• 한국식품영양과학회지
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• 제37권9호
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• pp.1109-1113
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• 2008

본 연구에서는 아로니아 추출물의 항산화제와 항알레르기 치료제로써의 유효성을 알아보기 위해 페놀성 화합물 및 플라보노이드 함량과 DPPH 라디칼 포착효능, superoxide 음이온 라디칼 포착효능, 5-LO억제 효능 및 COX억제효능을 측정하였다. 측정결과 아로니아는 유효성분으로 예상되는 페놀성 화합물과 플라보노이드가 각각 $745.4{\pm}3.7\;mg/g$, $74.63{\pm}2.2\;mg/g$으로 상당량 함유되어 있으며, 상당히 낮은 농도($6.15{\pm}0.343\;ppm$, $6.99{\pm}1.26\;ppm$)에서 DPPH 라디칼과 superoxide 음이온 라디칼을 50% 소거하는 것으로 나타났다. 아로니아의 항알레르기 효능에 관하여 5-LO의 $IC_{50}$값이 $47.07{\pm}0.15\;ppm$으로, EGCG의 $IC_{50}(15.83{\pm}0.98\;ppm)$보다는 높았지만 아로니아가 EGCG와 같은 단일물질이 아니라 천연혼합물임을 감안하여 다른 천연물들의 $IC_{50}$값과 비교하였을 때 5-LO를 비교적 낮은 농도에서 억제하고 있다고 볼 수 있다. 또한, COX-1과 COX-2의 저해 비율 비교를 통해 양성대조군으로 사용한 EGCG만큼 COX-2를 선택적으로 저해하고 있음을 확인하였다. 이상의 결과에 따르면 아로니아 추출물은 항산화 및 항알레르기 효능을 갖고 있으며, 따라서 알레르기성 비염이나 아토피와 같은 알레르기 관련 질병 치료에 유효하게 사용될 것이라 생각된다.

• 대한한의학회지
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• 제24권2호
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• pp.94-108
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• 2003

Objectives : This study was carried out to investigate the anti-ulcer effects of Pyeongwibunsoeum extract and Misoprostol on indomethacin-induced gastric mucosal lesions of mice. Methods : Experimental groups were classified into non-treated group, non-administered group, Misoprostol-administered group and Pyeongwibunsoeum-extract-administered group. This study examined the morphological change, distribution of mast cells and apoptic cells, PNA reaction, COX-1, BrdU, NF-B p50, COX-2, IL-2R-, and ICAM-1of gastric mucosa. Results : 1. The hemorrhagic erosion of gastric mucosa was reduced in the Misoprostol-administered and Pyeongwibunsoeum-extract-administered groups. 2. The Misoprostol-administered group and Pyeongwibunsoeum-extract-administered group showed positive reaction on the PNA distribution. 3. The distribution of apoptic cells, activity of NF-B p50, COX-2, IL-2R-, and ICAM-1 decreased in both the Misoprostol-administered group and Pyeongwibunsoeum-extract-administered group. 4. The Misoprostol-administered and Pyeongwibunsoeum-extract-administered groups showed increase on COX-1, BrdU. Conclusions : As the results indicate, hemorrhagic erosion of gastric mucosa were reduced in both the Misoprostol-administeredand Pyeongwibunsoeum-extract-administered groups, and severe inflammatory reaction of gastric mucosa was reduced. The effects on the Pyeongwibunsoeum-extract-administered group were superior to those on the Misoprostol-administered group. Pyeongwibunsoeum extract can be widely administered for gastric ulcer disease in clinical treatments.

• 대한한의학회지
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• 제29권5호
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• pp.111-117
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• 2008

Objectives and methods : Previous mechanistic studies suggest the cyclooxygenase-2 (COX-2) inhibitors represent the good candidates against tumor progression. MeOH extract of the stem barks of Euonymus alatus induced the strong inhibition of COX-2. A phenolic compound responsible for the anti- COX-2 known to involve in tumor adhesion and invasion has been studied through the methanol extracts. The compound, rosmarinic acid (ROS-A) was an ester of caffeic acid and 3,4-dihydroxyphenyllactic acid. ROS-A showed a strong inhibitory effect of COX-2 activity in a concentration-dependent manner. Then we have measured the IL-1${\beta}$, IL-6 and TNF-${\alpha}$ production related the immune regulation, induction of inflammatory related genes. Results and Conclusions :Hep3B cells produce proinflammatory cytokines of IL-1${\beta}$, IL-6 and TNF-${\alpha}$ while ROS A inhibited the cytokines production. Since IL-1${\beta}$, IL-6 and TNF-${\alpha}$ need the transcription factors such as nuclear factor- ${\kappa}$B (NF-${\kappa}$B) and activated protein-1 (AP-1), we measured the transcription factors. ROS-A inhibited the activation of p65, p50, c-Rel subunits of NF-${\kappa}$B and AP-1 transcription factors. These findings indicate that ROS A from the stem bark of E. alatus inhibits proliferation in metastatic cancer cells. It was suggested that stem barks of E. alatus could be suitable for anti-cancer drugs.

