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Biological properties of $\beta$-ketoacetoanilide chlorides against late blight of tomato (베타-케토아세트아닐라이드 염화물 유도체의 토마토 역병에 대한 작용 특성)

  • Choi, Gyung-Ja;Jang, Kyoung-Soo;Kim, Jin-Cheol;Lee, Seon-Woo;Cho, Kwang-Yun;Nam, Kee-Dal;Hahn, Hoh-Gyu
    • The Korean Journal of Pesticide Science
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    • v.8 no.2
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    • pp.137-144
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    • 2004
  • [ $\beta$ ]-Ketoacetoanilide chloride derivatives containing a substituent at 4 in phenyl group (para) reduced specifically the development of tomato late blight caused by Phytophthora infestans. Among $\beta$ketoacetoanilide chloride derivatives, five (KIST163, KIST170, KIST260, KIST263, and KIST267) were selected and tested for their protective, curative, systemic, persistent activities, and disease control efficacy against tomato late blight on adult plants. They exhibited a strong l-day protective activity and $EC_{50}$ of KIST163 and KIST170 were 21.9 and $14.5{\mu}g/mL$, respectively. However, they had little curative and systemic activities. Good persistence of KIST163 and KIST170 on tomato plants were observed against P. infestans; both KIST163 and KIST170 at $100{\mu}g/mL$ showed control values more than 75% in a 7-day protective applications. In addition, the two chemicals effectively controlled the occurrence of P. infestans on adult tomato plants. These results indicate that five $\beta$-ketoacetoanilide chloride derivatives are foliar fungicides with a preventive action and KIST163 and KIST170 have a potential for the control of tomato late blight in the fields.

Adsorption and residues of EPN in the soil of Cheju Island (제주도 토양에서 EPN의 용탈과 잔류)

  • Kim, Jung-Ho;Kam, Sang-Kyu
    • The Korean Journal of Pesticide Science
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    • v.4 no.1
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    • pp.19-25
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    • 2000
  • The adsorption and leaching of organophosphorus pesticide, EPN (O-ethyl-O-4 -nitrophenyl phenyl phosphonothioate) were investigated in Namwon soil(black volcanic soil), Aewol soil(very dark brown volcanic soil) and Mureung soil(dark brown nonvolcanic soil) in Cheju Island. The residue of EPN was surveyed on coastal environment of Cheju in Aug. 1996. The organic matter of Namwon soil, Aewol soil and Mureung soil was 19.8, 6.2 and 2.4%, respectively. The cation exchange capacity of Namwon soil, Aewol soil and Mureung soil was 24.8, 13.0 and 9.5 meq/100 g, respectively. The Freundlich constant, k value, was 89.4, 26.9 and 9.25 for Namwon soil, Aewol soil and Mureung soil, respectively. The k value of Namwon soil with very high organic matter content and cation exchange capacity was the highest for Aewol soil and Mureung soil. The Freundlich constant, 1/n, show a high correlation with organic matter content, i.e. it is less than unity for organic matter rich soil of Namwon soil and greater than unity for organic matter poor soil of Mureung soil. The leaching of EPN was slower for Namwon soil with high k values, and faster for Mureung soil with low k values. The results of the study was demonstrated the potential of pollution for EPN have little leached into soil environment. EPN was not detected in seawater and sediment in the coastal environment in Cheju Island. EPN used in the farm on tile Cheju island were not residued in the coastal environment.

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Changes in Volatile Compounds of Green Tea during Growing Season at Different Culture Areas (녹차엽의 채취 시기와 재배지역에 따른 휘발성 향기 성분의 변화)

