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Lignans and Macrolides from the Leaves of Houttuynia cordata with Inhibitory Activity against NO Production in Murine Macrophage RAW 264.7 Cells

  • Ahn, Jongmin;Chae, Hee-Sung;Chin, Young-Won
    • Natural Product Sciences
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    • v.28 no.1
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    • pp.33-39
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    • 2022
  • Eight lignans (1-8) and two macrolides (9-10) were isolated from the CHCl3-soluble fraction of Houttuynia cordata Thumb (Saururaceae). Structures of isolates were elucidated by extensive spectroscopic methods. Fatty acid-derived macrolides (9-10) have rarely been reported from nature. All the isolates were tested for their inhibitory activities against NO production in RAW 264.7 cells stimulated by LPS. It was found that compounds 3 and 9 remarkably down-regulated LPS-induced NO production with IC50 values, 5.4 and 40.3 μM, respectively, without cytotoxicity.

Insecticidal Activity of Metarhizium anisopliae FT83 against the Different Stages of Beet Armyworm, Spodoptera exigua (곤충병원성 곰팡이 Metarhizium anisopliae FT83의 파밤나방 생육단계별 살충활성)

  • Han, Ji Hee;Kim, Jeong Jun;Lee, SangYeob
    • The Korean Journal of Pesticide Science
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    • v.18 no.4
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    • pp.417-421
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    • 2014
  • The beet armyworm, Spodoptera exigua is pest which is difficult to control. For eco-friendly beet armyworm managements, we isolated entomopathogenic fungi from soil samples by insect-bait method using Tenebrio molitor and conducted bioassay to larvae of beet armyworm. The result of bioassay, a selected strain Metarhizium anisopliae FT83 caused 100% mortality against first ~ third instar larva of S. exigua at $1{\times}10^8conidia/ml$ and medial lethal time ($LT_{50}$) were 0.5 days, 2.6 days and 2.5 days respectively. Mortality against fourth and fifth larvae were $83.3{\pm}6.2%$ and $86.0{\pm}5.7%$ and medial lethal time ($LT_{50}$) were 4.2 days and 3.6 days respectively. Mortality against pupae and eggs of S. exigua were 100%. M. anisopliae FT83 showed high virulence at all developmental stages of S. exigua.

Beta glucan: Heath benefits of optimal ingredients via the mixture ratio of rice bran and Sarcodon aspratus

  • Seo, Yu-Ri;Kim, Hye-Been;Cheong, Kyu-Min;Lim, Ki-Taek
    • Proceedings of the Korean Society for Agricultural Machinery Conference
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    • 2017.04a
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    • pp.101-101
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    • 2017
  • Beta-glucan is a polymerized polysaccharide on beta-1,3 chemical bonds. It has the main pharmacological action of various anticancer mushrooms and is colorless and odorless. In addition, it enhances phagocytosis of macrophages against mycobacterium tuberculosism and increases resistance of host against food poisoning bacteria. Owing to these advantages, beta-glucan was used in various health supplement foods such as immune boosters, hypotensive agent and hypoglycemic agent. Our study was aimed to investigate the effective components of beta-glucan, which was optimized via the contents of Sarcodon aspratus and rice bran. First, the mixture ratio condition of Sarcodon aspratus and rice bran were respectively 10:0, 7:3, 5:5, 3:7, and 0:10. The raw materials were fabricated using hot water extraction method. Distilled water of 100 mL was added to the raw material and extracted. After the extraction processed, the content of effective components was analyzed. The absorbance of beta-glucan was measured using a beta-glucan kit (Megazyme, (1-3) (1-4) BETA-D-GLUCAN ASSAY KIT). The absorbance analysis was repeated three times for accurate analysis. After the extracts were lyophilized, the yields of extracted raw materials according to the mixture ratio conditions of Sarcodon aspratus and rice bran (10:0, 7:3, 5:5, 3:7, and 0:10) were respectively 33.1%, 34.5%, 35.3%, 30.7%, and 24.3%. The absorbance was 1.52, 1.47, 1.50, 1.79, and 1.56, respectively. As a result, the optimum ratio of beta-glucan is 3:7 at Sarcodon aspratus and rice bran. This study suggested that the optimal amount of beta-glucan could be used as a health supplement foods and food additive such as immune boosters, hypotensive agent and hypoglycemic agent. However, the new condition (temperature, time) of hot water extraction to maximize the content of beta-glucan could be considered, could be necessary to compare with the existing extracts.

