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Studies on the Synthesis and Antibacterial Activity of New $\beta$-Lactam Antibiotics (새로운 베타락탐 항생물질의 합성과 생물활성에 관한 연구)

  • Tae Heung Song;Young Ho Kim
    • Journal of the Korean Chemical Society
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    • v.36 no.2
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    • pp.293-300
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    • 1992
  • The synthesis of a series of 7-[(Z)-2-(2-aminothiazol-4-yl)-2-oxyiminoacetamido]-3-(4,6-diamino-1-alkyl-1,3,5-triazinium-2-yl)thiomethyl-3-cephem-4-carboxylates is described. Variations of an oxyimino moiety in the 7-side chain and quaternary ammonium moiety in the 3-side chain were examined and structure-activity relationship was studied. The 4,6-diamino-1-methyl-1,3,5-triazinium-2-yl derivative of the 7-$\alpha$-methoxyimino series of cephalospoins, particularly 7-[(Z)-2-(2-aminothiazol-4-yl)-2-(methoxyimino)acetamido]-3-(4,6-diamino-1-methyl-1,3,5-triazinium-2-yl)thiomethyl-3-cephem-4-carboxylate(C-1), exhibited broad antibacterial activity against Gram-positive and Gram-negative bacteria including Pseudomonas aeruginosa.

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Antioxidant Enzyme Activity and Antimicrobial Activity of Isatis tinctoria Extract (대청 추출물의 항산화 효소 활성 및 항균 효과)

  • Heo, Buk-Gu;Park, Yun-Jum;Lee, Seung-Jin;Kim, Kwan-Su;Cho, Ja-Yong;Boo, Hee-Ock
    • Korean Journal of Plant Resources
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    • v.25 no.5
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    • pp.543-549
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    • 2012
  • To gather the basic data for increasing the utilization of Isatis tinctoria, we examined the effects of both antioxidative enzyme activity and antimicrobial activity from the extract of Isatis tinctoria. Ascorbate Peroxidase activities reveal that there is an decrease in order; ethanol extract from its stem (1601.7 Unit/mg protein), methanol extract from its leaf (1133.7 Unit/mg protein) and distilled water extract from its leaf (524.3 Unit/mg protein). Catalase activities reveal that there is an decrease in order; ethanol extract from its flower petal (177.1 Unit/mg protein), methanol extract from its leaf (120.8 Unit/mg protein) and distilled water extract from its flower petal (55.4 Unit/mg protein). Peroxidase activities reveal that there is an decrease in order; ethanol extract from its flower petal (27.1 Unit/mg protein), methanol extract from its flower petal (14.6 Unit/mg protein) and distilled water extract from its stem (10.4 Unit/mg protein). Superoxide dismutase activities reveal that there is an increase in order; distilled water extract from its root (90.8%), methanol extract from its flower petal (80.1%) and ethanol extract from its root (75.5%). Its flower extract showed a antimicrobial activity only against Vibrio parahaemolyticus, its root extract had only against Staphylococcus aureus, and its stem extract had against Bacillus subtilis, Escherichia coli and Staphylococcus aureus, regardless of solvents. Especially, distilled water extract from its leaf showed a high antimicrobial activity against both Bacillus subtilis and Escherichia coli and inhibition diameters against those were 30.0 and 24.0 mm, respectively.

Phenolic Compounds from the Leaves of Stewartia pseudocamellia Maxim. and their Whitening Activities

  • Roh, Hyun Jung;Noh, Hye-Ji;Na, Chun Su;Kim, Chung Sub;Kim, Ki Hyun;Hong, Cheol Yi;Lee, Kang Ro
    • Biomolecules & Therapeutics
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    • v.23 no.3
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    • pp.283-289
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    • 2015
  • The half-dried leaves of Stewartia. pseudocamellia were extracted with hot water (SPE) and partitioned with n-hexane (SPEH), dichloromethane (SPED), and ethyl acetate (SPEE) successively. SPE and SPEE showed significant inhibitory effects against melanogenesis and tyrosinase activities. By bioassay-guided isolation, ten phenolic compounds were isolated by column chromatography from SPEE. The whitening effect of the isolated compounds from SPEE were tested for the inhibitory activities against melanogenesis using B16 melanoma cells, in vitro inhibition of tyrosinase, and L-3,4-dihydorxy-indole-2-carboxylic acid (L-DOPA) auto-oxidation assay. A cytotoxic activity assay was done to examine the cellular toxicity in Raw 264.7 macrophage cells. Of the compounds isolated, gallic acid and quercetin revealed significant inhibitory activities against melanogenesis compared to arbutin. In particular, quercetin exhibited similar inhibitory activities against tyrosinase and L-DOPA oxidation without cytotoxicity. These results suggested that SPE could be used as a potential source of natural skin-whitening material in cosmetics as well as in food products.

