• 제목/요약/키워드: Cyclooxygenase activity

검색결과 636건 처리시간 0.024초

Anticancer and Anti-Inflammatory Activity of Probiotic Lactococcus lactis NK34

  • Han, Kyoung Jun;Lee, Na-Kyoung;Park, Hoon;Paik, Hyun-Dong
    • Journal of Microbiology and Biotechnology
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    • 제25권10호
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    • pp.1697-1701
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    • 2015
  • The anticancer and anti-inflammatory activities of probiotic Lactococcus lactis NK34 were demonstrated. Treatment of cancer cells such as SK-MES-1, DLD-1, HT-29, LoVo, AGS, and MCF-7 cells with 106 CFU/well of L. lactis NK34 resulted in strong inhibition of proliferation (>77% cytotoxicity, p < 0.05). The anti-inflammatory activity of L. lactis NK34 was also demonstrated in lipopolysaccharide-induced RAW 264.7 cells, where the production of nitric oxide and proinflammatory cytokines (tumor necrosis factor-α, interleukin-18, and cyclooxygenase-2) was reduced. These results suggest that L. lactis NK34 could be used as a probiotic microorganism to inhibit the proliferation of cancer cells and production of proinflammatory cytokines.

Synthesis and $PGE_2$ Inhibitory Activity of 5,7-Dihydroxyflavones and Their Ο-Methylated Flavone Analogs

  • Dao, Tran-Thanh;Chi, Yeon-Sook;Kim, Jeong-Soo;Kim, Hyun-Pyo;Kim, Sang-Hee;Park, Haeil
    • Archives of Pharmacal Research
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    • 제26권5호
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    • pp.345-350
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    • 2003
  • 5,7-Dihydroxyflavones and their Ο-methylated flavone analogs were prepared and evaluated their anti-inflammatory activity to decipher the structure-activity relationships. Most of the analogs were achieved from 2,4,6-trihydroxyacetophenone in 4 steps. 5,7-Dihydroxy-4 -methoxyflavone (4c) and 7-hydroxy-4 ,5-dimethoxyflavone(6c) were prepared following a different synthetic pathway. Among the synthetic flavones tested, 5-hydroxy-7-methoxyflavone analogs (3a-3e) showed moderate inhibitory activities of $PGE_2$ production from LPS-induced RAW 264.7 cells.

새로운 캅사이신 유도체 DA-5018의 진통활성 기전연구: Opiate 수용체 및 :Prostanoid와의 상관성 (Analgesic Action Mechanism of DA-5018, a New Capsaicin Derivative : Relationship to Opiate :Receptors and Prostanoids)

  • 손미원;손문호;배은주;김순희;김원배;양중의
    • Biomolecules & Therapeutics
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    • 제5권1호
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    • pp.87-93
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    • 1997
  • DA-5018, a new capsaicin derivative, showed potent analgesic effect comparable to that of morphine in various experimental acute pain models. in this study, whether the analgesic mechanism of DA-5018 is related to opiate receptors or prostanoids was investigated. The affinity of DA-5018 for opiate receptor was determined by receptor binding assay. The Ki values of DA-5018 for nonspecific and specific $\mu$, $textsc{k}$, $\delta$-opiate receptor was 299$\pm$8.88, 735$\pm$215, 2930$\pm$ 163, 1550$\pm$813 nM, respectively and DA-5018 exhibited lower affinity than morphine. DA-5018 (10-"~3$\times$10-′M) inhibited electrically-evoked contractions of the guinea ply ileum and rat vas deferens, and these inhibition was not antagonized by naloxone(10 nM), an opiate receptor antagonist. Antagonism of analgesic effect of 7A-5018 by naloxone was examined by tail pinch test. Analgesic action of DA-5018(0.1 ~2 mg/kg, 5.c.) was not antagonized by naloxone(1 mg/rg, i.p.). These results indicate that pharmacological action of DA-5018 is not related with opiate receptor. Cyclooxygenase and 5-lipoxygenase activities in rat peritoneal neutrophil treated with A23187 and arachidonic acid were measured by radioimmunoassay. DA-5018 stimulated the cyclooxygenase activity and the concentration show-ing the two fold increase of activity was 124$\mu$M. DA-5018 slightly inhibited 5-lipoxygenase activity and these results together indicate that analgesic action of 3A-5018 is not mediated through inhibition of cyclooxy genase or lipoxygenase. These results suggest that the analgesic effect of DA-5018 is not due to blocking opiate receptor or to inhibiting the synthesis of prostanoids in the arachidonic acid metabolism pathway.

