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
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
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
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
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
Berbamine, a kind of alkaloid, was studied for anti-inflammatory activity. Thedrug was tested on carrageenan-induced rat paw oedema and kaolin-induced arthritis in rats.Berbamine has shown significant anti-inflammator...Berbamine, a kind of alkaloid, was studied for anti-inflammatory activity. Thedrug was tested on carrageenan-induced rat paw oedema and kaolin-induced arthritis in rats.Berbamine has shown significant anti-inflammatory and anti-arthritic activities.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
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
Phytochemical investigation of the leaves and twigs of Callicarpa cathayana led to the isolation of six new clerodane diterpenoids,cathayanalactones A-F(1-6),together with seven analogues(7-13).Their structures were e...Phytochemical investigation of the leaves and twigs of Callicarpa cathayana led to the isolation of six new clerodane diterpenoids,cathayanalactones A-F(1-6),together with seven analogues(7-13).Their structures were established by extensive NMR analyses together with experimental and calculated ECD spectra analyses.Compounds 1,2,3,7 and 11 showed inhibitory activities on lipopolysaccharide-induced nitric oxide production in RAW264.7 cells.展开更多
Collagen is a major extracellular matrix protein.Given the potential anti-inflammatory and antioxidant profiles of these bioactive compounds,there has been increasing interest in using collagen derived peptides and pe...Collagen is a major extracellular matrix protein.Given the potential anti-inflammatory and antioxidant profiles of these bioactive compounds,there has been increasing interest in using collagen derived peptides and peptide-rich collagen hydrolysates for skin health,due to their immunomodulatory,antioxidant and proliferative effects on dermal fibroblasts.However,all hydrolysates are not equally effective in exerting the beneficial effects;hence,further research is needed to determine the factors that improve the therapeutic applicability of such preparations.We used different enzymatic conditions to generate a number of different collagen hydrolysates with distinct peptide profiles.We found that the use of two rather than one enzyme for hydrolysis generates a greater abundance of low molecular weight peptides with consequent improvement in bioactive properties.Testing these hydrolysates on human dermal fibroblasts showed distinct actions on inflammatory changes,oxidative stress,type I collagen synthesis and cellular proliferation.Our findings suggest that different enzymatic conditions affect the peptide profile of hydrolysates and differentially regulate their biological activities and potential protective responses on dermal fibroblasts.展开更多
Three new rare cyclopiane diterpenes(1-3),together with thirteen known compounds(4-16),were isolated and identified from a sea sediment-derived fungus Penicillium sp.TJ403-2.The planar and relative structures of compo...Three new rare cyclopiane diterpenes(1-3),together with thirteen known compounds(4-16),were isolated and identified from a sea sediment-derived fungus Penicillium sp.TJ403-2.The planar and relative structures of compounds 1-3 were elucidated by HRESIMS,one-and two-dimensional NMR analyses,and their absolute configurations were further established by X-ray crystallography experiment.Compounds 1-3 were evaluated for the anti-inflammatory activity against LPS-induced NO production,and compound 1 showed notable inhibitory potency with an IC50 value of2.19±0.25μmol/L,which was three fold lower than the positive control indomethacin(IC50=8.76±0.92μmol/L).Further Western blot and immunofluorescence experiments demonstrated its mechanism of action to be that 1 inhibited the NF-κB-activated pathway,highlighting it as a promising starting point for the development of new anti-inflammatory agents.展开更多
A series of bioactive bis（indolyl）methanes are synthesized by one-pot green reaction of indole with various substituted aldehydes by microwave irradiation under solvent free conditions. The antibacterial activity ag...A series of bioactive bis（indolyl）methanes are synthesized by one-pot green reaction of indole with various substituted aldehydes by microwave irradiation under solvent free conditions. The antibacterial activity against Staphylococcus aureus and anti-inflammatory activity of the synthesized bis（indolyl）-methanes are evaluated in vitro and compared to standard drugs tetracycline and diclofenac,respectively. The majority of the compounds showed good antibacterial and anti-inflammatory activity.Interestingly, compounds 3j, 3i, 3k and 3g exhibited much higher anti-inflammatory activity than the standard diclofenac drug and thus qualify for clinical trials to be used as an anti-inflammatory compound.展开更多