Isolation of Antifungal Activity Substance from Rheum australe D. Don Roots against Fusarium oxysporum f. sp. lycopersici (Saccardo) Snyder & Hansen (장변대황(Rheum australe D. Don)으로부터 분리된 토마토 시들음병원균(Fusarium oxysporum f. sp. lycopersici (Saccardo) Snyder & Hansen)에 대한 항진균 활성물질 구명)

  • Choi, Ji-Su;Lee, Dong-Woon;Choi, Yong-Hwa
    • Korean Journal of Organic Agriculture
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    • v.28 no.1
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    • pp.95-108
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    • 2020
  • To develop an environment-friendly fungicide for controlling tomato wilt diseases, antifungal active substance was isolated Rheum australe D. Don roots against Fusarium oxysporum f. sp. lycopersici, a pathogen of tomato wilt, in this study. Methanol extract obtained from Rheum australe roots was successively fractionated with hexane, chloroform, ethyl acetate, butanol and water. The ethyl acetate fraction, which showed the highest antifungal activity, was separated by column chromatography, and 60 subfractions were obtained. The 60 subfractions were anlayzed for antifungal activities by bioassay. The active compound was identified as 5-[(E)-2- (3-hydroxy-4-methoxyphenyl)ethenyl]benzene-1,3-diol (rhapontigenin) by NMR and GC-MS analysis. As a result of testing antifungal activity of rhapontigenin against Fusarium oxysporum, EC50 of rhapontigenin was showed strong antifungal activity at 7.48 mg/L. Therefore, this study showed that the Rheum australe roots extract can be a potential candidate which is a environment-friendly fungicide against Fusarium oxysporum.

Inhibitory Effect of Chrysanthemum zawadskii var. latilobum Kitamura Extracts against Mutagenicity of Cigarette Smoke Condensates (CSC) (담배연기응축물로 유도된 돌연변이와 구절초 추출물의 억제 효과)

  • Lee, Jin-Hee;Lim, Heung-Bin
    • Korean Journal of Medicinal Crop Science
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    • v.19 no.3
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    • pp.170-176
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    • 2011
  • This study was carried out to investigate whether Chrysanthermum zawadskii var. latilobum Kitamura (C. zawadskii) extracts has an inhibitory effect against the mutagenicity by cigarette smoke condensates (CSC). C. zawadskii was extracted with 70% ethanol and the yield was 18.5%. We further fractioned 70% ethanol extract sequentially to diethylether, chloroform, dichloromethane, and aqueous water, and gained the yield of 17.5%, 5.6%, 5.8%, 32.8% and 35.5%, respectively. In the Ames test, there was no mutagenic effect of crude extract and its solvent fractions up to 2 mg/plate toward Salmonella typhimurium TA 98 with or without S-9 mix metabolic activations. On the contrary, the crude extract showed an inhibitory activity against the mutagenicity of CSC in the presence of S-9 mix metabolic activation. Diethyl ether layer among five solvent fractions showed the highest inhibitory activity. The inhibitory activity of diethyl ether fraction was also increased in a dose-dependent manner and the inhibitory rate was about 97.7% at the concentration of 1 mg/plate. In this study, we conclude that crude extract of C. zawadskii itself is potentially safe for mutagenicity, and the diethyl ether fraction has an inhibitory effect against the mutagenicity of CSC.