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자하차(紫河車)약침이 제2형 콜라겐 유발 관절염에 미치는 영향 (Effect of Hominis placenta Herbal Acupuncture on Type II Collagen-induced Arthritis in Mice)

  • 조영욱;이승우;강민주;김은정;이승덕;김갑성
    • Journal of Acupuncture Research
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    • 제24권6호
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    • pp.75-88
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    • 2007
  • Objectives : We investigated the effects of Hominis placenta Herbal acupuncture on rheumatoid arthritis. Methods : We investigated the Type II collagen-induced arthritis test, vascular permeability test, phenyl benzoquinone-induced writhing test, hot plate test, carbon clearance test, determination of prostaglandin $E_2$ content and cyclooxygenase-2 activity test. Results : Hominis placenta Herbal acupuncture suppressed Type II collagen-induced arthritis in DBA/1J mice and vascular permeability with 10.2% inhibition in ICR mice. We see the phenyl benzoquinone-induced writhing test and the hot plate test in the analgesic activity test. In the phenyl benzoquinone-induced writhing test, Hominis placenta Herbal acupuncture showed that it increased its analgesic effect more than the control(test?) by 85.5%. In the hot plate test, it was also shown that the analgesic effect increased more than the control(test) by 32.1%. In the carbon clearance test, the immuno-stimulatory effect showed more than the control(test) by 8.0%. The formation of prostaglandin $E_2$ was also reduced more than the control(test) by 10.1%. Finally, cyclooxygenase-2 activity was inhibitedwith 36.3%. Conclusions : Hominis placenta Herbal acupuncture may be useful for the treatment of rheumatoid arthritis after injection.

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

  • Kim, Dong-Wok;Chi, Yeon-Sook;Son, Kun-Ho;Chang, Hyeun-Wook;Kim, Ju-Sun;Kang, Sam-Sik;Kim, Hyun-Pyo
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 2001년도 추계학술대회 및 정기총회
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    • pp.82-82
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    • 2001
  • 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 the 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 without significantly affecting COX-2 activity at 1 50 $\mu$M. Other prenylated flavonoids including kuraridin and sanggenon D also down-regulated COX-2 induction at 10-25 $\mu$M, lirhile kurarinone and echinoisoflavanone did not. In addition, sophoraflavanone G shelved in vivo anti-inflammatory activity against mouse croton oil-induced ear edema and rat carrageenan paw edema via oral (2-250mg/kg) or topical administration (10 - 250 $\mu\textrm{g}$/ear). Although the potencies of inhibition were far less than that of a reference drug, prednisolone, this compound showed higher anti-inflammato교 activity when applied topically, suggesting a potential use for several eicosanoid-related skin inflammation such as atopic dermatitis.

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Inhibitory Action of Ulmus Davidiana Planch Extract Solution to Osteoclast Cell Proliferation and Prostaglandin E2 Synthesis in Mice

