• Title/Summary/Keyword: $PGE_1$

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Antioxidant, anti-inflammatory, and antibacterial activities of a 70% ethanol-Symphyocladia linearis extract

  • Jeong Min Lee;Mi-Jin Yim;Hyun-Soo Kim;Seok-Chun Ko;Ji-Yul Kim;Gun-Woo Oh;Kyunghwa Baek;Dae-Sung Lee
    • Fisheries and Aquatic Sciences
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    • v.25 no.11
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    • pp.579-586
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    • 2022
  • Research on the potential biological activity of red alga Symphyocladia spp. has been limited to Symphyocladia latiuscula, which is widely used as a food ingredient in Korea. Here, we examined the biological activity of another species, Symphyocladia linearis, which is found in Korea and was reported as a new species in 2013. The aim of this study was to evaluate the antioxidant, anti-inflammatory, and antibacterial properties of a 70% ethanol extract of S. linearis. Antioxidant activity, which was evaluated using radical scavenging assays, revealed half maximal inhibitory concentration values for 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH) and 2,2'-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) of 34.57 and 11.70 ㎍/mL algal extract, respectively. Anti-inflammatory activity of the S. linearis ethanolic extract was evaluated using RAW 264.7 cells by measuring the inhibition of lipopolysaccharide-induced nitric oxide (NO) and prostaglandin E2 (PGE2) production. The potential cytotoxicity of NO and PGE2 was first examined, confirming no toxicity at concentrations ranging from 10-100 ㎍/mL. NO production was inhibited 61.1% and 78.0% at 50 and 100 ㎍/mL S. linearis extract, respectively; and PGE2 production was inhibited 69.1%, 83.2%, and 94.8% at 25, 50, and 100 ㎍/mL S. linearis extract, respectively. Thus, the S. linearis extract showed very strong efficacy against PGE2 production. The cellular production of reactive oxygen species, measured using 2',7'-dichlorofluorescin diacetate fluorescence, was inhibited 48.8% by the addition of 100 ㎍/mL S. linearis extract. Antibacterial activity was evaluated using the disc diffusion method and minimum inhibitory concentration (MIC). S. linearis was effective only against gram-positive bacteria, exhibiting antibacterial activity against Staphylococcus aureus with a MIC of 256 ㎍/mL extract and against Bacillus cereus with a MIC of 1,024 ㎍/mL extract. Based on these results, we infer that a 70% ethanolic extract of S. linearis possesses strong anti-inflammatory properties, and therefore has the potential to be used in the prevention and treatment of inflammatory and immune diseases.

Cyclooxygenase-2 Induction in Porphyromonas gingivalis-Infected THP-1 Monocytic Cells

  • Choi, Eun-Kyoung;Oh, Byung-Ho;Kang, In-Chol
    • International Journal of Oral Biology
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    • v.31 no.1
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    • pp.21-26
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    • 2006
  • Periodontopathogens including Porphyromonas gingivalis interact with host periodontal cells and the excessive subsequent host responses contribute a major part to the development of periodontal diseases. Cyclooxygenase(COX)-2-synthesized $PGE_2$ has detrimental activities in terms of periodontal pathogenesis. The present study investigated induction of COX-2 expression by P. gingivalis in human monocytic THP-1 cells. Live P. gingivalis increased expression of COX-2, but not that of COX-1, which was demonstrated at both mRNA and protein levels. Elevated levels of $PGE_2$ were released from P. gingivalis-infected THP-1 cells. Pharma-cological inhibition of p38 mitogen-activated protein kinase(MAPK) and extracellular signal-regulated kinase(ERK) substantially attenuated P. gingivalis-induced COX-2 mRNA expression. Indeed, activation of p38 MAPK and ERK was observed in P. gingivalis-infected THP-1 cells. Also, P. gingivalis induced activation of nuclear $factor-{\kappa}B\;(NF-{\kappa}B)$ which is an important transcription factor for COX-2. These results suggest that COX-2 expression is up regulated in P. gingivalis-infected monocytic cells, at least in part, via p38 MAPK, ERK, and $NF-{\kappa}B$.

Anti-inflammatory Activity of Crinum asiaticum Linne var. Japonicum Extract and its Application as a Cosmeceutical Ingredient (문주란의 항염효과와 화장료적 특성)

