• Title/Summary/Keyword: cyclooxygenase inhibitory activity

Search Result 205, Processing Time 0.02 seconds

Study on the Anti-inflammatory Effects of Seungmagalgeuntanggamibang(SMG) (升麻葛根湯加味方이 消炎작용에 미치는 영향)

  • Song, Seong-Pil;Kim, Jin-Man;Lim, Kyu-Sang;Kim, Nam-Kwen;Kwen, Il-Ho
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
    • /
    • v.17 no.2
    • /
    • pp.12-30
    • /
    • 2004
  • This study was carried out to investigate the effects of SMG on the in vitro and in vivo inflammatory reactions. In experiment I, in vitro tests, ethanol extract of SMG showed potent radical scavenging activity tested by DPPH(I,1-diphenyl-2-picryl-hyrazyl) method and inhibited the lipopolysaccharide-induced gene expressions of interleukin-1${\beta}$, interleukin-6 and tumor necrosis factor-${\alpha}$ (above 50$\%$ at a concentration of 50㎍/㎖) by the macrophage RAW 246.7 cells. Among the herbal ingredients of SMG, ethanol extracts of Scutellaria baicalensis, Paeonia lactiflora, Glycyrrhiza glabra showed potent radical scavenging activity. And Glycyrrhiza glabra and Scutellaria baicalensis showed potent inhibitory activity of nitric oxide production. Especially, ethanol extract of Scutellaria baicalensis inhibited the gene expression of IL-1${\beta}$, IL-6 and TNF-${\alpha}$. In cyclooxygenase-2 assay, Scutellaria baicalensis and Glycyrrhiza glabra showed the potent inhibition of prostaglandin E2 generation. In experiment 2, in vivo tests, SMG showed inhibitory effects on vascular permeability (28.7$\%$) and leukocyte migration (11.5$\%$). These results mean that SMG has a anti-inflammatory effects by it's inhibitory effects of leukocyte migration and vascular permeability as well as it's inhibitory effects of lipopolysaccharide-induced gene expression of IL-1${\beta}$, IL-6 and TNF-${\alpha}$, and radical scavenging activity. Therefore, I expect that SMG may be used as a effective drug for treatment on inflammation.

  • PDF

The Anti-Inflammatory Effects of Persicaria thunbergii Extracts on Lipopolysaccharide-Stimulated RAW264.7 Cells (Lipopolysaccharide로 처리 된 RAW264.7 세포에서 고마리 추출물의 항염증 효과)

  • Kim, Sang-Bo;Seong, Yeong-Ae;Jang, Hee-Jae;Kim, Gun-Do
    • Journal of Life Science
    • /
    • v.21 no.12
    • /
    • pp.1689-1697
    • /
    • 2011
  • In this study, we investigated the anti-inflammation effect of Persicaria thunbergii (P. thunbergii) on RAW 264.7 murine macrophage cells. The anti-inflammatory activity of P. thunbergii was determined by measuring expression of the LPS-induced inflammatory proteins, inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) and nuclear factor-${\kappa}B$ (NF-${\kappa}B$), and the production of nitric oxide (NO) and prostaglandin $E_2$ ($PGE_2$). Methanol extract of P. thunbergii decreased the expression of iNOS, COX-2 and NF-${\kappa}B$, and increased the expression of HO-1 in LPS-stimulated RAW264.7 cells. Methanol extract was fractioned by n-butanol, hexane and ethyl acetate (EtOAc) and each fraction was tested for inhibitory effects on inflammation. Among the sequential solvent fractions, the EtOAc soluble fraction was investigated by the expression of prostaglandin $E_2$ ($PGE_2$), and showed decreasing form to the dose-dependent manner. EtOAc extract showed the most effective inhibitory activity of the expression of iNOS, COX-2 and NF-${\kappa}B$, and the production of NO. The study showed that P. thunbergii has anti-inflammatory activity through the decrease of NO and inhibition of iNOS, COX-2, $PGE_2$ and NF-${\kappa}B$ expression, and by the increase of HO-1 enzyme. This study needs for more investigation to find out the most effective single compound with anti-inflammatory activity.

