• Bulletin of the Korean Chemical Society
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• v.33 no.8
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• pp.2759-2761
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• 2012

• Journal of Physiology & Pathology in Korean Medicine
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• v.23 no.3
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• pp.599-607
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• 2009

Prunellae Spica is the spike or whole plant of Prunella vulgaris Linne, which has been used for clearing heat from the liver, brightening the eyes and treating headache in traditional oriental medicines. This study was conducted to evaluate the inhibitory effects of the aqueous extract of Prunellae Spica (PSE; PS extract) on the production of NO and PGE2 in LPS-activated Raw 264.7 cells. Cell viability was determined by MTT assay, and all three doses of PS extract (0.03, 0.1 and 0.3 mg/ml) had no significant cytotoxicity during the entire experimental period. The cells were treated with 1 ${\mu}g/ml$ of LPS 1 h before adding PS extract, and increased NO and PGE2 production were detected in LPS-activated cells compared to control. However, these increases were dose-dependently attenuated by treatment with PS extract. The inhibition of NO by PS extract was due to the suppression of iNOS expression via inhibition of $NF{\kappa}B$ nuclear translocation and proteolytic degradation of $I{\kappa}B{\alpha}$. The decreased level of PGE2 was derived from inhibition of COX-2 activity, but expression of COX-2 protein was not affected by PS extract. Moreover, PS extract reduced the elevated production of IL-${\beta}$ and IL-6 by LPS. These results demonstrate that PS extract has inhibitory effects on the production of NO and PGE2 as a consequence of the reduction of proinflammatory cytokines, especially IL-${\beta}$ and IL-6 in LPS-activated Raw 264.7 cells.

• Biomolecules & Therapeutics
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• v.28 no.1
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• pp.104-109
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• 2020

Probenecid is a representative drug used in the treatment of gout. A recent study showed that probenecid effectively inhibits oxidative stress in neural cells. In the present study, we investigated whether probenecid can affect osteoclast formation through the inhibition of reactive oxygen species (ROS) formation in RAW264.7 cells. Lipopolysaccharide (LPS)-induced ROS levels were dose-dependently reduced by probenecid. Fluorescence microscopy analysis clearly showed that probenecid inhibits the generation of ROS. Western blot analysis indicated that probenecid affects two downstream signaling molecules of ROS, cyclooxygenase 2 (COX-2) and c-Jun N-terminal kinase (JNK). These results indicate that probenecid inhibits ROS generation and exerts antiosteoclastogenic activity by inhibiting the COX-2 and JNK pathways. These results suggest that probenecid could potentially be used as a therapeutic agent to prevent bone resorption.

• Korean Journal of Food Science and Technology
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• v.39 no.3
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• pp.348-352
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• 2007

Inflammation is a complex process resulting from a variety of mechanisms. Combined inhibition of the activities of enzymes involved in the process may therefore be considered more important in anti-inflammatory property of plant extracts than any single contribution. In this study, the inhibitory effects of the ethanol extracts of thirty plant foods on the activities of secretory phospholipase $A_{2}$ ($sPLA_{2}$), cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2), and 12-lipoxygenase (12-LOX) were examined. Several legumes, mungbean sprout and some leaf vegetables inhibited the activity of $sPLA_2$, upstream enzyme of inflammation pathway. Only soybean sprout and mungbean sprout significantly inhibited 12-LOX activity. Although most of extracts inhibited the activities of both COX-1 and COX-2, water dropwort and amaranth showed selectivity for the inhibition of COX-2 over COX-1. Especially, mungbean showed anti-inflammatory property at both upstream and downstream of inflammation pathway with relatively low $IC_{50}$ values for $sPLA_{2}$ and COX-2 enzymes. Mungbean sprout exhibited inhibitory effects on all enzymes related to early and late inflammation and soybean sprout suppressed 12-LOX and COX-2 simultaneously, although the activities of these plants were showed at relatively high concentration. Therefore, mungbean, mungbean sprout, and soybean sprout appear to exhibit anti-inflammatory effects by combined inhibition of inflammatory enzymes.

