• Title/Summary/Keyword: $A^2B^6$ compounds

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Inhibition of protoporphyrinogen oxidase activity and selectivity of new compound EK-5439 (신규 화합물 EK-5439의 선택성 및 protoporphyrinogen oxidase 저해활성)

  • Hong, K.S.;Kim, H.R.;Jeon, D.J.;Lee, B.H.;Song, J.H.;Cho, K.Y.;Hwang, I.T.
    • The Korean Journal of Pesticide Science
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    • v.8 no.2
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    • pp.79-87
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    • 2004
  • 3-Chloro-2-[4-chloro-2-fluoro-5-(5-methyl-3-phenyl-4,5-dihydroisoxazol-5-ylmethoxy)-phenyl]-4,5,6,7-tetrahy dro-2H-indazole(EK-5439) demonstrated rice selectivity and herbicidal activity on annual weeds, such as Echinochloa oryzicola, Monochoria vaginalis, Lindernia pyxidaria, Rotala indica, Aneilema keisak, Cyperus difformis, and Ludwigia prostrata at doses of 16-63 g a.i./ha. However, the application window was limited from pre-emergence to 5 days after transplanting. The control efficacy of EK-5439 on barnyardgrass was 4 times higher than that of oxadiazon. EK-5439 was excellently safe to the 16 different transplanted rice cultivars treated 2 days after transplanting. These compounds have the mechanism of action on the chlorophyll biosynthesis like protoporphyrinogen IX oxidase inhibitors.

Effect of ${\gamma}$-mangostin through the inhibition of 5-hydroxytryptamine$_{2A}$ receptors in 5-fluoro-${\alpha}$-methyltryptamine-induced head-twitch responses of mice

  • Nattaya Chairungsrie;Furukawa, Ken-Ichi;Takeshi Tadano;Kensuke Kisara;Yasushi Ohizumi
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1998.11a
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    • pp.170-170
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    • 1998
  • In order to discover new types of 5-hydroxytryptamine antagonists, we have devoted our attention to investigating naturally occurring compounds having anti-5HT activity in vitro. Recently, ${\gamma}$-mangostin [1,3,6,7-tetrahydroxy-2,8-bis(3-methyl-2-bytenyl)-9H-xanthen-9-one] from the fruit hull of Garcinia mangostana Linn has been shown to be a selective antagonist for 5-hydroxytryptamine$_{2A}$ receptors in smooth muscle and platelets. It is of interesting that y-mangostin which does not have a nitrogen atom, possesses marked 5-$HT_{2A}$ receptor blocking activity. The present study was undertaken to investigate the effects of ${\gamma}$-mangostin on central 5-HT receptors by using animal behavioural models. Intracerebronventricular injection of ${\gamma}$-mangostin (10-40n mol/mouse) inhibited 5-fluoro-${\alpha}$-methyltryptamin (5-FMT) (45 mg kg$^{-1}$, i.p.)-induced head-twitch response in mice in the presence or absence of citalopram (5-HT-uptake inhibitor). Neither the 5-FMT- nor the 8-hydroxy-2-( di-n-propylamino )tetralin (5-HT$_{1A}$-agonist)-induced 5-HT syndrome (head weaving and hindlimb abduction) was affected by ${\gamma}$-mangostin. The locomotor activity stimulated by 5-FMT through the activation of at-adrenoceptors did not alter in the presence of ${\gamma}$-mangostin. 5-HT-induced inositol phosphates accumulation in mouse brain slices was abolished by ketanserin. ${\gamma}$-Mangostin caused a concentration-dependent inhibition of the inositol phosphates accumulation and the binding of [$^3H$]-spiperone, a specific 5-$HT_{2A}$ receptor antagonist, to mouse brain membranes. Kinetic analysis of the [$^H3$]-spiperone binding revealed that ${\gamma}$-mangostin increased the $_{d}$ value without affecting the $B_{max}$ value, indicating the mode of the competitive nature of the inhibition by ${\gamma}$-mangostin. These results suggest that ${\gamma}$-mangostin inhibits 5-FMT-induced head-twitch response in mice by blocking 5-$HT_{2A}$ receptors not by blocking the release of 5-HT from the central neurone. ${\gamma}$-Mangostin is a promising 5-$HT_{2A}$ receptors antagonist in the central nervous system.m.