Repellency of the Constituents of Caraway Oil, Carum carvi against, Tetranychus urticae (점박이응애에 대한 Caraway Oil의 기피활성)

  • Yu Jeong-Su;Bae Jeong-Sook;Shin Dong-Ku;Kim Gil-Hah
    • Korean journal of applied entomology
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    • v.44 no.2
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    • pp.161-164
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    • 2005
  • Essential oils of three plants (caraway oil, hyssop oil and lime oil) were screened for repellency against Tetranychus urticae female adults in the lab condition. Among them, caraway oil (Carum carvi) showed $92.2\%$ repellency against female adults at 1,000 ppm concentration. Through the constituent analysis using GC and GC/MS, we confirmed that the two main constituents were carvone $(73.3\%)$ and limonene (26.7). Limonene showed 87.8 and $83.1\%$ repellency against adult females at 1,000 and 100 ppm concentrations, respectively.

Immunoinformatics studies and design of a novel multi-epitope peptide vaccine against Toxoplasma gondii based on calcium-dependent protein kinases antigens through an in-silico analysis

  • Ali Dalir Ghaffari;Fardin Rahimi
    • Clinical and Experimental Vaccine Research
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    • v.13 no.2
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    • pp.146-154
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    • 2024
  • Purpose: Infection by the intracellular apicomplexan parasite Toxoplasma gondii has serious clinical consequences in humans and veterinarians around the world. Although about a third of the world's population is infected with T. gondii, there is still no effective vaccine against this disease. The aim of this study was to develop and evaluate a multimeric vaccine against T. gondii using the proteins calcium-dependent protein kinase (CDPK)1, CDPK2, CDPK3, and CDPK5. Materials and Methods: Top-ranked major histocompatibility complex (MHC)-I and MHC-II binding as well as shared, immunodominant linear B-cell epitopes were predicted and linked using appropriate linkers. Moreover, the 50S ribosomal protein L7/L12 (adjuvant) was mixed with the construct's N-terminal to increase the immunogenicity. Then, the vaccine's physicochemical characteristics, antigenicity, allergenicity, secondary and tertiary structure were predicted. Results: The finally-engineered chimeric vaccine had a length of 680 amino acids with a molecular weight of 74.66 kDa. Analyses of immunogenicity, allergenicity, and multiple physiochemical parameters indicated that the constructed vaccine candidate was soluble, non-allergenic, and immunogenic, making it compatible with humans and hence, a potentially viable and safe vaccine candidate against T. gondii parasite. Conclusion: In silico, the vaccine construct was able to trigger primary immune responses. However, further laboratory studies are needed to confirm its effectiveness and safety.

Antimicrobial activity of honeybee venom against fish pathogenic bacteria (국내산 봉독의 어류병원성 세균에 대한 항균활성)

  • Han, Sang-Mi;Lee, Kyung-Gill;Park, Kwan-Kyu
    • Journal of fish pathology
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    • v.24 no.2
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    • pp.113-120
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    • 2011
  • In this study, we examined antimicrobial activity of the bee venom isolated from honeybee (Apis mellifera L.) against fish pathogenic bacteria, Edwardsiella tarda, Vibrio ichthyoenteri and Streptococcus iniae of cultured olive flounder, Paralichthys olvaceus. The bee venom exhibited significant antimicrobial activity against the both Gram-negative bacteria, E. tarda and V. ichthyoenteri and Gram-positive bacteria, S. iniae. Minimum inhibitory concentration (MIC) and minimun bactericidal concentration (MBC) of the bee venom were 17.6 ${\mu}g$/ml 34.6 ${\mu}g$/ml against E. tarda., and 1.76 ${\mu}g$/ml, 6.8 ${\mu}g$/ml against V. ichthyoenteri, respectively. MIC and MBC of the bee venom were 3.49 ${\mu}g$/ml, 11 ${\mu}g$/ml, respectively against S. iniae. The postantibiotic effect (PAE) of the bee venom was 5 hr, 6 hr, and 7 hr against E. tarda, V ichthyoenteri, and S. iniae, respectively. In addition, its antimicrobial activity was stable under various pH conditions. According to these results, the bee venom showed the excellent antimicrobial activity against the tested pathogenic bacteria.

