• 한국식품과학회지
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• 제43권2호
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• pp.200-205
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• 2011

본 연구에서는 문헌을 통하여 항산화 혹은 항염증 활성을 가지는 6종의 생약재와 이들 생약재를 혼합하여 제조한 생약복합제의 항산화 및 항염증 활성을 측정하였다. 총 폴리페놀 함량은 어성초, 홍화, MIX-2 에탄올추출물이 각각 58.98, 60.79, 57.74 mg/g의 함량으로 다른 시료들 보다 높게 측정되었다. 또한 플라보노이드 함량도 어성초(HC), 홍화(CT), MIX-2에탄올추출물이 각각 36.86, 19.42, 14.74 mg/g으로 높게 측정되었다. 단일 생약재와 생약복합제 에탄올추출물의 라디칼 소거능을 측정한 결과 DPPH 라디칼의 RC50 값은 어성초, 홍화, MIX-2 에탄올추출물에서 각각 69.64, 50.70, $63.49{\mu}g/mL$로 추출물 가운데 우수한 DPPH 라디칼 소거능을 보였고, ABTS 라디칼의 $RC_{50}$ 값도 어성초, 홍화, MIX-2가 각각 24.06, 18.91, $41.61{\mu}g/mL$로 DPPH 라디칼 소거능과 유사한 경향을 보였다. 시료들의 항염증 효능을 측정하기 위해 5-LO 및 COX-2 효소 저해활성을 측정한 결과 단일 생약재 에탄올추출물보다 생약복합제 에탄올추출물이 5-LO와 COX-2 효소를 동시에 저해하는 효과가 증가되는 것으로 나타났다. 염증유발 효소 저해활성이 우수했던 생약복합제 에탄올추출물들의 NO 소거활성을 비교한 결과, MIX-2 에탄올추출물이 $50{\mu}g/mL$의 농도에서부터 유의적으로 NO의 생성을 저해하는 것을 확인하였다. 따라서 단일 생약재 보다는 생약복합제가 서로 혼합되면서 시너지 효과가 나타나는 것으로 생각되며 앞으로 명확한 기전에 대한 연구들이 지속된다면 기능성 식품 소재로서의 이용이 가능할 것으로 생각된다.

• 생명과학회지
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• 제19권10호
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• pp.1396-1402
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• 2009

본 연구에서는 갈조류의 일종인 톳(H. fusiforme)의 항염증 효과에 관한 생화학적 기전 해석을 위하여 U937 단핵구 세포를 이용하였으며, PMA에 의하여 인위적으로 유발된 COX-2의 발현 및 $PGE_2$의 생성 증가에 미치는 몇 가지 톳 추출물의 영향을 조사하였다. PMA는 U937 세포에서 처리 농도 의존적으로 COX-2의 전사 및 번역수준의 발현을 증가시켰으나, COX-1의 발현에는 큰 변화가 없었다. PAM에 의한 COX-2의 발현 증가는 $PGE_2$ 생성 증가와 연관성이 있었고, 톳의 열수 추출물에 비하여 에탄올 및 메탄올 추출물은 COX-2의 발현 증가는 $PGE_2$ 생성 증가를 매우 억제시켰으나, COX-1의 발현에는 영향을 주지 않았다. 아울러 PMA에 의한 NF-$\kappa$B의 핵내 이동 및 I$\kappa$B의 분해를 톳의 에탄올 및 메탄올 추출물이 완벽하게 차단시켰다. 본 연구의 결과는 톳의 에탄올 및 메탄올 추출물이 NF-$\kappa$B의 활성을 차단함으로서 COX-2의 발현 및 $PGE_2$ 생성을 저해하였음을 의미하며, 이는 톳이 강력한 항염증 효능을 가지고 있음을 뒷받침하여 주는 것이다.

• Food Science and Biotechnology
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• 제15권2호
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• pp.317-320
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• 2006

Octadeca-9,12-dienyl-3,4,5-hydroxybenzoate (GA-LA) was chemically synthesized from gallic acid and linoleic acid ester, and its biological functions were tested. Radical-scavenging activity of GA-LA was comparable to those of gallic and ascorbic acids at 0.24 mM, and tyrosinase inhibition effect was higher than that of ascorbic acid. Gallic and linoleic acids did not show any tyrosinase activity. Results of cyclooxygenase (COX) inhibition effect indicate GA-LA has higher selectivity in COX-1 inhibition. GA-LA from gallic and linoleic acids could be used as functional reagent for antioxidative, skin-whitening, and anti-inflammatory effects in food, pharmaceutrical, and cosmetic industries.

• 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.

• 생명과학회지
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• 제18권4호
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• pp.509-514
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• 2008

동 ${\cdot}$ 식물의 추출물은 예로부터 생약으로 많이 이용이 되었는데, 이는 추출물 내에 다양한 생리 활성 물질 및 화합물을 포함 하고 있기 때문이다. 본 연구는 한방에서 누고(樓姑)라고 알려진 땅강아지 추출물에 대한 항산화 활성을 1,1-diphenyl-2-picrylhydrazyl (DPPH)와 ferric reducing ability of plasma (FRAP)활성 실험을 통하여 알아보았다. 땅강아지는 DW, DMSO, 에탄올, 메탄올에 추출하였다. 실험 결과 땅강아지 추출물의 항산화활성은 DPPH radical 소거 활성의 경우 에탄올 추출물에서 가장 높은 활성을 나타났다. FRAP 활성의 경우 DW 추출물에서 가장 높게 나타났으며, 시간에 따른 활성의 증가는 에탄올 추출물에서 가장 높게 나타났다. Cyclooxygenase-2 promoter의 활성 저해는 DMSO와 에탄올 추출물에서 저해활성이 상대적으로 높은 것으로 미루어 보아서 이들 추출물간의 특성을 잘 응용할 경우 항산화 및 항염증에 좋은 생물학적 재료가 될 것으로 판단된다.

