• Natural Product Sciences
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• 제15권2호
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• pp.83-89
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• 2009

Polygoni multiflori Ramulus (PM), the stem of Polygonum multiflorum Thunb. has been widely used as a traditional medicine for the treatment of lots of diseases. In macrophages, nitric oxide is released as an inflammatory mediator and has been proposed to be an important modulator of many pathophysiological conditions in inflammation. In the present study, it was investigated that the inhibitory effects on NO and proinflammatory cytokines such as tumor necrosis factor alpha (TNF-${\alpha}$), interleukin-6 (IL-6) and the mechanism of down-regulation of immune response by 85% methanol extracts of PM in mouse (C57BL/6) peritoneal macrophages. Extracts of PM (0.1, 1 mg/ml) suppressed NO production and showed inhibition of proinflammatory cytokines like TNF-${\alpha}$, IL-6 and it attenuated iNOS and COX-2 expression via down-regulation of NF-${\kappa}$B activation. The present results indicate that the 85% methanol extracts of PM has an inhibitory effect on the production of NO through down-regulation of iNOS expression in LPS stimulated mouse peritoneal macrophages and therefore may be beneficial in diseases which related to macrophage-mediated inflammatory disorders.

• 동아시아식생활학회지
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• 제23권2호
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• pp.197-202
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• 2013

The objective of this study is to evaluate the anti-cancer and anti-inflammatory activities of plum (Formosa, Oishiwase, Soldam) for the future development of functional food products. To determine the anti-inflammatory effect of different types of plums, the inhibitory effect of plum extracts on nitric oxide (NO) production were measured in lipopolysaccharide (LPS)-stimulated Raw 264.7 mouse macrophage cells and human cancer cell lines (A549, Ags, Hela, Hep3B). Among the three different plum cultivars, Oishiwase at a concentration of 1 mg/mL showed the highest inhibitory effects on NO production (%) in Raw 264.7 macrophage cells. Moreover, Oishiwase exhibited a higher anti-cancer activity against A549 (renal carcinoma, 50%), Ags (gastric carcinoma, 35%), HeLa (cervical carcinoma, 50%), and Hep3B (hepatocellular carcinoma, 31%) at a concentration on 1 mg/mL, respectively, compared to Formosa and Soldam. Our findings suggest Oishiwase plum extracts may serve as potential dietary sources of natural health promoting substances.

• 한국식품저장유통학회지
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• 제18권1호
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• pp.65-71
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• 2011

본 연구에서는 도라지 분말을 유기용매로 추출한 후 도라지의 추출물과 분획물들에 의한 세포 내 활성산소종 및 glutathione (GSH)를 측정하여 항산화효과를 검토하였고 NO 생성 저해 효과를 알아보았다. 세포 내 활성산소종 생성억제 실험에서 건조 도라지의 A+M 및 MeOH 추출물과 추출물을 n-hexane, 85% aq. MeOH, n-BuOH, water로 다시 추출하여 얻어진 각각의 분획물들을 농도별로 HT1080 세포에 처리하였을 때 A+M과 MeOH 추출물 모두 측정시간 120분 동안 $500\;{\mu}M$ $H_2O_2$만을 처리한 control군에 비해 세포 내 활성산소종을 크게 억제시켰으며, MeOH 추출물에 의한 항산화 효과가 더 높게 나타났다. 또한, 각 분획물들 중 n-BuOH 분획물이 다른 분획물들에 비해 우수한 항산화 활성을 보였다. GSH 농도 측정 실험에서 A+M 및 85% aq. MeOH 분획물를 처리했을 때 GSH 함량이 증가하였다. NO 생성 저해 실험에서는 A+M 및 MeOH 추출물이 0.01 및 0.05 mg/mL의 농도에서 NO 생성을 억제하는 것으로 나타났으며, A+M 추출물에 의한 저해 효과가 높았다. 각 분획물들은 모두 control보다 낮은 NO 생성량을 나타내었으며, 특히 85% aq. MeOH 및 n-BuOH 분획물은 0.05 mg/mL 농도에서 blank에 가까운 NO 생성 억제율을 나타냈다. 이상의 연구결과로부터 n-BuOH 분획물에 의한 세포 내 활성산소종 생성 억제 효과 및 NO 생성 저해 효과가 우수함을 알 수 있었으며, 향후 분획물의 분리 정제를 통한 새로운 기능성 물질의 개발이 필요할 것으로 사료된다.

