• Title/Summary/Keyword: cyclooxygenase-1

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Inhibitory Effects of Complex of Mulberry Extract on Degenerative Arthritis (상심자추출물 등 복합물의 퇴행성관절염 억제효과)

  • Seo, Hyeong Ho;Jeong, Jong Moon
    • Korean Journal of Medicinal Crop Science
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    • v.22 no.4
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    • pp.262-269
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    • 2014
  • Complex of mulberry extract (CME) is composed of extracts of mulberry (Morus alba L.) fruit, mulberry leaves and black beans (Glycine max (L.) Merr.). In this study, we investigated prevention effects of CME on degenerative arthritis. The $SC_{50}$ value of DPPH radical scavenging by CME was $158.49{\pm}11.35{\mu}/mL$. We found that CME significantly reduced the production of nitric oxide (NO) and protein expression of cyclooxygenase-2 (COX-2) in RAW 264.7 cells which were activated by LPS. Experiments using animal model of degenerative arthritis showed that CME (400 mg/kg body weight) inhibited the production of TNF-${\alpha}$ (77.5%) and IL-$1{\beta}$ (95.0%). Furthermore, it was observed that CME reduced to 85.9% of paw edema induced by carrageenan. These results suggest that CME could improve degenerative arthritis.

Prasaplai: An essential Thai traditional formulation for primary dysmenorrhea treatment

  • Tangyuenyongwatana, Prasan;Gritsanapan, Wandee
    • CELLMED
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    • v.4 no.2
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    • pp.10.1-10.8
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    • 2014
  • Affecting more than half of menstruating women, dysmenorrhea is a cramp which causes abdominal or lower back pain just before or during a menstruation. In western medicine, non-steroidal anti-inflammatory drugs (NSAIDs) are normally used to treat primary dysmenorrheal symptoms. Despite their rapidity in relieving pain, NSAIDs have many serious side effects on the liver, kidney, and gastrointestinal tract. Thai traditional medicines comprise many preparations for treating dysmenorrhea, especially Prasaplai preparation which has been listed in the Thai traditional common household drug list since 2006. The use of Prasaplai was originated about 100 years ago and is still being used in the present time to treat dysmenorrhea. This review focuses on the history of the preparation, active ingredients, and biological activities especially on cyclooxygenase inhibitor, artifacts occurred in the preparation, quantitative analysis, and clinical trial of Prasaplai formulation.

Curcumin Inhibits Phorbol Ester-induced Expression of Cyclooxygenase-2 In Vivo through Suppression of Extracelluar Signal-regulated Kinase (ERK) 1/2 and NF-${\kappa}$/B in Mouse Skin

  • Chun, Kyung-Soo;Surh, Young-Joon
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.322.3-323
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    • 2002
  • Curcumin derived from turmeric (Curcuma longa L.. Zingiberaceae) has been shown to possess marked chemopreventive activities, but the underlying molecular mechanisms remain unclear. In the present work. curcumin was found to inhibit 12-Ο-tetradecanoylphorbol-13-acetate(TPA)-induced expression of cyclooxygenase-2 (COX-2) in female ICr mouse skin as determined by Western and Northern blot analysis as well as immunohistochemical staining. Curcumin treatment atlenuated TPA-stimulated epidermal NF-${\kappa}$B activation. which was associated with its blockade of degradation and phosphorylation of the inhibitory protein l${\kappa}$ Bu and also of subequent translocation of the p65 subunut to nucleus. (omitted)

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Synthesis and Screening of Cyclooxygenase Activity of Hydantoin and 2-Thiohydantoin Derivatives (Hydantoin 및 2-Thiohydantoin 유도체의 합성과 사이클로옥시게나제 활성 검색)

  • 신혜순;최희전;권순경
    • YAKHAK HOEJI
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    • v.48 no.2
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    • pp.141-146
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    • 2004
  • Selective COX-2 inhibitors were expected to retain anti-inflammatory activity by inhibition of prostaglandin production with reduction of gastric and renal side effect associated with non-steroidal anti-inflammatory drugs. This study reported the syntheses of novel 2-thiohydantoin and hydantoin derivatives which have the structure of 5-membered heterocyclic ring substituted with two aryl groups, phenyl group at 5-position and p-sulfamylphenyl or p-methoxyphenyl group at 1-position. These synthetic compounds showed significant COX-2 activities in vitro screening. Among them, 5-phenyl-2-thiohydantoin and hydantoin substituted with benzyl group at 3-position, compounds 5 and 8, could be considered as lead compounds with $IC_{50}$/=13.13∼18.78 $\mu\textrm{g}$/$m\ell$ for the development of COX-2 inhibitors.

INHIBITORY EFFECTS OF THE SOY ISOFLAVONE GENISTEIN ON INDUCTION OF COX-2 AND ACTIVATION OF ERK1/2 IN CULTURED MCF10A CELLS

  • Chung, Myung-Hoon;Kim, Jung-Hwan;Keum, Joo-Seob;Lee, Seung-Sei;Surh, Young-Joon
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2002.05a
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    • pp.87-87
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    • 2002
  • We have investigated the effects of genistein on induction of cyclooxygenase-2 (COX-2) that plays an important role in the pathophysiology of carcinogenesis as well as in cellular response to inflammatory stimuli. Treatment of MCF10A cells with 12-O-Tetradecanoylphorbol-13-acetate (TPA) or TNF-$\alpha$ resulted in increased COX-2 expression and PGE$_2$ production, which was inhibited by genistein.(omitted)

