Anti‐inflammatory Potential of Quercetin‐3‐O‐β‐D‐(“2”‐galloyl)‐glucopyranoside and Quercetin Isolated from Diospyros kaki calyx via Suppression of MAP Signaling Molecules in LPS‐induced RAW 264.7 Macrophages

Diospyros kaki (DK) contains an abundance of flavonoids and has been used in folk medicine in Korea for centuries. Here, we report for the first time the anti‐inflammatory activities of Quercetin (QCT) and Quercetin 3‐O‐β‐(“2”‐galloyl)‐glucopyranoside (Q32G) isolated from DK. We have determine the no cytotoxicity of Q32G and QCT against RAW 264.7 cells up to concentration of 50 μM. QCT and Q32G demonstrated potent anti‐inflammatory activities by reducing expression of nitric oxide (NO), tumor necrosis factor (TNF)‐α, interleukin (IL)‐1β, IL‐6 inducible NO synthase (iNOS), cyclooxygenase (COX)‐2, and mitogen‐activated protein kinase (MAPKs) in mouse RAW 264.7 macrophages activated with lipopolysaccharide (LPS). Both QCT or Q32G could decrease cellular protein levels of COX‐2 and iNOS as well as secreted protein levels of NO, PGE₂, and cytokines (TNF‐α, IL‐1β, and IL‐6) in culture medium of LPS‐stimulated RAW 264.7 macrophages. Immunoblot analysis showed that QCT and Q32G suppressed LPS‐induced MAP kinase pathway proteins p‐p38, ERK, and JNK. This study revealed that QCT and Q32G have anti‐inflammatory potential, however Q32G possess comparable activity as that of QCT and could be use as adjuvant to treat inflammatory diseases.     

Anti‐inflammatory and cytotoxic effects of ginseng extract bioconverted by Leuconostoc mesenteroides KCCM 12010P isolated from kimchi

A bioconversion technique using microorganisms has been applied to ginseng to increase content of bioactive ginsenoside and biofunctionality such as anticancer, anti‐obesity and antioxidant activities. The objective of this study was to screen lactic acid bacteria for bioconversion of ginsenosides and to evaluate anti‐inflammatory and cytotoxic effects of bioconverted ginseng extract. Strains isolated from kimchi were screened for their β‐glucosidase activities using esculin agar. Selected strain was identified based on 16S rRNA sequencing and carbohydrate fermentation. During ginseng fermentation, viable cell number and pH were determined. Bioconverted ginsenosides were analysed by HPLC. Anti‐inflammatory effects were evaluated using RAW 264.7 cells, and cytotoxic effects were determined by MTT assay. Among 166 isolates screened, Leuconostoc mesenteroides was selected for ginseng bioconversion, as it showed a higher β‐glucosidase activity and viable cell number than any of the other tested strains. After fermentation for 2 days, viable cell number was 8.8 log CFU mL^?1 and final pH was 4.8. Ginsenoside Rb₂ was bioconverted into ginsenoside Rg₃ (Rb₂ → Rd → Rg₃) by L. mesenteroides. The nitric oxide contents of 2‐day‐fermented extract decreased by as much as 25%, compared to a non‐fermented extract. The cell viabilities of HepG2, HT‐29, HeLa and LoVo treated with fermented ginseng extract also decreased by 49.7%, 20.2%, 21.0% and 8.7%, respectively, compared to those of control cells treated with non‐fermented extract. Ginseng extract bioconverted by L. mesenteroides showed anti‐inflammatory and anticancer effects. Therefore, bioconverted ginseng extract might have applications in the pharmaceutical and/or functional food industry.     

Polygonum viviparum L. inhibits the lipopolysaccharide‐induced inflammatory response in RAW264.7 macrophages through haem oxygenase‐1 induction and activation of the Nrf2 pathway

