• Title/Summary/Keyword: inhibitory compounds

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Characterization of different Dioxygenases isolated from Delftia sp. JK-2 capable of degrading Aromatic Compounds, Aniline, Benzoate, and p-Hydroxybenzoate (방향족 화합물인 Aniline, benzoate, p-Hydroxybenzoate를 분해하는 Delftia sp. JK-2에서 분리된 Dioxygenases의 특성연구)

  • 오계헌;황선영;천재우;강형일
    • KSBB Journal
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    • v.19 no.1
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    • pp.50-56
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    • 2004
  • The aim of this work was to investigate the purification and characterization dixoygenases isolated from Delftia sp. JK-2, which could utilize aniline, benzoate, and p-hydroxybenoate as sole carbon and energy source. Catechol 1,2-dioxygenase (C1, 2O), catechol 2,3-dioxygenase(C2, 3O), and protocatechuate 4,5-dioxygenase(4,5-PCD) were isolated by benzoate, aniline, and p-hydroxybenzoate. In initial experiments, several characteristics of C1 ,2O, C2, 3O, and 4,5-PCD separated with ammonium sulfate precipitation, DEAE-sepharose, and Q-sepharose were investigated. Specific activity of C1 ,2O, C2, 3O, and 4,5-PCD were approximately 3.3 unit/mg, 4.7 unit/mg, and 2.0 unit/mg. C1 ,2O and C2, 3O demonstrated their enzyme activities to other substrates, catechol and 4-methylcatechol. 4,5-PCD showed the specific activity to the only substrate, protocatechuate, but the substrates(e.g., catechol, 3-methylcatechol, 4-methylcatechol, 4-chlorocatechol, 4-nitrocatechol) did not show any specific activities in this work. The optimum temperature of C1, 2O, C2, 3O, and 4,5-PCD were 30$^{\circ}C$, and the optimal pHs were approximately 8, 8, and 7, respectively. Ag$\^$+/, Hg$\^$+/, Cu$\^$2+/ showed inhibitory effect on the activity of C1, 2O and C2, 3O, but Ag$\^$+/, Hg$\^$+/, Cu$\^$2+/, Fe$\^$3+/ showed inhibitory effect on the activity of 4,5-PCD. Molecular weight of the C1, 2O, C2, 3O, and 4,5-PCD were determined to approximately 60 kDa,35 kDa, and 62 kDa by SDS-PAGE.

Comparative Study on Biological Activities and Ingredient Contents of Different Solvent Extracts of Samchulkunbi-tang (삼출건비탕의 추출용매에 따른 성분 함량 및 효능 비교 연구)

  • Jin, Seong Eun;Seo, Chang-Seob;Ha, Hyekyung;Lim, Hye-Sun;Kim, Yeji;Jeon, Woo-Young;Yoo, Sae-Rom;Kim, Jung-Hoon;Shin, In-Sik;Kim, Seong-Sil;Shin, Na Ra;Lee, Mee-Young;Jeong, Soo-Jin;Kim, Ohn Soon;Shin, Hyeun-Kyoo
    • Korean Journal of Pharmacognosy
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    • v.43 no.4
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    • pp.328-337
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    • 2012
  • In order to investigate anti-inflammatory, anti-allergic and anti-obesity activities of Samchulkunbi-tang (SCT; Shen zhu jian pi-tang) water and 70% ethanol (EtOH) extracts, in vitro inhibitory activities against nitric oxide (NO), prostaglandin $E_2$ $PGE_2$), interleukin (IL)-6 and tumor necrosis factor (TNF)-${\alpha}$ production in lipopolysaccharide-stimulated RAW 264.7 cells, and macrophage-derived chemokine (MDC/CCL22) and regulated on activation of normal T-cell-expressed and -secreted (RANTES/CCL5) production in TNF-${\alpha}$/interferon-${\gamma}$-stimulated HaCaT and BEAS-2B cells as well as glycerol-3-phosphate dehydrogenase (GPDH) activity and leptin production in 3T3-L1 cells were determined. A HPLC was used for quantification of the seven marker components (albiflorin, paeoniflorin, liquiritin, naringin, hesperidin, poncirin and glycyrrhizin) of SCT water and 70% EtOH extracts. SCT showed inhibitory effects against MDC and RANTES production in HaCaT cells, as well as RANTES production in BEAS-2B cells. In addition, SCT reduced not only NO, $PGE_2$, IL-6 and TNF-${\alpha}$ production in RAW 264.7 cells, but also GPDH activity and leptin production in 3T3-L1 cells. Furthermore, the biological activities and the contents of six compounds (except paeoniflorin) were higher in 70% EtOH extract than water extract. These results suggest that SCT has anti-inflammatory, anti-allergic and anti-obesity activities. These efficacies of 70% EtOH extract are relatively higher than that of water extract.

