1α(HIF-1α)signaling pathway in this intricate interplay.Subsequent investigation further demonstrates that d AM facilitates anti-inflammatory M2 polarization of macrophage through the upregulation of epidermal growth factor(EGF),which,in turn,activates the phosphatidylinositol 3-kinase(PI3K)/protein kinase B(AKT)pathway and stabilizes HIF-1α.This cascade results in a noteworthy augmentation of anti-inflammatory gene expression.This study significantly contributes to advancing our comprehension of d AM's immunomodulatory role in tissue repair,thereby suggesting promising therapeutic potential.
基金supported by the National Natural Science Foundation of China(Grant No.:82474195)the Postgraduate Research&Practice Innovation Program of Jiangsu Province,China(Grant No.:021093002882)+2 种基金the Youth Medical Innovation Research Project of China(Grant No.:P24021887623)Taizhou Science and Technology Support Project,China(Grant No.:TS202420)grants from Nanjing Medical University,China(Grant Nos.:TZKY20230104 and 2024KF0292).
文摘Respiratory syncytial virus(RSV)is a ubiquitous respiratory virus that affects individuals of all ages;however,there is a notable lack of targeted treatments.RSV infection is associated with a range of respiratory symptoms,including bronchiolitis and pneumonia.Baicalin(BA)exhibits significant therapeutic effects against RSV infection through mechanisms of viral inhibition and anti-inflammatory action.Nonetheless,the clinical application of BA is constrained by its low solubility and bioavailability.In this study,we prepared BA nanodrugs(BA NDs)with enhanced water solubility utilizing the supramolecular self-assembled strategy,and we further conducted a comparative analysis of this pharmacological activity between free drugs and NDs of BA.Both in vitro and in vivo results demonstrated that BA NDs significantly enhanced the dual effects of viral inhibition and inflammation relief compared to free BA,attributed to prolonged lung retention,improved cellular uptake,and increased targeting affinity.Our study confirms that the nanosizing strategy,a straightforward approach to enhance drug solubility,can also increase biological activity compared to free drugs with the same content,thereby providing a potential ND for RSV treatment.This correlation analysis between the existing forms of drugs and their biological activity offers a novel perspective for research on the active ingredients of traditional Chinese medicine.
文摘Silica gel column chromatography(CC),Sephadex LH-20 CC and high performance liquid chromatography(HPLC)were used to study the chemical constituents of the fruits of the medicine-food plant Rubus idaeus Linnaeus.A new tetrahydrogenated naphthol syringic acid ester,named rubusnolicester(1),two new phenolic glycoside derivatives,4-chloro-2,6-dimethoxylphenol-1-O-β-D-glucopyranoside(2)and salicylic acid-2-O-(6'-O-acetyl)-β-D-glucopyranoside(3),together with one known salicylic acid glycoside derivative(4)and three known flavonoids derivatives(5~7),were isolated.Their structures were elucidated by HRESI-MS,NMR spectroscopy,and a comparison of optical rotation(OR).Compounds 1~7 were evaluated the inhibitory activities against the nitric oxide(NO)production induced by lipopolysaccharide(LPS)in mouse macrophage RAW264.7 cells in vitro.Compound 1 exhibited inhibitory effect with the IC50 value of(12.28±1.25)μmol/L.
文摘Eight sesquiterpenes were isolated from Ainsliaea glabra.Among them,a new guaianolide sesquiterpenoid,named ainsglaolide A(1),and seven known sesquiterpenoids 2~8 were identified.Compound 1 was a novel guaianolide sesquiterpenoid featuring a rare six-membered lactone ring formed between C-4 and C-15.The new compound structure was elucidated by HRESI-MS and NMR spectroscopy,as well as electrostatic circular dichroism(ECD)calculations were used to further confirm the absolute of 1.Anti-inflammatory activity tests were conducted on the separated compounds,indicating that compound 1 had significant inhibitory effect on NLRP3 inflammasome with an IC_(50) value of 1.86μmol/L.
