• Title/Summary/Keyword: Free agent

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Effects of Natural Products on the Inhibition of Lipopolysaccharide-Inducible Nitric Oxide Synthase Activity in RAW264.7 Cell Culture System

  • Park, Bong-Joo;Cho, Myung-Haing;Kim, Kyeong-Ho;Lee, Sang-Kook;Lee, Chong-Soon;An, Gil-Hwan;Mar, Woong-Chon
    • Natural Product Sciences
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    • v.5 no.3
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    • pp.113-120
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    • 1999
  • Nitric oxide (NO) is a free radical synthesized from L-arginine by nitric oxide synthase (NOS). It is believed that NO is an important mediator in numerous physiological and inflammatory responses. Particularly, a large amount of NO released from the inducible nitric oxide synthase (iNOS) is mostly associated with inflammatory processes. Overproduction of NO in these processes including sepsis and autoimmune diseases can have deleterious consequences and pathophysiologic relevance. Therefore, for the discovery of new inhibitory agents against iNOS activity, we have evaluated about 100 kinds of natural products after partition into three layers (n-hexane, ethyl acetate and aqueous) from 100% methanol extracts to study inhibitory effects on iNOS activity induced by lipopolysaccharide (LPS) in RAW264.7 cells culture system. As a positive control, curcumin, which is known as an anti-tumor promoter, anti-inflammatory agent as an iNOS inhibitor, was used and showed the dose-dependent inhibitory effect $(IC_{50},\;2.5\;{\mu}g/ml)$. Among tested fractions, the n-hexane fraction of Cimicifuga heracleifolia $(IC_{50}:\;9.65\;{\mu}g/ml)$, Forsythiae fructus $(IC_{50}:\;6.36\;{\mu}g/ml)$, Saposhnikovia divaricata $(IC_{50}:\;5.92\;{\mu}g/ml)$, and the ethyl acetate fraction of Chrysanthemum sibiricum $(IC_{50}:\;2.56\;{\mu}g/ml)$, Gastrodia elata $(IC_{50}:\;3.46\;{\mu}g/ml)$, and the aqueous fraction of Dianthus chinensis $(IC_{50}:\;6.73\;{\mu}g/ml)$, Euonymus alatus $(IC_{50}:\;6.78\;{\mu}g/ml)$, Mechania urticifoloria $(IC_{50}:\;8.01\;{\mu}g/ml)$ showed strong inhibitory activity against LPS-stimulated iNOS. Especially, the ethyl acetate fraction of Chrysanthemum sibiricum $(IC_{50}:\;2.56\;{\mu}g/ml)$, which exhibited the strongest inhibition against iNOS, was fractionated with silica-gel column chromatography. These subfractions exhibited dose-dependent inhibition against iNOS activity in the range of $2.59-5.6\;{\mu}g/ml$ except for fraction No. 3, 4, 5, 6, 8, 9, and 16. Our study shows that Chrysanthemum sibiricum has the strongest inhibitory effect against iNOS activity and has similar effect to curcumin. Therefore, further studies for the identification of active principles from Chrysanthemum sibiricum and investigation for the mechanism of the inhibition of iNOS by active principles will be performed.

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Effect of Polygala radix Hot Water Extract on Biological Activity in PC12 Cells (PC12 세포에서 생물학적 활성에 미치는 원지 열수 추출물의 효능)

  • Nam, Hyang;Kim, Moon-Moo
    • Journal of Life Science
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    • v.23 no.8
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    • pp.1041-1049
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    • 2013
  • The root of Polygala radix has been widely known as an oriental traditional medicinal stuff that improves memory. However, its mechanism of action remains unclear. In this study, the effect of Polygala radix hot water extracts (PRHWE) on cognitive function related to the activity of acetylcholinesterase (AchE) derived from neural cells (PC12) in addition to antioxidant activity was examined both in a cell-free system and live cells. First, in the study on cell viability using an MTT assay, PRHWE did not exhibit any cell toxicity at 0.1% (w/v) or below. It also was observed that PRHWE increased the scavenging activity of DPPH radical, hydrogen peroxide and superoxide, reducing power in a dose-dependent manner. In particular, PRHWE had a protective effect on DNA oxidation induced by hydroxyl radicals. Additionally, it inhibited the production of inducible nitric oxide in neuronal cells. Furthermore, the AchE activity decreased with increasing concentrations. In addition, PRHWE increased the expression level of SOD-1 and NOS-2 in PC12 cells. Moreover, the transcriptional activities of p53 and NF-${\kappa}B$ were reduced in the presence of PRHWE in an experiment using a reporter gene assay. Therefore, these results prove that PRHE has antioxidative and protective effects on neuronal cells, suggesting that it may have great potential as a therapeutic agent for human health.