Zinc(Zn)has recently been recognized as a promising bone repair material due to its inherent biodegradability and favorable biocompatibility.In this work,rare earth neodymium(Nd)was introduced into a Zn-based alloy fa...Zinc(Zn)has recently been recognized as a promising bone repair material due to its inherent biodegradability and favorable biocompatibility.In this work,rare earth neodymium(Nd)was introduced into a Zn-based alloy fabricated using a laser powder bed fusion(LPBF)process.Results showed that addition of Nd significantly improved the melt fluidity and reduced the evaporation of Zn,thereby achieving parts with a high densification rate of 98.71%.Significantly,the Nd alloying treatment effectively refined the grain size from 25.3 to 6.2μm.Nd Zn5 eutectics precipitated and contributed to a second-phase strengthening effect.As a result,the tensile strength increased to(119.3±5.1)MPa and the Vickers hardness to(76.2±4.1).Moreover,the Zn–Nd alloy exhibited good anti-inflammatory activity,as the Nd ions released during degradation had a strong affinity with cell membrane phospholipids and consequently inhibited the release of inflammatory cytokines.It also presented favorable cytocompatibility,showing great potential as a bone repair material.展开更多
The microbial transformation of glycyrrhetinic acid（1） by Cunninghamella blakesleana CGMCC 3.970 led to the production of five new metabolites（2-6）.The structures of the metabolites were determined by extensive sp...The microbial transformation of glycyrrhetinic acid（1） by Cunninghamella blakesleana CGMCC 3.970 led to the production of five new metabolites（2-6）.The structures of the metabolites were determined by extensive spectroscopic（HR-ESIMS,1D and 2D NMR） data analyses.The involved reactions exhibited specific hydroxylations at C-24,C-7,and C-15,and oxidation at C-3.Moreover,compounds 2,5,and 6showed significant neural anti-inflammatory activity by inhibiting lipopolysaccharide-induced NO production in mouse microglia BV2 cells with IC（50） values of 0.76,0.94,and 0.16μmol/L,respectively.展开更多
A series of 2-substituted-((N,N-disubstituted)-1,3-benzoxazole)-5-carboxamides derivatives were synthesized by the reaction of 2-substituted-5-carbomethoxy benzoxazole with different secondary amines.The newly synthes...A series of 2-substituted-((N,N-disubstituted)-1,3-benzoxazole)-5-carboxamides derivatives were synthesized by the reaction of 2-substituted-5-carbomethoxy benzoxazole with different secondary amines.The newly synthesized compounds were characterized on the basis of spectral(FT-IR,1H NMR,MS) & elemental analysis.All these compounds were screened for anti-inflammatory activity using carrageenan induced rat paw edema method.All of these compounds exhibited significant activity.Among the tested compounds Ve,Vg,Vf and Va were considered to have potent anti-inflammatory activity and was comparable with standard.展开更多
We aimed to explore the anti-infammatory bactivity of mollugin extracted from Rubia cordifolia L,a traditional Chinese medicine,on dextran sulfate sodium(DSS)-induced ulcerative colitis(UC)in mice.Thirty C57BL/6 mice ...We aimed to explore the anti-infammatory bactivity of mollugin extracted from Rubia cordifolia L,a traditional Chinese medicine,on dextran sulfate sodium(DSS)-induced ulcerative colitis(UC)in mice.Thirty C57BL/6 mice were divided into a control group(n=6),a model group(n=6),and three experimental groups(40,20,10 mg/kg of mollugin,n=6 each).DSS solution(3%)was given to mice in the model group and experimental groups from day 4 to day 10 to induce the mouse UC model.Mice in the experimental groups were intragastrically administrated mollugin from day 1 to day 10.Animals were orally given distilled water in the control group for the whole experiment time and in the model group from day 1 to day 3.The changes in colon pathology were detected by hematoxylin and eosin(HE)staining.Interleukin-1β(IL-1β)in the serum,and tumor necrosis factor-α(TNF-α)and interferon-γ(IFN)in the tissues were measured by enzyme linked immunosorbent assay.Expression levels of Toll-like receptor 4(TLR4)and myeloid differentiation factor 88 in the colon tissues were detected by immunohistochemistry.Results showed that mollugin could significantly reduce weight loss and the disease activity index in the DSS-induced UC mouse model.HE examinations demonstrated that mollugin treatment effectively improved the histological damage(P<0.05).The overproduction of IL-Iβand TNF-α was remarkably inhibited by mollugin treatment at doses of 20 and 40 mg/kg(P<0.05).Additionally,the levels of TLR4 in colon tissues were significantly reduced in mollugin-treated groups compared with the DSS group.Our findings demonstrated that mollugin ameliorates DSS-induced UC by inhibiting the production of pro-inflammatory chemocytokines.展开更多