• Journal of Applied Biological Chemistry
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• 제65권1호
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• pp.23-31
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• 2022

Oxidative stress and neuroinflammation play important roles in the pathogenesis of Alzheimer's disease (AD). This study investigated the protective effects of paeoniflorin (PF) against neuronal oxidative stress and neuroinflammation in lipopolysaccharide (LPS)-induced mice. The brains of LPS-injected control group showed significantly increased neuroinflammation by activating the nuclear factor kappa B (NF-κB) pathway and increasing inflammatory mediators. However, administration of PF significantly attenuated oxidative stress by inhibiting lipid peroxidation, nitric oxide levels, and reactive oxygen species production in the brain; PF at doses of 5 and 10 mg/kg/day downregulated the expression of NF-κB pathway-related proteins and significantly decreased inflammatory mediators including inducible nitric oxide synthase and cyclooxygenase-2. Moreover, the levels of brain-derived neurotrophic factor and its receptor, tropomycin receptor kinase B, were significantly increased in PF-treated mice. Furthermore, acetylcholinesterase activity and the ration of B-cell lymphoma 2 (Bcl-2)/Bcl-2 associated X were significantly reduced by PF in the brains of LPS-induced mice, resulting in the inhibition of cholinergic dysfunction and neuronal apoptosis. Thus, we can conclude that administration of PF to mice prevents the development of LPS-induced AD pathology through the inhibition of neuronal oxidative stress and neuroinflammation, suggesting that PF has a therapeutic potential for AD.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.202.4-203
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• 2003

The present study was carried out to clarify whether isoflavonoids isolated from Belamcandae Rhizoma (Iridaceae) inhibit inflammation and angiogenesis by the experimental methods in vitro and in vivo. Among the isolated isoflavonoids, such as irigenin, irisflorentine, and iristectorene B inhibited nitric oxide (NO) production, as measured by nitrite formation at 3-30 ${\mu}M$. Also these compounds reduced cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) enzyme expression in a concentration dependent manner, when measured by western blotting, at 3-30 ${\mu}M$. Irigenin, irisflorentine and iristectoren B decreased angiogenesis of chick embryos in the chorioallantoic membrane assay. These compounds also reduced the proliferation of calf pulmonary arterial endothelial (CPAE) cells and found to possess relatively weak gelatinase/collagenase inhibitory activity in vitro. These compounds, when administered subcataneously at the dose of 30mg/kg for 20 days to mice implanted with murine Lewis lung carcinoma (LLC), caused a significant inhibition of tumor volume. Therefore, antiangiogenic activities of isoflavonoids from Belamcandae Rhizoma might be due to antiproliferative activities under inhibition the induction of COX-2 and iNOS enzyme.

• Biomolecules & Therapeutics
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• 제27권4호
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• pp.381-385
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• 2019

We attempted to examine anti-inflammatory and anti-oxidant effects of 4'-O-${\beta}$-D-glucosyl-5-O-methylvisamminol (GOMV), the first epigenetic inhibitor of histone phosphorylation at Ser10. While GOMV did not affect the viability of murine macrophage RAW 264.7 cells, it significantly suppressed lipopolysaccharide (LPS)-induced generation of prostaglandin $E_2$ ($PGE_2$) and nitric oxide (NO) through transcriptional inhibition of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS). GOMV also scavenged free radicals in vitro, increased NF-E2-related factor 2 (NRF2), and activated antioxidant response element (ARE), thereby resulting in the induction of phase II cytoprotective enzymes in human keratinocyte HaCaT cells. Finally, GOMV significantly protected HaCaT cells against 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced oxidative intracellular damages. Together, our results illustrate that GOMV possesses anti-inflammatory and anti-oxidant activity.

• 동의생리병리학회지
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• 제24권2호
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• pp.242-248
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• 2010

The present study was designed in order to determine whether Lonicerae flos (LF) could mitigate rheumatoid arthritis through inhibition of cyclooxygenase (COX)-2 and matrix metalloproteinase (MMP)-9 by regulation of macrophage migration inhibitory factor (MIF). We found that MIF mRNA expression in synoviocytes stimulated with phorbol-12-myristate-13-acetate dose-dependantly decreased by LF extract treatment (0.4 - 1.0 mg/$m{\ell}$). The distribution of MIF, COX-2 and MMP-9 positive reacted cells in LPS induced arthritis of mice were decreased by LF (45 mg/kg/day) treatment for 28 days. These data likely indicate that LF may act as MIF inhibitor and may be possible to develop useful agent for rheumatoid arthritis.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.235.2-235.2
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• 2003

To decipher the structure-activity relationships of flavones for the inhibition of cyclooxygenase-2 catalyzed prostaglandin production, we synthesized 7-methxoyflavones, 7-hydroxyflavones, 5-methxoyflavones, 5-hydroxyflavones and flavones without any phenol group on A ring. Methoxyflavones were prepared from 2.6- and 2,4-dihydroxyacetophenones in 3 steps. Most of the methxoyflavones were converted to the corresponding hydroxyflavones by the reaction with BBr3 in good yields. (omitted)