BACKGROUND: Polygonum viviparum L. (PV) is a member of the family Polygonaceae and is widely distributed in high‐elevation areas. It is used as a folk remedy to treat inflammation‐related diseases. This study was focused on the anti‐inflammatory response of PV against lipopolysaccharide (LPS)‐induced inflammation in RAW264.7 macrophages. RESULTS: Treatment with PV did not cause cytotoxicity at 0–50 µg mL^?1 in RAW264.7 macrophages, and the IC₅₀ value was 270 µg mL^?1. PV inhibited LPS‐stimulated nitric oxide (NO), prostaglandin (PG)E₂, interleukin (IL)‐1β and tumour necrosis factor (TNF)‐α release and inducible NO synthase (iNOS) and cyclooxygenase (COX)‐2 protein expression. In addition, PV suppressed the LPS‐induced p65 expression of nuclear factor (NF)‐κB, which is associated with the inhibition of IκB‐α degradation. These results suggest that, among mechanisms of the anti‐inflammatory response, PV inhibits the production of NO and these cytokines by down‐regulating iNOS and COX‐2 gene expression. Furthermore, PV can induce haem oxygenase (HO)‐1 protein expression through nuclear factor E2‐related factor 2 (Nrf2) activation. A specific inhibitor of HO‐1, zinc(II) protoporphyrin IX, inhibited the suppression of iNOS and COX‐2 expression by PV. CONCLUSION: These results suggest that PV possesses anti‐inflammatory actions in macrophages and works through a novel mechanism involving Nrf2 actions and HO‐1. Thus PV could be considered for application as a potential therapeutic approach for inflammation‐associated disorders. © 2012 Society of Chemical Industry     

Anti‐inflammatory activity of rosemary extracts obtained by supercritical carbon dioxide enriched in carnosic acid and carnosol

The in vitro anti‐inflammatory activity of supercritical rosemary (Rosmarinus officinalis L.) extracts (rosemary A and B) is been reported in this study. To achieve that, THP‐1 macrophages were activated using lipopolysaccharide or human ox‐LDL and secretion and gene expression of TNF‐α, IL‐1β, IL‐6 and IL‐10 were evaluated, as well as COX‐2 gene expression. Results indicated that both rosemary extracts (A & B) exhibit high anti‐inflammatory activity although at a higher extent in case of rosemary B extract (5 μg mL^?1), representing a higher quantity of carnosic acid and carnosol than rosemary A. When comparing the activity of the extract to the standard itself, the anti‐inflammatory activity of standards of carnosic acid and carnosol was not as intense as that obtained with rosemary B. These data indicated that although carnosic acid content in the extracts is considered as the main anti‐inflammatory compound, a synergistic interaction with other compounds may play a significant role in enhancing its activity. Results provided the grounds for possible increase in the application of supercritical rosemary extracts in food formulations for mitigation or prevention of inflammatory diseases.     

Characterization,Anti‐Inflammatory and Antiproliferative Activities of Natural and Sulfonated Exo‐Polysaccharides from Streptococcus thermophilus ASCC 1275

Exo‐polysaccharides (EPS) isolated from Streptococcus thermophilus ASCC 1275 were sulfated (31%). High‐performance liquid chromatography identified that EPS was composed of mannose (30.19%), galactose (20.10%), glucose (18.05%), glucosamine (16.04%), galactosamine (9.06%), glucuronic acid (3.55%), and ribose (3.01%). Pro‐/anti‐inflammatory cytokine secretion ratios (IL‐1β/IL‐10, IL‐6/IL‐10, and TNF‐α/IL‐10) of lipopolysaccharide stimulated RAW 264.7 macrophages were significantly decreased by EPS and S.EPS treatments in a dose dependent manner. Furthermore, anti‐inflammatory activities of S.EPS improved 49.3% and 24.0% than those of EPS before or after LPS treatment. The reactive oxygen species were inhibited by EPS and S.EPS by 49.6% and 55.1% at 50 μg/mL, respectively. Inhibition activities of S.EPS on nitric oxide production were 12.9% and 55.4% higher than those of EPS at 10 and 50 μg/mL. Additionally, S.EPS exhibited stronger antiproliferative activity on Caco‐2 and HepG2 cells. Our results indicated that anti‐inflammatory and antiproliferative activities of EPS were significantly (P < 0.01) improved by sulfonation.     

J. Cosmet. Sci., 59, 419–430 (September/October 2008)Anti-inflammatory activity of Crinum asiaticum Linne var. japonicum extract and its application as a cosmeceutical ingredient

