• Title/Summary/Keyword: inhibiting activity

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Inhibitory Effects of Ethanol Extract of Modified Yukgunga-tang on Obesity and Hyperlipidemia in Rats Induced by High Fat Diet (육군자탕가감방 에탄올 추출물의 비만 및 고지혈증 유도 흰쥐에 대한 억제효능)

  • Park, Jung-Hyun;Kang, Hee;Ahn, Kwang-Seok;Shim, Bum-Sang;Kim, Sung-Hoon;Choi, Seung-Hoon;Ahn, Kyoo-Seok
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.23 no.3
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    • pp.685-694
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    • 2009
  • This experimental study was designed to investigate the inhibitory effects of ethanol extract of modified Yukgunja-tang(mYGJT) on high-fat diet-induced obesity and hyperlipidemia in Sprague-Dawley rats, Animals were divided into normal, control, mYGJT(100 mg/kg and 200 mg/kg) treated groups. Obesity with hyperlipidemia was induced by high fat diet treatment for 6 weeks. mYGJT was given to the amimals by oral gavage for 4 weeks, starting at the high-fat diet regimen, The effect of mYGJT on the differentiation of 3T3 L1 adipocytes in vitro and serological paramamters for obesity and hyperlipidemia in vivo were evaluated, mYGJT significnatly inhibited the differentiation of 3T3 L1 adipocytes in a concentration dependent manner. mYGJT treatment siginficantly reduced body weight, abdominal and epididymal fat weight, and FER(Food Efficiency Ratio) compared with control group in a dose dependent manner. It also signficantly inhibited the levels of serum total lipid, triglyceride, phospholipid, total cholesterol, LDL, AI(Atherosclerosis Index) and returned the serum HDL to normal. Total lipids, triglycerides and cholesterols in the liver, as well as malondialdehyde(MDA) and hydroxy radical in the serum were significantly reduced. However, superoxide dismutase(SOD) activity was significantly increased in mYGJT treated group compared with control group. Finally, mYGJT treatment signficantly decreased the MDA and protein carbonyl concentrations of the hepatic homogenate but signficantly increased the activities of SOD, GSH-Px and Catalase. Taken together, these results suggest that mYGJT can be clinically useful in inhibiting high-fat diet-induced obesity and hyperlipidemia.

Biorational Screening System Using Cyanobacteria(Anacystis nidulans $R_2$) for Searching the Photosynthetic Electron Transport Inhibitors (Cyanobacteria를 이용한 광합성 전자전달저해제의 생합리적 스크리닝)

  • Hwang, I.T.;Hong, K.S.;Cho, K.Y.;Yoshida, S.
    • Korean Journal of Weed Science
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    • v.13 no.2
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    • pp.81-88
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    • 1993
  • For searching the photosynthetic electron transport(PET) inhibitors, bio-rational screening system using thylakoid membranes extracted from wild and mutant cyanobacteria(Anacystis nidulans $R_2$) was developed. Generally, thylakoid membrane was more sensitive to the tested herbicides than the chloroplast from spinach in the Hill reaction. Higher resistant characteristics appeared in mutant D-5, Di-22 to diuron and mutant G-264 to atrazine as compared to wild type. To test the reaction of thylakoid membrane to herbicides, diuron and atrazine were applied simultaneously. Diuron and atrazine competed each other for binding with substituted amino acids, while diuron and dinoseb were non-competitive, and inhibiting activity was increased. Conclusively, bio-rational screening system using cyanobacteria was proved to be fast and efficient screening method for the development of PET inhibitors.

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Conjugated Linoleic Acid Induces Apoptosis by Activating AMPK in MCF-7 Breast Cancer Cells (MCF-7 유방암 세포에서 AMPK 활성에 의한 conjugated linoleic acid의 apoptosis 유도에 관한 연구)

