• Journal of Korean Neurosurgical Society
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• 제64권6호
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• pp.864-872
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• 2021

Objective : The aim of our study is to investigate the cytotoxic, antioxidant, and antimicrobial effects of newly synthesized boron compounds in U87MG glioblastoma cell treatment. Methods : We synthesized boron glycine monoester (BGM) and boron glycine diester (BGD) structures containing boron atoms and determined their cytotoxic activities on glioblastoma by the MTT method. The inhibitory concentration 50 (IC₅₀) value was calculated with GraphPad Prism 5.0 program. The IC₅₀ values were administered 48 hours on U87MG glioblastoma cell. Catalase (CAT), acid phosphatase (ACP) and alkaline phosphatase (ALP) enzyme activity, malondialdehyde (MDA), total glutathione (GSH), and total protein levels were detected using spectrophotometric methods. We determined the antimicrobial activities of BGM and BGD with the disc diffusion method. Results : After 48 hours of BGM and BGD application to U87MG glioblastoma cells, we found the IC₅₀ value as 6.6 mM and 26 mM, respectively. CAT and ACP enzyme activities were decreased in BGM and BGD groups. MDA which is a metabolite of lipid peroxidation was increased in both boron compounds groups. GSH level was reduced especially in BGD group. BGM and BGD have been found to be antimicrobial effects. Conclusion : Boron compounds, especially the BGM, can provide a new therapeutic approach for the treatment of glioblastoma with their anticancer, antioxidant, and antimicrobial effects.

• Applied Biological Chemistry
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• 제41권3호
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• pp.258-263
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• 1998

본 연구는 polyyne계 항생물질의 분자 구조와 활성관계를 체계적으로 살펴본 최초의 보고로서 친수성기와 tetrayne 부분을 갖고 있는 화합물이 강한 항균활성을 가질 것이라는 결과를 얻었다. 이와 같은 선행 연구결과를 바탕으로 보다 개선된 활성을 갖는 화합물을 합성하기 위하여 tetrayneol 부분 구조를 가지는 novel한 polyhydroxy 화합물인 당류 유도체를 합성하고 항균성과 구조와의 관계를 검토하였다.

• Advances in Traditional Medicine
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• 제8권1호
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• pp.47-52
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• 2008

The plant Eclipta prostrata, a member of the Compositae family, has folkloric reputation of being used as a medicinal agent in Bangladesh. In the present investigation, attempt was taken to explore the antimicrobial potency and cytotoxicity of its extractives and purified compounds. The methanolic extract of the whole plant, its n-hexane, carbon tetrachloride, chloroform, aqueous soluble fractions and two purified compounds, eclalbasaponin I (1) and II (2), obtained from Eclipta prostrata were subjected to screening for inhibition of microbial growth by the disc diffusion method at 300 and 100 ${\mu}g$/disc for extracts and pure compounds, respectively. In this case, the carbon tetrachloride and chloroform soluble fractions of the methanolic extract appeared very potent in terms of both zone of inhibition and spectrum of activity. However, all the extractives were also subjected to brine shrimp lethality bioassay for preliminary cytotoxicity evaluation. Here, the carbon tetrachloride soluble fraction of methanolic extract revealed the strongest cytotoxicity having $LC_{50}$ of 1.318 ${\mu}g$/ml.

• KSBB Journal
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• 제27권2호
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• pp.114-120
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• 2012

