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
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
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
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
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
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
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
The anti-inflammatory phytochemical investigation of the leaves of Illicium dunnianum(I.dunnianum)resulted in the isolation of five pairs of new lignans(1–5),and 7 known analogs(6–12).The separation of enantiomer mi...The anti-inflammatory phytochemical investigation of the leaves of Illicium dunnianum(I.dunnianum)resulted in the isolation of five pairs of new lignans(1–5),and 7 known analogs(6–12).The separation of enantiomer mixtures 1–5 to 1a/1b–5a/5b was achieved using a chiral column with acetonitrile−water mixtures as eluents.The planar structures of 1–2 were previously undescribed,and the chiral separation and absolute configurations of 3–5 were reported for the first time.Their structures were determined through comprehensive spectroscopic data analysis[nuclear magnetic resonance(NMR),high-resolution electrospray ionization mass(HR-ESI-MS),infrared(IR),and ultraviolet(UV)]and quantum chemistry calculations(ECD).The new isolates were evaluated by measuring their inhibitory effect on NO in lipopolysaccharide(LPS)-stimulated BV-2 cells.Compounds 1a,3a,3b,and 5a demonstrated partial inhibition of NO production in a concentration-dependent manner.Western blot and real-time polymerase chain reaction(PCR)assays revealed that 1a down-regulated the messenger ribonucleic acid(mRNA)levels of tumor necrosis factorα(TNF-α),interleukin-6(IL-6),COX-2,and iNOS and the protein expressions of COX-2 and iNOS.This research provides guidance and evidence for the further development and utilization of I.dunnianum.展开更多
Background:Calopogonium mucunoides(C.mucunoides)is traditionally used in southeastern Nigeria for managing pain and inflammation.The quest for safer options compared to traditional anti-inflammatory medications like i...Background:Calopogonium mucunoides(C.mucunoides)is traditionally used in southeastern Nigeria for managing pain and inflammation.The quest for safer options compared to traditional anti-inflammatory medications like ibuprofen,aspirin,diclofenac,indomethacin,and others has increasingly drawn interest.This research assessed the nutritional makeup and anti-inflammatory properties of the ethanol extract from C.mucunoides leaves(EECML)through in-vitro and in-vivo models.Methods:In vitro tests assessed EECML for its effects on platelet aggregation inhibition,phospholipase-A2 activity,albumin denaturation,hemolysis induced by hypotonicity,antioxidant capabilities,and nutrient makeup employing established biochemical techniques.The paw edema model was employed to assess in-vivo anti-inflammatory effects.Twenty-five male albino rats weighing 120–160 g each were split into five groups(n=5).Group 1 was administered normal saline;Group 2 was given 10 mg/kg body weight(b.w)of Indomethacin,whereas Groups 3,4,and 5 were administered 100,200,and 400 mg/kg b.w of EECML,respectively.Results:The extract of 1,500 g of plant material yielded 28.24 g,accounting for 1.88%of the sample used.The phytochemical analysis of EECML showed higher concentration of steroids(1.295±0.090 mg/100 g)and flavonoids(1.118±0.121 mg/100 g)compared to other secondary metabolites found.The EECML exhibited an LD50>5,000 mg/kg b.w,and contained significant antioxidant vitamins and minerals,plus appreciable amounts of carbohydrate(34.14±0.02%),moisture(32.05±0.02%)and protein(12.74±0.02%)contents.The paw sizes of rats administered escalating doses of the EECML and the standard medication,indomethacin,significantly(P<0.05)reduced markedly over time.At the 5-hour mark,the oedema inhibition percentage in the indomethacin group surpassed that of the 400 mg/kg EECML groups;nonetheless,this difference wasn’t statistically significant(P>0.05).The EECML demonstrated a strong inhibition of 2,2-diphenyl-1-picrylhydrazyl at 160µg/mL,showing a markedly(P<0.05)elevated IC50 value in comparison to the standard ascorbic acid.The EECML considerably(P<0.05)reduced platelet aggregation,phospholipase-A2 activity,albumin denaturation,and hypotonicity-induced hemolysis in a concentration-dependent manner,similar to the standard anti-inflammatory medication.Conclusion:The results indicate that EECML has substantial anti-inflammatory and antioxidant effects,as well as nutritional advantages,reinforcing its traditional application.展开更多