Constituents of the Fruits and Leaves of Euodia daniellii

  • Yoo, Sang-Woo;Kim, Ju-Sun;Kang, Sam-Sik;Son, Kun-Ho;Chang, Hyeun-Wook;Kim, Hyun-Pyo;Bae, Ki-Hwan;Lee, Chong-Ock
    • Archives of Pharmacal Research
    • /
    • v.25 no.6
    • /
    • pp.824-830
    • /
    • 2002
  • Four flavonoid glycosides, flavaprin (7), evodioside B (8), vitexin (11), and hesperidin (12), as well as the coumarins bergapten (1), xanthotoxin (2), and isopimpinellin (3), the lignan simplexoside (10), the steroids ${\beta}-sitosterol$ (4) and daucosterol (5), the limonoids isolimonexic acid (6) and limonin (9), and uracil (13) and myo-inositol (14) have been isolated from Euodia daniellii. The structures of these compounds were established from spectral data. Among the isolates, bergapten showed cyclooxygenase-2 inhibitory activity with an $IC_{50}$ value of $6.2{\;}{\mu\textrm{g}}/ml. Flavonoids isolated from this plant exhibited no cytotoxic activity against the human tumor cell lines, A549, SKOV-3, SKMEL-2, XF498, and HCT15.

Effects of the Geijibokryunghwan on Carrageenan-induced Inflammation and COX-2 in Hepatoma Cells

  • Joo, Shin-Tak;Ban, Chang-Gyu;Park, Soon-Gi;Park, Won-Hwan
    • Journal of Physiology & Pathology in Korean Medicine
    • /
    • v.20 no.4
    • /
    • pp.1027-1031
    • /
    • 2006
  • In oriental medicine, Geijibokryunghwan(GBH) was used to improvement various symptoms created by the thrombosis. We investigated the effects of an oriental medicinal prescriptions, Geijibokryunghwan (GBH) consisting of herbs of Cinnamomi Ramufus (Geiji; 桂枝), Poria cocos (Bokrung; 茯?), Moutan Cortex Radicis(Modanpi; 牧丹皮), Paeoniae Radix (Jakyak; 芍藥) and Persicae Semen (Doin; 桃仁) on tumor growth-inhibitory activity and cancer chempreventive activity in assays representing three maior stages of carcinogenesis. Cancer chempreventive agents include nonsteroidal anti-inflammatory drugs (NSAIDS) such as indomethacin, aspirin, piroxicam, and sulindac, all of which inhibit cyclooxygenase (COX). Effects of the GBH extracts on carrageenan-induced edema Inflammation using female (C57BL/6XC3H) Fl (B6C3Fl ) mice and tumorigenesis were examined. Finally, cyclooxygenase metabolites were determined after extracts treatment. These data suggest that GBH extracts merits investigation as a potential cancer chempreventive agent in humans.

Inhibition of COX-2 Activity and Proinflammatory Cytokines($TNF-{\alpha}{\;}and{\;}IL-1{\beta}$) Production by Water-Soluble Sub-Fractionated Parts from Bee (Apis mellifera) Venom

  • Nam, Kung-Woo;Je, Kang-Hoon;Lee, Jang-Hurn;Han, Ho-Je;Lee, Hye-Jung;Kang, Sung-Kil;Mar, Woongchon
    • Archives of Pharmacal Research
    • /
    • v.26 no.5
    • /
    • pp.383-388
    • /
    • 2003
  • Bee venom is used as a traditional medicine for treatment of arthritis. The anti-inflammatory activity of the n-hexane, ethyl acetate, and aqueous partitions from bee venom (Apis mellifera) was studied using cyclooxygenase (COX) activity and pro-inflammatory cytokines (TNF-$\alpha and IL-1\beta$) production, in vitro. COX-2 is involved in the production of prostaglandins that mediate pain and support the inflammatory process. The aqueous partition of bee venom showed strong dose-dependent inhibitory effects on COX-2 activity ($IC_{50} = 13.1 \mu$ g/mL), but did not inhibit COX-1 activity. The aqueous partition was subfractionated into three parts by molecular weight differences, namely, B-F1 (above 20 KDa), B-F2 (between 10 KDa and 20 KDa) and BF-3 (below 10 KDa). B-F2 and B-F3 strongly inhibited COX-2 activity and COX-2 mRNA expression in a dose-dependent manner, without revealing cytotoxic effects. TNF-$\alpha and IL-1\beta$ are potent pro-inflammatory cytokines and are early indicators of the inflammatory process. We also investigated the effects of three subfractions on TNF-$\alpha and IL-1\beta$ production using ELISA method. All three subfractions, B-F1, B-F2 and B-F3, inhibited TNF-$\alpha and IL-1\beta$production. These results suggest the pharmacological activities of bee venom on anti-inflammatory process include the inhibition of COX-2 expression and the blocking of pro-inflammatory cytokines (TNF-$\alpha and IL-1\beta$) production.

