• BMB Reports
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• v.51 no.6
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• pp.302-307
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• 2018

Pinosylvin is known to have anti-inflammatory activity in endothelial cells. In this study, we found that pinosylvin had a pro-apoptotic activity in lipopolysaccharide (LPS)-preconditioned leukocytes. This finding suggests that pinosylvin has an effect on the resolution of inflammation. To understand the detailed mechanism, we examined if pinosylvin enhances cyclooxygenase (COX) or lipoxygenase (LOX) activity in THP-1 and U937 cells. LOX activity was found to be markedly increased by pinosylvin, whereas COX activity was not altered. Furthermore, we found that pinosylvin enhanced both levels of ALOX 15 mRNA and protein, implying that LOX activity, elevated by pinosylvin, is attributed to upregulation of ALOX 15 expression. From this cell signaling study, pinosylvin appeared to promote phosphorylations of ERK and JNK. ERK or JNK inhibitors were found to attenuate ALOX 15 expression and LPS-induced apoptosis promoted by pinosylvin. In conclusion, pinosylvin enhances the apoptosis of LPS-preconditioned leukocytes by up-regulating ALOX 15 expression through ERK and JNK. These findings suggest that pinosylvin may induce the resolution of inflammation.

• 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 $(IC_{50}\;:\;127.6{\mu}M)$.

• Journal of Acupuncture Research
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• v.29 no.1
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• pp.127-137
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• 2012

Objectives : The purpose of this study is to investigate the effect of $Clematidis$ radix herbal-acupuncture solution, on collagen, adjuvant, lipopolysaccharide and phospholipase A2 induced rheumatoid arthritis in mice. Methods : Arthritis index was measured for mouse that was injected subcutaneously in solution mixed chicken type II collagen with Freund's complete adjuvant. We injected Freund's complete adjuvant into right posterior part of the sole of a ICR mouse foot, which was measured by plethysmometer. The solution mixed $CRHS$ with Tris-HCI, $CaCl_2$, substrate, enzyme was done a chemical action for thirty minutes, and then inhibitory activity of PLA2 enzyme was expressed with inhibition percentage by utilizing isolated arachidonic acid. COX-2 was induced by adding LPS to RAW 264.7 cell, and COX-2 activity was measured by western blot analysis and $PGE_2$ Biotrak kit. Results : $CRHS$ also inhibited Freund's complete adjuvant induced chronic rheumatoid arthritis in mice. $CRHS$ showed significant inhibition of type I and type II $PLA_2$ activities in a dose dependent manner. Furthermore, $PGE_2$ production was decreased with $CRHS$ and lipopolysaccharide-induced COX-2 protein expression was significantly inhibited by $CRHS$. Conclusions : These results suggest that $CRHS$ has an therapeutic effect on drug induced-rheumatoic arthritis by inhibiting $PLA_2$ and COX-2 activities.

• Biomolecules & Therapeutics
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• v.17 no.1
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• pp.86-91
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• 2009

In our ongoing search for biological components from the Korea endemic plants, the MeOH extract of Ailanthus altissima leaves (Simaroubaceae) showed cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) dual inhibitory activity by assessing their effects on the production of prostaglandin $D_2$ ($PGD_2$) and leukotriene $C_4$ ($LTC_4$) in mouse bone marrow-derived mast cells (BMMCs). In further study, eight compounds, squalene (1), ${\beta}$-sitosterol (2), scopoletin (3), quercetin (4), luteolin (5), astragalin (6), scopolin (7), and daucosterol (8) were isolated, the chemical structures were elucidated on the basis of physicochemical and spectroscopic data and by comparison with those of published literatures. Among the compounds, 2, 4, and 5 strongly inhibited both the COX-2-dependent PGD2 generation with $IC_{50}$ values of 2.6, 7.3 and 2.5 ${\mu}M$, respectively and the generation of $LTC_4$ in the 5-LOX dependent phase with $IC_{50}$ values of 2.0, 5.1 and 1.8 ${\mu}M$, respectively, which suggest that the anti-inflammatory activity of A. altissima might occur in part via the inhibition of both $PGD_2$ and $LTC_4$ generation by 2, 4 and 5.