  • Lee, Joo-Yeon;Wang, Li-Fei;Baik, Joo-Hyun;Park, Seung-Kook
    • Korean Journal of Food Science and Technology
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    • v.39 no.3
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    • pp.246-254
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    • 2007
  • Fresh tea leaves grown in Jeju Island and Jeonnam Province of South Korea were plucked and processed. Volatile compounds (VCs) were analyzed and identified with SPME-GC/GC-MS/GC-O. The VCs of green teas were classified into two major categories based on their aroma characteristics: the Greenish (Group I), and Floral (Group II) odorants. It was found that the VCs were decreased significantly in fresh tea leaves as they were plucked at the later stages of cultivation. The ratio of VCs responsible for Group I and Group II compounds was well-balanced in tea leaves plucked in May, but the balances were changed when the fresh leaves were processed. The major VCs of fresh tea leaves in Jeju and Jeonnam were n-hexanal, E-2-hexenal, Z-3-hexenal, myrcene, benzyl alcohol, linalool, and phenyl alcohol. Also, Jeju and Jeonnam tea leaves had different aroma composition. n-Heptanol, ${\beta}-pinene$, benzaldehyde, and ethyl salicylate were found in Jeju fresh tea leaves, and Z-3-hexenol, E-2-hexenol, and methyl n-heptanoate were detected in Jeju dry tea leaves. On the other hand, Z-linalool oxide and myrcene were found in Jeonnam dry tea leaves. The SPME-GC method showed high reproducibility (RSD, 7.4%) with no-artifact formation. In this study, optimum plucking period of tea leaves could be determined for production of high quality green tea with a well-balanced aroma and characteristic VCs in green tea according to growing areas.

Study of lubrication and rheological properties of urea grease with respect to PTFE powder addition (PTFE 분말 첨가에 따른 우레아 그리스의 윤활 및 유변학 특성 연구)

  • Son, Kihun;Lee, Dongkyu;Lee, Youngseok;Woo, Jaegu;Ha, KiRyong
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.21 no.2
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    • pp.634-643
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    • 2020
  • In this study, the rheological and tribological properties of urea grease were studied according to the type and amount of polytetrafluoroethylene (PTFE) powders added to the urea grease, which is the most widely used among solid lubricants, to develop an optimal lubrication system. Urea grease was synthesized using 4,4'-methylenebis(phenyl isocyanate)(MDI), oleylamine, and cyclohexylamine, and PTFE powders prepared by dispersion or suspension polymerization process were then added. The basic rheological and tribological properties of the prepared greases were compared. The worked penetration numbers of urea grease decreased with increasing amount of PTFE powders, but both PTFE powders caused no significant changes in heat resistance and copper corrosion resistance. The shear viscosity increased with increasing PTFE powder content, and the dispersion-type PTFE powder was more effective in increasing the viscosity. In the value of the loss coefficient = 1, the shear stress was higher for the grease containing PTFE powders than the non-PTFE added grease, and the dispersion-type PTFE-added grease showed higher viscosity than the suspension-type PTFE-added grease. Finally, urea grease was found to have a low-performance improvement in terms of wear reduction effects by adding PTFE powders, but the load-bearing performance was up to 2.5 times higher for the dispersion-type PTFE and five times higher for the suspension-type PTFE.

Characteristics of Microbial Pretense far Application to Abolished Protein Resource (폐단백자원에 이용하기 위한 미생물 Protease의 특성)

  • Chun, Sung-Sook;Cho, Young-Je;Sung, Tae-Soo;Son, Jun-Ho;Choi, Cheong
    • Applied Biological Chemistry
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    • v.41 no.1
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    • pp.6-12
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    • 1998
  • To extract insoluble proteins and to improve functional properties of abolished proteins, a protease producing Aspergillus sp. MS-18 was isolated from soil. The enzyme was purified and its enzymological characteristics were investigated. It was found that production of protease reached to the maximum when the wheat brae medium containing, 3% arabinose, 0.5% polypepton, 0.1% $(NH_4)_2SO_4$ and 0.2% magnesium chloride was cultured for 3 days. Protease was purified 16.9 folds after ion exchange chromatography and gel filtration and the specific activity was 340.4 unit/mg. Purified enzyme was confirmed as a single band by the polyacrylamide gel electrophoresis. The molecular weight of protease was estimated to be 30,000. Crystalization form of purified protease was a stick shape with rounding edges. The optimum pH and temperature for the protease activity were 9.0 and $60^{\circ}C$, respectively. The enzyme was stable in pH 7.0-12.0 at $50^{\circ}C$. The activity of purified enzyme was inhibited by $Hg^{2+}$, $Cu^{2+}$, $Zn^{2+}$ and $Pb^{2+}$, whereas it was activited by $Na^+$, $Mg^{2+}$ and $Mn^{2+}$. The activity of the protease was inhibited by the treatment with ethylenediaminetetraacetic acid and phenylmethane sulfonyl fluoride. The result suggests that the purified enzyme is a serine protease with metal ion at active site. Km and Vmax of purified protease were $29.33\;{\mu}mole/L$ and $5.13\;{\mu}g/min$, respectively.

