• Biomolecules & Therapeutics
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• 제21권1호
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• pp.72-78
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• 2013

This work aimed to assess some pharmacological activities of P. leptostachya var. asiatica Hara. The dried roots of P. leptostachya var. asiatica Hara were extracted with 70% ethanol to generate the powdered extract, named PLE. Anti-angiogenic activity was detected using chick chorioallantoic membrane (CAM) assay. In vitro anti-inflammatory activity was evaluated via analyzing nitric oxide (NO) content, inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage cells. Antioxidant activity was determined by 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay and reactive oxygen species (ROS) level in the stimulated macrophage cells. Matrix metalloproteinase-9 (MMP-9) and -2 (MMP-2) activities in the culture media were detected using zymography. PLE exhibits an anti-angiogenic activity in the CAM assay, and displays an inhibitory action on the generation of NO in the LPS-stimulated macrophage cells. In the stimulated macrophage cells, it is able to diminish the enhanced ROS level. It can potently scavenge the stable DPPH free radical. It suppresses the induction of iNOS and COX-2 and the enhanced MMP-9 activity in the stimulated macrophage cells. Both monooxygenase and oxidase activities of tyrosinase were strongly inhibited by PLE. Taken together, the dried roots of P. leptostachya var. asiatica Hara possess anti-angiogenic, anti-inflammatory, antioxidant and skin whitening activities, which might partly provide its therapeutic efficacy in traditional medicine.

• 약학회지
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• 제47권5호
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• pp.311-318
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• 2003

Eurya emarginata (Thunb.) Makino (Theaceae) is distributed in coastal areas of island. The leaves of Eurya are used in the traditional medicine of the coastal areas of jeju island with the aim of diuresis or to treat ulcers. Nevertheless, there are few reports on the biological activity and constituents of E. emarginata. In this study, we investigated the pharmacological activity of the solvent extracts of E. emarginata on the several inflammatory markers (TNF-$\alpha$, IL-1$\beta$, IL-6, NO, iNOS and COX-2). Also we examined the antioxidizing effect of the solvent extracts by determination of DPPH radical-scavenging activity. Among the solvent fractions, EtOAc and BuOH extracts showed potent radical scavenging activity (RC$_{50}$=10.9 and 12.7 respectively). The subtractions of EF 5-4-6-3-2 and BF 1 potentially inhibited the mRNA expression of pro-inflammatory cytokines (IL-1$\beta$, IL-6 and TNF-$\alpha$) at the concentration of 100 $\mu\textrm{g}$/mι. Also the fractions inhibited the mRNA expression of pro-inflammatory cytokines (IL-1$\beta$, IL-6 and TNF-$\alpha$) and protein expression of iNOS and COX-2 at the concentration of 100 $\mu\textrm{g}$/mι. And then, the inhibition of iNOS was correlated with the decrease of nitrite level. These results suggest that E. emarginata may have anti-inflammatory activity through the inhibition of pro-inflammatory cytokines, iNOS and COX-2.2.

• 한국축산식품학회지
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• 제32권5호
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• pp.635-643
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• 2012

As an appraisal for the application of a new starter culture, more than 200 lactic acid bacteria strains were isolated from raw milk and healthy human feces. The strains showing excellent growth and acid production ability in 10% skim milk media were selected and identified as Lactobacillus casei based on the results of their API carbohydrate fermentation patterns, as well as 16S rDNA sequence analysis. To assess the effect of L. casei strains on irritable bowel disease (IBD), the inhibitory effect of the selected strains against the nitric oxide (NO) production of lipopolysaccharide (LPS)-stimulated RAW 264.7 cells was measured. Among the tested L. casei strains, L. casei MCL was observed to have the greatest NO inhibitory activity. Additionally, L. casei MCL was found to inhibit mRNA expression of pro-inflammatory cytokines (interleukin-$1{\beta}$, IL-6, TNF-${\alpha}$), as well as cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) involved in pathophysiologic processes such as inflammation. The mRNA expression of anti-inflammatory cytokines, including IL-10 and transforming growth factor-$1{\beta}$ (TGF-${\beta}$) of L. casei MCL, was confirmed using quantitative real-time PCR. In conclusion, L. casei MCL showed decreases in the expression of pro-inflammatory cytokines and up-regulated expression of the anti-inflammatory cytokine.

