• Title/Summary/Keyword: active agent

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Effects of Cyclobuxine D on the Electrocardiogram (ECG) and Heart Rate in Anesthetized Rats and Isolated Frog Heart (Cyclobuxine D의 흰쥐에 있어서 ECG와 심박동수에 패한 작용과 적출 개구리 심장에 대한 작용)

  • Lee, Jong-Hwoa;Park, Young-Hyun;Cho, Byung-Heon;Kim, Yu-Jae;Kim, Jong-Bae;Kim, Chun-Sook;Cha, Young-Dong;Kim, Young-Suk
    • The Korean Journal of Pharmacology
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    • v.22 no.2
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    • pp.105-114
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    • 1986
  • This study was undertaken to search for a new antiarrhythmic agent in natural plants. Extracts of Buxus microphylla var. koreana Nakai have been used as folk remedies of several diseases, including malaria and venereal disease, but any study on the pharmacological actions of this plant has not yet been carried out and its active ingredients have not been identified. In our laboratory, we isolated buxuletin (nonalkaloid) and cyclobuxine D (steroidal alkaloid) from Buxus microphylla var. koreana Nakai and reported their pharmacological actions: diuretic effects of buxuletin in rabbits and hypotensive effect of cyclobuxine D in rats. In the present study, we investigated the effect of cyclobuxine D on isolated frog heart and heart rate in urethane anesthetized rats. In order to clarify the mechanism of bradycardic effect of cyclobuxine D, we examined the changes of the ECG parameters (PR, QRS and R ${\alpha}$ T interval) produced by intravenous injection of cyclobuxine D in anesthetized rats. Cyclobuxine D depressed the contractile force in isolated frog heart and exerted a dose-dependent bradycardic effect in anesthetized rats. Intracerebroventricular injection of cyclobuxine D caused a fall in blood pressure and an increase in heart rate, but those effects were not significant. Cyclobuxine D prolonged the PR interval and RaT interval (${\alpha}$ Tindicates the apex of T), but was without significant effects on the duration of the QRS complex and PRc in urethane anesthetized rats.

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Protective effects of perilla oil and alpha linolenic acid on SH-SY5Y neuronal cell death induced by hydrogen peroxide

  • Lee, Ah Young;Choi, Ji Myung;Lee, Myoung Hee;Lee, Jaemin;Lee, Sanghyun;Cho, Eun Ju
    • Nutrition Research and Practice
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    • v.12 no.2
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    • pp.93-100
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    • 2018
  • BACKGROUND/OBJECTIVE: Oxidative stress plays a key role in neuronal cell damage, which is associated with neurodegenerative disease. The aim of present study was to investigate the neuroprotective effects of perilla oil (PO) and its active component, alpha-linolenic acid (ALA), against hydrogen peroxide $(H_2O_2)$-induced oxidative stress in SH-SY5Y neuronal cells. MATERIALS/METHODS: The SH-SY5Y human neuroblastoma cells exposed to $250{\mu}M$ $H_2O_2$ for 24 h were treated with different concentrations of PO (25, 125, 250 and $500{\mu}g/mL$) and its major fatty acid, ALA (1, 2.5, 5 and $25{\mu}g/mL$). We examined the effects of PO and ALA on $H_2O_2$-induced cell viability, lactate dehydrogenase (LDH) release, and nuclear condensation. Moreover, we determined whether PO and ALA regulated the apoptosis-related protein expressions, such as cleaved-poly ADP ribose polymerase (PARP), cleaved caspase-9 and -3, BCL-2 and BAX. RESULTS: Treatment of $H_2O_2$ resulted in decreased cell viability, increased LDH release, and increase in the nuclei condensation as indicated by Hoechst 33342 staining. However, PO and ALA treatment significantly attenuated the neuronal cell death, indicating that PO and ALA potently blocked the $H_2O_2$-induced neuronal apoptosis. Furthermore, cleaved-PARP, cleaved caspase-9 and -3 activations were significantly decreased in the presence of PO and ALA, and the $H_2O_2$-induced up-regulated BAX/BCL-2 ratio was blocked after treatment with PO and ALA. CONCLUSIONS: PO and its main fatty acid, ALA, exerted the protective activity from neuronal oxidative stress induced by $H_2O_2$. They regulated apoptotic pathway in neuronal cell death by alleviation of BAX/BCL-2 ratio, and down-regulation of cleaved-PARP and cleaved caspase-9 and -3. Although further studies are required to verify the protective mechanisms of PO and ALA from neuronal damage, PO and ALA are the promising agent against oxidative stress-induced apoptotic neuronal cell death.