文摘Artemisia dracunculus L.,or tarragon,is a perennial herb from the Asteraceae family that is extensively cultivated for its aromatic leaves,which are valued for its preventative and therapeutic properties in both cookery and traditional medicine.This study aims to investigate the antibacterial,antioxidant,and anti-inflammatory properties of A.dracunculus(tarragon)essential oil(ADEO),with estragole(57.23%)identified as the major compound through gas chromatography-mass spectrometry(GC-MS)analysis.ADEO exhibited varying degrees of antibacterial activity,with Escherichia coli showing higher resistance inhibition zone(IZ)=14.7±0.58 mm,minimum (inhibitory concentration(MIC)=2%and minimum bactericidal concentration(MBC)=4%),while Bacillus subtilis(IZ=24.05±2.11 mm and MIC=MBC=0.125%)and Staphylococcus aureus(IZ=18.69±1.45 mm,MIC=0.0612%and MBC=0.125%)were more sensitive to its actions.Antioxidant ability was assessed using 1,1-diphenyl-2-picrylhydrazil(DPPH),2,2′-azinobis(3-ethylbenzothiazoline-6-sulfonic acid)(ABTS),xanthine oxidase inhibition,and beta-carotene bleaching assays.ADEO showed remarkable antiradical effect on DPPH(IC_(50)=127.05±3.47μg/mL)and ABTS radical(IC_(50)=89.60±8.73μg/mL)as well as significant inhibition of xanthine oxidase(IC_(50)=47.9±2.04μg/mL)and lipid peroxidation(IC_(50)=231.63±5.21μg/mL).ADEO also showed significant anti-inflammatory activity by inhibiting the enzymesCOX-1(IC_(50)=59.2±2.43μg/mL),Cyclo-oxygenase-2(COX-2)(IC_(50)=74.68±1.34μg/mL)and 5-lipooxygense(5-LOX)(IC_(50)=93.18±1.87μg/mL),which are involved in the inflammatory pathway.These findings suggest that ADEO,with its high estragole content,holds promising potential as a natural antibacterial,antioxidant,and anti-inflammatory agent for preventive and therapeutic applications.Further research is needed to explore its safety and efficacy in clinical settings.
基金funding agency in the public,commercial,or not-for-profit sectors.
文摘Background:The root of Desmodium gangeticum,a key component of“Dashamoola,”is a significant Ayurveda remedy for inflammatory conditions.Due to the less availability of D.gangeticum in Sri Lanka,indigenous physicians often substitute Alysicarpus vaginalis root without scientific validation.Further,no comparative study has been conducted on the whole plants of these species.This research is focused on comparing the aqueous extracts of roots and whole plants of A.vaginalis and D.gangeticum for anti-inflammatory activity,acute toxicity,and to quantify major phytochemicals.Methods:Freeze-dried aqueous extracts were prepared and assessed for anti-inflammatory potency using the egg albumin denaturation assay,heat-induced red blood cell membrane stabilization assay,and nitric oxide assay.Acute toxicity was evaluated using the zebrafish embryo assay,and major phytochemicals,were quantitatively screened.Results:In egg albumin denaturation assay,D.gangeticum whole plant(IC_(50)107.89±0.71μg/mL)and root(IC_(50)210.37±0.39μg/mL)exhibited superior anti-inflammatory potency compared to diclofenac sodium(IC_(50)826.04±0.27μg/mL)and A.vaginalis(whole plant IC_(50)1,336μg/mL,root IC_(50)3,162.28μg/mL).In red blood cell membrane stabilization assay,D.gangeticum(whole plant IC_(50)47.86±0.52μg/mL,root IC_(50)331.13±0.83μg/mL)showed the highest activity.Quercetin(IC_(50)285.01μg/mL)was the most potent,with D.gangeticum(IC_(50)2,080.03μg/mL)and A.vaginalis(IC_(50)7,183.87μg/mL)showing weaker inhibition in the nitric oxide assay.Regarding toxicity,lower toxicity showed for D.gangeticum(LC502,570.39μg/mL)compared to A.vaginalis(LC501,348.96μg/mL).In phytochemical analysis,phenols,flavonoids,tannins,alkaloids and saponins were quantified.Statistical analysis revealed significant differences between effects of all extracts and reference drugs(P<0.05).Conclusion:Comparative analysis revealed,D.gangeticum has higher anti-inflammatory activity and lower toxicity than A.vaginalis,suggesting its suitability over A.vaginalis in Sri Lankan practices.