The juice leaked from broken phloem of Paulownia elongate S.Y.Hu has been used to cure acute inflammation resulted from stung injury by poisonous insects for a long time in China,but its potential mechanism remains un...The juice leaked from broken phloem of Paulownia elongate S.Y.Hu has been used to cure acute inflammation resulted from stung injury by poisonous insects for a long time in China,but its potential mechanism remains unclear.The present study was designed to evaluate anti-inflammatory activity and mechanism of total flavonoids from the phloem of P.elongate S.Y.Hu in RAW264.7 cells.Lipopolysaccharide(LPS)-induced nitric oxide(NO)was measured by Griess and mRNA of pro-inflammatory mediators was analyzed by q-PCR.Cell viability was measured using cell counting kit(CCK)-8 assay.The protein level was analyzed by Western blot.The results showed that the total flavonoids of P.elongate significantly inhibited the production of the pro-inflammatory mediators such as NO,interleukin(IL)-1β and interleukin(IL)-6 in LPS-stimulated RAW264.7 cells.Total flavonoids of P.elongate exerted potential anti-inflammatory activity through the regulation of several signaling pathways.Total flavonoids of P.elongate inhibited JAK/STAT by blocking JAK2 and STAT3 phosphorylation levels.This is the first report on anti-inflammatory activity of total flavonoids from the phloem of P.elongate,which suggests that the total flavonoids of P.elongate may have great potential for the development of anti-inflammatory drug to treat inflammatory disorders.展开更多
Objective:To elucidate the potential anti-inflammatory mechanisms of Rhamnus crenata leaf extracts using RAW264.7 cells.Methods:We used 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide assay to measure ce...Objective:To elucidate the potential anti-inflammatory mechanisms of Rhamnus crenata leaf extracts using RAW264.7 cells.Methods:We used 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide assay to measure cell viability.Nitric oxide(NO)production was measured using Griess reagent.Western blotting and RT-PCR assays were carried out for analyzing the protein and gene expressions of pro-inflammatory mediators,respectively.Moreover,PD98059(ERK1/2 inhibitor),SB203580(p38 inhibitor),SP600125(JNK inhibitor),and BAY11-7082(NF-κB inhibitor)were used to evaluate the anti-inflammatory mechanism of Rhamnus crenata leaf extract.Results:Rhamnus crenata leaf extracts significantly inhibited the production of the pro-inflammatory mediators such as NO,iNOS,COX-2,IL-1β,and TNF-αin lipopolysaccharide(LPS)-stimulated RAW264.7 cells.Rhamnus crenata leaf extracts also suppressed LPS-induced degradation of IκB-αand nuclear accumulation of p65,which resulted in the inhibition of NF-κB activation in RAW264.7 cells.Additionally,the extracts attenuated the phosphorylation of p38,ERK1/2,and JNK in LPS-stimulated RAW264.7 cells.Moreover,HO-1 expression induced by Rhamnus crenata leaf extracts was significantly downregulated by SB230580,PD98059,SP600125 and BAY11-7082.Conclusions:Rhamnus crenata leaf extract may upregulate HO-1 expression through inhibition of p38,ERK1/2,and NF-κB activation,which may contribute to the anti-inflammatory activity of the extracts.Rhamnus crenata leaf extracts may have great potential for the development of anti-inflammatory drugs to treat acute and chronic inflammatory diseases.展开更多
Flavonoids exhibit a wide range of biological activities including anti-inflammatory activity, while some 1,3-benzoxazine derivatives show anti-inflammatory activity. In order to explore the novel anti-inflammatory ag...Flavonoids exhibit a wide range of biological activities including anti-inflammatory activity, while some 1,3-benzoxazine derivatives show anti-inflammatory activity. In order to explore the novel anti-inflammatory agents, based on the principles of bioisosterism and hybridization, ten novel ehromeno[8,7-e][1,3]oxazin-4-ones were syn- thesized and characterized with IR, ^1H NMR, MS and elemental analyses. The anti-inflammatory activities of the target compounds were evaluated via the croton oil-induced ear oedema test in Swiss mice. According to screened resuits, some target compounds show potent anti-inflammatory activity.展开更多
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.
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.