Bone Marrow Immunoscintigraphy for the Detection of Skeletal Metastasis in Malignant Tumors: A Comparison with $^{99m}Tc$-MDP Bone Scan (악성종양에서 골수면역신티그라피를 이용한 골수전이의 평가 : $^{99m}Tc$-MDP 뼈스캔과의 비교)

  • Lee, Kyung-Han;Choi, Chang-Woon;Bang, Yung-Jue;Chung, Jun-Key;Chung, Hong-Keun;Lee, Myoung-Chul;Kim, Byoung-Kook;Kim, Noe-Kyeong;Koh, Chang-Soon
    • The Korean Journal of Nuclear Medicine
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    • v.28 no.1
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    • pp.89-97
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    • 1994
  • Although bone scan is a highly sensitive test for detecting bone metastasis, its findings are often limited in specificity and cannot be used for assessing the bone marrow. Bone marrow scintigraphy may provide useful information but previous experience with radiolabelled colloid has been disappointing. Recently, $^{99m}Tc$ labeled anti-granulocyte monoclonal antibody (anti-NCA-95 MAb) has been introduced as a new bone marrow imaging agent. To evaluate the usefulness of $^{99m}Tc$ anti-NCA MAb bone marrow scans for detecting skeletal metastasis, bone marrow scans of 44 malignant tumor patients were evaluated and compared with bone scan findings. Bone scan showed abnormal lesions in 26(59%) cases, and 18 of these patients also had an abnormal bone marrow scan. Seven of the 8 patients who had normal bone marrow scan despite bone scan lesions were confirmed to be free from metastasis. There was one case with a marrow defect despite normal bone scan but the presence of metastasis was not determined due to loss of follow up. Bone scan demonstrated a total of 64 lesions while bone marrow scan showed 38 lesions. Fifty percent (32/64) of the bone scan lesions had matching marrow defects while the remaining 50% did not. Most of these non matched lesions were suggested to be nonspecific lesions such as rib fractures or degenerative change. Meanwhile bone marrow scan was able to detect 6 new lesions not detected by bone scan, bit metastasis in each lesion was not confirmed. Bone marrow scan was also helpful in assessing equivocal bone scan lesions to be of metastatic nature in 10 patients by demonstrating a matched marrow defect. Thus $^{99m}Tc$ anti-NCA MAb bone marrow scan can help exclude metastasis in patients with nonspecific bone scan lesions and may be able to detect metastatic lesions not seen with bone scan. It appears useful as a complementary study to bone scan in evaluating malignant tumor patients.

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Mechanism of Free Phosphate Production by Penicillium sp. GL-101, Phosphate Solubilizing Fungus, in the Submerged Culture (인산가용화균 Penicillium sp. GL-101의 유리인산 생성기작에 관한 연구)

  • Kang, Sun-Chul;Yang, Mi-Ok;Tae, Un-Hee
    • Korean Journal of Environmental Agriculture
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    • v.20 no.1
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    • pp.1-7
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    • 2001
  • We investigated the capability of the phosphate-solubilizing fungus, Penicillium sp. GL-101, to solubilize in vitro some insoluble rock phosphate via possible mechanisms: acidification of the medium, production of chelating metabolites, redox activity, and so on. GL-101 was able to solubilize rock phosphate (mostly calcium phosphate) in a liquid potato dextrose broth(PDB) medium, as determined by spectrophotometric analyses. Acidification was the major mechanism of solubilization since the pH of cultures fell below 4.0 and in cultures containing 1.0%(w/v) loess the pH dropped from 7.0 to 3.2. More than 10 mg/mL concentrations of citric acids were detected by high-performance liquid chromatography(HPLC) in the culture supernatants. Also this fungus showed the phosphatase activity (over 1.3 unit) to contribute partially releasing phosphate from rock phosphate, when supplemented with 1.0% loess in culture broth. The chelating activity of GL-101 in culture supernatants was not present because 2-ketogluconic acid, a chelating agent for the phosphate, was produced only a basal level. Therefore, the solubilization mechanism of rock phosphate by Penicillium sp. GL-101 involves both acidification due to citric acid production and phosphatase activity.

