• Title/Summary/Keyword: COX-1

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The Defensive Effect of Keuibi-tang on the Gastric Mucous Membrane of Mouse Injured by Stress and Ethanol (스트레스와 에탄올로 유발된 mouse의 위점막 손상에 대한 귀비탕의 예방효과)

  • 김학재;최준혁;임성우
    • The Journal of Korean Medicine
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    • v.24 no.1
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    • pp.155-168
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    • 2003
  • This study was carried out to investigate the effect of Keuibi-tang (KBT) on the injury of gastric mucous membrane by stress and ethanol in mice. The normal group was non-inflammation elicited mice. The two control groups were mice with gastro-inflammation elicited by stress and ethanol. The two sample groups were mice administered KBT before gastro-inflammation elicitation. In the common morphology and histochemical change, the two control groups were observed with various injuries such as hemorrhagic erosion and ulcer, while the sample group was the same as the normal group. In the immunohistochemical change, the distributions of PNA and COX-1 treated with KBT noticeably increased over the control group (P<0.05). The distributions of $NF-{\kappa}B$ p50, COX-2 and TUNEL in the group treated with KBT were noticeably lower than in the control group (P<0.05). The distribution of KBT was the same as the normal group. According to the above results, it is supposed that KBT is applicable to gastritis and gastric ulcer due to stress and alcoholic drinks.

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Treatment Effect of Jecksodoodangkuisan against Colonic Mucosal Ulcer Induced by Indomethacin in Mouse (Indomethacin으로 유발된 생쥐의 대장점막 손상에 대한 적소두당귀산(赤小豆當歸散)의 치료효과)

  • Hwang, Tae-Hyun;An, Joong-Hwan;Lee, Seong-Hwan;Lim, Seong-Woo;Choi, En-Young
    • The Journal of Internal Korean Medicine
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    • v.26 no.2
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    • pp.341-352
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    • 2005
  • Objectives: This study was carried out to investigate the effects of Jecksodoodangkuisan(JD) and Jecksodoodangkuisankahyunjicho(JH) against Colonic Mucosal Ulcer induced by indomethacin in mouse. Methods: The normal group consisted of mice that were not inflammation-induced. The control group was untreated gastro-inflammation-elicited mice. The sample group mice were those administered BO, JD and JH after gastro-inflammation elicitation. Results: In the immunohistochemical change, the distribution of COX-1 in mice treated with BO, JD and JH noticeably increased than control group(P<0.05). The distributions of $NF-{\kappa}B$, p50, COX-2, ICAM-1, HSP70 and Substance P in mice treated with BO, JD and JH noticeably decreased more than control group(P<0.05). And JH was most effective treatment against Colonic Mucosal Ulcer in the immunohistochemical change. Conclusions: According to the above results, Jecksodoodangkuisan and Jeckmdoodangkuisankahyunjicho are applicable treatments for Colonic Mucosal Ulcer.

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Effects of Sophoraflavanone G, a Prenylated Flavonoid from Sophora Flavescens, on Cyclooxygenase-2 and In Vivo Inflammatory Response

  • Kim, Dong-Wook;Chi, Yeon-Sook;Son, Kun-Ho;Chang, Hyeun-Wook;Kim, Ju-Sun;Kang, Sam-Sik;Kim, Hyun-Pyo
    • Archives of Pharmacal Research
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    • v.25 no.3
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    • pp.329-335
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    • 2002
  • Previously, several prenylated flavonoids having a C-8 lavandulyl moiety were found to inhibit cyclooxygenase-1 (COX-1) as well as 5-lipoxygenase (5-LOX), and sophoraflavanone G was the most potent inhibitor against these eicosanoid generating enzymes among 19 prenylated flavonoids tested. In this investigation, effects of sophoraflavanone G on COX-2 induction from RAW 264.7 cells and in vivo inflammatory response were studied. Sophoraflavanone G inhibited prostaglandin $E_2{\;}(PGE_2)$ production from lipopolysaccharide (LPS)-treated RAW cells by COX-2 down-regulation at 1-50 uM. Other prenylated flavonoids including kuraridin and sanggenon D also down-regulated COX-2 induction at 10-25 uM, while kurarinone and echinoisoflavanone did not. In addition, sophoraflavanone G showed in vivo anti-inflammatory activity against mouse croton oil-induced ear edema and rat carrageenan paw edema via oral (2-250 mg/kg) or topical administration (10-250 ug/ear). Although the potencies of inhibition were far less than that of a reference drug, prednisolone, this compound showed higher anti-inflammatory activity when applied topically, suggesting a potential use for several eicosanoidrelated skin inflammation such as atopic dermatitis.