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Berbamine, a kind of alkaloid, was studied for anti-inflammatory activity. Thedrug was tested on carrageenan-induced rat paw oedema and kaolin-induced arthritis in rats.Berbamine has shown significant anti-inflammatory and anti-arthritic activities.
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 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 Yunnan Applicative and Basic Research Program(Nos.2018FY001 and 2018FA048)the National Natural Science Foundation of China(Nos.81422046,81860615 and 21762048)+4 种基金the Foundation of Yunnan Educational Committee(No.2018JS002)the Natural Science Foundation of Yunnan University(No.2017YDQN03)the Key Laboratory of Medicinal Chemistry for Natural Resource,Ministry of Education(No.2017KF02)the Program for Changjiang Scholars and Innovative Research Team in University(No.IRT_17R94)Project of Innovative Research Team of Yunnan Province to XIAO Wei-Lie
文摘Phytochemical investigation of the leaves and twigs of Callicarpa cathayana led to the isolation of six new clerodane diterpenoids,cathayanalactones A-F(1-6),together with seven analogues(7-13).Their structures were established by extensive NMR analyses together with experimental and calculated ECD spectra analyses.Compounds 1,2,3,7 and 11 showed inhibitory activities on lipopolysaccharide-induced nitric oxide production in RAW264.7 cells.
基金This study was funded by grants from Alberta Livestock and Meat Agency(ALMA)and the Natural Sciences and Engineering Research Council(NSERC)of Canada to JW.The funders had no role in the study design,data collection and analysis,decision to publish or preparation of this manuscript。
文摘Collagen is a major extracellular matrix protein.Given the potential anti-inflammatory and antioxidant profiles of these bioactive compounds,there has been increasing interest in using collagen derived peptides and peptide-rich collagen hydrolysates for skin health,due to their immunomodulatory,antioxidant and proliferative effects on dermal fibroblasts.However,all hydrolysates are not equally effective in exerting the beneficial effects;hence,further research is needed to determine the factors that improve the therapeutic applicability of such preparations.We used different enzymatic conditions to generate a number of different collagen hydrolysates with distinct peptide profiles.We found that the use of two rather than one enzyme for hydrolysis generates a greater abundance of low molecular weight peptides with consequent improvement in bioactive properties.Testing these hydrolysates on human dermal fibroblasts showed distinct actions on inflammatory changes,oxidative stress,type I collagen synthesis and cellular proliferation.Our findings suggest that different enzymatic conditions affect the peptide profile of hydrolysates and differentially regulate their biological activities and potential protective responses on dermal fibroblasts.
基金financially supported by the Program for Changjiang Scholars of Ministry of Education of the People’s Republic of China (No.T2016088)the National Natural Science Foundation for Distinguished Young Scholars (No.81725021)+1 种基金the Innovative Research Groups of the National Natural Science Foundation of China (No.81721005)the National Natural Science Foundation of China (Nos.81573316 and 21702067)
文摘Three new rare cyclopiane diterpenes(1-3),together with thirteen known compounds(4-16),were isolated and identified from a sea sediment-derived fungus Penicillium sp.TJ403-2.The planar and relative structures of compounds 1-3 were elucidated by HRESIMS,one-and two-dimensional NMR analyses,and their absolute configurations were further established by X-ray crystallography experiment.Compounds 1-3 were evaluated for the anti-inflammatory activity against LPS-induced NO production,and compound 1 showed notable inhibitory potency with an IC50 value of2.19±0.25μmol/L,which was three fold lower than the positive control indomethacin(IC50=8.76±0.92μmol/L).Further Western blot and immunofluorescence experiments demonstrated its mechanism of action to be that 1 inhibited the NF-κB-activated pathway,highlighting it as a promising starting point for the development of new anti-inflammatory agents.
基金financial assistance through a Major Research Project (F. No. 42281/2013 (SR), Dated: 12-03-2013)
文摘A series of bioactive bis（indolyl）methanes are synthesized by one-pot green reaction of indole with various substituted aldehydes by microwave irradiation under solvent free conditions. The antibacterial activity against Staphylococcus aureus and anti-inflammatory activity of the synthesized bis（indolyl）-methanes are evaluated in vitro and compared to standard drugs tetracycline and diclofenac,respectively. The majority of the compounds showed good antibacterial and anti-inflammatory activity.Interestingly, compounds 3j, 3i, 3k and 3g exhibited much higher anti-inflammatory activity than the standard diclofenac drug and thus qualify for clinical trials to be used as an anti-inflammatory compound.