文摘Thymus serpyllum L.,often known as wild thyme,has been used since ancient times due to its multifaceted culinary and medicinal attributes.It is usually utilized in folk medicine to manage different health issues.This work aimed to investigate the chemical composition and biological characteristics of T.serpyllum essential oil(EO),including its antimicrobial,antioxidant,and anti-inflammatory capabilities.Moreover,we have prompted an in-silico simulation to reveal the underlying mode of action of these properties.The chemical characterization of T.serpyllum(EO)by Gas Chromatography-Mass Spectrometry(GC-MS)indicated sabinene(17.33%),terpinen-4-ol(11.73%),phellandral(13.18%),and thymol(10.54%)as main components.The antimicrobial screening utilized the disc-diffusion technique,MIC,and MBC assays.The disc-diffusion test’s results revealed significant anti-Candida activity and notable antibacterial efficacy.The MIC and MBC tests showed that T.serpyllum EO effectively stops bacterial growth,including Gram-positive and Gram-negative strains and Candida strains.The tolerance level ratio demonstrated that this EO exhibits bactericidal and fungicidal effects on all tested bacteria and Candida strains.Also,T.serpyllum EO presented effective inhibitory activity against the 5-lipoxygenase(5-LOX)enzyme(IC50=744.19±0.1µg/mL)(p<0.05).It also effectively affected FRAP,β-carotene,DPPH,and ABTS radicals.In light of these findings,T.serpyllum holds promise for diverse applications across pharmaceuticals,nutraceuticals,and the food industry.However,further research and collaboration between traditional knowledge and modern medicine are crucial to fully realizing its potential benefits in these fields.
文摘Gallstone disease(cholelithiasis)is a common gastrointestinal(GI)disorder characterized by the accumulation of hardened bile constituents,often leading to complications such as cholecystitis,cholangitis,and pancreatitis.Most gallstones are cholesterol-based and form due to bile supersaturation,gallbladder dysm-otility,and inflammation.Current treatment options–such as ursodeoxycholic acid,laparoscopic cholecystectomy,and dietary modifications–have limitations including invasiveness,prolonged duration,side effects,and recurrence risk.Melatonin,a hormone secreted by the pineal gland,has gained attention for its antioxidant and anti-inflammatory properties,as well as its regulatory effects on lipid metabolism and gallbladder motility.Experimental studies suggest that melatonin reduces biliary cholesterol,suppresses oxidative stress,and restores gallbladder muscle function,thereby preventing gallstone formation.It is also present in bile and shown to enhance cholesterol conversion into bile acids and inhibit intestinal cholesterol absorption.Beyond gallstone prevention,melatonin demonstrates protective effects against GI malignancies,including hepatocellular carcinoma and cholangiocarcinoma,by regulating mitochondrial function,inhibiting glycolysis,and modulating apoptosis.With a strong safety profile and minimal side effects,melatonin may serve as a promising adjunct or alternative for gallstone management,particularly in patients unfit for surgery.Further clin-ical research is warranted to validate its therapeutic role.
基金the National Natural Science Foundation of China(82070928 and 82171026).