• Journal of Life Science
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• v.30 no.4
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• pp.352-358
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• 2020

Red yeast rice has been extensively used as a food and traditional medicine for thousands of years in Korea. Monascus produces many secondary metabolites during its growth, including pigments, monacolins, and γ-aminobutyric acid. Some metabolites, specifically monacolin K, γ-aminobutyric acid, and dimerumic acid, have been reported to lower cholesterol and blood pressure because of certain antioxidant effects. This study investigated the total phenolic content of ethanol extract from red yeast rice fermented with Monascus sp. BHN-MK and its anti-inflammatory effect on LPS-stimulated RAW 264.7 macrophage cells. To assess its anti-inflammatory effect, the inhibitory activity of the ethanol extract on LPS-induced NO production and expression levels of iNOS and COX-2 proteins in macrophage cells were measured. Its total polyphenol content was higher than that of ordinary non-fermented rice. Its NO production inhibition activity was comparable to that of the negative control group treated with LPS at a concentration of 400 ㎍/ml. Western blot revealed a significant decrease in the inhibition of iNOS and COX-2 protein expression at concentrations of 400 and 800 ㎍/ml, respectively. Red yeast rice ethanol extracts exerted the strongest anti-inflammatory effects. The results indicate that red yeast rice could be used as a functional cosmetic and anti-inflammatory material.

• Microbiology and Biotechnology Letters
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• v.45 no.2
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• pp.178-183
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• 2017

This study examined a new functional cosmetic material possessing application possibility of Sambucus sieboldiana var. pendula (Nakai) (SS) extract. For this, we analyzed the toxic effect of the SS extract on macrophages (RAW 264.7 cells) by performing MTT assay. Results of the MTT assay showed ${\geq}100%$ cell viability after treatment with $500{\mu}g/ml$ SS extract. To determine the anti-inflammatory activity of the SS extract, we examined its inhibitory effect on lipopolysaccharide (LPS)-induced NO production in RAW 264.7 cells by performing Griess assay. Result of the Griess assay showed that the SS extract inhibited LPS-induced NO production in a concentration-dependent manner. Next, we examined the effect of the SS extract on the production of proinflammatory factors inducible NOS (iNOS) and cyclooxygenase-2 (COX-2) in LPS-stimulated RAW 264.7 cells. First, we determined the inhibitory effect of 50, 100, and $500{\mu}g/ml$ SS extract on iNOS and COX-2 protein expression by performing western blot analysis, with ${\beta}$-actin as a positive control. Results of western blotting showed that treatment with $500{\mu}g/ml$ SS extract decreased iNOS and COX-2 protein expression by 31.2% and 54.7%, respectively. Next, we determined the inhibitory effect of 50, 100, and $500{\mu}g/ml$ SS extract on iNOS and COX-2 mRNA expression by performing reverse transcription-polymerase chain reaction (PCR), with GAPDH as a positive control. Results of reverse transcription-PCR showed that treatment with $500{\mu}g/ml$ SS extract decreased the mRNA expression of iNOS and COX-2 by 72.2% and 89%, respectively. These results suggest that the SS extract is a highly valuable natural compound because of its functional components and anti-inflammatory activity.

• Archives of Pharmacal Research
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• v.28 no.2
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• pp.177-179
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• 2005

Nine known diarylheptanoids (1-9) isolated from the barks of Alnus japonica were evaluated for their inhibitory activities on nitric oxide (NO) and prostagrandin $E_2$ (COX-2) production in interferon-${\gamma}$ (INF-${\gamma}$) and lipopolysaccharide (LPS)-activated RAW 264.7 cells in vitro. The NO and COX-2 levels were moderately reduced by the addition of compounds (1-9). Among these compounds, compounds 6 and 8 inhibited NO production in a dose dependent manner with an $IC_{50}$ of 16.7 and $27.2\;{\mu}g/mL$, respectively (positive control, L-NMMA; $22.8\;{\mu}g/mL$), and compounds 6, 7, 8, and 9 reduced the COX-2 level in a dose dependent manner with an $IC_{50}$ of 20.7, 25.7, 25.0, and $27.3\;{\mu}g/mL$, respectively (positive control, indomethacin; $26.2\;{\mu}g/mL$). An analysis of the structural activity relationship among these diarylheptanoids suggests that the presence of a keto-enol group in the heptane moiety or a caffeoyl group in the aromatic ring were important for the efficacy on the inhibitory activities of NO and COX-2 production.