Inhibitory Effect of Scopoletin Isolated from Sorbus commixta on TNF-α-Induced Inflammation in Human Vascular Endothelial EA.hy926 Cells through NF-κB Signaling Pathway Suppression (마가목 수피에서 분리한 scopoletin의 EA.hy926 혈관내피세포에서 NF-κB 신호전달을 통한 TNF-α로 유도된 혈관염증 저해 효과)

  • Kang, Hye Ryung;Kim, Hyo Jung;Kim, Bomi;Kim, Sun-Gun;So, Jai-Hyun;Cho, Soo Jeong;Kwon, Hyun Sook
    • Journal of Life Science
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    • v.30 no.4
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    • pp.343-351
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    • 2020
  • Sorbus commixta Hedl. has traditionally been used as a remedy for cough, asthma, and other bronchial disorders. In this study, three major triterpenoids-lupeol, β-sitosterol, and ursolic acid and a coumarin, scopoletin, were isolated from a CHCl3-soluble fragment of the bark of S. commixta. Their structures were identified by spectroscopic analyses, including mass spectrometry (MS), 1D-, and 2D- nuclear magnetic resonance spectroscopy (NMR), as well as by comparing the data with data reported in the literature. Scopoletin was isolated from this plant for the first time. It is a nutraceutical compound contained in many plants that has been reported to exert diverse biological activities, including anti-inflammatory effects. This study examined the inhibitory effect of scopoletin on TNF-α-induced vascular endothelial inflammation. Unlike the marginal impact of other compounds against low-density lipoprotein (LDL) oxidation and vascular endothelial inflammation, scopoletin showed remarkable activity on LDL oxidation (IC50 = 10.2 μM) and exerted vascular anti-inflammatory effects in EA.hy926 human endothelial cells activated by TNF-α. It suppressed the expression of adhesion molecules, such as ICAM-1, VCAM-1, and E-selectin, and blocked the adhesion between THP-1 monocytes and EA. hy926 endothelial cells. It also inhibited TNF-α-induced NF-κB translocation from the cytosol to the nucleus. Moreover, IκBα phosphorylation, which was increased by TNF-α treatment, was reduced after treatment with scopoletin. Thus, scopoletin inhibited TNF-α-induced vascular inflammation in endothelial cells by suppressing the NF-κB signaling pathway. These results demonstrate that owing to its anti-inflammatory activity in the vascular endothelium, scopoletin has the potential to inhibit atherosclerosis development.

Antioxidative Activity and Componential Analysis of Chamaecyparis obtusa Leaf Extract (편백나무 잎 추출물의 항산화 활성과 성분분석에 관한 연구)

  • Lee, Dong Sook;Lim, Myoung Sun;Kwan, Soon Sik;Kim, Sun Young;Park, Soo Nam
    • Applied Chemistry for Engineering
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    • v.23 no.1
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    • pp.93-99
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    • 2012
  • In this study, the evaluation of antioxidative activity and componential analysis of C. obtusa leaf extracts was carried out. Reactive oxygen species (ROS) scavenging activities ($OSC_{50}$) of C. obtusa leaf extracts on ROS generated in $Fe^{3+}-EDTA/H_2O_2$ system were investigated using the luminol-dependent chemiluminescence assay. The ethyl acetate fraction ($OSC_{50}$; 0.22 ${\mu}g/mL$) and aglycone fraction of C. obtusa leaf extracts (0.20 ${\mu}g/mL$) showed about 7 times more prominent ROS scavenging activity than L-ascorbic acid (1.50 ${\mu}g/mL$). The cellular protective effects of fractions obtained from C. obtusa leaf extracts on the rose-bengal sensitized photohemolysis of human erythrocytes were investigated. The ethyl acetate fraction and aglycone fraction of C. obtusa leaf extracts showed the cellular protective effects in a concentration dependent manner (5~25 ${\mu}g/mL$). The inhibitory effect ($IC_{50}$) of ethyl acetate fraction and aglycone fraction on tyrosinase exhibited 74.43 and 53.80 ${\mu}g/mL$, repectively. The aglycone fraction showed four times higher tyrosinase inhibitory effect than arbutin (226.88 ${\mu}g/mL$), known as a whitening agent. The aglycone fraction of C. obtusa leaf extracts showed three bands in TLC chromatogram and three peaks in HPLC chromatogram (360 nm). Three compounds were identified as taxifolin, quercetin and kaempferol. These results indicate that the fractions of C. obtusa leaf extracts can function as antioxidants in biological systems, particularly skin exposed to UV radiation by scavenging $^1O_2$ and other ROS, and protect cellular membranes against reactive oxygen species. The fractions of C. obtusa leaf extracts can be applicable to new functional cosmetics for antioxidan and whitening effects.