Effects of Jaeumgeonbi-tang Extract on Indomethacin-Induced Gastric Mucosal Lesions (Indomethacin으로 유발된 위점막 손상에 대한 자음건비탕의 효과)

  • Lee Hae-Yeon;Baik Tae-Hyun
    • The Journal of Korean Medicine
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    • v.25 no.3
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    • pp.111-122
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    • 2004
  • Objectives : This study was carried out to investigate the effects of Jaeumgeonbi-tang extract on indomethacin-induced gastric mucosal lesions of mice. Methods : Experimental groups were classified into non-treatment group (CON group), non-administered group (GE group), misoprostol administered group (MA group) and Jaeumgeonbi-tang extract administered group (JG group). This study examined the morphological change, distribution of mast cells, mucous secreted cells and apoptotic cells, BrdU, COX-1, Hsp70, NF-κB p50, PKC, COX-2 and TNF-α of gastric mucosa. Results : 1. The hemorrhagic erosion of gastric mucosa and infiltrated mast cells were reduced in the MA and JG groups. 2. PNA reaction and mucous secreted cells were increased in the MA and JG groups. 3. The distribution of apoptotic cells, Hsp70, NF-κB p50, PKC, COX-2 and TNF-α were increased in the gastro­inflammation elicitated group, but decreased in the MA and JG groups. 4. The MA and JG groups showed increase on COX-1, BrdU. Conclusions : Jaeumgeonbi-tang extract had excellent effects on indomethacin-induced gastric mucosal lesions.

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Estimation of hazard function and hazard change-point for the rectal cancer data (직장암 데이터에 대한 위험률 함수 추정 및 위험률 변화점 추정)

  • Lee, Sieun;Shim, Byoung Yong;Kim, Jaehee
    • Journal of the Korean Data and Information Science Society
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    • v.26 no.6
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    • pp.1225-1238
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    • 2015
  • In this research, we fit various survival models and conduct tests and estimation for the hazard change-point with the rectal cancer data. By the log-rank tests, at significance level ${\alpha}=0.10$, survival functions are significantly different according to the uniporter of glucose (GLUT1), clinical stage (cstage) and pathologic stage (ypstage). From the Cox proportional hazard model, the most significant covariates are GLUT1 and ypstage. Assuming that the rectal cancer data follows the exponential distribution, we estimate one hazard change-point using Matthews and Farewell (1982), Henderson (1990) and Loader (1991) methods.

Anti-Allergic Effect of Fermented Extracts of Medicinal Plants Andrographis paniculate, Salvia plebeia R. Br., Canavalia gladiate, Eleuthorococcus senticosus, Ulmus davidiana var. japonica, and Clerodendrum trichotomum Thunb. ex Murray

  • Mi Jeong, Choi;Yu Ri, Kim
    • 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.