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Inhibitory Effect on Melanin Formation, Collagenase and Elastase Activity by synthesized Coenzyme $Q_{10}$ Derivatives (세포내 멜라닌 생성 및 Collagenase와 Elastase에 대한 Coenzyme $Q_{10}$ 유도체들의 억제활성)

  • Choi, Won-Sik;Jang, Do-Yoen;Nam, Seok-Woo;Eo, Jin-Yong;Lee, Kyoung-Ju
    • Applied Biological Chemistry
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    • v.51 no.3
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    • pp.164-170
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    • 2008
  • Coenzyme $Q_{10}$ and six derivatives of coenzyme Qn were synthesized and tested for their inhibitory effects on melanogenesis occurred in murine melanoma (B16/F1) cells and on collagenase/elastase activities as well. As the result, synthetic coenzyme Qn showed a potent inhibitory effect on melanin formation, collagenase and elastase activities in all tested concentrations. Among these synthetic compounds, coenzyme $Q_1$ and coenzyme $Q_2$ potentially inhibited melanin formation and elastase activity when compared to other coenzyme Qn derivatives. For the collagenase activities, all coenzyme Qn derivatives inhibited 80-85% of controls. As compared, coenzyme Qn derivatives exhibited strong inhibitory activities with the decrease of isoprenoid unit number of coenzyme Qn derivatives except for collagenase activity. For the inhibition of collagenase activity, moiety of benzoquinone might be considered as the active functional group. Taken together, coenzyme $Q_1$ and coenzyme $Q_2$ might be used for functional cosmetics.

Anti-Inflammatory Effect of Ethanol Extract from Onion (Allium cepa L.) Peel on Lipopolysaccharide-Induced Inflammatory Responses in RAW 264.7 Cells and Mice Ears (LPS로 유도된 RAW 264.7 세포와 마우스 귀 조직에 대한 양파(Allium cepa L.) 껍질 에탄올 추출물의 항염증 효과)

  • Ahn, Na-Kyung;Kang, Bo-Kyeong;Kim, Koth-Bong-Woo-Ri;Kim, Min-Ji;Bae, Nan-Young;Park, Ji-Hye;Park, Sun-Hee;Ahn, Dong-Hyun
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.44 no.11
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    • pp.1612-1620
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    • 2015
  • Inflammation is a complex process involving a variety of immune cells, which defend the body from harmful stimuli. However, pro-inflammatory cytokines and inflammatory mediators can also exacerbate diseases such as cancer. Onion peel contains several phenolic compounds, including quercetin at an amount 20 times greater in peel than edible flesh. Therefore, in this study, the anti-inflammatory effects of onion peel ethanol extract (OPEE) were investigated lipopolysaccharide-induced inflammatory response. In our results, NO production decreased in a dose-dependent manner. Secretion of IL-6, $TNF-{\alpha}$, and $IL-1{\beta}$ was suppressed by 44%, 53%, and 60% respectively, at $100{\mu}g/mL$. Moreover, OPEE also suppressed expression of COX-2, iNOS, $NF-{\kappa}B$, and MAPKs in a dose-dependent manner. Formation of mice ear edema was reduced at the highest dose tested compared to the control, and reduction of ear thickness was observed in the histological analysis as well. In the acute toxicity test, no morality was observed in mice administered 5,000 mg/kg body weight of OPEE over a 2-week observation period. These results suggest that OPEE may have significant effects on inflammatory factors and be a potential anti-inflammatory material.

Enhancement of Immune Activities of Kadsura Japonica Dunal. through Conventional Fermentation Process (오미자의 전통발효에 의한 면역활성 증진)

  • Kim, Cheol-Hee;Kwon, Min-Chul;Kim, Hyo-Sung;Ahn, Ju-Hee;Chio, Geun-Pyo;Choi, Young-Beom;Ko, Jung-Rim;Lee, Hyeon-Young
    • Korean Journal of Medicinal Crop Science
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    • v.15 no.3
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    • pp.162-169
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    • 2007
  • Immune activities of two different extracts of Kadsura japonica Dunal. by typical extraction processes using water and ethanol at 60 $^{\circ}$C and 100 $^{\circ}$C were compared to them by ultrasofication system and through traditional fermemtation process. The fermented broth Kadsura japonica Dunal. definitely improved the growth of human B and T cell up to 30% and 22%, respectively, compared to the control. The secretion of TNF-${\alpha}$ and IL-60 was also enhanced by the addition of the fermented broth, up to 35%. NK cell activation was significantly improved up to 1.4 times higher than the case of adding other extracts. It was also found that this broth could yield higher nitric oxide production from macrophage than Lipopolysaccharides (LPS). It can be concluded that Kadsura japonica has immune activities and, in general, the culture broth from a conventional fermentation has higher immune activities, possibly by yielding immuno-modulatory compounds, not existed in typcial extraction systems as the result of HPLC analysis.