Inhibitory Effect of IFN-$\beta$, on the Antitumor Activity of Celecoxib in U87 Glioma Model

  • Kim, Eun-Kyoung;Chung, Dong-Sup;Shin, Hye-Jin;Hong, Yong-Kil
    • Journal of Korean Neurosurgical Society
    • /
    • v.46 no.6
    • /
    • pp.552-557
    • /
    • 2009
  • Objective : Interferon-$\beta$, (IFN-$\beta$) has been used in the treatment of cancers. Inhibition of the enzyme cyclooxygenase (COX) with celecoxib had a significantly suppressive effect on tumor growth, angiogenesis, and metastasis in a variety of tumors. The aim of this study was to elucidate the antiglioma effect of combined treatment with IFN-$\beta$ and celecoxib in U87 glioma model. Methods : The in vitro effects of IFN-$\beta$ (50-1,000 IU/mL) and celecoxib ($50-250\;{\mu}M$) alone or combination of both on the proliferation and apoptosis of U87 cells were tested using MTT assay, FACS analysis and DNA condensation. To determine the in vivo effect, nude mice bearing intracerebral U87 xenograft inoculation were treated with IFN-$\beta$ intraperitoneally ($2{\times}10^5\;IU/day$ for 15 days), celecoxib orally (5, 10 mg/kg) or their combination. Results : IFN-$\beta$ or celecoxib showed an inhibitory effect on the proliferation of U87 cells. When U87 cells were treated with IFN-$\beta$ and celecoxib combination, it seemed that IFN-$\beta$ interrupted the antiproliferative and apoptotic activity of celecoxib. No additive effect was observed on the survival of the tumor bearing mice by the combination of IFN-$\beta$ and celecoxib. Conclusion : These results suggest that IFN-$\beta$ seems to inhibit the antiglioma effect of celecoxib, therefore combination of IFN-$\beta$ and celecoxib may be undesirable in the treatment of glioma.

Inhibitory Activities of Natural Products on Lipopolysaccharide Induced Prostaglandin Production in Mouse Macrophages (리포폴리사카라이드에 의해 유도되는 대식세포의 프로스타글란딘 생합성을 저해하는 천연물의 탐색)

  • Noh, Min-Soo;Ha, Jun-Yong;Lee, Chang-Hoon;Lee, Woo-Young;Lee, Soo-Hwan;Lee, Jung-Joon
    • YAKHAK HOEJI
    • /
    • v.42 no.6
    • /
    • pp.558-566
    • /
    • 1998
  • Two isoforms of cyclooxygenase (COX) have been identified - COX-1, which is constitlitively expressed in most tissues, and the inducible form, COX-2, of which expression is induced by inflammatory signals and mitogens. It has been considered that the beneficial effects of NSAIDs are due to the inhibition of COX-2 activity and the side effects are from the inhibition of COX-1 activity. Therefore, it is essential to develop selective COX-2 inhibitor for developing new GI-tolerable NSAIDS. To discover new leads for developing selective COX-2 inhibitors, three-hundred extracts of natural products were primarily screened with the system of prostaglandin accumulation in LPS-stimulated mouse peritoneal macrophages. To identify whether these inhibitory activities of crude extracts on the accumulation of Prostaglandins were derived from direct action against COX-2, the effects of selected extracts on exogenous arachidonic acid-derived production of prostaglandins by LPS-stimulated macrophages were determined. Among them, 5 methanol extracts of natural products, such as Zingiberis Rhizoma, Alpinae Officinarum Rhizoma, Caryophilli Flos, Scutellariae Radix, Dalbergia ordorifera. inhibited more than 70% of the prostaglandin production in LPS-stimulated mouse peritoneal macrophages at a con-centration of 1${\mu}$g/ml.

  • PDF

Inhibition of Cyclooxygenase and Prostaglandin E2 Synthesis by Crude Methanolic Extract from Euonymus Alatus (Thunb.) Sieb in SKBR3 Human Breast Cancer Cell Line