A novel pair of oleanane nor-triterpenes,with compound 1 featuring a unique 18α-H structure,was isolated from mastic,and this compound represents a noteworthy new entity not previously reported in the literature.The ...A novel pair of oleanane nor-triterpenes,with compound 1 featuring a unique 18α-H structure,was isolated from mastic,and this compound represents a noteworthy new entity not previously reported in the literature.The absolute configurations of their structures were further determined using a combination of different analytical methods such as NMR,high-resolution mass spectrometry(HR-MS),ultraviolet(UV),infrared(IR)and single-crystal X-ray diffraction(SXRD).The compound actively mitigated inflammations by efficiently quenching nitric oxide(NO)synthesis within an ex vivo system using lipopolysaccharide activated murine macrophage RAW264.7 cells.Moreover,compound 1 exhibit a better IC_(50) concentration of 11.69±1.39µM,surpassing the efficacy of the positive control dexamethasone,which exhibited an IC50 of 23.21±1.17μM.While compound 2 also demonstrated inhibitory activity,its potency was comparatively weaker,with an IC_(50) of 26.18±2.66μM.展开更多
Diseases resulting from exaggerated inflammatory responses present a significant peril to human beings,and its pathogenesis and treatment have not been fully elaborated.Traditional Chinese medicine offers the benefit ...Diseases resulting from exaggerated inflammatory responses present a significant peril to human beings,and its pathogenesis and treatment have not been fully elaborated.Traditional Chinese medicine offers the benefit of minimal adverse effects and favorable outcomes in the management of inflammatory diseases.Polygonum cuspidatum,a type of traditional Chinese medicine,refers to the dried rhizomes and roots of the plant species Polygonum cuspidatum from the Polygonaceae family.It has a slightly bitter taste and exhibits a cold nature,exhibiting therapeutic effects such as heat-clearing and detoxification,blood stasis removal and pain relief,phlegm resolution,and cough alleviation.Research has demonstrated that the bioactive constituents found in Polygonum cuspidatum can impede the inflammatory response through the modulation of pertinent pathways.The anti-inflammatory effects of it have been primarily observed in nonalcoholic fatty liver disease,arthritis,ischemic stroke,parkinson’s disease,ulcerative colitis,and diabetes mellitus.This review is conducted by combining papers from the past decade.The anti-inflammatory properties and mechanisms of Polygonum cuspidatum and its natural compounds are summarized.It provides a new theoretical basis for further research on the clinical pharmacological effects of Polygonum cuspidatum.展开更多
Photothermal therapy(PTT)is a non-invasive and highly selective tumor treatment.However,it triggers an inflammatory reaction and other adverse effects,including damage to the surrounding healthy tissue and an increase...Photothermal therapy(PTT)is a non-invasive and highly selective tumor treatment.However,it triggers an inflammatory reaction and other adverse effects,including damage to the surrounding healthy tissue and an increased risk of tumor proliferation and metastasis.The cyclooxygenase-2(COX-2)/prostaglandin E2(PGE2)pathway plays a crucial role in regulating tumor development.In this study,we revealed that PTT activates the COX-2/PGE2 pathway.To mitigate the PTT-induced inflammation,based on polydopamine(PDA)and HS-β-cyclodextrin(HS-β-CD),we constructed a photothermal/anti-inflammatory nanoparticle system(named ICG@PDA-β-CD/CEL)loaded with the anti-inflammatory drug celecoxib(CEL)and the photosensitizer indocyanine green(ICG),which targets COX-2.This system helps PTT by(1)reducing pro-inflammatory molecules such as PGE2,tumor necrosis factor-α,and interleukin-6 and inhibiting the COX-2 and nuclear factor kappa-B signaling pathways,(2)suppressing vascular endothelial growth factor production to inhibit tumor angiogenesis,and(3)preventing tumor cell migration and invasion.Further results indicated that ICG@PDA-β-CD/CEL significantly curtailed tumor cell invasion and migration in vitro and suppressed the COX-2/PGE2 pathway in vivo,thereby markedly inhibiting both orthotopic tumor growth and metastasis.ICG@PDA-β-CD/CEL exhibits potent antitumor effects through its combined anti-inflammatory and photothermal therapies,providing a promising strategy for alleviating PTT-related adverse effects.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.