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Preparation of Branched-chain Amino Acid (BCAA)-enriched Hydrolysates from Corn Gluten (고 분지아미노산 함유한 옥수수 단백가수물의 제조조건 탐색)

  • Chung, Yong-Il;Bae, In-Young;Lee, Hyeon-Gyu
    • Korean Journal of Food Science and Technology
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    • v.42 no.1
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    • pp.39-44
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    • 2010
  • The process of the preparation of branched-chain amino acid (BCAA)-enriched hydrolysates from corn gluten was optimized through the parameters of pre-treatment (heating and cellulosic hydrolysis), hydrolysis method (acid, protease, and microbe plus protease), concentration, and spray drying condition. The protein yield of corn gluten was increased by heating and cellulase treatments. Among three different hydrolysis methods, the combined use of microbes and protease was the most effective in terms of free amino acid (FAA) and BCAA content of the corn gluten hydrolysates. In addition, the FAA and BCAA content in the hydrolysates prepared by microbial and enzymatic combined treatment were improved by a concentration process. Spray drying conditions for the preparation of the powder from the hydrolyzed reactant were an inlet temperature of $185^{\circ}C$, outlet temperature of $80^{\circ}C$, and the use of maltodextrin as an anticaking agent. Thus, this study established an economical process for preparation of value-added hydrolysates of excellent productivity and quality, in terms of high BCAA content and product stability.

Studies on the Content of Lectin in Korean Mistletoe according to the Host Tree Species and Characterization for Its Application to the Quality Control (한국산 겨우살이 숙주별 렉틴 함량과 지표물질로서의 특성 조사)

  • Kim, Inbo;Yoon, Taek Joon;Park, Choon Ho;Lee, Woo Kyoung;Lee, So Hee;Kim, Jong Bae
    • The Korean Journal of Food And Nutrition
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    • v.28 no.6
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    • pp.1090-1097
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    • 2015
  • Traditionally, mistletoe is known as an effective anti-cancer medicinal plant, and lectin is recognized as a major component with cytotoxic and immuno-stimulant activity in mistletoe. A Korean mistletoe lectin (KML) has specificity to galactose and galactosamine and is distinguish from European mistletoe lectin (EML). When we examined the concentration of lectin in mistletoe originated from five different types of host trees, the result indicate that the lectin concentration is variable depending on the host tree. Noticeably, mistletoe from chestnut tree contains ten folds higher lectins than that of an oak tree. We also tested the concentration of KML and crude extract (KM-110) of Korean mistletoe that shows 90% cytotoxicity in L5178Y-ML25 lymphoma cell. In addition, the cells show 90% and 70% viability by the treatment of two neutralizing antibodies of KML, 9H7-D10 and 8B11-2C5 neutralization effect with two monoclonal antibodies of KML, 9H7-D10 and 8B11-2C5. Therefore, the result expected that the mistletoe contain some other cytotoxic components except lectin. Finally, the production of $TNF-{\alpha}$ and IL-6 by RAW 264.7 cells stimulated with lectin free-crude extract (LFKM-110) following neutralization by 9H7-D10 monoclonal antibody shows higher than that of lectin containing-crude extract (KM-110). These results suggest that the Korean mistletoe lectin ha a great potential to be developed as therapeutic agent of cancer.

Curcumin Induces Recovery from Indomethacin-Induced Gastric Mucosal Lesions in Rats (커규민의 인도메타신 유도 위점막 손상에 대한 치료 효과)

  • Kim, Jeong-Hwan;Kim, Byung-Woo;Kwon, Hyun-Ju;Kim, Yeon-Hee;Nam, Soo-Wan
    • Journal of Life Science
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    • v.24 no.1
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    • pp.20-25
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    • 2014
  • In the present study, the curative effect of curcumin on indomethacin-induced gastric mucosal lesions in rats was investigated. Indomethacin is a nonsteroidal anti-inflammatory drug (NSAID), with serious side effects, including erosion, ulcerative lesions, and petechial bleeding in the mucosa of the stomach. Gastric mucosal lesions were caused by oral administration of 25 mg/kg of indomethacin. Various doses (10, 50, and 100 mg/kg) of curcumin were treated for 3 days by oral gavage. Indomethacin clearly increased the gastric ulcer area in the stomach, and curcumin significantly decreased the gastric ulcer area in a dose-dependent manner. Curcumin also markedly inhibited lipid peroxidation in the gastric mucosa and activated radical scavenging enzymes, such as superoxide dismutase (SOD), catalase, and glutathione peroxidase, in a dose-dependent manner. These results suggest that curcumin can induce recovery from indomethacin-induced gastric mucosal lesions through inhibition of lipid peroxidation and activation of radical scavenging enzymes, such as SOD, catalase, and glutathione peroxidase. Curcumin appears to be a powerful free radical quencher, and it may offer an attractive strategy for healing gastric mucosal lesions in humans.