Synopsis Crinum asiaticum Linne var. japonicum has long been used as a rheumatic remedy, as an anti‐pyretic and as an anti‐ulcer treatment, and for the alleviation of local pain and fever in Korea and Malaysia. In order to investigate the possibility of Crinum asiaticum Linne var. japonicum extract as a cosmetic ingredient, we measured its anti‐inflammatory effect by its inhibition of iNOS (inducible nitric oxide synthase) and the release of PGE2, IL‐6, and IL‐8. We also measured its anti‐allergic effect by its inhibition of beta‐hexosamidase release. An HPLC experiment after extraction with 95% EtOH at pH 3.5 showed that Crinum asiaticum Linne var. japonicum was mainly composed of lycorine (up to 1%), a well‐known immunosuppressor. The content of lycorine varied, depending on the type of plant tissue analysed and the extraction method. In an anti‐inflammatory assay for inhibition of nitric oxide formation on lipopolysaccharide (LPS)‐activated mouse macrophage RAW 264.7 cells, the ethanol extract of Crinum asiaticum showed an inhibitory activity of NO production in a dose‐dependent manner (IC50 = 58.5 μg ml^‐1). Additional study by RT‐PCR demonstrated that the extract of Crinum asiaticum significantly suppressed the expression of the iNOS gene. Moreover, the extract of Crinum asiaticum did not show any cytotoxicity, but did show a cell proliferation effect against LPS (a 10–60% increase in cell viability). In an assay to determine inhibition of the H2O2‐activated release of PGE2, IL‐6, and IL‐8 in human normal fibroblast cell lines, the release of PGE2 and IL‐6 was almost completely inhibited above concentrations of 0.05% and 1%, respectively. Moreover, the release of IL‐8 was completely inhibited over the entire range of concentration (> 0.0025%). In order to investigate the skin‐sensitizing potentials of the extract of Crinum asiaticum, a human clinical test was performed after repeated epicutaneous 48‐h applicaticons under an occlusive patch (RIPT). The repeated and single cutaneous applications of Crinum asiaticum Linne var. japonicum extract under the occlusive patch did not provoke any cumulative irritation and sensitization reactions. The result showed that the extract of Crinum asiaticum Linne var. japonicum has a sufficient anti‐inflammatory effect. Therefore, Crinum asiaticum Linne var. japonicum extract may be useful for development as an ingredient in cosmetic products.     

Enhanced Anti‐Inflammatory Activities by the Combination of Luteolin and Tangeretin

Dietary components in combination may act synergistically and produce enhanced biological activities. Herein, we investigated the anti‐inflammatory effects of 2 flavonoids, that is luteolin (LUT) and tangeretin (TAN) in combination. Lipopolysaccharide (LPS)‐stimulated RAW 264.7 macrophages were treated with noncytotoxic concentrations of LUT, TAN, and their combinations. The results showed that LUT/TAN in combination produced synergistic inhibitory effects on LPS‐stimulated production of nitric oxide (NO). ELISA results demonstrated that LUT/TAN in combination caused stronger suppression on the LPS‐induced overexpression of proinflammatory mediators, such as prostaglandin E₂ (PGE₂), interleukin (IL)‐1β, and IL‐6 than LUT or TAN alone. Immunoblotting and Real‐Time PCR analyses showed that LUT/TAN combination significantly decreased LPS‐induced protein and mRNA expression of inducible nitric oxide synthase and cyclooxygenase‐2. These inhibitory effects of the combination treatment were stronger than those produced by LUT or TAN alone. Overall, our results demonstrated for the first time that combination of LUT and TAN produced synergistic anti‐inflammatory effects in LPS‐stimulated RAW 264.7 macrophages.     

Effect of the main ingredients of Rhizoma gastrodiae on mycelial biomass and exopolysaccharide productions by submerged culture of Grifola frondosa

Various concentrations of the main ingredients of Rhizoma gastrodiae including gastrodin (GA) and p‐hydroxybenzyl alcohol (HA) as well as p‐hydroxylbenzaldehyde (HBA) were separately added into the cultural medium of Grifola frondosa in submerged culture. The results showed that the additive concentration of gastrodin from 0.10 to 0.35 g L^?1, p‐hydroxybenzyl alcohol from 0.05 to 0.30 g L^?1 and p‐hydroxylbenzaldehyde from 0.05 to 0.30 g L^?1 can significantly promote the EPS production by submerged culture of G. frondosa (P < 0.05). Among them, the addition of p‐hydroxylbenzaldehyde at 0.15 g L^?1 exhibited the best results, and the EPS productions reached 2.2511 ± 0.0378 g L^?1, with an increase of 45.03% compared with the control (without additives). Furthermore, all of the additives had an effective stimulatory effect on mycelial biomass. In addition, there is an important and novel breakthrough that p‐hydroxylbenzaldehyde was more effective than R. gastrodiae extract on increasing the EPS productions.     