• Korean Journal of Oriental Medicine
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• v.14 no.3
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• pp.57-63
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• 2008

Glehnia littoralis (Umbelliferae) is the medicinal plant used traditionally for treatment of immune-related diseases. Prostaglandins and nitric oxide (NO) have been implicated as important mediators in the processes of inflammation and carcinogenesis. For understanding the mechanisms for pharmacological activities of Glehnia littoralis, we evaluated the inhibitory activity of Glehnia littoralis on lipopolysaccharide (LPS)-induced prostaglandin $E_2$ ($PGE_2$) and NO production in mouse macrophage RAW264.7 cells. The results showed that the extract of Glehnia littoralis inhibited LPS- induced $PGE_2$ production effectively, but not NO. Additional study revealed that the extract of Glehnia littoralis suppressed cyclooxygenase-2 (COX-2) expression in a dose-dependent manner. Present study suggests that Glehnia littoralis may have anti-inflammatory and/or cancer chemopreventive activity through the inhibition of $PGE_2$ production by the suppression of COX-2 activity.

• Archives of Pharmacal Research
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• v.28 no.1
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• pp.28-33
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• 2005

Seven diterpenes, four polyacetylenes, a lipid glycerol, and two sterols were isolated from the methylene chloride fraction of the root of Aralia cordata. Their chemical structures were determined as (-)-pimara-8(14), 15-dien-19-oic acid (2), pimaric acid (3), (-)-kaur-16-en-19-oic acid (4), 17-hydroxy-ent-kaur-15-en-19-oic acid (9), $7{\alpha}$-hydroxy-(-)-pimara-8(14), 15-dien-19-oic acid (10), $16\alpha$, 17 -dihydroxy-(-)-kauran-19-oic acid (11), 16-hydroxy-17-isovaleroyloxy-ent-kauran-19­oic acid (12), falcarindiol (5), dehydrofalcarindiol (6), dehydrofalcarindiol-8-acetate (7), falcarin­diol-8-acetate (8), alpha-mono palmitin (13), stigmasterol (1), and daucosterol (14) by the spectral evidences. These compounds were tested with COX-1 and COX-2 inhibition assays. This study found that compounds 2, 4, 5, 6, 7, 8, and 10 inhibited COX-1 dependent conversion of the exogenous arachidonic acid to $PGE_2$ in a dose-dependent manner with $IC_{50}$ values of $134.2{\mu}M$, $121.6{\mu}M$, $170{\mu}M$, $50.4{\mu}M$, $11.7{\mu}M$, $99.6{\mu}M$, and $69.6{\mu}M$, respectively. But, most of these compounds weakly inhibited COX-2 dependent $PGE_2$ generation. Among them, only compound 4 showed relatively significant inhibitory activity $(IC_{50}\;:\;127.6{\mu}M)$.

• The Korean Journal of Physiology and Pharmacology
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• v.10 no.1
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• pp.45-50
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• 2006

Melittin-induced pain model has been known to be very useful for the study of pain mechanism. Melittin-induced nociceptive responses are reported to be modulated by the changes in the activity of excitatory amino acid receptor, calcium channel, spinal serotonin receptor and extracellular signaling-regulated kinase. The present study was undertaken to investigate the role of cyclooxygenase (COX) in the melittin-induced nociception. Changes in mechanical threshold, flinchings and paw thickness were measured before and after intraplantar injection of melittin in the rat hind paw. Also studied were the effects of intraperitonealy administered diclofenac (25 mg & 50 mg/kg), piroxicam (10 mg & 20 mg/kg) and meloxicam (10 mg & 20 mg/kg) on the melittin-induced nociceptions. Intraplantar injection of melittin caused marked reduction of mechanical threshold that was dose-dependently attenuated by non-selective COX inhibitor (diclofenac) and selective COX-1 inhibitor (piroxicam), but not by COX-2 inhibitor (meloxicam). Melittin-induced flinchings were strongly suppressed by non-selective COX and COX-1 inhibitor, but not by COX-2 inhibitor. None of the COX inhibitors had inhibitory effects on melittin-induced increase of paw thickness (edema). These experimental findings suggest that COX-1 plays an important role in the melittin-induced nociceptive responses.