Study on Medium Ingredient Composition for Enhancing Biomass Productionand Anti-potato Common Scab Activity of Streptomyces sp. A020645 as a BCA Candidate (생물제제(BCA) 후보균주인 Streptomyces sp. A020645 의 대량 균체생산 및 항더뎅이병 활성증진을 위한 고체배지 조성에 관한 연구)

  • Lee, Hyang-Burm;Roh, Hyo-Young;Park, Dong-Jin;Lee, So-Keum;Ko, Young-wan;Koh, Jeong-Sam;Kim, Chang-Jin
    • Research in Plant Disease
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    • v.11 no.1
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    • pp.66-71
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    • 2005
  • The effect of medium components such as wheat bran, rice bran, oat meal, and soybean meal as basic ingredients and KH2PO4, glucose, and molasses as additives on mass production and anti-potato common scab activ ity of a streptomycete A020645 strain as a biocontrol agent (BCA) candidate was investigated. Of basicingredients, oat meal was the best one for mass poduction and enhancement of anti-potato common scabactivity. The biomass production of the active strain was more enhanced when 0.1-0.01.% glucose or molassesas additive were added into the basic medium. These information may have important implications in applying for effective formulation of BCA.

Efficacy of Antagonistic Bacteria for Biological Control of Rhizoctonia Blight (Large patch) on Zoysiagrass (잔디 갈색퍼짐병(Large patch)의 생물학적 방제를 위한 길항 미생물의 선발과 효력 검정)

  • Jung, Woo-Chul;Shin, Taek-Su;Kim, Bong-Su;Im, Jae-Seong;Lee, Jae-Ho;Kim, Jin-Won
    • Research in Plant Disease
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    • v.14 no.1
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    • pp.43-50
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    • 2008
  • Rhizoctonia blight (large patch) caused by Rhizoctonia solani AG2-2 is one of the major diseases on zoysiagrass in golf courses. In this study, anatgonistic bacteria to R. solani AG2-2 were selected in vitro tests using confrontation bioassay and triple layer agar diffusion method. The most active bacteria, Bacillus subtilis CJ-9 were tested for controlling large patch in pots. Relative Performance Indies (RPI) was used as a criterion for the selection of potential biocontrol agent. B. subtilis CJ-9 showed resistance to major synthetic agrochemicals used in golf course. In field tests at golf course, B. subtilis CJ-9 was more effective in suppression of large patch severity and population development of R. solani AG2-2 in soil than chemical fungicides. B. subtilis CJ-9 could be an alternative to chemical fungicides for eco-friendly management of large patch on zoysiagrass.

Betulinic Acid Inhibits LPS-Induced MMP-9 Expression by Suppressing NF-kB Activation in BV2 Microglial Cells

  • Lee, Jae-Won;Choi, Yong-Joon;Kim, Song-In;Lee, Sue-Young;Kang, Sang-Soo;Kim, Nam-Ho;Kwon, Yong-Soo;Lee, Hee-Jae;Chun, Wan-Joo;Kim, Sung-Soo
    • Biomolecules & Therapeutics
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    • v.19 no.4
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    • pp.431-437
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    • 2011
  • Aberrant activation of microglia has been reported to cause neuronal damages by releasing a variety of pro-inflammatory cytokines. Besides where microglia become active, damages have been also observed in remote places, which is considered due to the migration of activated microglia. Therefore, an agent that could suppress abnormal activation of microglia and their subsequent migration might be valuable in activated microglia-related brain pathologies. The objective of the present study was to evaluate anti-inflammatory effects of betulinic acid on lipopolysaccharide (LPS)-stimulated BV2 microglial cells. Pretreatment of betulinic acid significantly attenuated LPS-induced NO production and protein expression of iNOS. Betulinic acid also significantly suppressed LPS-induced release and expression of cytokines such as TNF-${\alpha}$ and IL-$1{\beta}$. Furthermore, betulinic acid significantly uppressed LPS-induced MMP-9 expression, which has been suggested to play an important role in the migration of activated microglia. In order to understand the possible mechanism by which betulinic acid suppresses LPS-induced cytokine production and migration of microglia, the role of NF-kB, a major pro-inflammatory transcription factor, was examined. Betulinic acid significantly suppressed LPS-induced degradation of IKB, which retains NF-kB in the cytoplasm. Therefore, nuclear translocation of NF-kB upon LPS stimulation was significantly suppressed with betulinic acid. Taken together, the present study for the first time demonstrates that betulinic acid possesses anti-inflammatory activity through the suppression of nuclear translocation of NF-kB in BV2 microglial cells.