Phase II enzyme induction and anti‐inflammatory effects of crude extracts and secondary fractions obtained from bran from five black glutinous rice cultivars

Methanolic extracts of bran from black glutinous rice cultivars were screened for potential health benefits using cellular bioassays for quinone reductase (QR) induction in murine hepatoma cells and inhibition of NO production in lipopolysaccharide (LPS)‐activated RAW 264.7 macrophages. Fractionation of the crude extract by semi‐preparative HPLC afforded respective fractions enriched in phenolic acids, anthocyanins and proanthocyanidins. The relative potency of QR induction was phenolic acids > proanthocyanidins > anthocyanins, and the activity of the crude extract was conserved among the aggregate of these fractions. In contrast, all three fractions were more potent than the crude extract in terms of anti‐inflammatory effect. This suggests synergism effects among anti‐inflammatory agents through partial purification. Inhibition of macrophage NO production by binary mixtures of gallic acid or caffeic acid with the anthocyanin‐rich fraction indicated potential synergism. These results warrant further efforts to identify the active agents and substantiate synergistic interactions through isobologram analysis.     

Phosphorylation of peptidoglycan from Lactobacillus acidophilus and its immunoregulatory function

Peptidoglycan (PG) is available from a wide variety of lactic acid bacteria (LAB) and is the main structure of cell wall components. Phosphorylated modification would bring new properties such as the potential antioxidant activities and antiviral capability to an organic molecule. In the present work, small molecular fragments of PG (derived from Lactobacillus acidophilus) hydrolysed by mutanolysin were phosphorylated under optimal conditions. P‐PG had a monomer molecular structure of GlcNAC[PO₃]–MurNAC–Ala–Glu–Lys–Ala, with a molecular mass of 884 Da and a phosphorus content of 8.9%. P‐PG displayed some immunoregulatory activity in lipopolysaccharides (LPS) stimulated RAW 264.7 macrophages. Compared with the LPS‐stimulated group, the addition of P‐PG inhibited the secretion of GM‐CSF, TNF‐α and IL‐1 in a dose‐dependent manner. The effect of 50 μg mL^?1 of P‐PG was more significant than 50 μg mL^?1 of PG. Lower fluorescence of lysosomes was observed in P‐PG‐treated RAW 264.7 cells may also reveal some immune defence function in the LPS‐induced macrophages.     

Antioxidant,immunomodulatory and antiproliferative effects of gelatin hydrolysates from seabass (Lates calcarifer) skins

This study investigated the antioxidant, immunomodulatory and antiproliferative potentials of gelatin hydrolysates from seabass skins in cell model systems. Gelatin hydrolysates were extracted from seabass skins using different processes and enzyme concentrations. The ability of the hydrolysates to protect against H₂O₂‐induced DNA damage was assessed on U937 cells using the Comet assay, and one of the samples showed DNA protective effects. All samples showed immunomodulatory potential by significantly (P < 0.05) reducing interleukin‐6 (IL‐6) and IL‐1β production in lipopolysaccharide (LPS)‐stimulated RAW 264.7 macrophage cells. Antiproliferative activities of seabass skin hydrolysates were measured using human colon cancer (Caco‐2) and liver cancer (HepG2) cell lines as the model cell cultures. The inhibition of cell proliferation of Caco‐2 and HepG2 cancer cells occurred in a dose‐dependent manner at concentrations of 1–25 mg mL^?1. Therefore, seabass skin hydrolysates prepared using an appropriate process could serve as a potential functional food ingredient with various health benefits.     

Chemical composition,antioxidant activity and anti‐lipase activity of Origanum vulgare and Lippia turbinata essential oils

This study reported the chemical composition, phenolic content, antioxidant and anti‐lipase activity of oregano and Lippia essential oils. The major compounds found in oregano essential oil were γ‐terpinene (32.10%), α‐terpinene (15.10%), p‐cymene (8.00%) and thymol (8.00%). In Lippia essential oil, α‐limonene (76.80%) and 1,8‐cineole (4.95%) represented the major compounds. Oregano essential oil had higher phenolic content (12.47 mg gallic acid mL^?1) and DPPH scavenging activity (IC₅₀ 0.357 μg mL^?1) than Lippia essential oil (7.94 mg gallic acid mL^?1 and IC₅₀ 0.400 μg mL^?1, respectively). Both essential oils had similar antioxidant indexes (about 1.2) determined by Rancimat. Moreover, oregano essential oil had also higher anti‐lipase activity (IC₅₀ 5.09 and 7.26 μg mL^?1). Higher phenolic content in the essential oils was related with higher scavenging and anti‐lipase activities. Oregano and Lippia essential oils could be used as natural antioxidants on food products.     