  • Lin, Sun-Kyo;Kim, Hyun-Sook;Park, Ock-Jin;Kim, Young-Min
    • Journal of Life Science
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    • v.18 no.12
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    • pp.1679-1685
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    • 2008
  • Conjugated linoleic acid (CLA) is a naturally occurring compound found in dairy and beef products. It has been shown to suppress cancer cells and to induce apoptosis. Practically, there is emerging evidence that CLA can inhibit chemically induced carcinogenesis in various tissues. However, the molecular mechanisms of CLA on human MCF-7 breast cancer cells have not been clearly explained yet. In this report, we investigated the anti-cancer activity of CLA in MCF-7 cells. It was found that CLA could inhibit the growth of the MCF-7 cells and induce apoptosis, through modulating AMP-activated protein kinase (AMPK) and cyclooxygenase-2 (COX-2). AMPK acts as a cellular fuel gauge and responds to decreased cellular energy status by inhibiting ATP-consuming pathways and increasing ATP-synthesis. CLA treatment with variable concentrations and different time of same-dose CLA on MCF-7 cells resulted in a strong activation of AMPK and an inhibition of COX-2 expression. It supports that CLA induces apoptosis in CLA-treated MCF 7 cells. Therefore, the effects of CLA induced COX-2 expression via activating AMPK can provide new possibility into the understanding the molecular mechanisms of anti-cancer component.

Ginsenoside Re Inhibits Osteoclast Differentiation in Mouse Bone Marrow-Derived Macrophages and Zebrafish Scale Model

  • Park, Chan-Mi;Kim, Hye-Min;Kim, Dong Hyun;Han, Ho-Jin;Noh, Haneul;Jang, Jae-Hyuk;Park, Soo-Hyun;Chae, Han-Jung;Chae, Soo-Wan;Ryu, Eun Kyoung;Lee, Sangku;Liu, Kangdong;Liu, Haidan;Ahn, Jong-Seog;Kim, Young Ock;Kim, Bo-Yeon;Soung, Nak-Kyun
    • Molecules and Cells
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    • v.39 no.12
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    • pp.855-861
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    • 2016
  • Ginsenosides, which are the active materials of ginseng, have biological functions that include anti-osteoporotic effects. Aqueous ginseng extract inhibits osteoclast differentiation induced by receptor activator of NF-${\kappa}B$ ligand (RANKL). Aqueous ginseng extract produces chromatography peaks characteristic of ginsenosides. Among these peaks, ginsenoside Re is a major component. However, the preventive effects of ginsenoside Re against osteoclast differentiation are not known. We studied the effect of ginsenoside Re on osteoclast differentiation, RANKL-induced tartrate-resistant acid phosphatase (TRAP) activity, and formation of multinucleated osteoclasts in vitro. Ginsenoside Re hampered osteoclast differentiation in a dose-dependent manner. In an in vivo zebrafish model, aqueous ginseng extract and ginsenoside Re had anti-osteoclastogenesis effects. These findings suggest that both aqueous ginseng extract and ginsenoside Re prevent bone resorption by inhibiting osteoclast differentiation. Ginsenoside Re could be important for promoting bone health.

Effects of Green Tea, Buckwheat and Grape Leaves Extracts on Lipid Metabolism, Antioxidative Capacity, and Antithrombotic Activity in Rats Fed High Cholesterol Diets (녹차, 메밀, 포도잎 추출물이 고콜레스테롤 급여 흰쥐의 지질대사, TBARS 및 혈액응고에 미치는 영향)

  • Kim, Young-Eon;Oh, Se-Wook;Kwon, Eun-Kyung;Han, Dae-Seok;Kim, In-Ho;Lee, Chang-Ho
    • Korean Journal of Food Science and Technology
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    • v.36 no.6
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    • pp.979-985
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    • 2004
  • Effects of green tea, buckwheat, and grape leaf extracts on factors related to blood circulation were studied using rats fed high-cholesterol diet for 4 weeks. Rats were randomly divided into five groups, and plant extracts were orally administered. Green tea extract increased bleeding time in rat tails, suggesting it could prevent platelet aggregation. Administration of green tea, buckwheat, and grape leaf extracts decreased total cholesterol level in liver. Grape leaf extracts decreased thiobarbituric acid-reactive substances in plasma, whereas buckwheat and grape leaf extracts decreased the substances in liver. These results showed extracts of green tea, buckwheat, and grape leaf were effective for improving lipid composition in blood and liver and inhibiting lipid peroxidation in animal tissue, suggesting they may have potential to prevent cardiovascular diseases.