基金the National Natural Science Foundation of China(Nos.51935014,82072084,and 81871498)the Jiangxi Provincial Natural Science Foundation of China(Nos.20192ACB20005 and 2020ACB214004)+4 种基金the Jiangxi Provincial Key R&D Program(No.20201BBE51012)the Guangdong Provincial Higher Vocational Colleges&Schools Pearl River Scholar Funded Scheme(2018)the China Postdoctoral Science Foundation(No.2020M682114)the Open Research Fund of Jiangsu Key Laboratory of Precision and Micro-Manufacturing Technologythe Project of Hunan Provincial Science and Technology Plan(No.2017RS3008),China。
文摘Zinc(Zn)has recently been recognized as a promising bone repair material due to its inherent biodegradability and favorable biocompatibility.In this work,rare earth neodymium(Nd)was introduced into a Zn-based alloy fabricated using a laser powder bed fusion(LPBF)process.Results showed that addition of Nd significantly improved the melt fluidity and reduced the evaporation of Zn,thereby achieving parts with a high densification rate of 98.71%.Significantly,the Nd alloying treatment effectively refined the grain size from 25.3 to 6.2μm.Nd Zn5 eutectics precipitated and contributed to a second-phase strengthening effect.As a result,the tensile strength increased to(119.3±5.1)MPa and the Vickers hardness to(76.2±4.1).Moreover,the Zn–Nd alloy exhibited good anti-inflammatory activity,as the Nd ions released during degradation had a strong affinity with cell membrane phospholipids and consequently inhibited the release of inflammatory cytokines.It also presented favorable cytocompatibility,showing great potential as a bone repair material.
文摘The microbial transformation of glycyrrhetinic acid（1） by Cunninghamella blakesleana CGMCC 3.970 led to the production of five new metabolites（2-6）.The structures of the metabolites were determined by extensive spectroscopic（HR-ESIMS,1D and 2D NMR） data analyses.The involved reactions exhibited specific hydroxylations at C-24,C-7,and C-15,and oxidation at C-3.Moreover,compounds 2,5,and 6showed significant neural anti-inflammatory activity by inhibiting lipopolysaccharide-induced NO production in mouse microglia BV2 cells with IC（50） values of 0.76,0.94,and 0.16μmol/L,respectively.
文摘A series of 2-substituted-((N,N-disubstituted)-1,3-benzoxazole)-5-carboxamides derivatives were synthesized by the reaction of 2-substituted-5-carbomethoxy benzoxazole with different secondary amines.The newly synthesized compounds were characterized on the basis of spectral(FT-IR,1H NMR,MS) & elemental analysis.All these compounds were screened for anti-inflammatory activity using carrageenan induced rat paw edema method.All of these compounds exhibited significant activity.Among the tested compounds Ve,Vg,Vf and Va were considered to have potent anti-inflammatory activity and was comparable with standard.
基金This work was supported by the National Natural Science Foundation of China(No.81703380)the Natural Science Foundation of Hubei Province(No.2017CFB782)+1 种基金the Scientific Research Project of Health and Family Planning Commission of Hubei Province(No.WJ2017M077)the Applied Basic Research Project of Wuhan Science and Technology Bureau(No.2017060201010215).
文摘We aimed to explore the anti-infammatory bactivity of mollugin extracted from Rubia cordifolia L,a traditional Chinese medicine,on dextran sulfate sodium(DSS)-induced ulcerative colitis(UC)in mice.Thirty C57BL/6 mice were divided into a control group(n=6),a model group(n=6),and three experimental groups(40,20,10 mg/kg of mollugin,n=6 each).DSS solution(3%)was given to mice in the model group and experimental groups from day 4 to day 10 to induce the mouse UC model.Mice in the experimental groups were intragastrically administrated mollugin from day 1 to day 10.Animals were orally given distilled water in the control group for the whole experiment time and in the model group from day 1 to day 3.The changes in colon pathology were detected by hematoxylin and eosin(HE)staining.Interleukin-1β(IL-1β)in the serum,and tumor necrosis factor-α(TNF-α)and interferon-γ(IFN)in the tissues were measured by enzyme linked immunosorbent assay.Expression levels of Toll-like receptor 4(TLR4)and myeloid differentiation factor 88 in the colon tissues were detected by immunohistochemistry.Results showed that mollugin could significantly reduce weight loss and the disease activity index in the DSS-induced UC mouse model.HE examinations demonstrated that mollugin treatment effectively improved the histological damage(P<0.05).The overproduction of IL-Iβand TNF-α was remarkably inhibited by mollugin treatment at doses of 20 and 40 mg/kg(P<0.05).Additionally,the levels of TLR4 in colon tissues were significantly reduced in mollugin-treated groups compared with the DSS group.Our findings demonstrated that mollugin ameliorates DSS-induced UC by inhibiting the production of pro-inflammatory chemocytokines.