Protective effect of dried safflower petal aqueous extract and its main constituent,carthamus yellow,against lipopolysaccharide‐induced inflammation in RAW264.7 macrophages

BACKGROUND: Safflower, whose botanic name is Carthamus tinctorius L., is a member of the family Compositae or Asteraceae. Carthamus yellow (CY) is the main constituent of safflower and is composed of safflomin A and safflomin B. Dried safflower petals are used in folk medicine and have been shown to invigorate blood circulation, break up blood stasis, and promote menstruation. In addition, dried safflower petals contain yellow dyes that are used to color food and cosmetics. In this study, we investigated the effects of dried safflower petals aqueous extracts (SFA) and CY on lipopolysaccharide (LPS)‐induced inflammation using RAW264.7 macrophages. RESULTS: Our data showed that treatment with SFA (1–1000 µg mL^?1) and CY (1–2000 µg mL^?1) does not cause cytotoxicity in cells. SFA and CY inhibited LPS‐stimulated nitric oxide (NO), prostaglandin E₂ (PGE₂), and interleukin 1β (IL‐1β) release, through attenuation of inducible nitric oxide synthase (iNOS) and cyclooxygenase‐2 (COX‐2) protein expression. Further, SFA and CY suppressed the LPS‐induced phosphorylation of nuclear factor‐κB, which was associated with the inhibition of IκB‐α degradation. CONCLUSION: These results suggest that SFA and CY provide an anti‐inflammatory response through inhibiting the production of NO and PGE₂ by the downregulation of iNOS and COX‐2 gene expression. Thus safflower petals have the potential to provide a therapeutic approach to inflammation‐associated disorders. Copyright © 2010 Society of Chemical Industry     

In vitro DNA damage protection and anti‐inflammatory effects of Tartary buckwheats (Fagopyrum tataricum L. Gaertn) fermented by filamentous fungi

The present work was designed to investigate the phenolic profiles, DNA damage protection and anti‐inflammatory effects of Tartary buckwheat fermented by Rhizopus oryzae 40469, Rhizopus oryzae 40503 and Rhizopus oligosporus 3152. Six phenolic compounds were characterised and quantified. Regardless of fermentation, rutin was the dominant phenolic substance in Tartary buckwheat. Fermentation significantly enhanced total phenolic and flavonoid contents, as well as DNA scission protection. Rhizopus oryzae 40469‐fermented sample had the highest content of phenolics, while R. oligosporus 3152‐fermented sample had the strongest inhibitory effect on DNA scission. Tartary buckwheat, regardless of fermentation, inhibited nitric oxide (NO) production and inducible nitric oxide synthase (iNOS) mRNA levels in LPS‐induced RAW 264.7 cells. Moreover, the sample fermented with R. oryzae 40503 had the strongest inhibitory activity. Those results indicated that fermented Tartary buckwheat has potential applications as a novel nutraceutical or functional food for preventing DNA damage‐induced disease and inflammation.     

Effects of physicochemical factors and in vitro gastrointestinal digestion on antioxidant activity of R‐phycoerythrin from red algae Bangia fusco‐purpurea

R‐phycoerythrin (R‐PE) was purified from the red algae Bangia fusco‐purpurea after 35–50% ammonium sulphate fractionation followed by ion‐exchange column chromatography on DEAE‐Sepharose, resulting in a purity (A₅₆₅/A₂₈₀) ratio of 5.1. The circular dichroism spectroscopy results suggested that the structure of R‐PE is predominately helical. The antioxidant activity of R‐PE was studied and revealed changes in conformation and antioxidant activity at different temperatures and pH values. After in vitro‐simulated gastrointestinal (GI) digestion of R‐PE, the scavenging activity of ABTS radical (EC₅₀, 769.9 μg mL^?1), DPPH radical (EC₅₀, 421.9 μg mL^?1), hydroxyl radical (EC₅₀, 32.4 μg mL^?1) and reducing power (A₇₀₀ = 0.5, 625.8 μg mL^?1) were measured. Gel filtration chromatography analysis showed that the molecular weight distribution of the final GI digest that still contained high antioxidant activity was <3 kDa. Our present results indicate that digestion‐resistant antioxidant peptides of R‐PE may be obtained by in vitro GI proteinases degradation.     