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Bioequivalence of Traline Tablet to Zoloft® Tablet (Sertraline HCI 50 mg)

  • Kang, Hyun-Ah;Cho, Hea-Young;Lee, Yong-Bok
    • Journal of Pharmaceutical Investigation
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    • v.41 no.5
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    • pp.317-322
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    • 2011
  • Sertraline HCl, (1S-cis)-4-(3, 4-dichloro-phenyl)-1, 2, 3, 4-tetrahydro-N-methyl-l-naphthalenamine hydrochloride, is a potent and selective serotonin reuptake inhibitor which is used in the treatment of depression and obsessivecompulsive disorders. The purpose of the present study was to evaluate the bioequivalence of two sertraline HCl tablets, Traline tablet (Myungin Pharm. Co. Ltd.) and Zoloft$^{(R)}$ tablet (Pfizer Inc.), according to the guidelines of the Korea Food and Drug Administration (KFDA). The in vitro release of sertraline from the two sertraline HCl formulations was tested using KP VIII Apparatus II method with various dissolution media. Twenty four healthy Korean male volunteers, $23.50{\pm}1.74$ years in age and $64.09{\pm}7.10\;kg$ in body weight, were divided into two groups and a randomized $2{\times}2$ crossover study was employed. After a single tablet containing 50 mg as sertraline HCl was orally administered, blood samples were taken at predetermined time intervals and the concentrations of sertraline in serum were determined using an online columnswitching HPLC method with UV/Vis detection. The dissolution profiles of two formulations were similar in all tested dissolution media. The pharmacokinetic parameters such as $AUC_t$, $C_{max}$ and $T_{max}$ were calculated, and computer programs (Equiv Test and K-BE Test) were utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t$, $C_{max}$ and un-transformed $T_{max}$. The results showed that the differences between two formulations based on the reference drug, Zoloft$^{(R)}$ tablet, were 0.04, 3.26 and -1.29% for $AUC_t$, $C_{max}$, and $T_{max}$, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log0.8 to log1.25. Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating Traline tablet was bioequivalent to Zoloft$^{(R)}$ tablet.

Phytochemical Constituents of Climacium dendroides (곧은 나무이끼(Climacium dendroides)의 식물 화학적 성분연구)

  • Nam, Jung-Hwan;Cho, In-Sook;Kim, Su-Jeong;Nam, Chun-Woo;Seo, Jong-Taek;Yoo, Dong-Lim;Kim, Won-Bae;Ryu, Seung-Yeol;Lee, Eung-Ho;Kim, Min-Young;Yoo, Young-Min;Park, Hee-Juhn;Jung, Hyun-Ju
    • Applied Biological Chemistry
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    • v.51 no.2
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    • pp.136-141
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    • 2008
  • The chromatographic separation of organic solvent extracts of liverwort led to the isolation of six compounds. 2-Chromenone (1), 3, 4-dihydroxy-cinnamic acid (2), 3, 3', 4', 5, 7-pentahydroxy-2-phenylchromen-4-one (3), kaemperol-3-O-${\beta}$-D-glucopyranoside (4), 3-[[3-(3,4-Dihydroxyphenyl)-1-oxo-2-propenyl]oxy]-1, 4, 5-trihydroxycyclohexane carboxylic acid (5) and quercetin-3-O-rutinoside (6) were isolated from the methanolic extracts of the all part of Climacium dendroides. Their structure were established by chemical and spectroscopic methods. All compounds were isolated for the first time from this plant Climacium dendroides.