  • Park, Sang-Dong;Kim, Kap-Sung;Cho, Hyun-Seok;Lee, Seung-Deok;Kim, Kyung-Ho
    • Journal of Acupuncture Research
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    • 제23권2호
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    • pp.91-102
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    • 2006
  • Objectives : Ulmus davidiana Planch (UD) has long been known to have anti-inflammatory and protective effects on damaged tissue, inflammation and bone among other functions. Methods : This study was undertaken to address whether the water extract of the bark of UD could modulate proliferation of mouse osteoclasts in vitro and to investigate its effect on cyclooxygenase-2 (COX-2), which converts arachidonic acid to prostaglandin E2 (PGE2) and is highly expressed in osteoclasts. Mouse osteoclasts were tested in vitro for growth inhibition, proliferation cell nuclear antigen expression, and COX-2 activity and expression after treatment with UD extract. Results : Its effects were compared with those of indomethacin (a nonselective COX inhibitor) and celecoxib (a selective COX-2 inhibitor) by Cell viability assay, Cell cycle analysis, Immunohistochemical analysis of PCNA expression, Western blot analysis and PGE2 Enzyme immunoassay (EIA). UD demonstrated a strong growth inhibitory action in both tested osteoclasts cells. The IC50s were $10\;{\mu}g/ml$ for UD, $6\;{\mu}M$ for celecoxib and $42\;{\mu}M$ for indomethacin. UD, as well as celecoxib and indomethacin, suppressed proliferation cell nuclear antigen expression and PGE2 synthesis in osteoclasts. UD inhibited COX-2 expression, whereas celecoxib inhibited COX-2 activity directly. Conclusion : UD selectively and effectively inhibits osteoclasts cell growth in vitro. Inhibitory action of PGE2 synthesis via suppression of COX-2 expression may be responsible for its anti-inflammatory activity.

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四君子湯이 免疫機能에 미치는 影響 (Effect of Sagunja-tang on Immune Function of Mouse Immune Cells)

  • 이상현;정명;임규상;윤용갑
    • 한방안이비인후피부과학회지
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    • 제28권3호
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    • pp.14-29
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    • 2015
  • Objectives : The extract of Sagunja-tang has been traditionally used for restorative treatment of constitutional weakness, vascular and immune disorder, and nervous disease in Oriental country. This study investigated the regulatory effects of Sagunja-tang on the expression, production, and activity of immune mediators.Methods : In this study, the extract of Sagunja-tang was prepared by extracting with distilled water at 100$^{\circ}C$ for 2.5h. The extract was freeze-dried following filtration through 0.45${{\mu}m}$ filter. The extract was dissolved in Hank's balanced salt solution (HBSS) and filtered again through 0.45${{\mu}m}$ filter before use. The level of nitrite, an oxidative product of nitric oxide(NO) was measured in the culture medium by the Griess reaction. The levels of prostaglandin E2(PGE2), Th1 cytokines (IFN-${\gamma}$, IL-2) and Th2 cytokines(IL-4, IL-5, IL-13) were measured by enzyme-linked immunosorbent assay and the protein levels of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expression were determined by Western blot analysis. Also examined the effects of the extract on T-cell proliferation and cytotoxic activity of natural killer cells.Results : In this investigation, Production levels of Th2 cytokines (IL-4, IL-5, IL-13) was inhibited in a dose dependent manner by treatment with the extract. I also found that the extract increased T-cell proliferation and cytotoxic activity of natural killer cells in a dose-dependent manner.Conculsions : These results suggest that the water extract of Sagunja-tang may be useful for a therapeutic drug against a sickly constitution and immune diseases, probably by regulating the production of immune mediators.

식물추출복합물(CME)의 퇴행성관절염 개선효과 (Beneficial Effects of Phyto-Extract Complex (CME) on Degenerative Arthritis)