• 대한한방부인과학회지
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• 제36권3호
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• pp.1-24
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• 2023

Objectives: Boeum-jeon (BEJ) is a herbal formula composed 8 Korean medicinal herbs and is traditionally used to treat inflammatory diseases. In this study, the authors tried to confirm the antioxidant efficacy of BEJ and its anti-inflammatory effect in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. Methods: In this experiment, results of BEJ on the following two were measured as follows: (1) Antioxidant effects was measured by DPPH Radical scavenging Activity, ABTS Radical scavenging Activity. (2) Anti-Inflammatory effects were evaluated by the production amount of ROS, NO, Cytokine (PGE2, IL-1β, IL-6, TNF-α), COX-2, iNOS, TNF-α, IL-1β, IL-6, HO-1, NQO1 (the previous seven are "mRNA Expression"), COX-2, iNOS, TNF-α, IL-1β, IL-6, HO-1, NQO1, NRF2 (the previous eight are "Protein Expression") ERK, JNK, p38 (the previous three are "Protein Phosphorylation") in LPS-stimulated RAW 264.7 cells. Results: The experimental measurement results are as follows: (1) DPPH Radical scavenging Activity, ABTS Radical scavenging Activity increased in a concentration -dependent manner in the BEJ-treated group. (2) As a result of measuring anti-inflammatory efficacy, the production of ROS, NO, and Cytokine (PGE2, TNF-α, IL-1β, IL-6) in the BEJ-administered group was significantly reduced compared to the control group. (3) Among mRNA Expression levels, COX-2, iNOS, IL-1β, IL-6 and TNF-α was significantly decreased in a concentration-dependent manner than in the control group, and HO-1 and NQO1 were significantly increased in a concentration -dependent manner than in the control group. (4) Among the Protein Expression levels, COX-2, iNOS, IL-1β, IL-6 and TNF-α was significantly decreased in a concentration -dependent manner compared to the control group, and HO-1, NQO1 and NRF2 was significantly increased in a concentration-dependent manner compared to the control group. (5) As a result of Protein Phosphorylation, ERK, p38 and JNK was significantly decreased compared to the control group in a concentration-dependent manner. Conclusions: Boeum-jeon has been experimentally confirmed to have antioxidant and anti-inflammatory effects, and if the evidence for efficacy is reinforced through further studies such as in vivo studies and clinical trials in the future, it can be effectively used to treat various inflammatory diseases such as bladder inflammation and chronic pelvic inflammation.

• Archives of Pharmacal Research
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• 제28권8호
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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.

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.138.2-138.2
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• 2002

• 한방안이비인후피부과학회지
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• 제18권1호
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• pp.154-171
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• 2005

Herbal mixture water extract of (Rheum coreanum Scutellaria baikalensis, Phellodendron amurese), which exhibit several beneficial effects including acne and skin diseases, was tested for anti-microbial activity and anti-inflammation effects. The herbal mixture extract showed antimicrobial activity against Stapylococcus epidermis and Propionbacterium acne. The growth of Stapylococcus epidermis and Propionibacterium acne was inhibited completely by addition of 1.0% of the extract. Also in the present study we examined the mixture extract on compound 48/80 induced allergy and LPS induced cyclooxygenase-2(COX-2) gene expression in RAW264.7 macrophage. The results indicated the ear swelling and histamine release induced by compound 48/80 were dose-dependently reduced, ranging 18-36% and 10-61%, respectively. Furthermore the extract inhibited the expression of LPS-induced COX-2 proteins and mRNAs without an appreciable cytotoxic effects on RAW264.1 cells. The cytotoxicity of the extract using MTT assay showed the cytotoxicity of 6% and 13% against L929 cell line. Based on these results, it is concluded that the herbal mixture water extract can be applied to this acne and skin diseases therapy.