• 한국환경과학회지
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• 제26권12호
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• pp.1355-1362
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• 2017

This study was performed to evaluate the possibility of application of lactic acid bacteria fermentation to increase the anti-allergic activity of the extracts from Houttuynia cordata Thunb. H. cordata Thunb was fermented on 25, 30, 35 and $40^{\circ}C$ for 5 days by two species of lactic acid bacteria, Leuconostoc mesenteroides 4395 and Lactobacillus sakei 383. The anti-allergic activity of water extracts of H. cordata Thunb was then analyzed both before and after fermentation. Anti-allergic activity was determined in vitro assays by using 5-lipoxygenase (5-LO), cyclooxygenase-2 (COX-2) and ${\beta}$-hexoseaminidase release of RBL-2H3 cells (degranulation marker). The extracts fermented at $35^{\circ}C$ by both bacteria had the highest inhibitory activities against 5-LO, and also higher than the control, and the one fermented at $30^{\circ}C$ by both bacteria had the highest inhibitory activity against COX-2. The degranulation of RBL-2H3 cells induced by IgE-antigen complex was estimated as ${\beta}$-hexoseaminidase release rate as reference of 100%, the release rates were inhibited in $25{\mu}g/ml$ of the extracts fermented at 30, 35 and $40^{\circ}C$ only by L. mesenteroides 4395. These results indicate that anti-allergic activity of H. cordata Thunb is increased by lactic acid bacteria fermentation.

• 한국식품영양과학회지
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• 제36권6호
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• pp.670-677
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• 2007

산화적인 스트레스(oxidative stress)는 신경염증의 발병 요인 중의 하나로 알려져 있다. 이에 본 연구는 약용곤충으로 알려진 청동풍뎅이(Anomala albopilosa) 성충과 3령 유충(궁벵이) 에탄올 추출물을 대상으로 항산화활성을 비교 측정하였으며, 또한 대식세포인 RAW 264.7 세포에서의 NO 의 생성억제 효과 및 세포독성 그리고 분자 염증관련 인자인 iNOS, COX-2와 $PGE_2$ 생성 및 활성 억제를 조사하여 항염 증효과 등의 생리활성을 측정 비교하였다. 우선, 분자염증은 활성산소 관련의 물질과 밀접한 관련이 있으므로 향산화 실험과 관련하여 청동풍탱이 성충과 3령 유충 에탄올 추출물 의 DPPH(1,1-diphenyl-2-picrylhydrazyl) radical 소거능, superoxide radical 소거능, xanthine oxidase 저해활성 그리고 nitric oxide 소거능에 대한 항산화활성 등의 assay를 실시하였다. 그 결과, 청동풍뎅이 에탄올 추출물은 항산화능을 갖고 있었으며, 3령 유충 추출물에서보다는 성충 추출물에서 다소 높은 항산화활성을 보여주었다. 또한 RAW 264.7 세포에 LPS로 자극을 주고 청동풍뎅이 성충과 3령 유충 에탄올 추출물을 처리하여 항염증관련 활성을 확인해본 결과, 고농도에서는 다소 세포독성을 나타냈지만 농도의존적으로 NO, iNOS, COX-2 그리고 $PGE_2$의 생성 억제효과가 나타났다. 이러한 결과는 유용곤충자원을 이용한 유효성분 추출을 통한 항산화 및 항염증 물질의 연구 또는 예방하거나 치료할수 있는 염증 억제 성분의 분리 및 그 작용기전 연구에 중요한 기초 자료가 될 것이라 사료된다.

• 한국식품과학회지
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• 제41권4호
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• pp.405-412
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• 2009

본 연구는 꾸지뽕 나무 열매로부터 75 kDa의 당단백질(꾸지뽕 당단백질)을 추출한 후 꾸지뽕 당단백질의 첨가에 따른 알레르기성 염증 인자인 histamine 유리 억제능력 및 COX-2의 활성 억제 효과를 평가하였다. RBL-2H3세포를 22시간 동안 IgE로 감작시킨 후, HSA를 처리하여 histamine의 유리양을 측정한 결과 꾸지뽕 당단백질을 처리한 농도가 증가함에 따라 histamine의 유리와 COX-2의 활성 억제율은 증가하였다. 또한 꾸지뽕 당단백질의 처리는 HSA에 의해 유도된 세포내 ROS 생성량을 농도에 의존적으로 억제하였다. 한편 꾸지뽕 당단백질을 농도별로 처리하여 세포내 단백질을 추출하여 western blot을 실시한 결과 100 ${\mu}g$/mL 농도의 꾸지뽕 당단백질을 처리한 그룹에서 ERK1/2, AP-1과 COX-2의 활성 수준은 현저히 억제 되었다(p<0.05). 따라서 이러 한 결과에 미루어볼 때, 꾸지뽕 당단백질은 세포내 해독효소의 활성을 증가시킴으로써 ROS 수준을 감소시켰으므로 꾸지뽕 당단백질의 역할이 다른 천연물 유래의 당단백질과 마찬가지로 특이적인 항산화 능력을 지니고 있음을 나타내며 histamine의 유리 억제와 COX-2의 활성이 억제되었을 것으로 생각된다. 이는 꾸지뽕 당단백질이 항 알레르기 효능을 갖는 물질로써 알레르기성 비염, 아토피 등과 같은 알레르기 관련 질환의 예방 및 치료제로 사용될 수 있을 것 사료된다.