Anti-inflammatory Effects of Asiaticoside on Inducible Nitric Oxide Synthase and Cyclooxygenase-2 in RAW 264.7 Cell Line (Asiaticoside가 RAW 264,7 세포에서 Inducible nitric oxide synthase와 Cyclooxygenase-2에 미치는 항염증 작용에 관한 연구)

  • 주상섭;배옥남;정진호
    • Toxicological Research
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    • v.19 no.1
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    • pp.33-37
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    • 2003
  • Asiaticoside has been tested for the ability as an anti-inflammatory drug using lipopolysaccharide (LPS)-stimulated macrophage cell line (RAW 264.7 cell). LPS treatment induced dramatically inducible nitric oxide synthase (iNOS) in RAW cells. However, asiaticoside inhibited LPS-stimulated iNOS induction in a concentration-dependent manner. Especially, higher concentrations (>50 $\mu\textrm{M}$) of asiaticoside completely blocked iNOS induction. In addition, LPS-stimulated expression of inducible cyclooxygenase (COX-2) and interleukin-1 $\alpha$ (IL-1 $\alpha$) was inhibited by asiaticoside treatment. Asiaticoside up to 50 $\mu\textrm{M}$ still required to inhibit COX-2 and IL-1 $\alpha$ induced by LPS. Consistent with these findings, treatment with asiaticoside suppressed do novo synthesis and cellular accumulation of prostaglandin $E_2$ to a lesser extent, suggesting that asiaticoside blocked the induction as well as the activity of COX-2 These results suggest the possibility that asiaticoside may be effective therapeutic agents for septic shock and other inflammatory diseases.

Synthesis and Characterization of Novel Hydantoins as Potential COX-2 Inhibitors: 1,5-Diarylhydantoins

  • Park, Hae-Sun;Choi, Hee-Jeon;Shin, Hea-Soon;Lee, Sang-Kook;Park, Myung-Sook
    • Bulletin of the Korean Chemical Society
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    • v.28 no.5
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    • pp.751-757
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    • 2007
  • To develop new COX-2 inhibitors, 1,5-diarylhydantoins and 1,5-diaryl-2-thiohydantoins were synthesized from phenylacetic acids by esterification, bromination, C-N bond formation and cyclization. Esters 1-3 were efficiently synthesized from the starting materials by reflux in absolute methanol for 3 h containing concentrated sulfuric acid as catalyst. Bromination was carried out with N-bromosuccinimide at rt in dichloromethane. Bromides 4-6 were reacted with aniline, p-anisidine, sulfanilamide in ethanol (or N,N-dimethylformamide) to provide the amines 7-15. Hydantoins and 2-thiohydantoins 16-46 were synthesized from amines 7-15 by treating them with potassium isocyanate (or potassium thiocyanate) and triethylamine. The synthetic process from alkyl α-anilinophenylacetate 7-15 to 3-alkylhydantoins was carried out in a one-pot reaction using alkyl isocyanate (alkyl isothiocyanate).

Synthesis of Novel 1-(4-Halophenyl)-5-arylhydantoins as Selective COX-2 Inhibitors

  • Kwon, Soon-Kyoung;Park, Hae-Sun;Choi, Hee-Jeon;Park, Myung-Sook;Yoon, Myung-Sun;Kim, Nan-Young;Shin, Hae-Soon
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.240.1-240.1
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    • 2003
  • Nonsteriodal antiinflammatory drugs(NSAIDs) are widely used to treat pain. fever, and inflammatory conditions including osteoarthritis. However, gastrointestinal (GI) and renal toxicity were related to common NSAIDs limits their usefulness because NSAIDs inhibit not only COX-2 associated with anti-inflammatory activity. but also COX-1 accompanied with side effects in the stomach and kidney. (omitted)

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Synthesis and COX Inhibitory Activities of Rutaecarpine Derivatives

  • Lee, Eung-Seok;Kim, Seung-Ill;Lee, Seung-Hoo;Jeong, Tae-Cheon;Moon, Tae-Chul;Chang, Hyeun-Wook;Jahng, Yurng Dong
    • Bulletin of the Korean Chemical Society
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    • v.26 no.12
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    • pp.1975-1980
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    • 2005
  • A series of substituted rutaecarpines were prepared by employing Fischer indole synthesis as key step and their inhibitory activities on COX-1 and 2 as well as selectivity on COX-2 were evaluated. The compounds with a methanesulfonyl and a bromo group at C10 showed promising inhibitory activity ($IC_{50}$ = 0.27, 0.35 $\mu$M, respectively) with selectivity.