  • 서형호;정종문
    • 대한본초학회지
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    • 제28권6호
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    • pp.87-93
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    • 2013
  • Objectives : Degenerative arthritis arises from several physiological factors. The purpose of this study is to investigate the beneficial effects of Phyto-extract Complex (CME) on degenerative arthritis. Methods : CME is composed of extracts of mulberry (Morus alba L.) fruit, mulberry leaves and black beans (Glycine max (L.) Merr.). To measure the toxicity of CME, we performed the single-dose toxicity study. For the evaluation of its effects on degenerative arthritis, we examined the inhibition of cyclooxygenase-2 (COX-2) activity, using in vitro enzyme activity assay, the reduction of protein expression of COX-2, 5-lipoxygenase (5-LO), and inducible nitric oxide synthase (iNOS) in RAW264.7 cells which were stimulated by lipopolysaccharide (LPS). We also examined the serum level of prostaglandins (PGs) and injury of the knee joint cartilage, using animal model of degenerative arthritis induced by mono-sodium iodoacetate (MIA). Results : CME did not have any toxicity in single-dose toxicity study. The CME inhibited the activity of COX-2 and could reduce the protein expression of COX-2, 5-LO and iNOS in RAW264.7 cells. The CME also reduced the serum level of PGs and prevented from the cartilage injury of knee joint in animal model of degenerative arthritis induced by MIA. Conclusions : Taken altogether, the CME could be useful for the improvement of degenerative arthritis through its various anti-inflammatory activities and prevention from the cartilage injury of knee joint.

인체 암세포에서 genistein에 의한 cyclooxygenase-2 및 telomerase의 활성 저하 (Genistein-induced Growth Inhibition was Associated with Inhibition of Cyclooxygenase-2 and Telomerase Activity in Human Cancer Cells.)

  • 김정임;김성윤;서민정;임학섭;이영춘;주우홍;최병태;정영기;최영현
    • 생명과학회지
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    • 제18권6호
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    • pp.884-890
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    • 2008
  • 본 연구에서는 대두의 대표적인 생리활성 물질인 genistein의 처리에 따른 암세포의 증식억제에서 telomerase 및 COX-2 활성의 변화 연관성을 조사하였다. 이를 위하여 4가지 종류의 암세포주를 사용하였으며, genistein 처리에 의하여 암세포들의 증식억제에서 백혈병 세포인 U937 세포의 감수성이 감장 높게 나타났으며, genistein 처리에 따라 telomere 조절인자들의 발현이 대부분 억제되었으며, telomerase의 활성도 매우 유의적으로 감소되었다. 또한 genistein처리 농도가 증가함에 따라 COX-2의 발현이 전사 및 번역 수준에서 모두 감소되었으며 이에 따른 $PGE_2$의 생성 역시 현저하게 감소되었으나, COX-1의 발현에는 큰 변화가 없었다. 이러한 결과들은 genistein의 항암 활성을 이해하는 귀중한 자료로서 활용될 것으로 생각된다.

대식세포 내에서의 홍화자 추출물의 항염증 활성 (Anti-Inflammatory Activity of Carthamus tinctorious Seed Extracts in Raw 264.7 cells)

  • 김동희;황은영;손준호
    • 생명과학회지
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    • 제23권1호
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    • pp.55-62
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    • 2013
  • 본 연구에서는 홍화자 추출물이 항염증에 대한 실험연구가 이루어져 있지 않은 것에 착안하여 LPS에 의해 활성화된 대식세포로부터 유도되는 염증반응에 대한 억제효과를 조사하였다. 홍화자 추출물을 이용하여 피부 염증에 대하여 연구를 하였다. 산화질소와 cytokine의 생산은 면역세포의 대표적인 염증인자이다. 세포는 LPS 처리 후 한 시간 뒤에 홍화자 추출물을 처리를 하였다. 세포 독성이 나타나지 않는 농도인 5, 10, 25 및 50 ${\mu}g/ml$를 사용하였다. 홍화자의 에틸아세테이트 분획물은 NO, $PGE_2$, TNF-${\alpha}$, IL-$1{\beta}$, IL-6, iNOS, COX-2의 생성을 저해 시켰다. $PGE_2$는 50 ${\mu}g/ml$의 농도에서 60%에 가까운 저해율을 나타내었다. iNOS와 COX-2 역시 ${\mu}g/ml$의 농도에서 각각 54%, 65%가 저해가 되었다. 게다가 홍화자 에틸아세테이트 분획물은 염증성 사이토카인인 TNF-${\alpha}$, IL-$1{\beta}$, IL-6의 생성을 감소 시켰다. 이러한 결과로 홍화자 추출물은 염증 예방과 치료에 효과적임을 확인 할 수 있었다.