• Journal of Acupuncture Research
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• 제29권1호
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• pp.127-137
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• 2012

Objectives : The purpose of this study is to investigate the effect of $Clematidis$ radix herbal-acupuncture solution, on collagen, adjuvant, lipopolysaccharide and phospholipase A2 induced rheumatoid arthritis in mice. Methods : Arthritis index was measured for mouse that was injected subcutaneously in solution mixed chicken type II collagen with Freund's complete adjuvant. We injected Freund's complete adjuvant into right posterior part of the sole of a ICR mouse foot, which was measured by plethysmometer. The solution mixed $CRHS$ with Tris-HCI, $CaCl_2$, substrate, enzyme was done a chemical action for thirty minutes, and then inhibitory activity of PLA2 enzyme was expressed with inhibition percentage by utilizing isolated arachidonic acid. COX-2 was induced by adding LPS to RAW 264.7 cell, and COX-2 activity was measured by western blot analysis and $PGE_2$ Biotrak kit. Results : $CRHS$ also inhibited Freund's complete adjuvant induced chronic rheumatoid arthritis in mice. $CRHS$ showed significant inhibition of type I and type II $PLA_2$ activities in a dose dependent manner. Furthermore, $PGE_2$ production was decreased with $CRHS$ and lipopolysaccharide-induced COX-2 protein expression was significantly inhibited by $CRHS$. Conclusions : These results suggest that $CRHS$ has an therapeutic effect on drug induced-rheumatoic arthritis by inhibiting $PLA_2$ and COX-2 activities.

• Natural Product Sciences
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• 제9권2호
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• pp.93-96
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• 2003

This research was undertaken to find the in vitro inflammatory action of the essenetial oil (CS-oil) extracted from Chrysanthemum sibiricum (Compositae) herbs. We investigated the effects of the CS-oil not only on the formation NO, $PGE_2$, and $TNF-{\alpha}$ but also on inducible nitric oxide synthase and cyclooxygenase-2 (COX-2) in lipopolysaccharide (LPS)-induced murine macrophage RAW 264.7 cells. The data obtained were consistent with the modulation of iNOS enzyme expression. A similar fashion was also observed when LPS-induced $PGE_2$ release and COX-2 expression were tested. The significant inhibitory effects were shown in concentration-dependent manners. In addition, CS-oil also mildly but significantly reduced the formation of TNF-a. These findings support the application of CS-oil as an antiinflammatory essential oil.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 2003년도 Annual Meeting of KSAP : International Symposium on Pharmaceutical and Biomedical Sciences on Obesity
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• pp.101-101
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• 2003

Prostaglandins (PGs) and nitric oxide (NO) produced by inducible cyclooygenase (COX-2) and nitric oxide synthase (iNOS), respectively, have been implicated as important mediators in the process of inflammation and carcinogenesis. On this line, the potential COX-2 or iNOS inhibitors have been considered as anti-inflammatory and cancer chemopreventive agents. In our continuing efforts of searching for novel cancer chemopreventive agents from natural products, we isolated natural sesquiterpenoids as potential COX-2 and iNOS inhibitors in cultured lipopolysaccharide (LPS)-activated mouse macrophage RAW 264.7 cells. Alantolactone, a natural eudesmane-type sesquiterpenoid, exhibited a potent inhibition of COX-2 (IC50 = 0.4 $\mu\textrm{g}$/$m\ell$) and iNOS activity (IC50 = 0.08 $\mu\textrm{g}$/$m\ell$) in the assay system determined by PGE2 and NO accumulation, respectively. The inhibitory potential of alantolactone on the PGE2 and NO production was well coincided with the suppression of COX-2 and iNOS protein and mRNA expression in LPS-induced macrophages. Furthermore, alantolactone inhibited NF-kB but not AP-l binding activity on nuclear extracts evoked by LPS-stimulated macrophage cells, suggesting the possible involvement of NF-kB in the regulation of COX-2 and iNOS expression. In further study with COX-2-expressing human colon HT-29 cells, alantolactone inhibited the cell proliferation, down-regulated COX-2, and inhibited the ERK phosphorylation in the early time. These results suggest that a natural sesquiterpenoid alantolactone might be a potential lead candidate for further developing COX-2 or iNOS inhibitor possessing cancer chemopreventive or anti-inflammatory activity

• 동의생리병리학회지
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• 제22권4호
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• pp.878-883
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• 2008

Conchiolin is a complex protein which is secreted by the mollusc's outer epithelium to be the organic basis of mollusc shell. This study is to investigate a potential anti-inflammatory activity of conchiolin of oyster shell (COS). We tested the effects of COS on the lipopolysaccharide (LPS)-induced production of nitric oxide (NO) and prostaglandin E2 (PGE 2) in a murine macrophage cell line, RAW 264.7. COS inhibited production of NO and PGE2 in a dose dependent manner and also decreased the expression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), tumor necrosis $factor-{\alpha}$ ($TNF-{\alpha}$) and interleukin-6 (IL-6). These results suggest that COS can inhibit production of pro-inflammatory mediators and might be a useful source to treat inflammation.