• 대한화장품학회지
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• 제45권3호
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• pp.287-297
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• 2019

본 연구는 청보리 추출물 및 용매 분획물의 항산화 활성, 항염활성 및 미백 활성을 평가하기 위해 수행하였다. 청보리의 용매별 분획물의 총 폴리페놀 함량은 13.58 ~ 40.06 mg GAE/g, 총 플라보노이드 함량은 7.67 ~ 13.67 mg CE/g으로 확인되었다. 청보리 용매 분획물의 1,1-diphenyl-2-picrylhydrazyl(DPPH) 라디칼 소거활성을 평가한 결과 클로로폼 분획물 $400{\mu}g/mL$ 처리 시 대조구인 ascorbic acid ($30{\mu}M$)와 유사한 DPPH 라디칼소거능이 확인되었다. RAW 264.7 세포를 대상으로 한 NO생성 억제 활성 평가에서는 클로로폼 및 헥산 분획물이 대조구인 quercetin ($15{\mu}M$)과 유사한 활성이 확인되었으며, 클로로폼 분획물 $100{\mu}g/mL$ 처리 시 IL-6, iNOS 및 COX2 유전자의 발현이 대조구 (lipopolysaccharide $1{\mu}g/mL$) 보다 통계적으로 유의한 수준으로 감소함이 확인되었다. 청보리 용매 분획물 중 클로로폼 분획물은 RBL-2H3 세포의 ${\beta}$-hexosaminidase 탈과립, IL-4 및 IL-13 유전자의 발현을 유의한 수준으로 억제하는 것이 확인되었다. 청보리 용매 분획물은 tyrosinase활성을 농도 의존적으로 억제하였으며, 헥산 분획물 $50{\mu}g/mL$ 및 클로로폼 분획물 $100{\mu}g/mL$은 유의한 수준으로 B16F10 세포의 멜라닌 생성을 억제하는 것이 확인되었다. 이러한 결과들은 청보리가 항염 및 미백 활성을 가지는 효과적인 화장품 소재로 활용 가능하다는 것을 시사한다.

• Journal of Microbiology and Biotechnology
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• 제17권9호
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• pp.1554-1557
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• 2007

Artemisia princeps Pampanini (AP) was fermented with Bifidobacterium infantis K-525 and its antiasthmic effect investigated. AP and fennented AP (FAP) reduced the IgE level in the blood of ovalbumin-induced asthmic mice. Moreover, FAP reduced the IgE, proinflammatory cytokine IL-6, and IL-4 levels in the trachea, as well as in the lung of the experimental asthmic mice, whereas AP only reduced the IgE and IL-6 levels in the lungs. Nonetheless, AP and FAP both inhibited the mRNA expression of IL-6 and TNF-${\alpha}$ in IgE-induced RBL-2H3 cells. The in vivo antiasthmic effect of FAP was more potent than that of AP. Therefore, these findings suggest that the enhanced antiasthmic effect of AP after bifidus fermentation was possibly due to the regulation of the proinflammatory cytokine biosynthesis of IL-6 and TNF-${\alpha}$.

• Advances in Traditional Medicine
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• 제4권1호
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• pp.60-64
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• 2004

The effect of aqueous extract of processed Xanthii fructus (PXF) on cell viability and histamine release from mast cell has been investigated. PXF showed higher cell viability than unprocessed Xanthii fructus (XF) at the concentrations of 5 and 10 mg/ml. Aqueous extract of PXF and unprocessed XF inhibited compound 48/80-induced systemic anaphylaxis in mouse. Both PXF and unprocessed XF dose-dependently inhibited histamine release from rat peritoneal mast cells by compound 48/80 to the similar extent at 0.01, 0.1 and 1 mg/ml. Our studies provide evidence that processing of XF may be beneficial to reduce cytotoxicity in high concentration (at 5 and 10 mg/ml) but does not affect on anti-allergic activity.

• Biomolecules & Therapeutics
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• 제19권1호
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• pp.102-108
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• 2011

We examined the effects of essential oil from Thujopsis dolobrata Sieb. et Zucc. var. hondai Makino (EOTD) (Cupressaceae) on atopic dermatitis (AD)-like skin lesions in NC/Nga mice. Treatment with EOTD twice daily for two weeks ameliorate AD-like skin lesions induced by DNCB (2,4 dinitrochlorobenzene), and clinical scores were reduced to 7.29, 7.07, and 4.5 points in the groups treated with 1.5%, 3.0%, and 6.0% extract (p<0.01) respectively, from the 15.0 score obtained using vehicle. EOTD inhibited the infiltration of mast cells into the AD-like skin lesion in NC/Nga mice (p<0.01) and also reduced serum histamine and IgE levels (p<0.05). Furthermore, it dose-dependently inhibited the release of beta-hexosaminidase from rat basophilic leukemia RBL 2H3 cells. These results indicate that EOTD reduces AD-like skin lesions by inhibiting the production of IgE and histamine, and, thus, IgE-mediated degranulation.

