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Exploration of Essential Structure of Malloapelta B for the Inhibitory Activity Against TNF Induced $NF-{\kappa}B$ Activation

  • Luu, Chinh Van;Chau, Minh Van;Lee, Jung-Joon;Jung, Sang-Hun
    • Archives of Pharmacal Research
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    • v.29 no.10
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    • pp.840-844
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    • 2006
  • For the exploration of pharmacophoric moiety of malloapelta B (1) possessing the inhibitory activity of $NF-{\kappa}B$ activation, structural variation of ${\alpha},{\beta}-unsaturated$ carbonyl motif was attempted. 1 was reduced by catalytic hydrogenation, sodium borohydride, and lithium aluminumhydride. Catalytic hydrogenation with 30 psi or 15 psi of $H_2$ gas of 1 generated 8-butyl-5,7-dimethoxy-2,2-dimethylchroman (2) and 1-(5,7-dimethoxy-2,2-dimethylchroman-8-yl)butan-1-one (3), respectively. Reduction with sodium borohydride occurred at the double bond of ${\alpha},{\beta}-unsaturated$ ketone of 1 to give 1-(5,7-dimethoxy-2,2-dimethyl-2H-chromen-8-yl)butan-1-one (4). Reduction of 1 with lithium aluminumhydride and then quenched with methanol and water produced unexpected products, 1-(5,7-dimethoxy-2,2-dimethyl-2H-chromen-8-yl)-3-methoxy-1-butene (5) and 1-(5,7-dimethoxy-2,2-dimethyl-2H-chromen-8-yl)-3-hydroxy-1-butene (6). These are formed from the isomerization of initial product 9 through the continuous conjugate carbocation intermediate 11. Addition of ethylmagnesium bromide and dimethyl malonate anion to 1 gave the conjugate adducts 7 and 8. Ethylmagesium bromide and sodium borohydride reduction unusually gave the conjugate addition due to steric congestion around carbonyl group of 1. Compound 2 exhibits the reduced inhibitory activity against $NF-{\kappa}B$ activation and the others do not show the activity. Therefore ${\alpha},{\beta}-unsaturated$ carbonyl group of 1 should be important for its inhibitory activity.

Preparation of Selectively Permeable Membrane Materials with Enhanced Protective Capability against Blister Agents (수포작용제 방호성능이 향상된 선택투과막 제조)

  • Kwon, Tae-Geun;Kim, Jin-Won;Kang, Jae-Sung;Park, Hyen-Bae;Lee, Hae-Wan;Seo, Hyeon-Kwan
    • Membrane Journal
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    • v.24 no.2
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    • pp.167-175
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    • 2014
  • For selectively permeable membrane based on cellulose acetate butyrate (CAB) and polyethyleneimine (PEI) with water vapor transportability and DMMP protective performance, we intended to improve protective performance of the membrane against CEES using several additives. Results showed that CAB/PEI membranes possessed performance with good water vapor permeation (${\geq}1,800g/m^2/day$) and enhanced protective capability against CEES contamination ($7.1{\sim}11.5{\mu}g/cm^2{\cdot}day$). Of these membranes, the membrane containing $Ag^+$ ion and ionic exchange resin showed the best protective performance. And, we identified that the CAB/PEI membranes show excellent protection against aerosols with various particle sizes ($0.005{\sim}3{\mu}m$) simulating biological agents.