文摘Objective:To investigate the anti-inflammatory,antioxidant,and goblet cell-stimulating effects of a suspension of Ophiopogon japonicus(L.f.)Ker Gawl.(O.japonicus,Mai Dong)extract combined with hyaluronic acid(HA)in the mouse model with dry eye disease(DED).Methods:A DED mouse model was induced using benzalkonium chloride(BAK),followed by treatment with O.japonicus extract-containing eye drops at varying concentrations.Experimental groups included a normal control,a DED model control,a positive control,and an O.japonicus extract-treated group.Corneal fluorescein staining and tear break-up time(TBUT)were used to assess tear film stability and ocular surface integrity.Enzyme-linked immunosorbent assay(ELISA)measured inflammatory factor levels in corneal and conjunctival tissues,whereas Western blot(WB)analyzed key antioxidant and inflammatory markers,including nuclear factor erythroid 2-related factor(2Nrf2)and heme oxygenase 1(HO-1).Periodic acid-schiff(PAS)staining and immunofluorescence were used to evaluate goblet cell density and mucin secretion.Results:O.japonicus extract significantly improved corneal damage,reduced fluorescein staining scores,prolonged TBUT,and increased tear secretion.It downregulated inflammatory markers,including interleukin-8(IL-8),interleukin-1β(IL-1β),and interferon-g(IFN-γ)while upregulating Nrf2,HO-1,and the interleukin-13(IL-13)/IFN-γ ratio,alleviating oxidative stress and inflammation.PAS staining showed increased conjunctival goblet cell density and restored mucin secretion,enhancing tear film stability.Conclusion:O.japonicus extract demonstrated significant anti-inflammatory,antioxidant,and goblet cell-stimulating effects in a DED model,with good biocompatibility and promising therapeutic potential.Future research should optimize extraction processes and validate their efficacy and safety in clinical settings.
基金supported by the National Natural Science Foundation of China(No.81874369)the Excellent Youth Project of the Hunan Provincial Department of Education(No.22B0388)the Project of Hunan Administration of Traditional Chinese Medicine(No.B2023143)。
文摘Five new flavan-4-ol glycosides jixueqiosides A-E(1-5)and two new flavan glycosides jixueqiosides F and G(6 and 7),along with twelve known flavan-4-ol glycosides(8-19),were isolated from the roots of Pronephrium penangianum.Comprehensive spectral analyses,X-ray single-crystal diffraction,and theoretical electronic circular dichroism(ECD)calculations established structures and absolute configurations.A single crystal structure of flavan-4-ol glycoside(14)was reported for the first time,while the characteristic ECD and NMR data for all isolated flavan-4-ol glycosides(1-5,8-19)were analyzed,establishing a set of empirical rules.Activity screening of these isolates showed that 8 and 9 could inhibit the proliferation of MDA-MB-231 and MCF-7 cells with IC50 values of 7.93±2.85μmol·L^(-1)and 5.87±1.58μmol·L^(-1)(MDA-MB-231),and 2.21±1.38μmol·L^(-1)and 3.52±1.55μmol·L^(-1)(MCF-7),respectively.Western blotting and flow cytometry analyses demonstrated that 8 and 9 dose-dependently induced apoptosis in MDA-MB-231 cells by up-regulating BAX,activating caspase-3 and down-regulating BCL-2.Additionally,compound 8 affected autophagy-related proteins,increasing the ratio of LC3-II/LC3-I and Beclin-1 levels to inhibit MDA-MB-231 cell proliferation.Moreover,anti-inflammatory studies indicated that 2,3,7,13,14,and 18 moderately inhibited tumor necrosis factor-α(TNF-α),interleukin-6(IL-6),and nitric oxide(NO)release.
基金supported by the National Natural Science Foundation of China(Nos.21937006,U23A20510,82204245,82222072,and U24A20806)the Strategic Priority Research Program of the Chinese Academy of Sciences(No.XDB1230000)the Research Project of Yunnan Province(Nos.202401BC070016 and 202402AA310047)。
文摘Gentianopsis barbata(G.barbata)represents a significant plant species with considerable ornamental and medicinal value in China.This investigation sought to elucidate the primary constituents within the plant and investigate their pharmacological properties.Fifty triterpenoids(1-50),including nine previously undescribed compounds(1,2,7,10,20,28,29,37,and 41)were isolated and characterized from the whole plants of G.barbata.Notably,compounds 1 and 2 exhibited the novel 3,4;9,10-diseco-24-homo-cycloartane triterpenoid skeleton.The isolated triterpenoids demonstrated substantial anti-inflammatory activity through inhibition of tumor necrosis factorα(TNF-α)and interleukin-6(IL-6)cytokine secretion in LPS-induced RAW264.7 macrophages,and hepatoprotective effects by preventing tertbutyl hydroperoxide(t-BHP)-induced oxidative injury in HepG2 cells.These results demonstrate both the presence of diverse triterpenoids in G.barbata and their therapeutic potential for inflammatory and hepatic conditions,providing scientific evidence supporting the clinical application of this traditional Mongolian medicinal plant.