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Structure-Activity Relationship of Fluoroquinolone in Escherichia coli

  • Lee, Soon-Deuk;Park, Tae-Ho;Lee, Yeon-Hee
    • Archives of Pharmacal Research
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    • v.21 no.2
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    • pp.106-112
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    • 1998
  • Structure-activity relationship of 20 fluoroquinolones was studied using the susceptible and 4 resistant Escherichia coli which were developed against 4 fluoroquinolones [ciprofloxacin (1), KR-10755 (6), norfloxacin (2), and ofloxacin (3)] in our laboratory. The C-7 and C-8 substituents of fluoroquinolone were important in various functions such as the inhibitory activity on DNA gyrase, permeability, and efflux. Among 20 fluoroquinolones, compounds with a 3-methyl-3,7-diazabicyclo[3.3.0]octan-1(5)-ene-7-yl substituent at the C-7 position or a chlorine substituent at the C-8 position showed a good inhibitory activity on DNA gyrase (especially a mutated DNA gyrase). Compounds with a 3,7-diazabicyclo [3.3.0]octan-1(5)-ene-7-yl substituent at the C-7 position showed good permeability in the susceptible and resistant strains, while compounds with a fluorine substituent at the C-8 position were less eff luxed from cells.

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Antimutagenic and Cytotoxic Effects of Aster scaber Root Ethanol Extract (참취뿌리 에탄올추출물의 항돌연변이성 및 암세포 성장억제효과)

  • Hwangbo, Hyun-Su;Ham, Seung-Shi
    • Korean Journal of Food Science and Technology
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    • v.31 no.4
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    • pp.1065-1070
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    • 1999
  • This study was performed to determine the antimutagenic and cytotoxic effect of Aster scaber root ethanol extract on Salmonella typhymurium TA98, TA100 and cancer cell lines using Ames test and cytotoxicity assay, respectively. Cancer cell lines include chronic myelogenous leukemia(K562), human gastric carcinoma(KATOIII), human hepatocellular carcinoma(Hep3B) and human breast adenocarcinoma(MCF-7). Futher fractionations with hexane, chloroform, ethyl acetate, butanol and water from ethanol extract of Aster scaber root were performed to obtain effective fraction. Ethanol extract and ethyl acetate fraction showed 79% and 82% inhibitory effect on the mutagenesis induced by N-methyl-N'-nitro-N-nitrosoguanidine(MNNG) against TA100, while 48% and 60% inhibition was observed on the mutagenesis induced by 4-nitroquinoline-l-oxide(4NQO) against TA98. In the meanwhile, ethyl acetate fraction showed 78% and 85% inhibitory effect on the mutagenesis induced by benzo(${\alpha}$)pyrene[B(${\alpha}$)P] against TA98 and TA100, respectively, while 83% inhibition was observed on the mutagenesis induced by 3-amino-l,4-dimethyl-5H-pyrido(4,3-b) indole(Trp-P-1) against TA98. Ethyl acetate fraction (0.125 mg/ml) showed the strongest cytotoxic effect against K562, KATOIII, Hep3B and MCF-7 at the same concentration compared to those of other fractions. Ethanol extract and water fraction showed the least inhibitory effect.

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Evaluation of in Vitro and in Vivo Antibacterial Activity of DWQ-217, a Fluoroquinolone (Fluoroquinolone계 항생제인 DWQ-217의 in vitro와 in vitro 항균작용)

  • 김병오;최문정;한승희;김지연;심점순;박남준;손호정;이재욱;유영효
    • YAKHAK HOEJI
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    • v.39 no.4
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    • pp.351-359
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    • 1995
  • The in vitro and in vivo antibacterial activities of DWQ-217 (1-cyclopropyl-6-fluoro-8-chloro-7-(3-amino-4-methylthiomethylpyrrolidinyl )-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid) were compared with those of ciprofloxacin (CPFX) and vancomycin(VCM). DWQ-217 was superior to those of CPFX and VCM against gram positive bacteria. DWQ-217 showed excellent activity against MRSA (MIC of methicillin; $\geq$12.5 $\mu\textrm{g}$/ml), MIC$_{90}$=0.013. DWQ-217 possessed strong bactericidal action against gram positive and gram negative strains by MIC/MBC test and killing curve. DWQ-217 and CPFX were administered orally and subcutaneously to mice infected systematically with S. aureus and S. pyogenes, DWQ-217 was $\geq$5-16 fold(p.o.) and $\geq$3-5 fold(s.c.) more active than CPFX.

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Optimum Condition of Marine Actinomycetes, Streptomyces sp. NS 13239 for Growth and Producing Antibiotics

  • Shin Il-Shik;Lee Jung-Mo;Park Uk-Yeon
    • Fisheries and Aquatic Sciences
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    • v.3 no.3_4
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    • pp.217-221
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    • 2000
  • In previous study, marine actinomycetes producing the antibiotics were investigated to invent new antibiotics from east coast of Korea. The optimum growth conditions of Streptomyces sp. NS 13239 were $28^{\circ}C$, pH 7.0 and $3\%$ of NaCl concentration in various media. Streptomyces sp. NS 13239 showed strong antimicrobial activity against gram-positive bacteria, specially Methicillin resistant Staphylococcus aureus (MRSA), but just weak antimicrobial activity against yeasts and mold. On the other hand, it did not show antimicrobial activity against gram-negative bacteria. The optimum conditions for producing antibiotics were almost consistent with optimum growth conditions except carbon source and nitrogen source.