• 생약학회지
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• 제36권3호통권142호
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• pp.245-251
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• 2005

Phytochemical examination of the barks of Actinidia arguta led to the isolation of five flavonoids. Structures of compounds were elucidated as catechin (1), (-)-epicatechin (2), quercetin (3), $quercetin-3-O-{\beta}-D-glucopyranoside$ (4), $quercetin-3-O-{\beta}-D-galactopyranoside$ (5) by comparison with previously reported spectral evidences. To investigate the anti-oxidative effect and nitric oxide (NO) production inhibitory activity of these compounds, DPPH radical scavenging activity and nitric oxide production inhibitory activity in $IFN-{\gamma}$, LPS stimulated RAW 264.7 cell were examined. The $IC_{50}s$ were determinied as follows : $1\;$IC_{50}=26.61\;{\mu}g/ml$, $2\;IC_{50}=25.30\;{\mu}g/ml$, $3\;IC_{50}=20.41\;{\mu}g/ml$, $4\;IC_{50}=18.23\;{\mu}g/ml$ , $5\;IC_{50}=30.46\;{\mu}g/ml$, $6\;IC_{50}=28.0;{\mu}g/ml$, $7\;IC_{50}=27.24\;{\mu}/ml$. These NO production inhibitory effects were significantly different compared with the positive control, L-NMMA $(IC_{50}=20.77\;{\mu}g/ml)$, respectively. Compound $1\;(IC_{50}=6.19\;{\mu}g/ml)$, $2\;(IC_{50}=8.98\;{\mu}g/ml)$, $3\;(IC_{50}=7.30\;{\mu}g/ml)$ and $4\;(IC_{50}=7.64\;{\mu}g/ml)$ also showed potent antioxidative activities similar level to ascorbic acid $(IC_{50}=9.22\;{\mu}g/ml)$. These results suggest that barks of A. arguta have a potent anti-oxidative and anti-inflammatory activity.

• KSBB Journal
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• 제29권5호
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• pp.343-352
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• 2014

In the present study, antioxidant activities of two crude pigments (acetone and MeOH) and their solvent fractions (n-hexane, 85% aq.MeOH, n-BuOH, and water fractions) from red crab shell were evaluated by measuring 1,1-diphenyl-2-picryl hydrazyl (DPPH), peroxynitrites, and degree of production of reactive oxygen species (ROS) in HT 1080 cells as well as the extent of oxidative damage of genomic DNA purified from HT 1080 cells. From comparative analysis, 85% aq.MeOH fraction showed the strongest scavenging effect on both peroxynitrite in vitro and intracellular ROS in HT 1080 cells. Protective activities of these samples against hydroxyl radical-mediated genomic DNA damage were also investigated. 85% aq.MeOH and n-BuOH fractions significantly inhibited oxidative damage of purified genomic DNA. On the other hand, we investigated their inhibitory effects on nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated Raw 264.7 cells. All samples significantly reduced NO production. Among the samples, n-hexane and water solvent fractions most effectively inhibited NO.

• Archives of Pharmacal Research
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• 제27권10호
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• pp.1053-1059
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• 2004

$N^1$-Benzyl-4-methylbenzene-1,2-diamine (JSH-21) and its analogs were chemically synthesized and their anti-inflammatory potentials investigated. JSH-21 inhibited nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7 in a dose-dependent manner, with an $IC_{50}$ value of 9.2 ${\mu}M$, where pyrrolidine dithiocarbamate and parthenolide as positive controls exhibited $IC_{50}$ values of 29.3 and 3.6 ${\mu}M$, respectively. The inhibitory effect of JSH-21 on the NO production was attributable to its down-regulatory action on LPS-inducible NO synthase (iNOS), which was documented by iNOS promoter activity. In the mechanism of the anti-inflammatory action, JSH-21 exhibited inhibitory effects on LPS-induced DNA binding activity and transcriptional activity of nuclear factor-kappa B (NF-$_KB$). Structural analogs of JSH-21 also inhibited both the LPS-induced NO production and NF-$_KB$). transcriptional activity, where diamine substitution at positions 1 and 2 of JSH-21 seems to play an important role in the anti-inflammatory activity.

• The Korean Journal of Physiology and Pharmacology
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• 제7권5호
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• pp.283-287
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• 2003

While nitric oxide (NO) produced by inducible nitric oxide synthase (iNOS) is beneficial for host survival, it is also detrimental to the host. Thus, regulation of iNOS gene expression may be an effective therapeutic strategy for the prevention of unwanted reactions at various pathologic conditions. During the screening process for the possible iNOS regulators, we observed that esculetin is a potent inhibitor of cytokine-induced iNOS expression. The treatment of 3T3-L1 adipocytes with the tumor necrosis factor-${\alpha}$ (TNF) induced iNOS expression, leading to enhanced NO production. TNF-induced NO production was inhibited by esculetin in a dose-dependent manner. Esculetin inhibited the TNF-induced NO production at the transcriptional level through suppression of iNOS mRNA and subsequent iNOS protein expression. These results suggest esculetin, a component of natural products, as a naturally occurring, nontoxic means to attenuate iNOS expression and NO-mediated cytotoxicity.