Pro-Apoptotic Activity of 4-Isopropyl-2-(1-Phenylethyl) Aniline Isolated from Cordyceps bassiana

  • Kim, Mi Seon;Lee, Yunmi;Sung, Gi-Ho;Kim, Ji Hye;Park, Jae Gwang;Kim, Han Gyung;Baek, Kwang Soo;Cho, Jae Han;Han, Jaegu;Lee, Kang-Hyo;Hong, Sungyoul;Kim, Jong-Hoon;Cho, Jae Youl
    • Biomolecules & Therapeutics
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    • v.23 no.4
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    • pp.367-373
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    • 2015
  • Cordyceps species including Cordyceps bassiana are a notable anti-cancer dietary supplement. Previously, we identified several compounds with anti-cancer activity from the butanol fraction (Cb-BF) of Cordyceps bassiana. To expand the structural value of Cb-BF-derived anti-cancer drugs, we employed various chemical moieties to produce a novel Cb-BF-derived chemical derivative, KTH-13-amine-monophenyl [4-isopropyl-2-(1-phenylethyl) aniline (KTH-13-AMP)], which we tested for anti-cancer activity. KTH-13-AMP suppressed the proliferation of MDA-MB-231, HeLa, and C6 glioma cells. KTH-13-AMP also dose-dependently induced morphological changes in C6 glioma cells and time-dependently increased the level of early apoptotic cells stained with annexin V-FITC. Furthermore, the levels of the active full-length forms of caspase-3 and caspase-9 were increased. In contrast, the levels of total forms of caspases-3, caspase-8, caspase-9, and Bcl-2 were decreased in KTH-13-AMP treated-cells. We also confirmed that the phosphorylation of STAT3, Src, and PI3K/p85, which is linked to cell survival, was diminished by treatment with KTH-13-AMP. Therefore, these results strongly suggest that this compound can be used to guide the development of an anti-cancer drug or serve as a lead compound in forming another strong anti-proliferative agent.

Repurposing Auranofin, an Anti-Rheumatic Gold Compound, to Treat Acne Vulgaris by Targeting the NLRP3 Inflammasome

  • Yang, Gabsik;Lee, Seon Joo;Kang, Han Chang;Cho, Yong-Yeon;Lee, Hye Suk;Zouboulis, Christos C.;Han, Sin-Hee;Ma, Kyung-Ho;Jang, Jae-Ki;Lee, Joo Young
    • Biomolecules & Therapeutics
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    • v.28 no.5
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    • pp.437-442
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    • 2020
  • Activation of the NLRP3 inflammasome is critical for host defense as well as the progression of inflammatory diseases through the production of the proinflammatory cytokine IL-1β, which is cleaved by active caspase-1. It has been reported that overactivation of the NLRP3 inflammasome contributes to the development and pathology of acne vulgaris. Therefore, inhibiting activation of the NLRP3 inflammasome may provide a new therapeutic strategy for acne vulgaris. In this study, we investigated whether auranofin, an anti-rheumatoid arthritis agent, inhibited NLRP3 inflammasome activation, thereby effectively treating acne vulgaris. Auranofin suppressed NLRP3 inflammasome activation induced by Propionibacterium acnes, reducing the production of IL-1β in primary mouse macrophages and human sebocytes. In a P. acnes-induced acne mouse model, injection of P. acnes into the ears of mice induced acne symptoms such as redness, swelling, and neutrophil infiltration. Topical application of auranofin (0.5 or 1%) to mouse ears significantly reduced the inflammatory symptoms of acne vulgaris induced by P. acnes injection. Topical application of auranofin led to the downregulation of the NLRP3 inflammasome activated by P. acnes in mouse ear skin. These results show that auranofin inhibits the NLRP3 inflammasome, the activation of which is associated with acne symptoms. The results further suggest that topical application of auranofin could be a new therapeutic strategy for treating acne vulgaris by targeting the NLRP3 inflammasome.