• Molecules and Cells
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• 제41권6호
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• pp.545-552
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• 2018

Spleen tyrosine kinase (SYK) is a cytosolic non-receptor protein tyrosine kinase. Because SYK mediates key receptor signaling pathways involving the B cell receptor and Fc receptors, SYK is an attractive target for autoimmune disease and cancer treatments. To date, representative oral SYK inhibitors, including fostamatinib (R406 or R788), entospletinib (GS-9973), cerdulatinib (PRT062070), and TAK-659, have been assessed in clinical trials. Here, we report the crystal structures of SYK in complex with two newly developed inhibitors possessing 4-aminopyrido[4,3-D]pyrimidine moieties (SKI-G-618 and SKI-O-85). One SYK inhibitor (SKI-G-618) exhibited moderate inhibitory activity against SYK, whereas the other inhibitor (SKI-O-85) exhibited a low inhibitory profile against SYK. Binding mode analysis indicates that a highly potent SYK inhibitor might be developed by modifying and optimizing the functional groups that interact with Leu377, Gly378, and Val385 in the G-loop and the nearby region in SYK. In agreement with our structural analysis, one of our SYK inhibitor (SKI-G-618) shows strong inhibitory activities on the ${\beta}$-hexosaminidase release and phosphorylation of SYK/Vav in RBL-2H3 cells. Taken together, our findings have important implications for the design of high affinity SYK inhibitors.

• Journal of Applied Biological Chemistry
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• 제58권1호
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• pp.13-19
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• 2015

본 연구에서는 우슬 열수 추출물을 n-BuOH과 $H_2O$로 용매 분획 한 후 n-BuOH 분획물을 컬럼 크로마토그래피를 수행하여 6개의 소분획물(Fr. 1-6)을 얻었다. 소분획물 6개에 대해 tumor necrosis factor (TNF)-${\alpha}$ 저해활성 검정을 통하여 가장 높은 활성을 나타낸 분획물 5에서 preparative-high performance liquid chromatography를 이용해 3종의 phytoecdysone계열 화합물들을 분리하였다. 분리된 화합물들은 NMR 및 MS 분석을 통해 ecdysterone (1), 25S-inokosteron (2), 25R-inokosteron (3)임을 동정 하였고, 이들의 활성은 TNF-${\alpha}$ 생산 저해활성은 $200{\mu}g/mL$에서 80-95%의 TNF-${\alpha}$ 저해활성을 나타내었다. 또한 각질형성 세포에 분리한 3종의 화합물을 처리한 결과 각각 51와 23% 이상의 TARC의 생성 억제 효과를 확인 할 수 있었다. 이들의 결과로써, 우슬 추출물과 분리된 화합물들에 대한 항 아토피 활성 결과로 천연물 기능성 식품 또는 화장품으로의 응용가능성이 높다고 사료된다.

• Journal of Pharmaceutical Investigation
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• 제41권6호
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• pp.355-362
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• 2011

This work was performed to investigate the protective effect of ethanol extract (AEx) from acorn (Quercus acutissima CARR.) against allergic mediated responses in asthma model cells and mice. The AEx inhibited antigen-stimulated cytokine production such as interleukin (IL)-4, IL-13 and tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$) and AEx also inhibited intracellular reactive oxygen species (ROS) generation against IgE-mediated allergic response in rat basophilic leukaemia RBL-2H3 cells. The ovalbumin (OVA)-sensitized mice were orally administered with AEx (100 or 300 mg/kg) and authentic tannic acid (75 mg/kg) every day for 15 days. Increased TNF-${\alpha}$ production by OVA-sensitization/challenge was significantly reduced by administration of AEx. The serum triglyceride levels of asthma mice were significantly reduced after feeding for 15 days with tannic acid or AEx. The mice fed with tannic acid or AEx also exhibited a significant reduction in body weights compared to those of asthma control group. The AEx increased the heme oxygenase (HO)-1 mRNA expression in the asthma model mice and showed DPPH radical scavenging activity. These results indicate that AEx protects against IgEmediated allergic and OVA-induced asthmatic responses via direct and indirect antioxidant activities. Reduced triglyceride and body weights may provide additional protective benefits of AEx on allergic asthma.