基金Henan Provincial Department of Science&Technology(172102310165)Henan Provincial Department of Education(21B350001).
文摘The juice leaked from broken phloem of Paulownia elongate S.Y.Hu has been used to cure acute inflammation resulted from stung injury by poisonous insects for a long time in China,but its potential mechanism remains unclear.The present study was designed to evaluate anti-inflammatory activity and mechanism of total flavonoids from the phloem of P.elongate S.Y.Hu in RAW264.7 cells.Lipopolysaccharide(LPS)-induced nitric oxide(NO)was measured by Griess and mRNA of pro-inflammatory mediators was analyzed by q-PCR.Cell viability was measured using cell counting kit(CCK)-8 assay.The protein level was analyzed by Western blot.The results showed that the total flavonoids of P.elongate significantly inhibited the production of the pro-inflammatory mediators such as NO,interleukin(IL)-1β and interleukin(IL)-6 in LPS-stimulated RAW264.7 cells.Total flavonoids of P.elongate exerted potential anti-inflammatory activity through the regulation of several signaling pathways.Total flavonoids of P.elongate inhibited JAK/STAT by blocking JAK2 and STAT3 phosphorylation levels.This is the first report on anti-inflammatory activity of total flavonoids from the phloem of P.elongate,which suggests that the total flavonoids of P.elongate may have great potential for the development of anti-inflammatory drug to treat inflammatory disorders.
基金supported by the research project of the National Institute of Forest Science(project No.FP0400-2019-01-2022).
文摘Objective:To elucidate the potential anti-inflammatory mechanisms of Rhamnus crenata leaf extracts using RAW264.7 cells.Methods:We used 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide assay to measure cell viability.Nitric oxide(NO)production was measured using Griess reagent.Western blotting and RT-PCR assays were carried out for analyzing the protein and gene expressions of pro-inflammatory mediators,respectively.Moreover,PD98059(ERK1/2 inhibitor),SB203580(p38 inhibitor),SP600125(JNK inhibitor),and BAY11-7082(NF-κB inhibitor)were used to evaluate the anti-inflammatory mechanism of Rhamnus crenata leaf extract.Results:Rhamnus crenata leaf extracts significantly inhibited the production of the pro-inflammatory mediators such as NO,iNOS,COX-2,IL-1β,and TNF-αin lipopolysaccharide(LPS)-stimulated RAW264.7 cells.Rhamnus crenata leaf extracts also suppressed LPS-induced degradation of IκB-αand nuclear accumulation of p65,which resulted in the inhibition of NF-κB activation in RAW264.7 cells.Additionally,the extracts attenuated the phosphorylation of p38,ERK1/2,and JNK in LPS-stimulated RAW264.7 cells.Moreover,HO-1 expression induced by Rhamnus crenata leaf extracts was significantly downregulated by SB230580,PD98059,SP600125 and BAY11-7082.Conclusions:Rhamnus crenata leaf extract may upregulate HO-1 expression through inhibition of p38,ERK1/2,and NF-κB activation,which may contribute to the anti-inflammatory activity of the extracts.Rhamnus crenata leaf extracts may have great potential for the development of anti-inflammatory drugs to treat acute and chronic inflammatory diseases.
基金Supported by the National Natural Science Foundation of China(No.40724053)
文摘Flavonoids exhibit a wide range of biological activities including anti-inflammatory activity, while some 1,3-benzoxazine derivatives show anti-inflammatory activity. In order to explore the novel anti-inflammatory agents, based on the principles of bioisosterism and hybridization, ten novel ehromeno[8,7-e][1,3]oxazin-4-ones were syn- thesized and characterized with IR, ^1H NMR, MS and elemental analyses. The anti-inflammatory activities of the target compounds were evaluated via the croton oil-induced ear oedema test in Swiss mice. According to screened resuits, some target compounds show potent anti-inflammatory activity.