基金financially supported by the National Natural Science Foundation of China(Nos.22277147,22177139)the State Key Laboratory of Applied Microbiology South China(No.SKLAM003–2022)。
文摘Two unusual sesquiterpenoids,irpexlactones A(1)and B(2),were isolated from cultures of the basidiomycete Irpex lacteus.Their structures were established by means of spectroscopic methods,the single crystal X-ray diffraction,as well as electronic circular dichroism(ECD)calculations.They possess a novel carbon skeleton with a 5/6/3-fused ring system that may derive from tremulane type sesquiterpenoids with ring-rearrangement.Both compounds show significant inhibitory activities against nitric oxide production with half maximal inhibitory concentration(IC50)values of 2.2 and 1.4μmol/L,respectively.Their anti-inflammatory effects were further evaluated by enzyme-linked immunosorbent assay(ELISA)and Western blot.
基金supported by the second batch of Bureaulevel Projects of the Xizang Medicine Administration of the Xizang Autonomous Region in 2020(No.JJKT20200024).
文摘Five meroterpenoids,rhodonoids K-M(1-2),daurichromene E(3),and grifolins A-B(4-5),together with seven known compounds(6-12),were isolated from Rhododendron anthopogonoides.The chemical structures of these compounds were elucidated through comprehensive analysis of high-resolution electrospray ionization mass spectrometry(HR-ESI-MS),ultraviolet(UV),infrared spectroscopy(IR),and nuclear magnetic resonance(NMR)data.Their absolute configurations were determined by comparing experimental electronic circular dichroism(ECD)spectra with computed values.Notably,compounds 1 and 3 demonstrated significant inhibitory effects on lipopolysaccharide(LPS)-induced inflammation in RAW264.7 cells.These compounds markedly suppressed the mRNA expressions of inflammatory factors,including interleukin(IL)-1β,IL-6,and tumor necrosis factor-α(TNF-α)while also down-regulating the protein expressions of inducible nitric oxide synthase(iNOS)and cyclooxygenase-2(COX-2).
基金Shenzhen Science and Technology Program(JCYJ2022-0530150408018,JCYJ20250604180541051)Shenzhen Basic Discipline Layout Project(JCYJ20220818101806014)。
文摘Objective To investigate the protective effects of morusin on lipopolysaccharide(LPS)-induced acute liver injury in mice and its underlying mechanisms.Methods Thirty-two male specific pathogen-free(SPF)C57BL/6J mice were randomly divided into four groups(n=8 per group):control,LPS,low-dose morusin(morusin-L,10 mg/kg),and high-dose morusin(morusin-H,20 mg/kg)groups.The mice in each group were administered the corresponding drugs or normal saline via continuous gavage daily for 16 consecutive days.Except for control group,which received an equal volume of normal saline,other groups were intraperitoneally injected with LPS(5 mg/kg)2 h after the last gavage to establish the acute liver injury model.Serum and liver tissues were collected for subsequent analysis 6 h after LPS injection.The activities of alanine aminotransferase(ALT)and aspartate aminotransferase(AST)in serum were detected with biochemical methods.The levels of tumor necrosis factor(TNF)-α,interleukin(IL)-6,and IL-1βin serum were measured by enzyme-linked immunosorbent assay(ELISA).Hepatic pathological changes were evaluated by hematoxylin-eosin(HE)staining.The 16S ribosomal RNA(16S rRNA)sequencing was performed to assess the composition of intestinal flora,linear discriminant analysis effect size(LEfSe)was applied for multi-level species discrimination,and Spearman’s correlation analysis was performed.The liver tissues of mice with acute liver injury were analyzed by RNA sequencing(RNA-seq)technology to identify differentially expressed genes(DEGs),and then enrichment analysis of the Kyoto Encyclopedia of Genes and Genomes(KEGG)pathway was conducted.The expression levels of selected genes was validated by quantitative reverse