  • Kim, Ki-Ho;Kim, Young-Heui;Kim, Ki-Soo;Park, Sun-Hee;Lee, Soo-Hee;Kim, Young-Jin;Kim, Young-Sil;Kim, Jong-Heon
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.32 no.1 s.55
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    • pp.59-64
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    • 2006
  • Crinum asiaticum Linne var. japonicum has long been used as a rheumatic remedy, an anti-pyretic, an anti-ulcer treatment, and for the alleviation of local pain and fever in Korea and Malaysia. In order to investigate the possibility of Crinum asiaticum Linne var. japonicum extract as a cosmetic ingredient, we measured its anti-inflammatory effect by inhibition of iNOS (inducible nitric oxide synthase), and the release of PGE2, IL-6, and IL-8. HPLC experiment after extraction with 95% ethanol at pH 3.5 showed that Crinum asiaticum Linne var. japonicum was mainly composed of lycorine (up to 1%), a well-known immunosuppressant. The content of lycorine varied depending on the type of tissue analyzed and the extraction method. In anti-inflammatory assay for inhibition of nitric oxide formation on lipopolysaccharide (LPS)- activated mouse macrophage RAW 264.7 cells, the ethanolic extract of Crinum asiaticum showed inhibitory activity of NO production in dose-dependent manner ($IC_{50} = 83.5 {\mu}g/mL$). Additional study by RT-PCR demonstrated that the extract of Crinum asiaticum significantly suppressed the expression of the iNOS gene. Moreover, the extract of Crinum asiaticum did not show my cytotoxicity, but did show cell proliferation effect against LPS ($10{\sim}60%$ increase of tell viability). In an assay to determine inhibition of the $H_2O_2$-activated release of PGE2, IL-6, and IL-8 in human normal fibroblast cell lines, the release of PGE2 and IL-6 was almost completely inhibited above concentrations of 0.05% and 1%, respectively. Moreover, the release of IL-8 was completely inhibited over the entire range of concentrations (> 0.0025%). The result showed that the extract of Crinum asiaticum Linne var. japonicum has sufficient anti-inflammatory effect. There-fore, Crinum asiaticum Linne var. japonicum extract may be useful as an ingredient of cosmetic products.

Prostaglandin E Synthase, a Terminal Enzyme for Prostaglandin E2 Biosynthesis

  • Kudo, Ichiro;Murakami, Makoto
    • BMB Reports
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    • v.38 no.6
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    • pp.633-638
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    • 2005
  • Biosynthesis of prostanoids is regulated by three sequential enzymatic steps, namely phospholipase $A_2$ enzymes, cyclooxygenase (COX) enzymes, and various lineage-specific terminal prostanoid synthases. Prostaglandin E synthase (PGES), which isomerizes COX-derived $PGH_2$ specifically to $PGE_2$, occurs in multiple forms with distinct enzymatic properties, expressions, localizations and functions. Two of them are membrane-bound enzymes and have been designated as mPGES-1 and mPGES-2. mPGES-1 is a perinuclear protein that is markedly induced by proinflammatory stimuli, is down-regulated by anti inflammatory glucocorticoids, and is functionally coupled with COX-2 in marked preference to COX-1. Recent gene targeting studies of mPGES-1 have revealed that this enzyme represents a novel target for anti-inflammatory and anti-cancer drugs. mPGES-2 is synthesized as a Golgi membrane-associated protein, and the proteolytic removal of the N-terminal hydrophobic domain leads to the formation of a mature cytosolic enzyme. This enzyme is rather constitutively expressed in various cells and tissues and is functionally coupled with both COX-1 and COX-2. Cytosolic PGES (cPGES) is constitutively expressed in a wide variety of cells and is functionally linked to COX-1 to promote immediate $PGE_2$ production. This review highlights the latest understanding of the expression, regulation and functions of these three PGES enzymes.

Protective Effect of Baicalin on the TNF-${\alpha}$-Mediated Development of Insulin Resistance in Differentiated 3T3-L1 Cells

  • Chae, Byeong Suk
    • Natural Product Sciences
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    • v.19 no.4
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    • pp.316-323
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    • 2013
  • Adipose tissue-derived chronic inflammation contributes to development of insulin resistance in obesity, leading to type 2 diabetes and cardiovascular disease. Baicalin, a flavonoid, has antioxidant, anti-inflammatory, antihyperglycemic, anti-adipogenic, and antiobesity effects. However, whether baicalin attenuates adipose tissue-derived development of insulin resistance remains still unclear. This study was to investigate effect of baicalin on the inflammatory changes involved in the development of insulin resistance in adipose tissue. RAW 264.7 cells and differentiated 3T3-L1 adipocytes were pretreated with various concentrations of baicalin in complete media for 1 h and then cultured in the presence or absence of LPS or TNF-${\alpha}$. Our results demonstrated that baicalin remarkably inhibited LPS-induced production of TNF-${\alpha}$, IL-6, and NO by RAW 264.7 cells in a dose-dependent manner. Baicalin also inhibited TNF-${\alpha}$-induced production of IL-6 and $PGE_2$ in differentiated 3T3-L1 cells in a dose-dependent manner, while upregulated TNF-${\alpha}$-suppressed expression of adiponectin and PPAR-${\gamma}$ mRNA and IRS-1 protein. These findings suggest that baicalin may prevent the adipose tissue-derived development of insulin resistance in obesity.