Effect of Packaging Materials on the Quality of Radish Sprout during Storage (포장재가 무순의 저장 중 품질특성에 미치는 영향)

  • Lee, Hyeon-Jeong;Jang, Ji-Hyun;Kwon, Joong-Ho;Moon, Kwang-Deog
    • Food Science and Preservation
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    • v.16 no.2
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    • pp.147-154
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    • 2009
  • Radish sprout was packaged with different materials. PO and PC are both hard case PET(polyethylenterephthalate) and has 6 holes and no holes, respectively. LO, LM and LH are anti-fogging OPP(oriented polypropylene) film which have different oxygen transmission rates. The oxygen concentration and weight loss rate in PO packaged were higher than any other packages. The soluble solid contents of radish sprouts packaged with PO showed much increased during storage. The pH increased during storage but pH of the samples packaged with high oxygen transmission rate was relatively low. Radish sprouts in LO had lower b value as compared to other samples. The result of ${\Delta}E$ value was generally high during storage period, especially at 7 days storage. The contents of total polyphenolic compounds and free radical scavenging activity of radish sprout packaged with PC and LO were high. Total aerobic bacteria of sprouts in PC and LO was much higher than others. The result of organoleptic qualities showed that the radish sprouts packaged with LM had a good score in terms of overall acceptability until 7 days storage.

Chungkook-jang Koji Fermentation with Rice Straw (볏짚을 이용(利用)한 청국장 제조(製造)에 관(關)한 연구(硏究))

  • Kim, Kyung-Ja;Ryu, Myung-Ki;Kim, Sang-Soon
    • Korean Journal of Food Science and Technology
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    • v.14 no.4
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    • pp.301-308
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    • 1982
  • Chungkook-jang Koji was fermented with rice straw at $40^{\circ}C\;and\;50^{\circ}C$ for 72 hours. The changes of proximate composition, pH, titrable acidity, nitrogen compounds, protease activity and free-amino acids during the fermentation were investigated. Moisture, lipid and protein contents remained essentially unchanged during the fermentation. The pH was gradually increased from 6.4 to 7.46 and 7.82 at $40^{\circ}C\;and\;50^{\circ}C$, respectively, after 72 hour fermentation. Amino type and water soluble nitrogen increased as fermentation progressed. however, the former slightly decreased after 60 hour fermentation. Chungkook-jang fermented at $40^{\circ}C$ showed somewhat higher protease activity than $50^{\circ}C$. However, protease activity at both fermentation temperatures showed the same trend; that is, it increased until 48 hour fermentation and thereafter decrease. Free amino acid content of Chung-kook-jang after 72 hour fermentation at $40^{\circ}C$ was 6 times greater than that of the steamed soybean, while it was 2.5 times greater at $50^{\circ}C$. Based on these results. it seems that the optimum fermentation conditions for Chungkook-jang were $40^{\circ}C$ and 72 hours.

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Biological Activities and Physiochemical Properties of Gangwon-do Endemic Makjang Products (강원도 시판 막장제품의 이화학적 품질특성 및 생리활성 조사)

  • Kim, Byoung-Mok;Jung, Jee-Hee;Lim, Ji-Hoon;Jung, Min-Jeong;Jeong, Jae-Whung;Choi, Yong-Suck;Sim, Jea-Man;Jeong, In-Hak;Kim, Young-Myoung
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.44 no.6
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    • pp.862-873
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    • 2015
  • In this study, we investigated the physiochemical properties and biological activities of Gangwon-do endemic Makjang (MJ) products (12 types). The pH levels of all samples were in the range of 4.43 to 5.69, and MJ5 showed the highest pH (5.69). The salinities of all samples ranged from 11.1% to 16.9%. Hunter color values for L (lightness), a (redness), and b (yellowness) ranged from 26.2 to 36.9, 3.9 to 11.5, and 6.5 to 16.6, respectively. The amino nitrogen content of MJ2 was highest, whereas the total content of free amino acids of MJ11 (4,657.7 mg%) was highest. Total fatty acid contents of all samples ranged from 1,598.6 mg% to 2,874.4 mg%, with MJ10 showing the highest fatty acid content. The content of total polyphenolic compounds ranged from 401.48 to $746.67{\mu}g$ tannic acid equivalent/mL, with MJ11 showing the highest content. The 1,1-diphenyl-2-picrylhydrazyl and 2,2'-azino-bis(3-ethylbenzothiozoline-6-sulfonic acid) radical scavenging effects of MJ11, MJ8, and MJ4 were 51.30% and 82.5%, 41.29% and 67.0%, and 49.88% and 87.7%, respectively. MJ12 showed the strongest growth inhibitory effect on lung cancer A549 cells, whereas MJ5 showed the strongest growth inhibitory effect on AGS gastric cancer cell and MCF-7 breast cancer cell. MJ7 showed greater lipid accumulation inhibitory activity in HepG2 cells than the others. ACE inhibitory activity of MJ11 was the highest among the samples.