transcription polymerase chain reaction(qRT-PCR),while immunohistochemistry(IHC)was performed to examine the expression levels of IL-6,myeloid differentiation primary response 88(MYD88),and toll-like receptor 2(TLR2).Results Morusin significantly reduced the serum levels of ALT,AST,and inflammatory factors(TNF-α,IL-6,and IL-1β)(P<0.05,P<0.01,or P<0.001),while alleviating the hepatic pathological damage in mice.Based on efficacy comparisons,morusin-H group was selected for subsequent microbiome and transcriptome analyses.Microbiome analysis revealed that morusin-H effectively mitigated LPS-induced gut dysbiosis and restored the Firmicutes/Bacteroidota balance(P<0.01).At the genus level,morusin-H significantly reduced the abundances of norank_f_Muribaculaceae,Desulfovibrio,Parabacteroides,and Muribaculum(P<0.05,P<0.01,or P<0.001).At the phylum,family,and genus levels,our findings indicated that morusin-H treatment caused a significant decrease in the abundance of Desulfobacterota,Desulfovibrionaceae,and Desulfovibrio(P<0.01).Importantly,the abundance of Desulfovibrio was positively correlated with the levels of ALT,AST,TNF-α,IL-1β,and IL-6.Transcriptomic and molecular analyses showed that the therapeutic mechanism of morusin-H involved suppression of the IL-17/TNF signaling pathways and downregulating the mRNA levels of Tlr2,Tlr3,Myd88,Il6,and Cxcl10(P<0.05 or P<0.001),as well as the protein levels of key inflammatory mediators(IL-6,MYD88,and TLR2)(P<0.001).Conclusion Morusin demonstrates protective effects against LPS-induced acute liver injury,likely through modulation of gut microbiota and suppression of pro-inflammatory factor expression.These findings indicate that morusin exerts its effects through the"microbiota-inflammation-liver"axis,providing a theoretical basis for its use as a multi-target plant-based drug in the treatment of metabolic inflammation-related liver diseases.
基金Supported by Natural Science Foundation of Chongqing(No.CSTB2024NSCQ-MSX0900No.CSTB2023NSCQ-MSX0593).
文摘AIM:To assess and rank the efficacy of various nonsteroidal anti-inflammatory drugs(NSAIDs)in preventing postoperative macular edema(PME)after cataract surgery.METHODS:A comprehensive search was conducted across PubMed,Embase,Cochrane Library,and Web of Science databases.Randomized controlled trials(RCTs)comparing different NSAIDs and control treatments for the prevention of PME were included.Data from the studies were synthesized using the“gemtc”package in R.Risk of bias was assessed with the Cochrane RoB 2 tool,and heterogeneity was evaluated using the global I2 statistic.Surface under the cumulative ranking curve(SUCRA)values were calculated for each treatment.RESULTS:Of 132 identified records,9 RCTs met the inclusion criteria.The Network Meta-analysis indicated that nepafenac had the highest efficacy in preventing PME,followed by artificial tear substitute,ketorolac,diclofenac,and bromfenac.The league table comparisons and rankograms corroborated these findings,with nepafenac consistently ranking highest.Heterogeneity analysis yielded high I2 values,indicating substantial variability across studies.CONCLUSION:This Network Meta-analysis suggests that nepafenac is the most effective NSAID for preventing PME following cataract surgery.Given the substantial heterogeneity observed,further high-quality RCTs are required to confirm these findings and explore the sources of variability.Clinicians should consider these results when selecting NSAIDs for PME prophylaxis in cataract surgery patients.
基金supported by the National Natural Science Foundation of China(Nos.82274069,82030116,and 82141212)the Young Scientific and Technological Talents(Level Two)in Tianjin(No.QN20230212)+1 种基金Tianjin Education Commission Research Program Project(No.2024KJ004)the Eaglet Plan Project of Tianjin University of Traditional Chinese Medicine(No.XJS2024101).