• Natural Product Sciences
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• v.4 no.4
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• pp.263-267
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• 1998

From the dried flower-buds of Syzygium aromaticum Merr. et Perry (Myrtaceae), seven compounds, i.e., eugenol (1), oleanolic acid (2), kaempferol 7-O-metylether (3), 3,3',4-tri-O-methylellagic acid (4), maslinic acid (5), ${\beta}-sitosterol-3-O-glucoside$ (6), and isorhamnetin 3-O-glucoside (7) were isolated. Compound 1 showed cyclooxygenase-2 (COX-2) inhibitory activity.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.286.1-286.1
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• 2003

Chrysin, a natural flavone compound contained in plants. has anti-inflammatory activity. Its anti-inflammatory effect has been previously explained in part by the suppression of promoter activities of inducible pro-inflammatory enzymes (cyclooxygenase-2 (COX-2) and inducible nitrogen synthase (iNOS)). Nitrate production triggered by the activation of lipopolysaccharides (LPS) was most highly suppressed by the treatment of chrysin, follwed by 5-hydroxy-7-methoxyflavone (Ch-2), 5,7-diacetylflavone (Ch-4) in cultured Raw 264.7 cells. (omitted)

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.258.1-258.1
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• 2002

Piperine (piperinoyl-piperidine) is a nitrogenous pungent substance contained in black pepper. the well know spice obtained from Piper nigrum L. (Piperaceae). Pharmacological studies have shown that piperine reduces inflammation and pain. possesses anticonvulsant and antiulcer activity. protects the liver and has deleterious effects on testis function. Prostaglandins(PGs) are a family of intercellular and intracellular messengers derived from arachidonic acid(AA) by phospholipase(PL) and cyclooxygenase(COX). (omitted)

• Journal of the Korean Society of Food Science and Nutrition
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• v.43 no.1
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• pp.110-117
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• 2014

In this study, the biological activity of water and ethanol extracts from Chrysanthemum incidicum Linne by ultrafine grinding for functional food source are examined. The content of phenolic compounds from Chrysanthemum incidicum Linne were the highest when extracted for 6 hr with 70% ethanol. The extraction yield of water and ethanol extracts were $7.12{\pm}1.61$ mg/g and $7.51{\pm}2.14$ mg/g, respectively. With ultrafine grinding, water and ethanol extracts were $8.63{\pm}1.15$ mg/g and $9.33{\pm}1.35$ mg/g, respectively. In determining anti-oxidative activity of Chrysanthemum incidicum Linne extracts, DPPH of normal grinding extracts was 83.52% and ultrafine grinding was 92.37%. In ABTS radical cation decolorization, normal grinding, fine grinding, and ultrafine grinding extracts were 90% or higher. In antioxidant protection factor (PF), water and ethanol extracts of ultrafine grinding showed relatively high anti-oxidative activities of each 1.82 PF and 2.16 PF, respectively. The TBARS value of ultrafine grinding extracts were lower than normal grinding and fine grinding extracts. The inhibition activity on xanthin oxidase of Chrysanthemum incidicum Linne extracts was 67.53% in ultrafine grinded water extracts and 83.45% in ultrafine grinded ethanol extracts. Inhibition on xanthin oxidase of ethanol extracts showed a higher inhibition effect than water extracts, and ultrafine grinding was higher than normal grinding. In angiotensin converting enzyme inhibition activity, ultrafine grinding water extract was 24% or higher, and ethanol extract was 34% or higher. The elastase inhibition activity of ultrafine grinding extract was 25.56%, which was higher than 20.34% of fine grinding extracts. Water extracts did not show hyaluronidase inhibition activity but ethanol extracts showed 35% of hyaluronidase inhibition activity. The determining expression inhibition of iNOS and COX-2 protein in macrophage by Chrysanthemum incidicum Linne extracts with a Western blot analysis, iNOS and COX-2 protein expression inhibition by Chrysanthemum incidicum Linne ethanol extracts were 40% and 15%, respectively at 100 ${\mu}g/mL$ concentration. The inhibitory patterns of iNOS and COX-2 protein expression was concentration dependent. The result suggests that Chrysanthemum incidicum Linne extracts by ultrafine grinding may be more useful than normal grinding as potential sources due to anti-oxidation, angiotensin converting enzyme and xanthine oxidase inhibition, anti-inflammation effect.

