• Title/Summary/Keyword: Biological potency

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Molecular Mechanism of Macrophage Activation by Exopolysaccharides from Liquid Culture of Lentinus edodes

  • Lee, Ji-Yeon;Kim, Joo-Young;Lee, Yong-Gyu;Rhee, Man-Hee;Hong, Eock-Ki;Cho, Jae-Youl
    • Journal of Microbiology and Biotechnology
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    • v.18 no.2
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    • pp.355-364
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    • 2008
  • Mushrooms are regarded as one of the well-known foods and biopharmaceutical materials with a great deal of interest. ${\beta}$-Glucan is the major component of mushrooms that displays various biological activities such as antidiabetic, anticancer, and antihyperlipidemic effects. In this study, we explored the molecular mechanism of its immunostimulatory potency in immune responses of macrophages, using exopolysaccharides prepared from liquid culture of Lentinus edodes. We found that fraction II (F-II), with large molecular weight protein polysaccharides, is able to strongly upregulate the phenotypic functions of macrophages such as phagocytic uptake, ROS/NO production, cytokine expression, and morphological changes. F-II triggered the nuclear translocation of NF-${\kappa}B$ and activated its upstream signaling cascades such as PI3K/Akt and MAPK pathways, as assessed by their phosphorylation levels. The function-blocking antibodies to dectin-1 and TLR-2, but not CR3, markedly suppressed F-II-mediated NO production. Therefore, our data suggest that mushroom-derived ${\beta}$-glucan may exert its immunostimulating potency via activation of multiple signaling pathways.

The Inhibitory Potency of Hesperidin on Protein Kinase C Activity Using a Biochip (바이오칩을 이용한 Protein Kinase C의 활성에 대한 헤스페리딘의 저해 효과)

  • Kang, Jung Ae;Rho, Jong Kook;Choi, Mi Hee;Jung, Young Jin;Park, Sang Hyun
    • Journal of Radiation Industry
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    • v.5 no.1
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    • pp.15-20
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    • 2011
  • Protein kinases are the most important drug targets for the treatment of numerous diseases. The involvement of protein kinase C (PKC) in many biological processes such as development, memory, cell differentiation, and proliferation has been demonstrated. PKC is recognized as an important player in carcinogenesis. Thus, a variety of PKC inhibitors have been investigated. Among them, flavonoids have been demonstrated to affect the activity of many mammalian in vitro enzyme systems. The recent investigation was performed to evaluate the inhibitory effects of hesperidin, which is a flavonoid, on the proliferation and carcinogenesis of many cancers. In this study, an efficient kinase assay based on a biochip using radio-phosphorylation was established and performed for an examination of the inhibitory effects of hesperidin on PKC activity at different concentrations of 50, 200, 500 nM. It was found that hesperidin shows inhibitory potency on PKC, and that the biochip can be used to rapidly screen kinase inhibitors resulting in the therapeutic agents.

Protective Effects of a Ginseng Component, M altol(2- M ethyl-3- Hydroxy-4- Pyrone) against Tissue Damages Induced By Oxygen Radicals

  • Jae-Gook Shin;Jon
    • Proceedings of the Ginseng society Conference
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    • 1990.06a
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    • pp.45-48
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    • 1990
  • Maltol(2-methyl-3-hydroxy-r-pyrone), a component known to be present in Korean Ginseng root showed an antioxidant action but its potency as an antioxidant was low; about 1150th that of other antioxidants such as p-phenylenediamine , BHA and BHT. However, maltol was able to protect the oxidation adamants in biological systems such as adriamycin-induced membrane damage in isolated cardiomyocytes, parquet-induced toxicities in isolated hepatocytes and repercussion injury in isolated hearts. The antioxidant action of maltol was also shown to be effective in vivo. The antioxidant action of this compound was probably due to the removal of hydroxyl radicals. In view of the roles of oxygen radical in various pathological processes, Korean Ginseng root, which contains several antioxidants including maltol, is expected to have beneficial efforts on the oxygen radical-involved processes. Keywords Maltol, Oxygen free radicals, Lipid preoccupation, Repercussion injury and Korean ginseng

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Tocopherols and Tocotrienols in Cereal Grains (화곡류 종실의 토코페롤과 토코트리에놀 연구현황과 전망)

  • 이동진;이지영
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.48
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    • pp.1-12
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    • 2003
  • Vitamin E is a fat-soluble vitamin that exists in eight different forms, which are $\alpha$, $\beta$, $\gamma$, and $\delta$ tocopherol, and $\alpha$, $\beta$, $\gamma$, and $\delta$ tocotrienol. Tocopherols and tocotrienols are important antioxidant in foods, feeds and their raw materials, where they scavenge lipid radicals. Each form has its own biological activity, the measure of potency or functional use in the body. Antioxidants such as vitamin E act to protect cells against the effects of free radicals, which are potentially damaging by-products of the body's metabolism. Free radicals can cause cell dam-age that may contribute to the development of cardiovascular disease and cancer, The content of tocopherols and tocotrienols vary depending on the environmental condition such as growing regions, temperature, crops and varieties. This report deals with chemical and physical properties and extends to their nutritional and health effect on the tocopherols and tocotrienols in cereal grains.