Screening for Antifungal Endophytic Fungi Against Six Plant Pathogenic Fungi

  • Park, Joong-Hyeop;Park, Ji-Hyun;Choi, Gyung-Ja;Lee, Seon-Woo;Jang, Kyoung-Soo;Choi, Yong-Ho;Cho, Kwang-Yun;Kim, Jin-Cheol
    • Mycobiology
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    • v.31 no.3
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    • pp.179-182
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    • 2003
  • A total of 187 endophytic fungi were isolated from 11 plant species, which were collected from 11 locations in Korea. Their antifungal activities were screened in vivo by antifungal bioassays after they were cultured in potato dextrose broth and rice solid media. Antifungal activity against plant pathogenic fungi such as Magnaporthe grisea(rice blast), Corticium sasaki(rice sheath blight), Botrytis cinerea(tomato gray mold), Phytophthora infestans(tomato late blight), Puccinia recondita(wheat leaf rust), and Blumeria graminis f. sp. hordei(barley powdery mildew) was determined in vivo by observing the inhibition of plant disease development. Twenty(11.7%) endophytic fungi fermentation broths were able to control, by more than 90%, at least one of the six plant diseases tested. Among 187 liquid broths, the F0010 strain isolated from Abies holophylla had the most potent disease control activity; it showed control values of more than 90% against five plant diseases, except for tomato late blight. On the other hand, fourteen(7.5%) solid culture extracts exhibited potent disease control values of more than 90% against one of six plant diseases. The screening results of this study strongly suggested that metabolites of plant endophytic fungi could be good potential sources for screening programs of bioactive natural products.

Evaluation of effectiveness and bioassay of insecticide residues of chlorfenapyr(ac303 630) against Thrips palmi Karny(Thysanoptera ; Thripidae) under laboratory and vinyl house conditions (오이총채벌레에 대한 클로르페나피르(AC303 630) 약효와 약효지속기간)

  • Park, Jong-Dae;Lee, Ho-Bum;Kim, Do-Ik;Kim, Seon-Gon;Song, Seong-Do
    • The Korean Journal of Pesticide Science
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    • v.3 no.2
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    • pp.69-73
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    • 1999
  • The insecticidal activities and residues of chlorfenapyr [4-bromo-2-(4-chlorophenyl)-1-ethoxymethyl-5-trifluorornethyl pyrrole-3-carbonitrile] against Thrips palmi was evaluated under laboratory and vinyl house conditions. Effectiveness of chlorfenapyr against T. palmi on red pepper leaves was lasted for 9 days at a concentration of 50 ppm but there was no significant differences between emulsifiable concentration and wettable granule under laboratory conditions. In vinyl house, high toxicity was investigated at 6 hours after application of chlorfenapyr in a concentration of 50 and 100 ppm and insecticidal effect was maintained for 11days after 2 times weekly application in cucumber. Control effect was above 97% against T. palmi larva and larva+adults after 2 times weekly application in vinyl house.

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Methyl salicylate and trans-anethole affect the pheromonal activity of homofarnesal, the female sex pheromone of azuki bean beetle

  • CHILUWAL, Kashinath;KIM, Junheon;BAE, Soon Do;ROH, Gwang Hyun;PARK, Chung Gyoo
    • Entomological Research
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    • v.48 no.5
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    • pp.354-361
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    • 2018
  • Plant essential oils (EOs) exhibit an array of biological activities against insect pests. However, their negative influences on the pheromonal activity of azuki bean beetle (ABB), Callosobruchus chinensis L. have not received research attentions. ABB is a field-to-storage pest of legumes, and its female produces the sex pheromone known as homofarnesal with two isomeric components: 2E- and 2Z-homofarnesal, (2E,6E)-7-ethyl-3,11-dimethyl-2,6,10-dodecatrienals and (2Z,6E)-7-ethyl-3,11-dimethyl-2,6,10-dodecatrienals. We evaluated the effects of three EOs and their two major components on the attractiveness of male ABBs to synthetic homofarnesal (2E-:2Z-homofarnesal = 6:4) using Y-tube olfactometry in laboratory and rocket traps in the semi-open polyhouse. Y-tube olfactometry showed the significant negative effect of EOs of Illicium verum, Croton anisatum at 10 and 100 ng, and Gaultheria fragrantissima at 100 ng against homofarnesal (100 ng) in attracting male ABBs. Similarly trans-anethole (at 10 and 100 ng) and methyl salicylate (at 100 ng) also ascertained significant negative effect against homofarnesal (100 ng) in Y-tube olfactometry. When 10 mg of each of trans-anethole and methyl salicylate was released at the downstream of 30 mg homofarnesal lure in rocket traps, highly significant effect was achieved against attractiveness of homofarnesal to ABB males. This study ascertained significant level of negative effect of the tested EOs and their major components to homofarnesal, tracing out a new opportunity of integrating them in ABB management programs both in field and storage.