The Effect of Glucono delta Lactone, Starter Clulture and NaCl on the Production of Staphylococcal Enterotoxign A in the Processing of Fermented Sausage (발효 소세지의 숙성 중 Starter Culture, Glucono delta Lactone 및 소금첨가량이 Staphylococcal Enterotoxin의 생성에 미치는 영향)

  • Shin, Heuyn-Kil;Jin, Young-Ku;Lee, Young-Jin;Park, Woo-Moon;Kim, Jong-Bae
    • Korean Journal of Food Science and Technology
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    • v.23 no.2
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    • pp.150-156
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    • 1991
  • This research was conducted to investigate the effect of starter culture(Lactobacillus plantarum), glucono-delta-lactone(GdL), and NaCl on the production of staphylococcal enterotoxin A in the processing of fermented sausages. With the increasing amount of GdL(0, 0.23, 0.50 and 0.75%) added the production of enterotoxin was significantly decreased(p>0.01). Lactobacillus plantarum as starter culture were inoculated at the level of $10^6\;cells/g$. When GdL was not added, the amount of production of enterotoxin in the group with and without the starter culture were 40 and 80 ng/10g, respectively. With the addition of 0.5%, GdL, the maximum amount of enterotoxin produced in the group with and without starter culture were 30 and 50 ng/10g. These results showed the inhibiting effect of starter culture in the production of enterotoxin. When the amount of enterotoxin production was compared with the addition of 2.7 and 1.7% NaCl, the production of enterotoxin was higher at 2.7% NaCl level.

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The Effect of Fresh Paprika and Paprika powder dried by far-infrared ray on Inhibition of Lipid Oxidation in Lard Model System (돈지 모형계에서 생 파프리카와 원적외선 건조 파프리카 분말의 지질 산화 억제 효과 비교)

  • Park Jae-Hee;Kim Chang-Soon;Noh Sang-Kyu
    • Korean journal of food and cookery science
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    • v.21 no.4 s.88
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    • pp.475-481
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    • 2005
  • This study was conducted to determine the antioxidant activity of paprika in a lard model system. The effect of paprika (ground fresh paprika (FP) $3\%$, $50^{\circ}C$ far-infrared ray dried Paprika Powder (PP) $3\%$ and $5\%$) on the inhibition of lipid oxidation in lard was examined by pH, peroxide value (POV), thiobarbituric acid (TBA) value and fatty acid composition during 8 days of storage at $4^{\circ}C$. With paprika, POV and TBA values in lipid oxidation of lard were significantly lower than those of the control without paprika. Especially, in lard with FP $3\%$, there was hardly any change of lipid oxidation values such as POV, TBA values and destruction of unsaturated fatty acid inhibiting lipid oxidation. Heating of paprika during far-infrared ray drying decreased the inhibition effect on lipid oxidation in the lard model system probably due to loss of antioxidant substances, such as vitamin C, polyphenols and carotenoids including capsanthin, by heating. Therefore, FP containing a hish amount of antioxidant substance could be used as a good antioxidant in Pork Products containing large amounts of lard.

LC15-0133, a DPP IV Inhibitor: Efficacy in Various Animal Models (LC15-0133, DPP IV 저해제: 여러 동물 모델에서의 효능)

  • Yim, Hyeon-Joo
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2008.04a
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    • pp.5-20
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    • 2008
  • GLP-1-based drugs (GLP-1 analogues and DPP IV inhibitors) and incretin mimetics are currently one of the most exciting classes of agents for type II diabetes. GLP-1, a gut peptide, is an incretin that potentiates glucose-dependent insulin release from the pancreas, slows GI-transit and stimulates the proliferation of beta-cells. DPP IV inhibitors act like incretins by inhibiting DPP IV which inactivates GLP-1. LC15-0133 is a competitive, reversible DPP IV inhibitor ($IC_{50}$ = 24 nM, Ki=0.247 nM) with excellent selectivity over other critical human proteases such as DPP II, DPP 8, elastase, trypsin. and urokinase. LC15-0133 showed long half-life and good bioavailability in rats and dogs. Inhibition of plasma DPP IV activity by LC15-0133 was kept more than 50% 24 hours after oral dosing in rats and dogs at 0.1 mg/kg and 0.02 mg/kg, respectively. The Minimum effective doses of LC15-0133 were 0.01 mg/kg for lowering blood glucose excursion during oral glucose tolerance test and 0.1 mg/kg for increasing glucose-induced GLP-1 response in C57BL/6 mice. Repeat oral administration of LC15-0133 for 1 month delayed the progression to diabetes and reduced HbA1c levels in a dose-dependent manner in Zucker Diabetic Fatty rats. In conclusion, LC15-0133 is a novel, potent, selective and orally active DPP IV inhibitor and showed an excellent blood glucose lowering effects in various animal models.