Bioassays of Plant Hormones and Plant Growth Regulating Substances II. Abscisic Acid and Brassinolide (식물홀몬 및 생장조절물질의 생물검정기술 II. Abscisic Acid 및 Brassinolide)

  • 최충돈
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.34 no.s01
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    • pp.16-25
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    • 1989
  • A bioassay is a test system using a living organism (in whole or in part) to determine the presence or relative potency of chemical substances. The development and uses of bioassay are intimately linked to the discovery and characterization of the major classes of plant hormones. An application of this relationship is helpful for understanding the concept of plant hormones as well as the use of bioassay. And plant bioassay have been development and employed not only for the discovery and characterization of the biological activity of plant growth regulators but also have served several important secondary roles. The ideal bioassay should possess the characteristic of high specificity. great sensitivity. short response time, low cost and ease of obtaining plant material. acceptable ease of manipulation, and minimal space and equipment requirements.

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Synthesis and Biological Activities of (4-Arylpiperazinyl)piperidines as Nonpeptide BACE 1 Inhibitors

  • Boja, Poojary;Won, Sun-Woo;Suh, Dong-Hoon;Chu, Jeong-Hyun;Park, Woo-Kyu;Lim, Hee-Jong
    • Bulletin of the Korean Chemical Society
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    • v.32 no.4
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    • pp.1249-1252
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    • 2011
  • Inhibition of BACE 1 activity is considered as a promising therapeutic target for Alzheimer's Disease (AD). Synthesis and inhibitory activities of (4-arylpiperazinyl)piperidines by bioisosteric replacement of a biaryl group with an arylpiperazine as BACE 1 inhibitors are described. The resulting (4-arylpiperazinyl)piperidines represent novel nonpeptide BACE 1 inhibitors with improved in vitro potency.

Protective Effects of a Ginseng Component, Malto1(2-Mlethyl-3-Hydrox)-4-Pyrone) against Tissue Damages Induced By Oxygen Radicals (활성산소에 의한 조직손상에 미치는 인삼성분의 보호효과)

  • Jae-Gook Shin;Jon
    • Journal of Ginseng Research
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    • v.14 no.2
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    • pp.187-190
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    • 1990
  • Maltol(2-methyl-3-hydroxy-r-pyrone), a component known to be present in Korean Ginseng root showed an antioxidant action but its potency as an antioxidant was low: about 1150th that of other antioxidants such as pphenylenediamine, BHA and BHT. However, maltol was able to protect the oxidation damages in biological systems such as adriamycin-induced membrane damage in isolated cardiomyocytes, paraquat-induced toxicities in isolated hepatocytes and reperfusion injury in isolated hearts. The antioxidant action of maltol was also shown to be effective in vivo. The antioxidant action of this compound was probably due to the removal of hydroxyl radicals. In view of the roles of oxygen radical in various pathological proceises, Korean Ginseng root which contains several antioxidants including maltol is expected to have beneficial effects on the oxygen radical-involved processes.

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Synthesis and Biological Activity of Fungal Metabolite, 4-Hydroxy-3-(3'-Methyl-2'-Butenyl)-Benzoic Acid

  • Kim, Hye-Jin;Kwon, Ho-Jeong
    • Journal of Microbiology and Biotechnology
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    • v.17 no.3
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    • pp.543-545
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    • 2007
  • 4-Hydroxy-3-(3'-methyl-2'-butenyl)-benzoic acid (HMBA) was previously isolated from Curvularia sp. KF119 as a cell-cycle inhibitor. However, the present study used a novel and practical synthetic method to prepare a large quantity of HMBA. The synthetic HMBA was found to inhibit the cell-cycle progression of HeLa cells with a comparable potency to the natural fungal metabolite. The inhibition of the cell-cycle progression by the synthetic HMBA involved both the activation of $p21^{WAF1}$ and the inhibition of cyclin D1 expression in the cells. Consequently, this new synthetic procedure provides an easy and convenient way to produce or manipulate the original fungal metabolite.

Synthesis and Biological Evaluation of Furo[2,3-d]pyrimidines as Akt1 Kinase Inhibitors

  • Kim, Se-Young;Kim, Dong-Jin;Yang, Beom-Seok;Yoo, Kyung-Ho
    • Bulletin of the Korean Chemical Society
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    • v.28 no.7
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    • pp.1114-1118
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    • 2007
  • Based on the hit compound 4 derived from focused library, a series of furo[2,3-d]pyrimidines were designed, synthesized and evaluated for the inhibitory activity against Akt1 kinase. And their structure-activity relationships were investigated. Of these compounds, 3a having 2-thienyl and methyl groups at R1 and R2 showed the most potent activity with an IC50 value of 24 μ M. Introduction of the thienyl groups at C-5 and C- 6 positions significantly improved potency compared to furyl and phenyl groups.

Antioxidant Effects of the Extracts of Acanthopanax senticosus (가시오갈피 추출물의 항산화효과)

  • Jin, Li-Hua;Han, Sang-Sup;Choi, Yong-Soon
    • Korean Journal of Pharmacognosy
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    • v.33 no.4 s.131
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    • pp.359-363
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    • 2002
  • Antioxidant properties of the extracts of Acanthopanax senticosus were investigated. The dried roots, stems or leaves were extracted with hot water or ethanol each. The ethanol extracts exhibited higher potency than aqueous extracts in scavenging free radicals and in inhibiting microsomal lipid peroxidation: the aqueous extracts of stems showed higher anti-oxidant effects than the root extracts. Copper-mediated LDL oxidation was also protected by the ethanol exlracts: antioxidant effects of the extracts tested were stronger than ascorbic acid, but not butylated hydroxytoluene. The activity of angiotensin converting enzyme was effectively suppressed by the aqueous extracts of the stems. However, in vivo antioxidant properties of the ethanol extracts of the stems did not seem to be significant, judged from the lipid peroxide values of serum and liver in normal mice. Thus, the ethanol extracts of the stems were shown to be more potent for protecting biological systems against various oxidant stresses in vitro, but not in vivo.