Inhibitory Activity of 8-Aminowogonin Analogues Against Prostaglandin $E_2$ Production (8-아미노우고닌 유도체의 Prostaglandin $E_2$ 생성에 대한 저해작용)

  • Jang, Jin-Hee;Sin, Kwan-Seog;Kim, Hyun-Pyo;Park, Hae-Il
    • YAKHAK HOEJI
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    • v.52 no.1
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    • pp.85-91
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    • 2008
  • 8-Acyl and 8-sulfonylamidowogonin analogues were synthesized as potential anti-inflammatory agents. Nitration of 5,7-dihydroxyflavone (chrysin) followed by methylation of phenol groups and reduction of nitro group yielded 8-aminowogonin analogues. Acylation and sufonylation of 8-aminowogonin followed by demethylation reactions gave the title compunds. The synthesized wogonin analogues showed much reduced inhibitory activity on prostaglandin $E_2\;(PGE_2)$ production.

THE EFFECTS OF MECHANICAL FORCE ON CULTURED PERIODONTAL LIGAMENT CELLS IN VITRO (물리적 외력이 배양중인 치주인대세포에 미치는 영향)

  • Kim, Hyun-young;Cha, Kyung-Suk
    • The korean journal of orthodontics
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    • v.24 no.2
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    • pp.295-301
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    • 1994
  • The movement of teeth during orthodontic treatment requires bone remodeling process in periodontal tissue. To find out the changes occuring in the cell itself, mechanical force was applied to the cultured periodontal ligament cells. Following results were obtained from measuring the changes in cyclic AMP and $PGE_2$, $^3H$-thymidine incorporation amount in time lapse after application of mechanical force. 1. When mechanical force was applied to cultured PDL cells, the amount of cAMP in cells were increased significantly after 15 min. of force application, but were decreased gradually as time lapsed. 2. When mechanical force was applied to cultured PDL cells, the amount of PGE2 were increased at 20,40,60 min. and was significantly increased at 20 min. 3. When mechanical force was applied to cultured PDL cells, the amount of $^3H$-thymidine incorporation was some increased, but was not statistically significant.

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Structure and Antiinflammatory Activity Relationships of Wogonin Derivatives

  • Jang, Jin-Hee;Kim, Hyun-Pyo;Park, Hae-Il
    • Archives of Pharmacal Research
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    • v.28 no.8
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    • pp.877-884
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    • 2005
  • A number of wogonin derivatives have been synthesized as congeners of wogonin and evaluated for their inhibitory activities of $PGE_2$ production. Wogonin derivatives modified at the B ring of wogonin were obtained from 2,4-Dihydroxy-3,6-dimethoxyacetophenone (1) via several steps. Most wogonin derivatives exhibited much reduced inhibitory activities against COX-2 catalyzed $PGE_2$ production compared to that of wogonin. Alkylation of 5,7-phenol groups and substitution at the B ring of wogonin generally caused reduction of inhibitory activity.

Regulatory Effects of Cyclic AMP on Osteoclast Formation (조골세포내 cAMP 농도 변화가 파골세포 형성에 미치는 영향)

  • Chun Yunna;Yim Mijung
    • YAKHAK HOEJI
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    • v.49 no.1
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    • pp.109-113
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    • 2005
  • In the present study treatment of IBMX, a phosphodiesterase (PDE) inhibitor, alone induced osteoclast formation in co-cultures of mouse bone marrow cells and calvarial osteoblasts. However, treatment of IBMX in combination with prostaglandin $E_2\;(PGE_2)$ inhibited osteoclast formation in a dose-dependent manner. Among various isozyme-specific PDE inhibitors, a PDE4 specific inhibitor, rolipram, showed similar effects as IBMX on osteoclast formation. To address the involvement of cyclic adenosine monophosphate (cAMP) in osteoclast formation, cAMP concentration in calvarial osteoblasts was investigated. When calvarial osteoblasts were co-cultured with IBMX alone or in combination with $PGE_2$, the patterns of cAMP concentration in calvarial osteoblasts were differ each other suggesting that cAMP in calvarial osteoblasts subtly regulates osteoclast formation.

Nitric Oxide and PGE$_2$ production Inhibitory Activities of Phenolic Compounds from Sophora japonica Linne

  • Kim, Hyun-Jung;Sim, Jae-Geul;Yeom, Seung-Hwan;Kim, Min-Kee;Lee, Jae-Hee;Lee, Min-Won
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.193.2-193.2
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    • 2003
  • Phytochemical examination of Sophorae Fructus yielded six phenolic compounds. The structures were elucidated as genistein(1), genistin(2) and genistein 7-O-${\alpha}$- L-rhamnopyranoside(3) by phytochemical and spectral evidences. The other compounds(4, 5, 6) are understudied by 2D-NMR. Nitric Oxide and PGE$_2$ production inhibitory activities in INF-${\gamma}$, LPS stimulated RAW 264.7 cell were examined. Compound 2 and 4 showed significant nitrogen monoxide(NO) production inhibitory activity in IFN-${\gamma}$, LPS stimulated RAW 264.7 cell. (omitted)

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