Physiological Activities of Gymnopilus spectabilis Mycelium Extract and Supernatant of its Broth (갈황색 미치광이버섯 균사체 추출물 및 배양액의 생리활성)

  • Son, Jung-A;Seok, Soon-Ja;Lee, Kyoung-Jin;Lee, Kang-Hyo;Park, Jeong-Sik;Park, Ki-Moon
    • The Korean Journal of Mycology
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    • v.35 no.2
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    • pp.85-95
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    • 2007
  • This study was carried out to investigate the physiological activities of the ethanol extract from Gymnopilus spectabilis mycelium (EGM) and of the supernatant obtained from fermentation broth (SGB). The contents of polysaccharides, phenol compounds and total ${\beta}-glucans$ of EGM were found to be 80.14%, 3.5 mg/ml and 5.91%, respectively and those for SGB were 78.68%, 3.32 mg/ml and 3.28%, respectively. Both EGM and SGB exhibited dose-dependent nitrate-scavenging abilities at pH 1.2. In addition, both EGM and SGB on the autoxidation rate of the linoleic acid demonstrated powerful antioxidant activities at 1 mg/ml level. With respect to fibrolytic activity, EGM showed 1,180 unit/g, which was the same activity as streptokinase, while SGB was 1,011 unit/g. The angiotensin converting enzyme inhibition activity of EMG determined by both the normal and pretreatment methods were estimated to be 8.2% and 10.2%, respectively. However, SGB showed no corresponding activity. The growth inhibitory effects of EGM on AGS, A549, HeLa and NCTC cells were over 58.88%, respectively. And the growth inhibitory effects of the SGB on HeLa and NCTC cells were 44.92 and 76.76%, respectively. Also, EGM and SGB activated the components of the alternative complement pathway from 51 and 62% at the concentration of 100 mg/ml, The xanthine oxidase inhibition activities of EGM and SGB (1 mg/ml) were 9.53 and 16.92%, respectively.

Anti-inflammatory Activity of Peel Extracts in Color-fleshed Potatoes (컬러감자외피 추출물의 항염활성)

  • Nam, Jung-Hwan;Jeong, Jin-Cheol;Kwon, Oh-Keun;Hong, Su-Young;Kim, Su-Jeong;Soh, Hwang-Bae;Lee, Jong-Nam;Lee, Kyung-Tea;Park, Hee-Jhun
    • Korean Journal of Plant Resources
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    • v.26 no.5
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    • pp.533-538
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    • 2013
  • Potatoes were first introduced outside the Andes region four centuries ago, and have become an integral part of much of the world's food. Potatoes were first introduced into Europe in the 16th century and Korea in the early 19th century. In the nutritional aspects, potatoes contain abundant vitamins and minerals, as well as an assortment of phytochemicals such as carotenoids and natural phenols. Chlorogenic acid constitutes up to 90% of potato natural phenols. Due to the high content of potato functional compounds, it has known that potatoes are effective in the prevention of various human diseases. Recently, color-fleshed potatoes 'Hongyoung' and 'Jayoung' were developed by RDA, and it has reported that they have high content of anthocyanin. Additionally they show higher radical scavenging activity compared to white or yellow fleshed potatoes. So it will be expected that the consumption of color-fleshed potatoes grandually increase by pre-peeled potatoes and color potato chips. This study was conducted to enhance the peel of color-fleshed potatoes utilization and to determine the biological activity of peel of color-fleshed potatoes extract. The anti-inflammatory effects on ethanol extract and its solvent fraction were also evaluated. The anti-inflammatory activities of $CHCl_3$ fraction was evaluated for inhibitory activities against lipopolysacchride(LPS) induced nitric oxide(NO) and prostaglandin $E_2(PGE_2)$ production as well as inducible nitric oxide synthase(iNOS) and cyclo oxygenase-2(COX-2) protein expressions in RAW264.7 cell lines. The fraction inhibitory activity for both tests with $IC_{50}$ values showed in the ranges of $25{\sim}50{\mu}g/ml$. This result revealed that $CHCl_3$ fraction of Jayoung's peel is expected to be good candidate for development into source of anti-inflammatory agent.