Effect of Opioid on Nicotinic Receptor-Mediated Catecholamine Secretion in the Rat Adrenal Gland (횐쥐 부신에서 Opioid가 니코틴 수용체를 통한 카테콜아민 분비작용에 미치는 영향)

  • Lim, Dong-Yoon;Lee, Jong-Jin;Choi, Cheol-Hee
    • The Korean Journal of Pharmacology
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    • v.28 no.2
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    • pp.181-190
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    • 1992
  • The present study was conducted to investigate the effect of opioids on catecholamine (CA) secretion evoked by a selective cholinergic nicotinic agonist, 1,1-dimethyl-4-phenyl piperazinium (DMPP) and acetylcholine from the retrogradely perfused rat adrenal glands. Methionine-enkephalin $(9.68{\times}10^{-6}\;M)$ caused a significant inhibition of CA secretion evoked by DMPP (100 uM) and $ACh\;(50\;{\mu}g)$, but had no effect on the spontaneous (basal) CA release. Morphine $(1.73{\times}10^{-5}\;M)$ attenuated considerablely the increase in CA release induced by DMPP and ACh. Morphine itself also did not affect the basal CA output. A 20 to 65% reduction of the DMPP- and ACh-evoked increase in CA release was observed after the pretreatment with methionine-enkephalin or morphine. The increase in CA release evoked by DMPP and ACh was reduced markedly by preloading with an opiate antagonist naloxone $(1.22{\times}10^{-7}\;M)$ while basal CA output was not affected by naloxone. These present experimental results suggest that the nicotinic stimulation-evoked CA release from the perfused rat adrenal gland is inhibited by endogenously released opioid peptides through activation of opiate receptors located in the adrenal gland.

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Comparative molecular field analysis(CoMFA) on the fungicidal activity of 2-thienyl and 2-furyl substituents in bis-aromatic ${\alpha},{\beta}$-unsaturated ketone derivatives (비스 방향족 ${\alpha},{\beta}$ 불포화 케톤 유도체 중 2-thienyl 및 2-furyl 치환체의 항균활성에 관한 비교분자장 분석(CoMFA))

  • Sung, Nack-Do;Yu, Seong-Jae;Lim, Chi-Hwan;Akamatsu, Miki
    • The Korean Journal of Pesticide Science
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    • v.2 no.2
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    • pp.16-21
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    • 1998
  • Bis-aromatic ${\alpha},{\beta}$-unsaturated ketone derivatives represented as substrate(S) were synthesized and their fungicidal activities in vivo against rice blast(Pyricularia oryzae) and tomato leaf blight(Phytophthora infestans) were examined with the quantitative structure activity relationships(QSAR) using 3D QSAR, comparative molecular field analysis (CoMFA). The 3D CoMFA results and those of 2D QSAR were compared and the results reveal that both results show similar trend. The two important factors, steric and electronic, contribute toward the activity. We assumed that fungicidal activity for rice blast was greatly improved by increasing with positive charge of ${\beta}$-carbon and introduction of bulky derivatives into $R_{2}$ group, while that for tomato leaf blight was improved by decreasing the positive charge of ${\beta}$-carbon and introduction of smaller molecular derivative into $R_{2}$ group. The CoMFA analyses clearly demonstrate its potential in unraveling the steric and electronic features of the molecules through contour maps.

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A Synthesis of New Fluorine-containing Phenylformamidines Possessing N-Dialkylaminosulfenyl Group and Their Insecticidal Activities (N-Dialkylaminosulfenyl 치환체를 갖는 새로운 불소 함유 Phenylformamidine 유도체의 합성과 살충활성)

  • Lee, Dong-Guk;Chung, Kun-Hoe;Ko, Young-Kwan;Ryu, Jae-Wook;Woo, Jae-Chun;Koo, Dong-Wan;Choi, Yong-Ho;Park, No-Joong;Kim, Tae-Joon;Choi, In-Young
    • The Korean Journal of Pesticide Science
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    • v.14 no.3
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    • pp.199-208
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    • 2010
  • Phenylformamidine derivatives are well known as insecticides for their specific activity against the insects. It has now been established that they show insecticidal activity as agonists on the octopamine receptor. In order to get a highly active compound we have intensively exploited fluorine substituted-aromatic formamidines possessing N-dialkylaminosulfeny group. Up to now, there are several candidates we found: N-(dialkylamino)sulfenyl-N-methyl-N'-(4-fluoro-2-methylphenyl)formamidines. The miticidal activity of Compound 29 show five-fold higher than Amitraz.