  • Kim Joong-Oh;Jang Tae-Hyun;Kim Min-Sung;Kim Dong-Il;Lee Tae-Kyun
    • The Journal of Korean Medicine
    • /
    • v.26 no.1 s.61
    • /
    • pp.37-45
    • /
    • 2005
  • In the present study, we examined the effect of crude methanolic extract (CME) from Euonymus alatus (Thunb.) Sieb on arachidonic acid (AA) cascade in SKBR3 human breast cancer cell line. CME had a potent inhibitory activity of prostaglandin E2 (PGE2) release induced by A23187, a $Ca^{2+}$ ionophore. The inhibition was concentration-dependent, with the 50 value of about 5 M. CME had no inhibitory effect on A23187-induced phosphorylation of p42/p44 extracellular signal regulated kinase/mitogen-activated protein kinase or on the liberation of [14C]-AA from the cells labeled with [14C]-AA. However, CME concentration-dependently inhibited the conversion of AA to $PGE_2$ in microsomal preparations, showing its possible inhibition of cyclooxygenase (COX). In enzyme assay in vitro, CME inhibited the activities of both constitutive COX (COX­I) and inducible COX (COX-2) in a concentration-dependent manner, with the 50 values of about 0.8 and 2M, respectively. Lineweaver-Burk plot analysis indicated that CME competitively inhibited the activities of both COX-l and -2. This study is a first demonstration that CME directly inhibits COX activity.

  • PDF

Study on the Antiinflammatory Effect of Gleditschiae Spina -Focussed on Takrisodokum and Kwaluubangtang- (조각자의 소염작용(消炎作用)에 대(對)한 실험적(實驗的) 연구(硏究) 부제(附題) : 탁이소독음(托裏消毒飮)과 과루우방탕(瓜蔞牛蒡湯)의 가감(加減)에 따른 효능비교(效能比較))

  • Park, Yong Ki;Kang, Byung Soo
    • The Journal of Dong Guk Oriental Medicine
    • /
    • v.4
    • /
    • pp.237-265
    • /
    • 1995
  • The inhibitory effects of Gleditschiae Spina, Cleditschia saponin, two complex prescriptions such as Takrisodokum and Kwaluubangtang, which contain Gleditschiae Spina, and their altered prescriptions on the activity of cyclooxygenase in vitro were investigated. The water extract of Gleditschiae Spina and Gleditschia saponin markedly inhibited the cyclo-oxygenase activity by 59% and 67%, respectively, at a concentration of $1mg/m{\ell}$, on the other hand, Takrisodokum and Kwaluubangtang showed 15% and 7% inhibition, respectively. The extracts with the substraction of Gleditschiae Spina and/or Platycodi Radix inhibited to a much smaller extent than Takrisodokum. However, in case of the extracts with the substraction of Gleditschiae Spina and/or Trichosanthis Semen, only one prescription, which does not contain Trichosanthis Semen, exhibited the same inhibition as Takrisodokum. From above results, Gleditschiae Spina was found to be most important for the effect of Takrisodokum and Kwaluubangtang on their antiinflammatory action. Instead of Gleditschiae Spina, another parts of this plant were added to both complex prescriptions and tested according to above methods, indicating that Gleditschiae Spina is more important than another parts for both prescriptions. When the administered dose of Gleditschiae Spina is increased(twofold and threefold) in both complex prescriptions, the inhibitory effect in Takrisodokum was diminished. however, the effect in Kwaluubangtang was increased.

  • PDF

Anti-Inflammatory Activity of Compounds from the Whole Plant of Patrinia saniculaefolia

  • An, Ren-Bo;Na, Min-Kyun;Min, Byung-Sun;Chang, Hyeun-Wook;Bae, Ki-Hwan
    • Natural Product Sciences
    • /
    • v.17 no.2
    • /
    • pp.90-94
    • /
    • 2011
  • An in vitro bioassay-guide revealed that the methanol (MeOH) extract of the whole plant of Patrinia saniculaefolia (Valerianaceae) 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). Phytochemical study of the MeOH extract of this plant led to the isolation of twelve compounds; ${\beta}$-farnesene (1), squalene (2), nardostachin (3), patridoid I (4), patridoid II (5), patridoid II-A (6), oleanolic acid (7), oleanonic acid (8), 23-hydroxyursolic acid (9), oleanolic acid 3-O-${\alpha}$-L-arabinopyranoside (10), oleanolic acid 3-O-${\beta}$-D-glucopyranoside (11), oleanolic acid 3-O-[${\beta}$-D-xylopyranosyl-(1${\rightarrow}$3)-${\beta}$-D-(6-O-butyl)glucuronopyranoside] (12). Among the compounds, 4 and 5 strongly inhibited both the COX-2-dependent $PGD_2$ generation with $IC_{50}$ values of 8.7 and 13.6 ${\mu}M$, respectively, and the generation of $LTC_4$ in the 5-LOX dependent phase with $IC_{50}$ values of 41.7 and 46.9 ${\mu}M$, respectively, which suggest that the anti-inflammatory activity of P. saniculaefolia might occur in part via the inhibition of both $PGD_2$ and $LTC_4$ generation by 4 and 5.