$^{131}I-MIBG$ Therapy in Malignant Pheochromocytoma and Medullary Thyroid Carcinoma (악성 갈색세포종 및 갑상선수질암의 $^{131}I-MIBG$을 이용한 치료)

  • Yoon, Jong-Kil;Ryoo, Baek-Yeol;Lee, Chang-Hee;Jeong, Sang-Hoon;Cheon, Young-Kug;Choi, Chang-Woon;Lim, Sang-Moo;Hong, Sung-Woon
    • The Korean Journal of Nuclear Medicine
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    • v.29 no.3
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    • pp.319-327
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    • 1995
  • $^{131}I$-metaiodobenzylguanidine(MIBG) has been used for the diagnosis and treatment of neural crest tumors. We report our experience with this agent in 8 patients[1 multiple endocrine neoplasia(MEN) type IIb; 2 malignant pheochromocytoma; 5 medullary thyroid carcinoma(MTC)]. The therapeutic procedure consisted of 30-200 mCi of $^{131}I-MIBG$ administered by slow I.V. infusion, given at 3-6 months intervals. Commutative activity ranged from 150 mCi to 410 mCi, in 1 to 4 courses. $^{131}I-MIBG$ therapy resulted in significant disease free interval in 1 malignant pheochromocytoma(no measurable lesion) after surgery; complete hormonal and tumoral response in 2 MTC(1 MEN IIb): stable disease in 1 recurred pheochromocytoma(MEN IIb): stable disease but symptomatic improvement in 1 MTC, progressive disease in 1 malignant pheochromocytoma and 2 MTC. The patients who showed progression appeared to have large inoperable tumors or postoperative remnant tumors.

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Chemical Components and Nitrite Scavenging Activity of Various Solvent Extracts from Onions (양파 추출물의 화학성분과 아질산염 소거능 효과)

  • Shon, Mi-Yae;Park, Seok-Kyu
    • Food Science and Preservation
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    • v.13 no.6
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    • pp.762-768
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    • 2006
  • To assess utilization of onions extract as natural food additives, ethyl acetate, ethanol and hot water extract of freeze dried onions (red, white and yellow) were exmined for their chemical component and nitrite scavenging activity. Contents of total organic acid and total free sugar were in the range of $135.4{\sim}1,2557mg%$ and $51.7{\sim}62.9%$ as dry matter bases, respectively, and then their content of three onions were higher in ethylacetate and hor water extracts than in ethanol extract. Contents of total phenol and total flavonoids were in the range of $9.3{\sim}$13.3 % and $159.8{\sim}584.1mg%$ as dry matter bases, respectively, and their content of red onion extract by three solvent were higher than those of other onion extract. Nitrite-scavenging activities (NSA) of onion extracts were increased by lowering pH and elevating onion concentrations, and their values of ethanol and hot water were about 55% in addition of 10 mg/mL of red onion extract showing that NSA of red onion was twice higher than that of the other onions. In conclusion, the result indicated that red onion extract was very effective to inhibit nitrosamine formation at low pH condition as natural nitrite scavenging agent.

Comparison of Biological Activities of Opuntia humifusa and Opuntia ficus-indica (손바닥선인장의 생리활성 비교 연구)

  • Park, Chul Min;Kwak, Byoung Hee;Park, Si Hyung;Kim, Hui;Rhyu, Dong Young
    • Korean Journal of Plant Resources
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    • v.26 no.5
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    • pp.519-525
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    • 2013
  • The Opuntia extract has been traditionally used to treat diabetes, inflammation, and rheumatoid arthritis in oriental medicine. The purpose of this study is to investigate characteristics of biological activity between Opuntia humifusa and Opuntia ficus-indica which is cultivating in korea using cell-free system or cell-based assay. O. humifusa extract effectively inhibited ${\alpha}$-glucosidase activity or improved the immune function, and its biological activity was more effective than O. ficus-indica extract. The scavenging activity of DPPH radical and the inhibitory effect of tyrosinase similarly showed by O. humifusa and O. ficus-indica extract, however neuroprotective effect only showed a tendency to increase compared with control in PC12 cells. Therefore the results suggest that O. humifusa can be a useful agent for treatment of diabetes and immunodeficiency.