Phenethyl isothiocyanate suppresses nitric oxide production via inhibition of phosphoinositide 3‐kinase/Akt‐induced IFN‐γ secretion in LPS‐activated peritoneal macrophages

Phenethyl isothiocyanate (PEITC), a constituent of many cruciferous vegetables, is well known to have versatile physiological activities, including chemopreventive effects. On the other hand, its anti‐inflammatory effects are poorly reported. Nitric oxide (NO) is associated with a wide variety of inflammatory diseases. In this study, we investigated the effects of PEITC on NO production in LPS‐activated peritoneal macrophages from ICR mice. The signaling pathway of LPS‐induced NO production was examined using neutralizing antibodies [anti‐interferon (IFN)‐γ and anti‐interleukin (IL‐12)] and specific protein kinase inhibitors, as well as others. The activity of PEITC toward NOx production was assessed in mice that received LPS via intraperitoneal administration. The neutralizing antibody of anti‐IFN‐γ, but not anti‐IL‐12, suppressed LPS‐induced NO production by 90%. LY294002, a specific inhibitor of phosphoinositide‐3‐kinase, suppressed Akt and IFN‐γ mRNA expression up‐regulated by LPS, whereas PEITC exhibited a similar inhibition profile. Furthermore, oral administration of PEITC significantly suppressed the serum concentration of NOx in ICR mice. Our results suggest that PEITC suppresses LPS‐induced NO production via inhibition of Akt activation and the resultant decrease in expression of IFN‐γ. This is one of the first reports to demonstrate a marked anti‐inflammatory effect of PEITC following its oral administration.     

In vitro antioxidant and in vivo xanthine oxidase inhibitory activities of Pandanus amaryllifolius in potassium oxonate‐induced hyperuricemic rats

Xanthine oxidase (XO) plays an important role in the regulation of uric acid and prevents it from being overproduced as in hyperuricemia disease. The combined effects of antioxidant and xanthine oxidase inhibitor would become a promising approach for hyperuricemia treatment. In this research, the antioxidant and xanthine oxidase inhibitory activities of Pandanus amaryllifolius leaf were evaluated. The leaf water extract (PA‐W) showed highest total phenols, and petroleum ether extract (PA‐PE) showed highest total flavonoids contents. The antioxidant activity of DPPH, metal chelating and hydrogen peroxide was highest in PA‐W extract. The treatment of PA‐W extract at 1000 mg kg^?1 body weight in potassium oxonate‐induced hyperuricemic rats showed significant (P < 0.001) decrease in serum uric acid level by 85% and XO activity by 64%, respectively, as compared to the hyperuricemic rats. In conclusion, the P. amaryllifolius possess the dual effect of antioxidant and XO inhibition as potential therapeutic agents in the hyperuricemia treatment.     

Suppressive effects of extracts from the aerial part of Coriandrum sativum L. on LPS‐induced inflammatory responses in murine RAW 264.7 macrophages

BACKGROUND: Coriandrum sativum is used not only as a spice to aid flavour and taste values in food, but also as a folk medicine in many countries. Since little is known about the anti‐inflammatory ability of the aerial parts (stem and leaf) of C. sativum, the present study investigated the effect of aerial parts of C. sativum on lipopolysaccharide (LPS)‐stimulated RAW 264.7 macrophages. We further explored the molecular mechanism underlying these pharmacological properties of C. sativum. RESULTS: Ethanolic extracts from both stem and leaf of C. sativum (CSEE) significantly decreased LPS‐induced nitric oxide and prostaglandin E₂ production as well as inducible nitric oxide synthase, cyclooxygenase‐2, and pro‐interleukin‐1β expression. Moreover, LPS‐induced IκB‐α phosphorylation and nuclear p65 protein expression as well as nuclear factor‐κB (NF‐κB) nuclear protein–DNA binding affinity and reporter gene activity were dramatically inhibited by aerial parts of CSEE. Exogenous addition of CSEE stem and leaf significantly reduced LPS‐induced expression of phosphorylated mitogen‐activated protein kinases (MAPKs). CONCLUSION: Our data demonstrated that aerial parts of CSEE have a strong anti‐inflammatory property which inhibits pro‐inflammatory mediator expression by suppressing NF‐κB activation and MAPK signal transduction pathway in LPS‐induced macrophages. Copyright © 2010 Society of Chemical Industry