• Microbiology and Biotechnology Letters
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• v.50 no.4
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• pp.512-521
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• 2022

Since the main symptoms of COVID-19 involve the respiratory system, the infection rate of this disease is predicted to be higher in patients with other respiratory conditions such as allergic rhinitis. In such a situation, it will be meaningful to conduct research on an allergy treatment that has fewer side effects and can effectively reduce allergy symptoms. Here, we prepared experimental samples under various fermentation conditions with mixed extracts of six medicinal plants. To examine the anti-allergic efficacy of these samples, an egg albumin-induced allergic rhinitis animal model experiment, a serum histamine and IgE experiment, and a COX and LO inhibitory activity experiment were conducted. As a result of animal experiments, OVA+SP-4 showed superior efficacy compared to OVA+SP-1 in nasal rubbing and sneezing experiments and had anti-allergic efficacy similar to that of OVA-cetirizine. The serum histamine concentration of OVA+SP-4 was also 1.3 times higher than that of the OVA+cetirizine group, showing a high histamine reduction ability, and IgE showed the same trend. An analysis of COX inhibitory efficacy also confirmed that COX-1 and COX-2 inhibitory efficacy is high, and the longer the fermentation time, the higher the antiallergic efficacy. The composition proposed by this study is expected to have a significant effect on sustainable allergy prevention and treatment in the future by applying it to human patients.

• Korean Journal of Medicinal Crop Science
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• v.26 no.1
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• pp.8-18
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• 2018

Background: This present study was conducted to evaluate the anti-inflammatory and immune regulatory effects of Aucklandia lappa Decne (AL). Methods and Results: We measured cytotoxicity, nitric oxide (NO) content, mRNA expression (iNOS, IL-1${\alpha}$, IL-$1{\beta}$, and TNF-${\alpha}$), protein expression (iNOS, COX-2, and $I{\kappa}B$) and phagocytic activity in RAW264.7 cells. Male BALB/c mice were fed 100 mg/kg AL (Aucklandia lappa Decneon 70% ethanol extract) and 250 mg/kg AL for 4 weeks; thereafter, we observed B/T or $CD4^+/CD8^+$ lymphocyte subpopulation change, and expression patterns of $CD4^+$ and $CD8^+$ lymphocytes by immunohistochemical staining in mouse splenocytes and/or thymocytes. To determine the experimental concentration of AL, cell viability was measured by MTT assay and tested at $12.5{\mu}g/m{\ell}$ or less. AL inhibited the levels of NO, lymphokine production (IL-$1{\beta}$, and TNF-${\alpha}$), and mRNA (iNOS, IL-1${\alpha}$, IL-$1{\beta}$, and TNF-${\alpha}$) and protein (iNOS, and COX-2) expression. Additionally, the levels of $I{\kappa}B$, phagocytic activity, and splenic and thymic T lymphocytes, especially $T_H$ and $T_C$ cells were significantly increased in AL administered mice. The immuno-reactive density of $CD4^+$ and $CD8^+$ lymphocytes was stronger in AL groups than in the normal group. AL stimulated NO, iNOS, and COX-2, and regulated IL-1${\alpha}$, IL-$1{\beta}$, TNF-${\alpha}$, and $I{\kappa}B$ in macrophages treated with LPS (lipopolysaccharide). In addition, AL increased the phagocytic activity of macrophages and the immunity of mouse T ($T_H$, and $T_C$) cells. Conclusions: These results suggested that AL might show anti-inflammatory activity via the suppression of various inflammatory markers and immuno-regulatory activity.