Anti-Oxidative Effects of Cymbopoton Citratus Ethanol Extract through the Induction of HO-1 Expression in RAW 264.7 Cells (RAW264.7 세포에서 Cymbopogon Citratus 에탄올 추출물의 HO-1 유도를 통한 항산화 효과)

  • Chung-Mu Park;Hyun-Seo Yoon
    • Journal of The Korean Society of Integrative Medicine
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    • v.11 no.4
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    • pp.73-82
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    • 2023
  • Purpose : Cymbopogon citratus, also known as lemongrass, has widely spread around the world and its essential oil is usually applied in food, perfume, and other industrial purposes. In addition, C. citratus has also been used for the treatment of inflammation, digestive disorders, and diabetes in traditional medicine. In this study, the antioxidative activity of C. citratus ethanol extract (CCEE) was analyzed in RAW 264.7 cells through the induction of one of phase II enzymes, heme oxygenase (HO)-1 by nuclear factor-erythroid 2 p45-related factor (Nrf)2, mitogen-activated protein kinase (MAPK), and phosphoinositide 3-kinase (PI3K)/Akt. Methods : The antioxidative activity of CCEE against oxidative stress and its underlying molecular mechanisms were analyzed by the cell viability assay, intracellular reactive oxygen species (ROS) formation assay, and Western blot analysis in RAW 264.7 cells. Results : The results exhibited that CCEE potently attenuated tert-butyl hydroperoxide (t-BHP) induced intracellular ROS levels in a dose-dependent manner without any cytotoxicity. CCEE treatment significantly induced the expression of HO-1 which is known for its antioxidative capacity. In addition, CCEE treatment significantly upregulated the expression of Nrf2, a corresponding transcription factor for the regulation of antioxidative enzymes, which was in accordance with the HO-1 overexpression. MAPK and PI3K/Akt were also evaluated for their important roles in the regulation of cellular redox homeostasis against oxidative damage. As a result, the potent HO-1 expression was mediated by not extracellular regulated kinase (ERK), c-Jun NH2 terminal kinase (JNK), p38, but phosphoinositide 3-kinase (PI3K) phosphorylation. To confirm the antioxidative activity of CCEE-induced HO-1 expression, oxidative damage was initiated by t-BHP and attenuated by CCEE treatment, which was identified by HO-1 selective inhibitor and inducer. Conclusion : Consequently, CCEE potently induced the HO-1-mediated antioxidative potential through the modulation of Nrf2 and PI3K/Akt signaling pathways in RAW 264.7 cells. These results suggest that CCEE could be a promising strategy for the mitigation against cellular oxidative damage.

Differential Susceptibility of Tetranychus urticae and its Predator, Phytoseiulus persimilis (Acari: Tetranychidae, Phytoseiidae) against Individual and Combined Treatments of Plant Extracts (점박이응애와 포식성 천적인 칠레이리응애의 식물추출물 단독 및 혼합 처리에 대한 감수성 비교)

  • Lee, Chan-Joo;Kuk, Yong-In;Kim, Sang-Soo
    • Korean Journal of Organic Agriculture
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    • v.27 no.3
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    • pp.327-339
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    • 2019
  • The differential susceptibility of the two spotted spider mite, Tetranychus urticae and its predator, Phytoseiulus persimilis against extracts of Gleditsia japonica var. koraiensis, Camellia sinensis, Cinnamomum cassia, Lantana camara and their mixtures was evaluated. The plant extracts tested were much less toxic to P. persimilis than to T. urticae. The plant extracts tested had little effect on the survival of P. persimilis adult females. Moreover, reproduction of P. persimilis adult females and eclosion of eggs deposited by treated predators were not seriously affected. The treatments of the plant extracts tested showed no serious toxic effect on P. persimilis eggs and exhibited 84~100% hatchability. The treatments with mixtures 3 and 1 were effective against the adult females of T. urticae and yielded 76.0% and 72.7% adulticidal activity at 7 days after treatment, respectively. The treatment of mixture 2 revealed 63.3% adulticidal activity. Generally, the acaricidal activity of the individual treatment of each plant extract was lower than the mixtures. The adult females of T. urticae treated with mixtures 3 and 1 produced only 29.5~31.3% as many eggs as the control females did. All the plant extracts tested exhibited no noticeable toxic effect to the eggs of T. urticae. These results suggest that mixtures 3 and 1 might be used for the control of T. urticae, and expected to be promising candidates for use in integrated mite management program with P. persimilis.