Evaluation of Comprehensive Effects of Methanol Extracts of Coptidis rhizoma against Several Oral Pathogenic Bacteria (황련 메탄올 추출물의 주요 구강 병원성 세균에 대한 포괄적 활성 평가)

  • Chae Hyeon Seo;Youngcheon Song;Dongsool Yim;Sungsook Choi
    • Korean Journal of Pharmacognosy
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    • v.54 no.1
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    • pp.27-37
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    • 2023
  • This research was conducted to investigate the comprehensive effects of methanol extract of Coptidis rhizoma (MECR) against oral pathogen. We studied the antibacterial, anti-biofilm, anti-gingipain and anti-inflammatory activity of MECR. The minimum bactericidal concentration (MBC) of MECR was 100 ㎍/mL against several oral pathogens. The formation of biofilm of Streptococcus mutans was reduced to 8.93~24.12% in the presence of 25 ㎍/mL of MECR. The gingipain activity of Porphyromonas gingivalis were reduced to 3.91~6.23% in case of Kgp and 5.73~7.78% in case of Rgp in the presence of 10 mg/mL of MECR. The expression of fadA mRNA, virulence factor of Fusobacterium nucleatum (F. nucleatum) was 3 folds decreased in the presence of 25 ㎍/mL of MECR. In case of YD-38 cells challenged with F. nucleatum, RQ values of IL-8 and IL-6 were reduced about 12 folds and 5.45 folds in the presence of 2 ㎍/mL of MECR. In case of RAW 264.7 murine cell challenged with F. nucleatum, RQ values of IL-1β and IL-6 were 2.52 folds and 2.55 folds reduced in the presences of 2 ㎍/mL of MECR. Conclusively, MECR showed potent antibacterial and anti-inflammatory effects against oral pathogenic bacteria.

Evaluation of Toxicity of 83 Pesticides against Aphid Parasitoid, Aphidius colemani (Hymenoptera: Braconidae), and Control Effects of the Green Peach Aphid, Myzus persicae with a Combination of Aphid Parasitoid and Pesticides (콜레마니진디벌에 대한 83종 농약의 독성평가 및 천적과 농약의 혼용에 의한 복숭아혹진딧물의 방제효과)

  • Kim, Jin-Ju;Seo, Dong-Kyu;Kim, Gil-Hah
    • Korean journal of applied entomology
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    • v.45 no.2 s.143
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    • pp.217-226
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    • 2006
  • As the results achieved by the evaluation of toxicities on an aphid parasitoid, Aphidius colemani by 79 pesticides registered as horticultural pesticide and 4 adjuvants far pest control, 6 insecticides including a-cypermethrin, 13 fungicides including metalaxyl-M+mancozeb and 4 acaricides including bifenazate showed low toxicity against A. colemani adult. Low toxicity was showed in all the 4 adjuvants as well. In residual toxicity test from 40 pesticides which showed toxicity more than 50%, A. colemani was safe from 11 pesticides from the 3th day after treatment, 7 pesticides from the 5th day after treatment and 14 pesticides from the 7th day after treatment, respectively. But, chlorpyrifos-methyl, diflubenzuron+chlorpyrifos, etofenprox+diazinone and imidachloprid+chlorpyrifos showed high toxicities reaching 100%, 97.7%, 100% and 100% respectively, even from the 7th day after treatment. To evaluate the control effect by A. colemani against Myzus persicae in a greenhouse, A. colemani was released at parasitoid versus aphids rates of 1:50 and 1:100 when the population of M persicae was 50 per plant. After release, aphids population remained steady for 20 days after release at the level of around 60 aphids per plant. During the investigation, insecticides fur thrips control and fungicides for powdery mildew control were treated, but didn't affect the mummy forming of A. colemani. It may be suggested from these results that the selected insecticides, fungicides, acaricides and adjuvent could be incorporated into the integrated M. persicae management system with A. colemani on greenhouse cultivation.