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Cytotoxic Neoflavonoids and Chalcones from the Heartwood of Dalbergia melanoxylon

  • Chung, Ha Sook
    • Natural Product Sciences
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    • v.28 no.3
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    • pp.115-120
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    • 2022
  • Ten compounds, consisting of neoflavonoids (1-5), isoflavonoids (6 and 7), flavanone (8), and chalcones (9 and 10) were isolated from the ethyl acetate and n-butanol-soluble fractions of the heartwood of Dalbergia melanoxylon. The chemical structures were identified on the basis of spectroscopic evidence and compared to previously reported spectra. Compounds 1-10 were evaluated for cytotoxicity against HCT116 human colorectal cancer, MDA-MB-231 human metastatic breast cancer, and A2058 human melanoma cell lines. Among them, compounds 3 and 10 showed the strongest cytotoxic activity with IC50 values of 11.92±1.07 μM, 10.83±1.02 μM, and 14.37±1.02 μM, 13.62±1.09 μM against HCT116 and MDA-MB-231 cell lines, respectively. Compounds 9 and 10 also had cytotoxic activity with IC50 values of 13.49±1.18 μM and 9.82±0.91 μM against A2058 cell lines, respectively. To the best our knowledge, compounds 2 and 5-10 were isolated from this source for the first time.

A Study on Incidence of Bacteriuria according to Bladder Irrigation in Patients with Indwelling Catheter (유치도요관 환자의 방광 세척에 따른 요로 감염 발생 빈도에 관한 연구)

  • 고경옥
    • Journal of Korean Academy of Nursing
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    • v.20 no.1
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    • pp.38-49
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    • 1990
  • The Purpose of this study is for clinical nurses to be aware of the significance of prevention against bacteriuria caused form foley catheterization, through probing variables related to the occurrence of bacteriuria which appears as the most frequent occurring infection, and try to lower bacteriuria by applying to nursing care at the clinical. For this study 46 patients with catheterization and the closed drainage system were sampled and investigated from among patients at Intensive Care Unit in Two hospitals affiliated to K University in Seoul. Those patients sampled had not shown bacteriuria before foley catheterization. The research design is to explore the effectiveness of prevention against bacteriuria in accordance with bladder irrigation and no bladder irrigation. Especially, the frequency of occurrence of bacteriuria examined so as to compare the effectiveness of bladder irrigation depending on the type of foley catheter between 2-lumen foley catheter and 3-lumen foley catheter. The results Were as follows. 1. The occurrence of bacteriuria in patient with bladder irrigation was 21.7%, while in patient without bladder irrigation 26.1%. 2. The occurrence of bacteriuria in patient without bladder irrigation according to duration of Indwelling catheter, was 4.3% after 48 h, 8.7% after 72 h and 21.7% after 96 h. 3. In case of 2-lumen foley catheter the occurrence of bacteriuria in patient with bladder irrigation was 0% after 72 h, and 4.35% after 96 h. In case of 3-lumen foley catheter, the occurrence of bacteriuria in patient with bladder irrigation was 13% after 48 h, 8.7% after 72 h and 4.3% after 96 h. 4. The occurrence of bacteriuria according to duration of catheterization was 8.7% after 48 h, 8.7% after 72 h and 15.2% after 96 h. In sex, female was 35% and male 15.4%. 5. The occurrence of bacteriuria according to mental state was 15% in clear state, while 29.6% in mental disorder. 6. In regard to a kind of microorganism induced bacteriuria, Gram negative bacteria was 63.7%, Gram positve bacteria 36.3%.

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Synthesis of 7-Deazapurine Derivatives (7-데아자퓨린 유도체의 합성)

  • 신관석;남재우;이창규;전종갑
    • YAKHAK HOEJI
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    • v.37 no.3
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    • pp.228-234
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    • 1993
  • A new series of 7-deazapurine derivatives[7,8] as purine antagonists was prepared. Diethyl 4-cyano-N-(diphenyimethylene)-3-arylglutamate[3] were synthesized by LDA-catalyzed Michael addition of N-(diphenylrnethylene)glycine ethyl ester with (E)-2-cyano-3-arylacrylate. Deprotection yields diethyl 4-cyano-3-arylglutamate, which were easily cyclized to 4-cyano-2-ethoxycarbonyl-5-oxo-3-arylpyrrolidine[4]. The compounds[4] were treated with NaBH$_{4}$ and then with (C$_{2}$H$_{5}$)$_{3}$OBF$_{4}$ to give 4-cyano-5-ethoxy-2H-2-ethoxymethyl-3-aryl-3,4-dihydropyrrole[6], which were converted to 7-aryl-6-amino-8-ethoxymethyl-7,8-dihydro-7(3H, 9H)-deazapurine-2-thione[7] and 7-aryl-2,6-diamino-8-ethoxymethyl-7,8-dihydro-7(9H)-deazapurine[8] with possible activity against neoplastic disease.

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