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.
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.
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.
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.
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 Basic Research Program of the Natural Science Fund-Frontier Leading Technology Basic Research Special Project(No.SBK2023050003)by the University Science and Technology Innovation Team of Department of Education of Guizhou Province(No.QJ[2023]099).
文摘The anti-inflammatory phytochemical investigation of the leaves of Illicium dunnianum(I.dunnianum)resulted in the isolation of five pairs of new lignans(1–5),and 7 known analogs(6–12).The separation of enantiomer mixtures 1–5 to 1a/1b–5a/5b was achieved using a chiral column with acetonitrile−water mixtures as eluents.The planar structures of 1–2 were previously undescribed,and the chiral separation and absolute configurations of 3–5 were reported for the first time.Their structures were determined through comprehensive spectroscopic data analysis[nuclear magnetic resonance(NMR),high-resolution electrospray ionization mass(HR-ESI-MS),infrared(IR),and ultraviolet(UV)]and quantum chemistry calculations(ECD).The new isolates were evaluated by measuring their inhibitory effect on NO in lipopolysaccharide(LPS)-stimulated BV-2 cells.Compounds 1a,3a,3b,and 5a demonstrated partial inhibition of NO production in a concentration-dependent manner.Western blot and real-time polymerase chain reaction(PCR)assays revealed that 1a down-regulated the messenger ribonucleic acid(mRNA)levels of tumor necrosis factorα(TNF-α),interleukin-6(IL-6),COX-2,and iNOS and the protein expressions of COX-2 and iNOS.This research provides guidance and evidence for the further development and utilization of I.dunnianum.
文摘Background:Calopogonium mucunoides(C.mucunoides)is traditionally used in southeastern Nigeria for managing pain and inflammation.The quest for safer options compared to traditional anti-inflammatory medications like ibuprofen,aspirin,diclofenac,indomethacin,and others has increasingly drawn interest.This research assessed the nutritional makeup and anti-inflammatory properties of the ethanol extract from C.mucunoides leaves(EECML)through in-vitro and in-vivo models.Methods:In vitro tests assessed EECML for its effects on platelet aggregation inhibition,phospholipase-A2 activity,albumin denaturation,hemolysis induced by hypotonicity,antioxidant capabilities,and nutrient makeup employing established biochemical techniques.The paw edema model was employed to assess in-vivo anti-inflammatory effects.Twenty-five male albino rats weighing 120–160 g each were split into five groups(n=5).Group 1 was administered normal saline;Group 2 was given 10 mg/kg body weight(b.w)of Indomethacin,whereas Groups 3,4,and 5 were administered 100,200,and 400 mg/kg b.w of EECML,respectively.Results:The extract of 1,500 g of plant material yielded 28.24 g,accounting for 1.88%of the sample used.The phytochemical analysis of EECML showed higher concentration of steroids(1.295±0.090 mg/100 g)and flavonoids(1.118±0.121 mg/100 g)compared to other secondary metabolites found.The EECML exhibited an LD50>5,000 mg/kg b.w,and contained significant antioxidant vitamins and minerals,plus appreciable amounts of carbohydrate(34.14±0.02%),moisture(32.05±0.02%)and protein(12.74±0.02%)contents.The paw sizes of rats administered escalating doses of the EECML and the standard medication,indomethacin,significantly(P<0.05)reduced markedly over time.At the 5-hour mark,the oedema inhibition percentage in the indomethacin group surpassed that of the 400 mg/kg EECML groups;nonetheless,this difference wasn’t statistically significant(P>0.05).The EECML demonstrated a strong inhibition of 2,2-diphenyl-1-picrylhydrazyl at 160µg/mL,showing a markedly(P<0.05)elevated IC50 value in comparison to the standard ascorbic acid.The EECML considerably(P<0.05)reduced platelet aggregation,phospholipase-A2 activity,albumin denaturation,and hypotonicity-induced hemolysis in a concentration-dependent manner,similar to the standard anti-inflammatory medication.Conclusion:The results indicate that EECML has substantial anti-inflammatory and antioxidant effects,as well as nutritional advantages,reinforcing its traditional application.