• Biomolecules & Therapeutics
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• 제19권1호
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• pp.126-133
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• 2011

The fruit of Actinidia arguta (AA) has been used mainly for the treatment of skin diseases, diuresis, diabetes mellitus and osteoporosis in Korean traditional medicine. It is known that AA (hardy kiwi) fruit extract has an effect on 2-chloro-1,3,5-trinitrobenzene-induced atopic dermatitis-like skin lesions in NC/Nga mice. Mode of action for it is associated with the modulation of biphasic Th1/Th2 cytokines. Furthermore, DA9102 containing AA is a herbal medicine currently under phase II clinical trial for atopic dermatitis in Korea. However, no active principles of AA on the decrease of Th2 cytokines including IL-4 and IL-10 have been identified. In this study, bioactivity-guided fractionation of an alcohol extract from the dried fruits of AA using ELISA assay for IL-4 production led to the isolation of $\alpha$-linolenic acid (I), linoleic acid (II), ethyl linolenate (III), ethyl linoleate (IV) and ethyl stearate (V) as the major active components. These compounds showed the down-regulatory effects of IL-4 production in A23187-stimulated RBL-2H3 cells without cytotoxicity.

• 한국식품영양과학회지
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• 제38권8호
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• pp.977-982
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• 2009

비파엽 열수추출물을 이용하여 항산화성과 항히스타민 및 항염증 효과를 조사하였다. 비파엽 열수추출물의 총 폴리페놀 함량은 28.91$\pm$2.1 mg/g, 총 플라보노이드 함량은 10.54$\pm$4.6 mg/g으로 분석되었다. 전자공여능은 400 $\mu g$/mL 에서 81.04$\pm$1.55%로 가장 높았으며, 아질산염 소거능은 pH 1.2($49.52\pm1.04\sim72.52\pm$0.84%)> pH 4.2($35.28\pm0.78\sim51.20\pm$1.10%)> pH 6.0($27.90\pm0.36\sim32.26\pm$1.20%) 순으로 pH가 낮을수록 비파엽 열수추출물 농도가 높을수록 높았다. 비파엽 열수추출물 100, 200, 300 $\mu g$/mL에서 $\beta$-hexosaminidase 방출 억제능은 각각 14.58$\pm$0.97%, 43.69$\pm$0.96%, 95.58$\pm$0.75%로 농도에 의존적으로 증가하였다. 비파엽 열수추출물을 이용하여 RAW cell을 대상으로 항염증 활성을 조사한 결과, 농도가 증가함에 따라 증가하여 400 $\mu g$/mL에서 44.35$\pm$0.63%를 나타내어 다양한 생리활성을 보여주었다.

• 한방안이비인후피부과학회지
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• 제24권3호
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• pp.1-16
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• 2011

Objective : In the theory of Korean medicine, Scrophulariae Radix (SR) can clear away heat and cool the blood, nourish yin and promote the production of the body fluids, relieve toxin and benefit the throat. The present study was carried out to investigate effects of SR on allergic contact dermatitis (ACD) induced by 2,4-dinitrochlorobenzene (DNCB) in mice. Methods : In this experiment, effects of SR on clinical aspects on the skin, histopathological changes such as spongiosis, mast cell distribution, immune cell infiltration in tissue, spleen / body ratio and production levels of serum cytokines were investigated in vivo. In addition, effects on cell viability and release of b-hexosaminidase and histamine were also investigated in vitro. Results : SR treatment diminished erythema, desquamation and keratosis which were induced by repeated painting of DNCB. Spongiosis and edema were diminished by painting of SR in histopathological observation, infiltrations of mast cell and monocytes were also decreased in SR group. In addition, spleen / body ratio was lowered compared to ADC control group. Production level of IFN-${\gamma}$ in serum was decreased, but level of IL-4 did not affected by SR. Finally, more than 400 ${\mu}g/ml$ of SR treatment groups showed decreased cell viabilities in RBL-2H3 cells. Treatment with over 200 ${\mu}g/ml$ of SR decreased b-hexosaminidase release, and treatment with over 400 ${\mu}g/ml$ decreased histamine release in vitro. Conclusion : these data suggest that SR can decrease symptoms of ACD, then SR is useful to treat patient with ACD.