Effects of Onion Flesh and Peel on Chemical Components, Antioxidant and Anticancer Activities (양파 육질 및 껍질의 화학성분과 항산화 및 항암 활성 비교)

  • Jang, Joo-Ri;Lim, Sun-Young
    • Journal of Life Science
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    • v.19 no.11
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    • pp.1598-1604
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    • 2009
  • In order to determine chemical components of onion flesh and peel, general nutrients, vitamin C, and total flavonoids were measured. Onion peel showed less moisture (14.3%) and no vitamin C compared to onion flesh. Onion peel contained more amounts of total flavonoids compared to onion flesh. In addition, the inhibitory effects of solvent extracts from onion flesh and peel on $H_2O_$-induced oxidative stress and growth of cancer cell lines (AGS human gastric adenocarcinoma and HT-29 human colon cancer cells) were investigated. Acetone with methylene chloride (A+M) and methanol (MeOH) extracts from onion flesh and peel appeared to significantly reduce the levels of intracellular reactive oxygen species (ROS) (p<0.05) and a greater antioxidant effect was observed in onion peel. Among fractions, 85% aq. methanol showed a higher protective activity against oxidative stress in both flesh and peel and there was no effect in the water and hexane fractions. The growth of cancer cells exposed to medium containing extracts and fractions from onion flesh and peel was inhibited dose-dependently. The growth of AGS was inhibited more in both flesh and peel compared to HT-29, and onion peel was more effective than onion flesh. Among fractions, 85% aq. methanol showed the greatest effect on growth inhibition in both flesh and peel. $IC_{50}$ values of 85% aq. methanol fraction from onion flesh and peel on AGS were 0.04 and 0.03 mg/ml, respectively, while those on HT-29 were 0.23 and 0.04 mg/ml. From our results, 85% aq. methanol fraction had an inhibitory effect against oxidative stress and growth of cancer cells, suggesting that it may contain biological active compounds.

Matrix metalloproteinase-1 suppression and type-1 procollagen synthesis promoting effects of Uncaria gambir (아선약 추출물의 matrix metalloproteinase-1(MMP-1) 억제 및 제1형 프로콜라겐 합성 촉진 활성)

  • Lee, Jaemin;Kim, Dong-Hee;Kim, Eun-Woo;Kwon, Hyun Ju;Kim, Byung Woo;Cho, Jae-Hyon;Kim, Hyun-Joo;Kim, Tae Hoon
    • Food Science and Preservation
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    • v.24 no.1
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    • pp.93-99
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    • 2017
  • Collagen synthesis is decreased and matrix metalloproteinase-1 (MMP-1) levels are increased in naturally aged human skin, and these alterations cause changes such as skin wrinkling and decreased elasticity. As a part of our ongoing search for bioactive ingredients, MMP-1 inhibitory and type-1 procollagen synthesis inducing activities of aqueous methanolic extract of manufactured gambir product from Uncaria gambir were investigated in in vitro bioassay systems. In addition, total phenolic contents were quantified using a spectrophotometric method. Among tested samples, 40% MeOH eluate from 80% methanolic extract of manufactured U. gambir using open column chromatography packed with Diaion HP-20 resin showed significant MMP-1 inhibitory activities with an $IC_{50}$ value of $15.6{\pm}1.3{\mu}g/mL$. Furthermore, type-1 procollagen synthesis promoting property of 40% MeOH eluate ($IC_{50}$ value; $6.9{\pm}0.7{\mu}g/mL$) from 80% methanolic extract of manufactured gambir was higher than other eluates. Additionally, the present investigation revealed that 40% MeOH eluate of manufactured gambir product contained a high level of total phenolic compounds. The result suggests a distinct relationship between anti-wrinkle activity and total phenolic contents, and manufactured gambir product could be considered a new effective source of natural bioactive ingredients. Systematic investigation of manufactured gambir product will be performed for further development of its biological properties.