• 대한약침학회지
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• 제15권2호
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• pp.11-14
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• 2012

Objectives: The purpose of this study was to compare the antioxidant and anti-inflammatory effects of Alum (AL) and Burnt Alum (BAL), which are commonly used as external ointments. Methods: Extracts of AL and BAL were classified into three groups: 20, 50, and $100mg/{\mu}{\ell}$. The cytotoxicity was measured by using MTT assays in human keratinocyte cell line (HaCaT). The anti-oxidant effect was measured by using the DPPH (1, 1-diphenyl-2-picryl-hydrazyl-hydrate) radical scavenger. The anti-inflammatory effect was measured by using the inhibitory efficacy for the amount of nitric-oxide (NO) produced in mouse macrophage cell line (RAW 264.7). Results: BAL showed a higher level of cytotoxicity than AL. The AL groups showed a concentration-dependent scavenging effect on DPPH radicals, but no significant relevance was found. The BAL groups showed a concentration-dependent scavenging effect on DPPH radicals. The scavenging effects of the BAL groups were almost insignificant, but the values for the 20, 50, and $100{\mu}g/m{\ell}$ trials were different. The BAL groups showed significant concentration-dependent inhibitory effects on NO production, but the AL groups did not. Conclusions: AL showed an anti-oxidant effect more efficiently than BAL did, which demonstrated a superior anti-inflammatory effect. Therefore, for external usage, AL must be distinguished from BAL.

• 한국식품과학회지
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• 제44권5호
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• pp.621-627
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• 2012

항염증효과가 있는 기능성 식품 및 의약품 소재의 개발을 위하여 천연 식물 자원으로부터 NOS 저해 활성 물질을 분리하고 그 이화학적인 특성에 대해 알아보기 위해 항염증 효과가 있다고 알려져 있는 58가지의 생약재에서 NO 저해효과를 확인해 본 결과 독활에서 80% 이상의 높은 저해활성을 가진 것을 알 수 있었다. 독활 생약재 에탄올 추출물에서 n-hexane, chloroform, ethyl acetate, n-butanol, water 순으로 용매 분획을 실시한 후 NO 생성 저해 활성을 측정한 결과, chloroform 분획에서 가장 높은 저해 활성을 보여 최종 분리 시료로 선정하였으며, open column chromatography(silica gel, $C_{18}$)를 이용하여 최종적인 활성 물질(AC8-MV)을 분리할 수 있었다. 분리한 활성 물질(AC8-MV)의 순도를 확인하기 위하여 analytical HPLC와 LC-ESI-mass spectrum를 분석한 결과 순수한 단일 물질로 분리 되었음을 확인할 수 있었으며, 차후 nuclear magnetic resonance spectrometer(NMR)를 통해 구조분석을 실시할 것이다. 또한 AC8-MV와 NO저해효과가 유의적으로 차이가 없던 AC8-MVI 활성물질에 대한 순도 및 구조분석을 연구할 것이다. 이를 통해 독활로부터 분리한 활성물질(AC8-MV)이 NO inhibitor 로서 일반 항염증 약물 및 기능성 식품 소재로 실용화될 수 있는 가능성을 시사하였다.

• IMMUNE NETWORK
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• 제8권1호
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• pp.13-20
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• 2008

Background: Coptis chinensis rhizome has been used as a medicinal herb in traditional Oriental medicine. We investigated the effects of Coptis chinensis extract on inflammatory mediators and delayed type hypersensitivity in mice. Methods: The inhibitory effect of ethanolic extract of Coptis chinensis (CCE) on cell proliferation was evaluated using MTS assay. The lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages and the Con A-activated mouse splenocytes were cultured with various concentrations of CCE. Total nitric oxide (NO) production was determined by Griess reaction. The amounts of secreted prostaglandine E2 ($PGE_2$), interleukin (IL)-2 and IFN-${\gamma}$ were measured by ELISA. To investigate the in vivo anti-inflammatory effect of CCE, oxazolone-induced delayed type hypersensitivity (DTH) model was used. Results: The CCE at $100{\mu}g/ml$ significantly blocked the LPS-induced production of pro-inflammatory mediators (NO and PGE) in RAW264.7 macrophages. Also, it significantly inhibited cell proliferation and cytokine (IL-2 and IFN-${\gamma}$) production in splenocytes. Furthermore, when splenocytes from CCE fed mice (200 mg/kg for 2 weeks) were activated with Con A, cell proliferation and cytokine production were significantly inhibited. In addition, CCE decreased in vivo inflammation in oxazolone-induced DTH model mice. Conclusion: We suggest that Coptis chinensis can be used as an anti-inflammatory drug by exerting an inhibitory effect in inflammatory mediator- and cell-mediated inflammation.