• Title/Summary/Keyword: NO production inhibitory activity

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Inhibition of Nitric Oxide Synthesis by Ergosterol Derivative from Phellinus pini in LPS-Activated RAW 264.7 Cells (낙엽송층버섯으로부터 Ergosterol 유도체의 분리 및 RAW 264.7 세포주의 Nitric Oxide 생성 저해활성)

  • Jang, Hyun-Jin;Yang, Ki-Sook
    • YAKHAK HOEJI
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    • v.50 no.6
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    • pp.367-371
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    • 2006
  • Phellinus pini (Hymenocaetaceae) has been used for the immunomodulating activity hypolipidemic effect, gastric cancer non-insulin dependant diabetes, diarrhea, and menstrual irregularity. From the screening of each fraction for the inhibitory activity of NO production in lipopolysaccaride (LPS) activated RAW 264.7 cells, methanol extract of Phellinus pini and hexane soluble fraction exhibited inhibition of NO production compared with LPS control without toxicity. The hexane soluble fraction showed dose dependent inhibition of NO production. According to activity guided fractionation, the active hexane fr. was repeatedly chromatographed over silica gel, ergosta-4,6,8(14),22- tetraen-3-one was isolated. The compound inhibited NOS activation (IC$_{50}$ = 29.7 uM) and NO production of activated macrophage at 30 uM.

Inhibitory Effect of the Culture Broth Extract of Aspergillus tamarii on Nitric Oxide Production and Its Antioxidative Activity

  • Lee, Ki Man;Lee, Geum Seon;Shim, Hong;Kim, Seung Hyun;Nam, Sung Hee;Kang, Tae Jin
    • International Journal of Industrial Entomology and Biomaterials
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    • v.25 no.2
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    • pp.153-157
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    • 2012
  • Many studies have explored suppression of aflatoxin produced by Aspergillus Genus. On the other hand, this study examined the inhibitory effect of the culture broth extract (CE) of A. tamarii obtained from dead silkworm on nitric oxide (NO) production and its antioxidative activity. The culture broth was extracted with EtOAc, dried, and then used in this experiment. As a result, CE did not show cytotoxicity on RAW 264.7 cells at any concentration. Moreover, CE suppressed lipopolysaccharide (LPS)-induced NO production of RAW 264.7 cells in a dose-dependent manner. The total phenol content according to the Folin-Dennis method, the antioxidative activity by DPPH, and the nitrate radical scavenging capacity of CE were increased in a dose-dependent manner. Thus, many of the phenolic compounds were considered to represent the antioxidative activity.

Physiological activities of water extract and solvent fractions of Grifola frondosa (잎새버섯 물추출물 및 유기용매 분획물의 생리활성)

  • Kim, Eun-Jung;Kim, Jun-Ho
    • Journal of Mushroom
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    • v.13 no.3
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    • pp.192-198
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    • 2015
  • This study was performed in order to analyze the fibrinolytic, thrombin inhibitory, anti-oxidative, acetylcholinesterase inhibitory, and immuno-enhancing activities of the water extract and solvent fractions isolated from Grifola frondosa. Fibrinolytic activity was analyzed using the fibrin plate method, and thrombin inhibitory activity was assayed using the substrate H-D-Phe-piparg- pna. Anti-oxidative activity was estimated using the DPPH assay, and AChE inhibitory activity was measured using the spectrophotometric method. Immuno-enhancing activity was examined using the nitric oxide (NO) production in RAW 264.7 macrophage cells. Cell viability was determined using the MTS assay. Fibrinolytic activities were the highest in water extract (1.55 plasmin units/mL) followed by water fraction (0.85 plasmin units/mL). The thrombin inhibitory activities of the water and ethyl acetate fractions were determined to be 76.43% and 72.59%, respectively. The acetylcholinesterase inhibitory activities of chloroform and hexane fractions exhibited values of 95.14% and 94.74%, respectively. The butanol fraction showed the highest anti-oxidative activity at 94.47%. Anti-proliferating activity against Raw 264.7 cells showed no cytotoxicity. The production of NO in Raw 264.7 cells increased up to 2-fold by adding the water fraction compared to the untreated control. These results suggest that Grifola frondosa may serve as a useful functional food for the enhancement of immune function and the prevention and therapy of cardiovascular diseases.

Anti-Inflammatory Effects of N1-Benzyl-4-Methylbenzene-1,2-Diamine (JSH-21) Analogs on Nitric Oxide Production and Nuclear Factor-kappa B Transcriptional Activity in Lipopolysaccharide-Stimulated Macrophages RAW 264.7

  • Min, Kyung-Rak;Shin, Hyun-Mo;Lee, Jee-Hyun;Kim, Byung-Hak;Chung, Eun-Yong;Jung, Sang-Hun;Kim , Young-Soo
    • Archives of Pharmacal Research
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    • v.27 no.10
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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.