Inhibition of Adipocyte Differentiation through G1 Arrest by Extract of Sophora tonkinensis Gapnep in 3T3-L1 Preadipocytes (산두근 추출물의 세포주기 정지를 통한 3T3-L1 지방전구세포의 분화 억제)

  • Jeong, Hyun-Young;Hyun, Sook-Kyung;Choi, Yung-Hyun;Kim, Byung-Woo;Kwon, Hyun-Ju
    • Journal of Life Science
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    • v.21 no.9
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    • pp.1346-1353
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    • 2011
  • Sophora tonkinensis Gapnep has been used as a traditional herbal medicine in oriental regions since ancient times. In this study, the effect and mechanism of the MeOH extract of Sophora tonkinensis Gapnep (STME) on adipocite differentiation and adipogenesis in 3T3-L1 preadipocites were investigated. Treatment with STME in the concentration range of 0-200 ${\mu}g$/ml significantly inhibited the differentiation of 3T3-L1 preadipocites in a dose-dependent manner, as determined by a decrease in intracellular lipid droplets and lipid contents measured by Oil Red O staining. In association with the inhibitory effect of lipid accumulation, the expressions of the proteins concerned with adipogenesis in 3T3-L1 preadipocites were also investigated. Treatment with STME reduced the expressions of peroxisome proliferator-activated receptor ${\gamma}$ (PPAR${\gamma}$), cytidine-cytidine-adenosine-adenosine-thymine (CCAAT)/enhancer-binding proteins ${\alpha}$ and ${\beta}$ (C/EBP${\alpha}$ and C/EBP${\beta}$) and sterol regulatory element binding protein (SREBP), which are adipocyte specific markers. In flow cytometry analysis, the inhibitory effect of differentiation was caused by G1 arrest and following mitotic clonal expansion cease. Therefore, we also investigated the alteration of G1 phase arrest-related proteins. As a result, the expression of p21 protein was significantly increased, while the expressions of Cdk2, E2F-1 and phospho-Rb were reduced in a dose-dependent manner in STME treated 3T3-L1 cells. According to these results, STME might inhibit differentiation through G1 arrest in 3T3-L1 preadipocytes adipogenesis, and further studies, which are in progress, have to be completed to identify the active compounds.

Quality Characteristics and Physiological Functionality of Traditional Rice Wines in Chungnam Province of Korea (충남지역 주요 전통주의 품질특성 및 생리기능성)

  • Lee, Mi-Young;Sung, Si-Youl;Kang, Heun-Kag;Byun, Hong-Seob;Jung, Sang-Mi;Song, Jung-Hwa;Lee, Jong-Soo
    • Microbiology and Biotechnology Letters
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    • v.38 no.2
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    • pp.177-182
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    • 2010
  • The goal of this study was to characterize the quality and physiological functionality of some traditional rice wines in Chungnam province, Korea. Non-sterilized and commercial sterilized traditional rice wines from five traditional rice wine factories of Chungnam province were collected and investigated for nutritional components, noxious compounds and physiological functionality. Ethanol content ranged from 16.1~18.3% and pH ranged from 3.27~4.76, and they also contained 0.15% to 0.55% of total acid. All traditional rice wines contained 10.15~139.9 mg% of amino nitrogen and 2.5~25.7% of total sugar. Among organic acids, lactic acid was contained 7.4~29.6 mg%, and succinic acid and propionic acid was also contained 0.2~2.7 mg% and 0.7~8.3 mg%, respectively. Antihypertensive angiotensin I-converting enzyme inhibitory activity were showed 37.0~86.0% in all rice wines, however, fibrinolytic activity, antioxidant activity, SOD-like activity and acetylcholinesterase inhibitory activity were low or not detected.