文摘In continuation of research aimed at identifying anti-inflammatory agents from natural sesquiterpenoids,an activity-guided fractionation approach utilizing lipopolysaccharide(LPS)-mediated RAW264.7 cells was employed to investigate chemical constituents from Inula Britannica(I.britannica).Seven novel sesquiterpenoid dimers inulabritanoids A−G(1−7)and two novel sesquiterpenoid monomers inulabritanoids H(8)and I(9)were isolated from I.britannica together with eighteen known compounds(10−27).The structural elucidation was accomplished through comprehensive analysis of 1D and 2D nuclear magnetic resonance(NMR),high-resolution mass spectrometry(HR-MS),and electronic circular dichroism(ECD)spectra,complemented by quantum chemical calculations.Compounds 1,2,12,16,19,and 26 demonstrated inhibitory effects on NO production,with IC50 values of 3.65,5.48,3.29,6.91,3.12,and 5.67μmol·L^(−1),respectively.Mechanistic studies revealed that compound 1 inhibited IκB kinaseβ(IKKβ)phosphorylation,thereby blocking nuclear factorκB(NF-κB)nuclear translocation,and activated the kelch-like ECH-associated protein 1(Keap1)/nuclear factor erythroid 2-related factor 2(Nrf2)signal pathway,leading to decreased expression of NADPH oxidase 2(NOX-2),inducible nitric oxide synthase(iNOS),tumor necrosis factorα(TNF-α),interleukin-6(IL-6),monocyte chemotactic protein-1(MCP-1),IL-1β,and IL-1αand increased expression of NAD(P)H:quinone oxidoreductase 1(NQO-1)and heme oxygenase-1(HO-1),thus exhibiting anti-inflammatory effects in vitro.These results indicate that dimeric sesquiterpenoids may serve as promising candidates for anti-inflammatory drug development.
文摘[Objectives]To observe the effects of chloramphenicol prednisone liniment on anti-inflammatory and anti-pruritic responses and skin barrier function in an acute eczema mouse model and explore its potential underlying mechanism.[Methods]Twenty-four female SPF-grade ICR mice were randomly and equally assigned to three groups:the blank control group,the acute eczema group,and the chloramphenicol prednisone liniment group according to the random number table method,with 8 mice per group.Except for the blank control group,the acute eczema model was established by applying 2,4-dinitrochlorobenzene(DNCB)to the right dorsal area.On day 10(d10),0.1 mL of normal saline was administered to the modeling site in both the blank control group and the acute eczema group,whereas chloramphenicol prednisone liniment was applied to the positive drug group.Medication was applied twice daily in all three groups for a total duration of 14 d.Sixty minutes following the final administration of the drug,the development of eczema in mice was visually assessed,and the severity of skin lesions was scored.Trans-epidermal water loss(TEWL)was measured using a multifunctional skin tester.Experiments inducing and alleviating pruritus were performed to compare the frequency of mice licking their bodies,the latency period before pruritus onset,and the duration of pruritus episodes.Levels of histamine and substance P(SP)in the lesion tissues were quantified using enzyme-linked immunosorbent assay(ELISA).[Results]Compared to the acute eczema group,the chloramphenicol prednisone liniment group exhibited a prolonged latency period of pruritus,an increased inhibition rate,and a shortened duration of pruritus.Additionally,there was a significant reduction in the frequency of mice licking their bodies,as well as in six eczema severity indicators:redness and swelling,scratch marks,papules,blisters,exudation or erosion at the lesion site,and the degree of skin swelling.Furthermore,levels of TEWL,histamine,and SP were also significantly decreased(P<0.05).[Conclusions]Chloramphenicol prednisone liniment exhibits anti-inflammatory and anti-pruritic properties.Its mechanism of action may involve the inhibition of mast cell activation within the lesion tissues of eczema model mice,thereby reducing the release of histamine and other active substances.This process alleviates inflammatory damage associated with eczema and contributes to the restoration of skin barrier function.