Inhibitory Effects of Water Extracy of Prunellae Spica on the Production of Pro-inflammatory Mediator in LPS-activated Raw 264.7 Cells (하고초물추출물이 LPS로 활성화된 Raw 264.7 cell에서의 염증매개물질 억제효과)

  • Chang, Hyun-Ju;Park, Sook-Jahr;Lee, Jong-Rok;Kim, Sang-Chan
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.23 no.3
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    • pp.599-607
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    • 2009
  • Prunellae Spica is the spike or whole plant of Prunella vulgaris Linne, which has been used for clearing heat from the liver, brightening the eyes and treating headache in traditional oriental medicines. This study was conducted to evaluate the inhibitory effects of the aqueous extract of Prunellae Spica (PSE; PS extract) on the production of NO and PGE2 in LPS-activated Raw 264.7 cells. Cell viability was determined by MTT assay, and all three doses of PS extract (0.03, 0.1 and 0.3 mg/ml) had no significant cytotoxicity during the entire experimental period. The cells were treated with 1 ${\mu}g/ml$ of LPS 1 h before adding PS extract, and increased NO and PGE2 production were detected in LPS-activated cells compared to control. However, these increases were dose-dependently attenuated by treatment with PS extract. The inhibition of NO by PS extract was due to the suppression of iNOS expression via inhibition of $NF{\kappa}B$ nuclear translocation and proteolytic degradation of $I{\kappa}B{\alpha}$. The decreased level of PGE2 was derived from inhibition of COX-2 activity, but expression of COX-2 protein was not affected by PS extract. Moreover, PS extract reduced the elevated production of IL-${\beta}$ and IL-6 by LPS. These results demonstrate that PS extract has inhibitory effects on the production of NO and PGE2 as a consequence of the reduction of proinflammatory cytokines, especially IL-${\beta}$ and IL-6 in LPS-activated Raw 264.7 cells.

Chemical Constituents from Buddleja officinalis and Their Inhibitory Effects on Nitric Oxide Production

  • Park, Tae Wook;Lee, Chul;Lee, Jin Woo;Jang, Hari;Jin, Qinghao;Lee, Mi Kyeong;Hwang, Bang Yeon
    • Natural Product Sciences
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    • v.22 no.2
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    • pp.129-133
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    • 2016
  • Bioactivity-guided fractionation of a methanolic extract of Buddleja officinalis led to the isolation of two monoterpenes, crocusatin M (1), crocusatin C (2), a flavonoid, acacetin (3), three lignans, lariciresinol (4), pinoresinol (5), and syringaresinol (6), and two triterpenoidal saponins, mimengoside B (7) and songarosaponin A (8). The structures of isolates were identified based on 1D-, 2D-NMR, and MS data analysis. All isolates were tested for their inhibition on LPS-induced NO production in RAW 264.7 cells. As a result, mimengoside B (7) and songarosaponin A (8) showed a mild inhibitory activity of NO production.

Evaluation of Biological Activities of Invasive Alien Plants for Development of Functional Biomaterials

  • So Jin Kim;Su Hyeong Heo;Min Gun Kim;Kyung Hwan Boo;Chang Sook Kim
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2022.09a
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    • pp.112-112
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    • 2022
  • This study aims to confirm the possibility of using the invasive alien plants in Jeju as a functional biomaterial. To achieve this purpose, 70% ethanol extract and solvent fractions were prepared for five invasive alien plants (Hypochaeris radicata, Rumex acetosella, Humulus japonicus Siebold & Zucc., Solanum viarum, Lactuca scariolar) and their antioxidant, antibacterial anti-inflammatory and anti-obesity effects were investigated. The DPPH radical scavenging activity of ethanol extract from invasive alien plants was shown in the order of Rumex acetosella > Hypochaeris radicata > Humulus japonicus. Antimicrobial activity of ethanol extract against food poisoning bacteria (4 species) and oral cavity-induced microorganisms (6 species) was measured. As a result, the extract of Humulus japonicus showed high antibacterial effects against food poisoning bacteria (E. coli, V. parahaemolyticus) and oral microbes (L. casei, S. epidermidis, E. faecalis). In LPS-induced RAW 264.7 cells, the anti-inflammatory effect of ethanol extract from invasive alien plants was investigated. As a result, the NO production inhibition activity was highest in the Rumex acetosella and the Humulus japonicus Siebold & Zucc. ethanol extract, and the NO production inhibition activity was concentration-dependent. In addition, the Rumex acetosella and the Humulus japonicus Siebold & Zucc. ethanol extract showed a concentration-dependent inhibitory effect on cytokine (IL-6) production. These extracts also showed inhibitory activity of COX-2, an inflammatory protein. This suggests that NO production inhibition activity by the extract of invasive alien plants is the result of inhibition of iNOS and COX-2 expression. Currently, organic solvent fractions of crude extract are manufactured and the investigation of active ingredients is continuing along with evaluation of biological activity such as anti-inflammatory. These results are expected to be a major data for the study on the separation and utilization of active ingredients with antioxidant, antibacterial and anti-inflammatory effects using foreign plant crude extract and solvent fractions, and are highly likely to be applied to the development of functional food and cosmetics materials.