基金National Natural Science Foundation of China(Grant No.82060774)Key Special Projects for Enhancing Subject Comprehensive Strength at Yili Normal University(Project No.22XKZZ08)Open Project of Jiangxi Provinicial Key Laboratory of Natural and Biomimetic Drugs Research(Project No.2024SSY07051).
文摘A novel pair of oleanane nor-triterpenes,with compound 1 featuring a unique 18α-H structure,was isolated from mastic,and this compound represents a noteworthy new entity not previously reported in the literature.The absolute configurations of their structures were further determined using a combination of different analytical methods such as NMR,high-resolution mass spectrometry(HR-MS),ultraviolet(UV),infrared(IR)and single-crystal X-ray diffraction(SXRD).The compound actively mitigated inflammations by efficiently quenching nitric oxide(NO)synthesis within an ex vivo system using lipopolysaccharide activated murine macrophage RAW264.7 cells.Moreover,compound 1 exhibit a better IC_(50) concentration of 11.69±1.39µM,surpassing the efficacy of the positive control dexamethasone,which exhibited an IC50 of 23.21±1.17μM.While compound 2 also demonstrated inhibitory activity,its potency was comparatively weaker,with an IC_(50) of 26.18±2.66μM.
基金supported by grants from Zhejiang Chinese Medicine University affiliated hospital research project(2023FSYYZZ18)scientific research item(2022FH001),School of Life Sciences,Zhejiang Chinese Medicine University.
文摘Diseases resulting from exaggerated inflammatory responses present a significant peril to human beings,and its pathogenesis and treatment have not been fully elaborated.Traditional Chinese medicine offers the benefit of minimal adverse effects and favorable outcomes in the management of inflammatory diseases.Polygonum cuspidatum,a type of traditional Chinese medicine,refers to the dried rhizomes and roots of the plant species Polygonum cuspidatum from the Polygonaceae family.It has a slightly bitter taste and exhibits a cold nature,exhibiting therapeutic effects such as heat-clearing and detoxification,blood stasis removal and pain relief,phlegm resolution,and cough alleviation.Research has demonstrated that the bioactive constituents found in Polygonum cuspidatum can impede the inflammatory response through the modulation of pertinent pathways.The anti-inflammatory effects of it have been primarily observed in nonalcoholic fatty liver disease,arthritis,ischemic stroke,parkinson’s disease,ulcerative colitis,and diabetes mellitus.This review is conducted by combining papers from the past decade.The anti-inflammatory properties and mechanisms of Polygonum cuspidatum and its natural compounds are summarized.It provides a new theoretical basis for further research on the clinical pharmacological effects of Polygonum cuspidatum.
基金the Hebei Natural Science Foundation(Nos.H2023203003 and C2021203004).
文摘Photothermal therapy(PTT)is a non-invasive and highly selective tumor treatment.However,it triggers an inflammatory reaction and other adverse effects,including damage to the surrounding healthy tissue and an increased risk of tumor proliferation and metastasis.The cyclooxygenase-2(COX-2)/prostaglandin E2(PGE2)pathway plays a crucial role in regulating tumor development.In this study,we revealed that PTT activates the COX-2/PGE2 pathway.To mitigate the PTT-induced inflammation,based on polydopamine(PDA)and HS-β-cyclodextrin(HS-β-CD),we constructed a photothermal/anti-inflammatory nanoparticle system(named ICG@PDA-β-CD/CEL)loaded with the anti-inflammatory drug celecoxib(CEL)and the photosensitizer indocyanine green(ICG),which targets COX-2.This system helps PTT by(1)reducing pro-inflammatory molecules such as PGE2,tumor necrosis factor-α,and interleukin-6 and inhibiting the COX-2 and nuclear factor kappa-B signaling pathways,(2)suppressing vascular endothelial growth factor production to inhibit tumor angiogenesis,and(3)preventing tumor cell migration and invasion.Further results indicated that ICG@PDA-β-CD/CEL significantly curtailed tumor cell invasion and migration in vitro and suppressed the COX-2/PGE2 pathway in vivo,thereby markedly inhibiting both orthotopic tumor growth and metastasis.ICG@PDA-β-CD/CEL exhibits potent antitumor effects through its combined anti-inflammatory and photothermal therapies,providing a promising strategy for alleviating PTT-related adverse effects.