Survey on the Distrributions of Swine Toxoplasma Antibodies by Latex Agglutination Test in Gyeongnam Central Area (경남 중부지역에서의 Latex응집반응을 이용한 돼지 톡스플라즈마병 항체분포 조사)

  • 이병훈;황보훈;변유성;이순선;김차용;서명득
    • Korean Journal of Veterinary Service
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    • v.15 no.2
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    • pp.174-183
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    • 1992
  • This study was conducted to determine the serum antibodies against toxoplasma in swine from breeding-pig farm, pig farm and abattoir by latex agglutination(LA) test. LA test was carried out with commercial Toxo-MT kit (Eiken chemical co.). The results obtained were summerized as follows : 1. The cut-off titer of positive and negative reactions by Toxo-MT antigen used in this experiment was determined as the serum dilution of 1 ; 32. 2. positive rates of toxoplasma antibodies in 823 swine sera were 17.0%(140 cases) by LA test. 3. The toxoplasma antibody detection rates against 194 swine sera in breeding-pig farm, 273 swine sera in pig farm and 356 swine in abattoir were 46.9%(91 cases), 8.4%(23 cases) and 7.3% (26 cases) , respectively. 4. In LA test serum antibody titers in 823 test sera were shown as 51 cases (36.4%) in 1 : 32, 40(28.6%) in 1;64, 17(12.1%) in 1:128, 14(10.0%) in 1:256, 10(7.1%) in 1:512, 5(3.6%) in 1:1,024, and 3(2.1%) in 1 : 2,048. 5. Positive rates of toxoplasma antibodies in swine sera from each breeding-pig farm were 20.0∼61.9%.

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Partial cross-resistance between Strongyloides venezuelensis and Nippostrongylus brasiliensis in rats

  • Baek, Byeong-Kirl;Islam, M.-Khyrul;Kim, Jin-Ho;Lee, John-Wha;Hur, Jin
    • Parasites, Hosts and Diseases
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    • v.37 no.2
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    • pp.101-107
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    • 1999
  • Rats were immunized through an initial infection with 1,000 filariform larvae (L3) of Nippostrongylus brasiliensis and after complete expulsion of worms they were challenged with 1,000 L3 of Strongyloides venezuelensis to investigate whether cross-resistance developed against a heterologous parasite. Nippostrongylus brasiliensis immunized rats developed a partial cross-resistance against S.venezuelensis migrating larvae (MSL3) in the lungs and adult worms in the small intestine. The population of MSL3 in the lungs were significantly lower (p<0.05) in immunized rats($22.0{\;}{\pm}{\;}7.4$) compared with controls ($105.0{\;}{\pm}{\;}27.6$). The populations of adult worms, egg output and fecundity were initially decreased but from day 14 post-challenge they did not show any significant difference between immunized and control rats. However, the length of worm in immunized rat was revealed as retardation. Peripheral blood eosinophilia was significantly decreased (P<0.05) on day 7 post-challenge and then gradually increased which peaked on da 42 post-challenge when most of the worms were expelled. these results suggest that peripheral blood eosinophilia is strongly involved in the worm establishment and expulsion mechanisms.

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A Differential Fault Attack against Block Cipher HIGHT (블록 암호 HIGHT에 대한 차분 오류 공격)

  • Lee, Yu-Seop;Kim, Jong-Sung;Hong, Seok-Hee
    • Journal of the Korea Institute of Information Security & Cryptology
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    • v.22 no.3
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    • pp.485-494
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    • 2012
  • The block cipher HIGHT is designed suitable for low-resource hardware implementation. It established as the TTA standard and ISO/IEC 18033-3 standard. In this paper, we propose a differentail fault attack against the block cipher HIGHT. In the proposed attack, we assume that an attacker is possible to inject a random byte fault in the input value of the 28-th round. This attack can recover the secret key by using the differential property between the original ciphertext and fault cipher text pairs. Using 7 and 12 error, our attack recover secret key within a few second with success probability 87% and 51%, respectively.