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Puerariae flos inhibits inflammatory responses in interferon-γ and lipopolysaccharide-stimulated mouse peritoneal macrophages

  • Hong, Seung-Heon;Kim, Hong-Joon;Cha, Dong-Seok;Lee, Ju-Young;Na, Ho-Jeong
    • Advances in Traditional Medicine
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    • v.7 no.3
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    • pp.229-234
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    • 2007
  • In macrophages, nitric oxide (NO) is released as an inflammatory mediator and has been proposed to be an important modulator of many pathophysiological conditions including inflammation. In this study, we have examined the inhibition effects of NO production by 85% methanol extract of the flower of Pueraria thunbergiana (PF) in mouse macrophages. Extract of PF (1, 10, 100 ${\mu}g/ml$) inhibited NO production, inducible NO synthase and cyclooxygenase-2 expression in interferon-g and lipopolysaccharide-stimulated mouse peritoneal macrophages and it had no cytotoxicity. These data suggest that 85% methanol extract of PF might be useful in controlling macrophages mediated inflammatory disease.

Tribulus terrestris Suppresses the Lipopolysaccharide-Induced Inflammatory Reaction in RAW264.7 Macrophages through Heme Oxygenase-1 Expressions

  • Kim, Jai Eun
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.28 no.1
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    • pp.63-68
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    • 2014
  • The fruit of Tribulus terrestris L. (Zygophyllaceae) is an important source of traditional Korean and Chinese medicines. In this study, NNMBS223, consisting of the ethanol extract of T. terrestris, showed potent anti-inflammatory activities in RAW264.7 macrophages. We investigated the effect of NNMBS223 in suppressing the protein expression of inducible nitric oxide synthase (iNOS), cyclooxygenase (COX)-2 and production of iNOS-derived nitric oxide (NO), COX-2-derived prostaglandin E2 (PGE2) in lipopolysaccharide (LPS)-stimulated macrophages. In addition, NNMBS223 induced expression of heme oxygenase (HO)-1 through nuclear translocation of nuclear factor E2-related factor 2 (Nrf2) in macrophages. The effects of NNMBS223 on LPS-induced production of NO and PGE2 were partially reversed by the HO activity inhibitor tin protoporphyrin (SnPP). These findings suggest that Nrf2-dependent increases in expression of HO-1 induced by NNMBS223 conferred anti-inflammatory activities in LPS stimulated RAW264.7 macrophages.

Anti-inflammatory Compounds from the Leaves of Ailanthus altissima Meihua JIN

  • Jin, Me-Ihua;Bae, Ki-Hwan;Chang, Hyeun-Wook;Son, Jong-Keun
    • 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.

Production of Prostaglandin $E_2$ and $I_2$ is Coupled with Cyclooxygenase-2 in Human Follicular Dendritic Cells

  • Cho, Wha-Jung;Kim, Jin-I;Cho, Kyu-Bong;Choe, Jong-Seon
    • IMMUNE NETWORK
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    • v.11 no.6
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    • pp.364-367
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    • 2011
  • Background: Prostaglandins (PGs) play pathogenic and protective roles in inflammatory diseases. The novel concept of PGs as immune modulators is being documented by several investigators. By establishing an in vitro experimental model containing human follicular dendritic cell-like cells, HK cells, we reported that HK cells produce prostaglandin $E_2$ ($PGE_2$) and prostaglandin $I_2$ ($PGI_2$) and that these PGs regulate biological functions of T and B cells. Methods: To investigate the respective contribution of cyclooxygenase-1 (COX-1) and COX-2 to $PGE_2$ and $PGI_2$ production in HK cells, we performed siRNA technology to knock down COX enzymes and examined the effect on PG production. Results: Both $PGE_2$ and $PGI_2$ productions were almost completely inhibited by the depletion of COX-2. In contrast, COX-1 knockdown did not significantly affect PG production induced by lipopolysaccharide (LPS). Conclusion: The current results suggest that mPGES-1 and PGIS are coupled with COX-2 but not with COX-1 in human follicular dendritic cell (FDC) and may help understand the potential effects of selective COX inhibitors on the humoral immunity.

Cyclooxygenase-2 Expression is not a Marker of Poor Survival in Lung Cancer

  • Turk, H. Mehmet;Camci, Celalettin;Sevinc, Alper;Bukyukberber, Suleyman;Sari, Ibrahim;Adli, Mustafa
    • Asian Pacific Journal of Cancer Prevention
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    • v.13 no.1
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    • pp.315-318
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    • 2012
  • Objective: Cyclooxygenase-2 (COX-2) has been claimed to play role in carcinogenesis and be related to a bad prognosis in tumours. The aim of this study was to investigate the relationship between COX-2 expression and clinical and pathological parameters in early and advanced stage lung cancer patients. Materials and Methods: A total of 73 patients with lung cancer (27 adenocarcinomas, 33 squamous cell carcinomas, 4 large cell carcinomas and 9 small cell cancer) were analysed retrospectively. COX-2 expression was evaluated by immunohistochemistry in resection materials or lung biopsies. Tumor cells demonstrating more intense staining than smooth muscle and endothelial cells were recorded as COX-2 positive. We investigated the correlation between increased COX-2 expression and histological type of the tumor, the stage of the disease and survival. Results: COX-2 expression was observed in 55% of the adenocarcinomas, 45% of the squamous cell carcinomas and 22% of the small cell carcinomas. No correlation was apparent between COX-2 expression and disease stage, histological type and the survival. Conclusion: The results of this study do not support COX-2 expression as an independent prognostic factor in lung cancer. However, since results of the literature are different, further studies made in larger series are needed.