Inhibitory Effect of Linum usitatissimum and Perilla frutescens as Sources of Omega-3 Fatty Acids on Mutagenicity and Growth of Human Cancer Cell Lines (식물성 오메가-3계 지방산 급원인 아마씨 및 들깨의 항돌연변이 및 암세포 증식 억제 효과)

  • Lim, Sun-Young
    • Journal of Life Science
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    • v.19 no.12
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    • pp.1737-1742
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    • 2009
  • It has been known that Linum usitatissimum and Perilla frutescens are dietary sources of possible chemopreventive compounds such as lignans and $\alpha$-linolenic acid. Here, we investigated and compared the inhibitory effects of methanol extracts from Linum usitatissimum and Perilla frutescens on mutagenicity using the Ames test, and growth of human cancer cells (AGS human gastric adenocarcinoma, HT-29 human colon cancer, Hep 3B hepatocellular carcinoma cells). In the Ames test system using Salmonella typhimurium TA100, aflatoxin $B_1$ ($AFB_1$)-induced mutagenicity was significantly inhibited by treatment with the methanol extract from either Linum usitatissimum or Perilla frutescens (p<0.05) in a dose dependent manner. As for N-methyl-N'-nitro-N-nitrosoguamidine (MNNG)-induced mutagenicity, the methanol extracts (5 mg/assay) from Linum usitatissimum and Perilla frutescens showed 63% and 78% inhibitory rates, respectively, indicating that Perilla frutescens possessed stronger antimutagenic activity than did Linum usitatissimum. Inhibitory effects of methanol extracts from Linum usitatissimum and Perilla frutescens on the growth of human cancer cells (AGS, HT-29 and Hep 3B) appeared to increase dose dependently, and the inhibition was more effective against AGS and HT-29 compared to Hep 3B cells. Our results suggested that the methanol extract from Perilla frutescens showed stronger antimutagenic activity than that from Linum usitatissimumas assayed by the Ames mutagenic test, whereas the methanol extract from Linum usitatissimum was more effective than its counterpart for growth inhibition of human cancer cells. It is concluded that intake of Linum usitatissimum and Perilla frutescens as sources of omega-3 fatty acids will be beneficial for preventing cancer.

Magnetic Hardening of Rapidly Solidified $SmFe_{7+x}M_{x}(M=Mo,\;V,\;Ti)$ Compounds (급속냉각된 $SmFe_{7+x}M_{x}(M=Mo,\;V,\;Ti)$ 화합물에서 생성된 신 강자성상)

  • Choong-Jin Yang;E. B. Park;S. D. Choi
    • Journal of the Korean Magnetics Society
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    • v.4 no.3
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    • pp.226-232
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    • 1994
  • Rapidly solidified $SmFe_{7+x}M_{x}(M=Mo,\;V,\;Ti)$ compound were found to crystallize in the ${Sm(Fe,\;M)}_{7}$ based stable magnetic phase by introducing a second transition element into the Sm-Fe binary system. The ${Sm(Fe,\;M)}_{7}$ phase exhibits the highest Curie temperatuer ($T_{c}=355^{\circ}C$) ever Known in the Sm-Fe magnetic systems with a quite high intrinsic coercivity($_{i}H_{c}=3~6\;kOe $). The ${Sm(Fe,\;M)}_{7}$ phase remains stable even after annealing if once form during the rapid solidification. The primary reason for the high coercive force is due to the fine grain size($2000~8000\;{\AA}$)of the magnetic ${Sm(Fe,\;M)}_{7}$ matrix phase, and the enhanced Curie temperature is attributed to the extended solid-solubility of the additive transition elements in Fe matrix, which leads to volume expansion of the ${Sm(Fe,\;M)}_{7}$ cell causing an enhanced coupling constant of Fe atoms.

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