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Effect of phlorotannins isolated from Ecklonia cava on angiotensin I-converting enzyme (ACE) inhibitory activity

  • Wijesinghe, W.A.J.P.;Ko, Seok-Chun;Jeon, You-Jin
    • Nutrition Research and Practice
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    • v.5 no.2
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    • pp.93-100
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    • 2011
  • Inhibition of angiotensin I-converting enzyme (ACE) activity is the most common mechanism underlying the lowering of blood pressure. In the present study, five organic extracts of a marine brown seaweed Ecklonia cava were prepared by using ethanol, ethyl acetate, chloroform, hexane, and diethyl ether as solvents, which were then tested for their potential ACE inhibitory activities. Ethanol extract showed the strongest ACE inhibitory activity with an $IC_{50}$ value of 0.96 mg/ml. Five kinds of phlorotannins, phloroglucinol, triphlorethol-A, eckol, dieckol, and eckstolonol, were isolated from ethanol extract of E. cava, which exhibited potential ACE inhibition. Dieckol was the most potent ACE inhibitor and was found to be a non-competitive inhibitor against ACE according to Lineweaver-Burk plots. Dieckol had an inducible effect on the production of NO in EAhy926 cells without having cytotoxic effect. The results of this study indicate that E. cava could be a potential source of phlorotalnnins with ACE inhibitory activity for utilization in production of functional foods.

Synthesis of Yakuchinone Derivatives and Their Inhibitory Activities on Nitric Oxide Synthesis (Yakuchinone과 그 유도체의 합성 및 Nitric Oxide생성 저해효능)

  • 윤정화;안한나;류재하;김희두
    • YAKHAK HOEJI
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    • v.45 no.1
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    • pp.16-22
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    • 2001
  • Novel yakuchinone derivatives have been designed, synthesized and evaluated their inhibitory activity of NO production in lipopolysaccharide (LPS)-activated macrophages. From this study, some enone compounds have been found to be highly active in the assay. In view of the importance of NO in septic shock and inflammation, these compounds may be useful candidates for the development of new drug to treat endotoxemia and inflammation accompanying overproduction of NO.

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Nitric Oxide Production Inhibitory Effects of Three Caffeoylquinic Acids Isolated from Hot Water Extract of Eriobotrya japonica L. Leaves (비파엽 열수 추출물에서 분리한 Caffeoylquinic Acid 3 종의 Nitric Oxide 생성 억제 효과)

  • Kim, Sun Min;Kim, A Young;Lee, Kyoung In
    • Korean Journal of Medicinal Crop Science
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    • v.28 no.4
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    • pp.245-253
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    • 2020
  • Background: Research on hot water extracts of medicinal plants that are easily applicable in the clinical setting is essential. To confirm the anti-inflammatory-related active compounds present in the hot water extract of Eriobotrya japonica leaves, ability to inhibit nitric oxide (NO) production was measured and active compounds isolated from the extract were analyzed. Methods and Results: Sovent fractionation by solvent was performed to identify the active compounds present in the hot water extract, and the ability of the extract and the fractions obtained to inhibit NO production was measured. Subsequently, based on the results of liquid chromatography (LC) profile analysis of the n-butanol fraction that had a relatively high inhibitory ability of NO production, six subfractions were separated around the main peak. Among the separated subfractions spectra from mass spectroscopy (MS) were analyzed and standard comparisons were performed on the compounds of the three main peaks on the chromatogram. NO production inhibitory activity of subfraction 2 identified as neochlorogenic acid was the highest with an IC50 of 18.49 ㎍/㎖ followed by that of subfraction 5 identified as cryptochlorogenic acid with IC50 of 25.82 ㎍/㎖. Conclusions: Our result, it was confirmed that several caffeoylquinic acids, including neochlorogenic acid and cryptochlorogenic acid present in the hot water extract of E. japonica leaves have an important role as compounds exhibiting anti-inflammatory activity.