Pancreatic lipase inhibitory activity of taraxacum officinale in vitro and in vivo

  • Zhang, Jian;Kang, Min-Jung;Kim, Myung-Jin;Kim, Mi-Eun;Song, Ji-Hyun;Lee, Young-Min;Kim, Jung-In
    • Nutrition Research and Practice
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    • v.2 no.4
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    • pp.200-203
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    • 2008
  • Obesity has become a worldwide health problem. Orlistat, an inhibitor of pancreatic lipase, is currently approved as an anti-obesity drug. However, gastrointestinal side effects caused by Orlistat may limit its use. In this study the inhibitory activities of dandelion (Taraxacum officinale) against pancreatic lipase in vitro and in vivo were measured to determine its possible use as a natural anti-obesity agent. The inhibitory activities of the 95% ethanol extract of T. officinale and Orlistat were measured using 4-methylumbelliferyl oleate (4-MU oleate) as a substrate at concentrations of 250, 125, 100, 25, 12.5 and $4\;{\mu}g/ml$. To determine pancreatic lipase inhibitory activity in vivo, mice (n=16) were orally administered with com oil emulsion (5 ml/kg) alone or with the 95% ethanol extract of T. officinale (400 mg/kg) following an overnight fast. Plasma triglyceride levels were measured at 0, 90, 180, and 240 min after treatment and incremental areas under the response curves (AUC) were calculated. The 95% ethanol extract of T. officinale and Orlistat, inhibited, porcine pancreatic lipase activity by 86.3% and 95.7% at a concentration of $250\;{\mu}g/ml$, respectively. T. officinale extract showed dose-dependent inhibition with the $IC_{50}$ of $78.2\;{\mu}g/ml$. A single oral dose of the extract significantly inhibited increases in plasma triglyceride levels at 90 and 180 min and reduced AVC of plasma triglyceride response curve (p<0.05). The results indicate that T. officinale exhibits inhibitory activities against pancreatic lipase in vitro and in vivo. Further studies to elucidate anti-obesity effects of chronic consumption of T. officinale and to identify the active components responsible for inhibitory activity against pancreatic lipase are necessary.

Implications from the Analysis of National Curriculum Implementation Supporting Cases in Australia and England (호주와 영국의 국가교육과정 적용 지원 사례 분석)

  • Ka, Eun-A;Lee, Joo-Youn;Lee, Keun-Ho;Lee, Byeong-Cheon
    • Korean Journal of Comparative Education
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    • v.27 no.3
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    • pp.75-100
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    • 2017
  • The 2015 revised national curriculum has been implemented to first year students in elementary school, and will be expanded to middle school and high school from next year, 2018 school year. As of this year, the ways of implementing the curriculum and supporting teachers to better implement the curriculum into their classrooms are crucial. This study explores the implications for building curriculum supporting and implementing system by investigating relevant systems in foreign countries, such as Australia and England. In order to achieve the purpose, this study conducts literature review and previous studies in regards to the curriculum implementing and supporting system, interviews with curriculum developers and teachers, and analyzes their web-sites of the two countries. The results shows that active communication is essential among curriculum developers and curriculum implementers including school teachers and other stake-holders, and this communication can be achieved by building systematic ways; second, professional development for teachers should be recommended by supporting integrated and systematic teaching-learning process; third, the principal agent for curriculum implementation, school teachers, should have the autonomy for implementing the curriculum. The detailed ways for realizing the three implications are suggested.

Experimental Study on the Properties of Surface Treatment Fly Ash Using Arc Discharge (아크방전을 이용한 표면개질 플라이애시의 특성에 관한 실험적 연구)

  • Kim, Sun-A;Park, Sun-Gyu
    • Journal of the Korean Recycled Construction Resources Institute
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    • v.6 no.4
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    • pp.357-364
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    • 2018
  • Fly ash is a material used as a concrete admixture. When fly ash is used for concrete manufacturing, it is expected to improve the performance such as reduction of cement usage and increase of chemical resistance. However, fly ash have some problems such as unburned carbon content and amorphous film on the surface of fly ash particles. When concrete is manufactured using fly ash containing a large amount of unburned carbon, there is a problem that the slump is lowered due to adsorption of AE agent. In addition, the amorphous film on the surface of the particles prevents the reactive substances from leaching out of the fly ash. Therefore, a method of surface treatment of fly ash using plasma has been studied to remove such unburned carbon and amorphous films. However, plasma has the problem that $O_3$ is generated when $O_2$ is used as an active gas. $O_3$ is a harmful substance and adversely affects the health of the experimenter. In this study, the surface of fly ash was treatment by arc discharge. Experimental results show that the unburned carbon is removed when the surface of fly ash is treatment by arc discharge and the amorphous film was broken and the reactivity was improved. Therefore, it is considered that arc discharge can treatment the surface of fly ash and improve the quality of fly ash.