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Anticancer Activities of the Methanolic Extract from Lemon Leaves in Human Breast Cancer Stem Cells (인간 유방암 줄기세포에서 레몬잎 메탄올 추출물의 항암 효능)

  • Moon, Jeong Yong;Nguyen, Linh Thi Thao;Hyun, Ho Bong;Osman, Ahmed;Cho, Minwhan;Han, Suyeong;Lee, Dong-Sun;Ahn, Kwang Seok
    • Journal of Applied Biological Chemistry
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    • v.58 no.3
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    • pp.219-226
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    • 2015
  • The anticancer activity of a methanolic extract from lemon leaves (MLL) was assessed in MCF-7-SC human breast cancer stem cells. MLL induced apoptosis in MCF-7-SC, as evidenced by increased apoptotic body formation, sub-G1 cell population, annexin V-positive cells, Bax/Bcl-2 ratio, as well as proteolytic activation of caspase-9 and caspase-3, and degradation of poly (ADP-ribose) polymerase (PARP) protein. Concomitantly, MLL induced the formation of acidic vesicular organelles, increased LC3-II accumulation, and reduced the activation of Akt, mTOR, and p70S6K, suggesting that MLL initiates an autophagic progression in MCF-7-SC via the Akt/mTOR pathway. Epithelial-mesenchymal transition (EMT), a critical step in the acquisition of the metastatic state, is an attractive target for therapeutic interventions directed against tumor metastasis. At low concentrations, MLL induced anti-metastatic effects on MCF-7-SC by inhibiting the EMT process. Exposure to MLL also led to an increase in the epithelial marker E-cadherin, but decreased protein levels of the mesenchymal markers Snail and Slug. Collectively, this study provides evidence that lemon leaves possess cytotoxicity and anti-metastatic properties. Therefore, MLL may prove to be beneficial as a medicinal plant for alternative novel anticancer drugs and nutraceutical products.

Isolation and Structure Identification of Antifungal Substance from Aspergillus terreus (Aspergillus terreus로부터 항진균성 물질의 분리 및 구조분석)

  • Kim, Keun-Ki;Park, Ki-Hun;Moon, Suk-Sik;Kang, Kyu-Young
    • Applied Biological Chemistry
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    • v.40 no.6
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    • pp.593-596
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    • 1997
  • In the course of search antagonistic fungi from soil in green house, four kind of fungi (AF1, AF2, AF3, AF4) were isolated, which have activities against Phytophthora capsici, Botrytis cinera, Rhizoctonia solani, Pythium ultimum and Fusarium oxysporum. The AF2 was identified according to the morphological description of Aspergillus terreus. This antagonistic fungus inhibiting various plant pathogens was effective to reduce disease incidence of cucumber seedlings caused by mixed inoculum of Rhizoctonia solani, Pythium ultimum and Fusarium oxysporum. Antifungal compound I was isolated and purified by fresh chromatography from A. terreus. The $^1H$ and $^{13}C$ assignment of compound I was achieved from two-dimensional $^1H-^1H\;COSY$, HMQC, HMBC with the add of homonuclear and heteronuclear double resonance experiment. The compound I was identified butyrolactone I (${\alpha}$-oxo-${\beta}$-(p-hydroxyphenyl)-${\gamma}$-(p-hydroxy-m-3,3-dimethyl-allylbenzyl)-${\gamma}$-methoxycarbonyl-${\gamma}$-butyrolactone, $C_{24}H_{24}O_7$, M.W.=424).

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