基金supported by the Natural Science Foundation of China(32122079,32072633)Earmarked Fund for China Agriculture Research System(CARS-19)+2 种基金Anhui Key Research and Development Plan(202104b11020001)Young Elite Scientist Sponsorship Program by National CAST(2016QNRC001)High-level Introduced Talent Sponsorship Program by Anhui Agricultural University(rc352203)。
文摘This work aims to compare the chemical composition and anti-inflammatory effects on RAW264.7 macrophages of Keemun black tea stems and leaves.A total of 50 volatile compounds were identified in tea stems and leaves,and aldehydes,alcohols,and esters were the main volatile compound categories.There were 11 key volatile compounds,including geraniol,benzeneacetaldehyde,methyl salicylate,linalool,etc.contributed to distinguishing the tea stems from the tea leaves.In the quantitative and liquid chromatography-mass spectrometry(LC-MS)-based metabolomics analysis,higher contents of amino acids,monosaccharides,and quinic acids were found in stems than those in leaves.Inversely,higher contents of tea pigments,flavan-3-ols,gallic acid,purine alkaloids,and flavonol glycosides were present in tea leaves than in stems.LC-MS-based metabolomics also revealed that organic acids were the most critical non-volatile compounds responsible for the differences between tea stems and leaves.Furthermore,tea stems had better inhibiting effects of pro-inflammatory cytokines(interleukin(IL)-1βand IL-6)in lipopolysaccharide-challenged RAW264.7 macrophages than tea leaves,while no significant differences exist between leaves and stems for inhibiting the secretion of tumor necrosis factorα(TNF-α)and NO.In conclusion,our results support using Keemun black tea stems as a novel source of anti-inflammatory compounds.
基金funded by grants from Beijing Fishery Innovation Team Project(BAIC07-2023-13)National Natural Science Foundation of China(32201994)。
文摘Chondroitin sulfate(CS)is one of the main bioactive compounds in animal cartilage.In this study,the antiinflammatory activity of sturgeon-derived chondroitin sulfate(SCS)was evaluated in the dextran sulfate sodium(DSS)-induced BALB/c mice model.Orally administration of SCS significantly alleviated the DSSinduced colitis symptoms,including the reduction of crypt depth,inhibition of the abnormal crypt foci formation,down-regulation of the proinflammatory biomarkers(NO,interleukin(IL)-6,IL-1βand tumor necrosis factor-α)and up-regulation of the anti-inflammatory biomarkers(IL-10 and IL-4).The gut microbiota analysis revealed that SCS alters the intestinal microbiota composition in colitis mice,especially the increase of the relative abundance of Ruminococcaceae and Lachnospiraceae.This alternation further induced primary bile acids convert into secondary bile acids.With SCS administration,the levels of deoxycholic acid(DCA)and litho cholic acid(LCA)were increased by 1.5-and 2.5-fold,respectively.The stimulated secretion of DCA and LCA showed further activation of the NF-κB signaling pathway,thereby suppressing the inflammatory response and attenuating inflammatory bowel disease(IBD)in mice.This study provided a valuable strategy for colitis prevention and treatment with sturgeon cartilage by-products.
基金supported by the National Key Research and Development Program of China(No.2021YFA1201304)Fundamental Research Funds for the Central Universities。
文摘Scarring poses a significant challenge in wound healing,especially for chronic wounds like those linked to diabetes.This study developed a dual drug-loaded core-shell fiber scaffold(PSPC)containing curcumin(Cur)in the shell and salvianolic acid B(SAB)in the core via electrospinning to address this challenging issue through synergistic anti-inflammatory and anti-fibrosis efficacy.The PSPC scaffold presented favorable tensile properties(3.78±0.29 MPa of tensile strength and 337.64%±32.07%of elongation at break)and suture retention(2.71±0.17 N).In vitro experiments confirmed that this scaffold was biocompatible,supporting cell adhesion and proliferation.Additionally,it also scavenged excessive intracellular reactive oxygen species(ROS)and promoted macrophage polarization towards the regenerative M2 phenotype.In vivo studies using a mouse diabetic wound model showed that the PSPC scaffold effectively mitigated inflammatory responses,promoted neoangiogenesis,and facilitated epidermal formation and re-epithelialization.More importantly,the scaffold also modulated collagen synthesis,decreased the collagen type I/III ratio,supported the functional regeneration of hair follicles,sebaceous glands,and other skin appendages,then ultimately achieved the goal of chronic diabetic wound healing and scar reduction.The developed dual drug-loaded fiber scaffold integrating anti-inflammatory and anti-fibrosis presents a promising strategy for the anti-scarring treatment of chronic wounds.