• BMB Reports
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• 제42권5호
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• pp.277-280
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• 2009

We examined the effects of polysaccharides extracted from Asterina pectinifera on the activities of quinone reductase (QR), glutathione S-transferase (GST), ornithine decarboxylase (ODC), cyclooxygenase (COX)-2 and glutathione (GSH) levels in HT-29 human colon adenocarcinoma cells. We found that the polysaccharides extract induced QR activity in a dose-dependent manner over a concentration range of $20-60\;{\mu}g/ml$ and increased GST activity as much as 1.4-fold over controls. GSH levels were increased 1.3- and 1.5-fold with the extract at 40 and $60\;{\mu}g/ml$, respectively. The activity and protein expression of ODC in 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced colon cancer cells was inhibited by the extract. The polysaccharides suppressed TPA-induced prostaglandin (PG) production. These data indicate that polysaccharides from A. pectinifera increase phase II detoxification enzyme activity and inhibit ODC and COX-2 activities in HT-29 human colon adenocarcinoma cells. Consequently, this effect may contribute to the protective effect of polysaccharides from A. pectinifera against colon cancer.

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.339.1-339.1
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• 2002

Since two selective COX-2 inhibitors. celecoxib and rofecoxib, showed good biological activity as antiinflammatory agents. many medicinal chemists are interested in specific COX-2 inhibitors. The distinguished feature of these drugs is that the 5-membered heterocycle ring is substituted with two aryl groups. Therefore, in this study, we designed a new hydantoin derivatives via the reaction of unnatural amino acids as selective COX-2 inhibitors, In systematically steps. 5-phenyl-1 (or substituted) hydantoin derivatives were prepared through esterification. bromination, C-N bond formation, cyclization from phenyl acetic acid. Particularly. a novel hydantoin ring was converted from unnatural amino acids with potassium isoyanate. In last step. the final analogs were synthesized the substitution at 3-position with alkyl reagents.

• IMMUNE NETWORK
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• 제3권3호
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• pp.201-210
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• 2003

Objective: The role of prostaglandin $E_2$ (PGE2) in the etiopathogenesis of immune and inflammatory diseases has become the subject of recent debate. To determine the role of PGE2 in rheumatoid arthritis (RA), we tested the effect of exogenous PGE2 on the production of cyclooxygenase-2 (COX-2) by rheumatoid synoviocytes. Methods: Fibroblast-like synoviocytes (FLS) were prepared from the synovial tissues of RA patients, and cultured in the presence of PGE2. The COX-2 mRNA and protein expression levels were determined by RT-PCR and Western blot analysis, respectively. The PGE2 receptor subtypes in the FLS were analyzed by RT-PCR. Electrophoretic mobility shift assay (EMSA) was used to measure the NF-${\kappa}B$ binding activity for COX-2 transcription. The in vivoeffect of PGE2 on the development of arthritis was also tested in collagen induced arthritis (CIA) animals. Results: PGE2 ($10^{-11}$ to $10^{-5}M$) dose-dependently inhibited the expression of COX-2 mRNA and the COX-2 protein stimulated with IL-$1{\beta}$, but not COX-1 mRNA. NS-398, a selective COX-2 inhibitor, displayed an additive effect on PGE2-induced COX-2 downregulation. The FLS predominantly expressed the PGE2 receptor (EP) 2 and EP4, which mediated the COX-2 suppression by PGE2. Treatment with anti-IL-10 monoclonal antibodies partially reversed the PGE2-induced suppression of COX-2 mRNA, suggesting that IL-10 may be involved in modulating COX-2 by PGE2. Experiments using an inducer and an inhibitor of cyclic AMP (cAMP) suggest that cAMP is the major intracellular signal that mediates the regulatory effect of PGE2 on COX-2 expression. EMSA revealed that PGE2 inhibited the binding of NF-${\kappa}B$ in the COX-2 promoter via a cAMP dependent pathway. In addition, a subcutaneous injection of PGE2 twice daily for 2 weeks significantly reduced the incidence and severity of CIA as well as the production of IgG antibodies to type II collagen. Conclusion: Our data suggest that overproduced PGE2 in the RA joints may function as an autocrine regulator of its own synthesis by inhibiting COX-2 production and may, in part, play an anti-inflammatory role in the arthritic joints.