To investigate the antimicrobial activity on bacteria causing a respiration disease and antioxidant effects of water extracts from 12 kinds of wild edible vegetables, we extracted the water extracts for 72 h in $7^{\circ}C$ using distilled water as solvent. The water extracts except Ixeris dentate and Allium monanthum had high concentrations of phenol compounds and flavonoids. Liguraia fischeri specially had the highest level on total phenol compounds and flavonoids with 205 ${\mu}g/mL$ and 98. 86 ${\mu}g/mL$, respectively. The each 0.05% extracts of Sedum sarmentosum and Liguraia fischeri had high effect on the DPPH radical scavenging activity among wild edible vegetables and the most extracts promoted antioxidant activity with increasing concentration of extract. The catalase activity of Erysimum aurantiacum and Aralia elata showed more than 150 units per g of fresh tissue. The effect of antimicrobial activity on water extracts showed characteristic activity. Only Staphylococcus aureus KCTC 1928 and Corynebacterium diptheriae KCTC 3075 were inhibited cell growth on the other hands, the remainder of bacteria was not inhibited cell growth. Nevertheless, the extracts of wild edible vegetables had specific concentration as MIC for antimicrobial activity respectively. In case of the extract of Aster scaber, Erysimum aurantiacum, and Allium monanthum had over 30% antimicrobial activity on the bacteria causing a respiration disease. In results, the wild edible vegetables include high concentrations of total phenol compounds and flavonoids that give a good antioxidant activity and antimicrobial activity. Therefore the wild edible vegetables are functional food for anti-aging and physiological activation.

• 한국식품영양학회지
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• 제11권6호
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• pp.629-634
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• 1998

1-Deoxynojirimycin which is a potent intestinal ${\alpha}$-glucosidase inhibitor was purified from the culture broth by ion exchange chromatography, Sephadex LH20 column chromatography, TSK gel chromatography and HPLC respectively. Acute toxicity of 1-deoxynojirimycin, which was loaded through the oral as dose of 200mg/kg, was investigated in IRC mouse. None of the tested IRC mice were not dead and increase of body weight showed also the same results in comparison with control mice. The antimicrobial susceptibility of 20 pathogenic strains against 3 antidiabetic compounds (1-deoxynojirimycin, AO-128, acarbose) were obtained by agar dilution method. All of the three antidiabetic compounds has very weak antimicrobial activity (MIC>100$\mu\textrm{g}$/ml).

• Bulletin of the Korean Chemical Society
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• 제35권2호
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• pp.562-568
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• 2014

In this work, synthesis, characterization and antimicrobial activity of series of imidazolines-oxazolines scaffolds 5a-f and 10a-d have been investigated. All the imidazolines-oxazolines derivatives were prepared from acid derivatives 1 and 6a-c, and enantiomerically pure (S)-2-amino-3-methyl-1-butanol in four steps with excellent optical purity. The structures of all newly synthesized compounds have been elucidated by $^1H$, $^{13}C$ NMR, GCMS, and IR spectrometry. Their purity was confirmed using elemental analysis. Some newly synthesized compounds were examined to in-vitro antimicrobial activity. Among the prepared products 10d was found to exhibits the most active against all tested bacteria and fungi with minimal inhibitory concentration (MIC) ranged between 21.9 and $42.6{\mu}g/mL$.

• The Plant Pathology Journal
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• 제26권1호
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• pp.57-62
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• 2010

Low-molecular-weight secondary metabolites from plants play an important role in reproductive processes and in the defense against environmental stresses or pathogens. In the present study, we isolated various volatiles and phenolic compounds from white Rosa rugosa flowers, and evaluated the pharmaceutical activities of these natural products in addition to their ability to increase survival in response to environmental stress and pathogen invasion. The DPPH and hydroxyl radical-mediated oxidation assay revealed that the white rose flower extract (WRFE) strongly scavenged free radicals in a dose dependent manner. Moreover, WRFE inhibited the growth of E. coli and fatally attacked those cells at higher concentration (>0.5 mg/mL). FITC-conjugated Annexin V stain provided further evidence that WRFE had strong antimicrobial activity, which may have resulted from a cooperative synergism between volatiles (e.g. 1-butanol, dodecyl acrylate and cyclododecane) and phenolic compounds (e.g. gallic acid) retained in WRFE. In conclusion, secondary metabolites from white rose flower hold promise as a potential natural source for antimicrobial and non-chemical based antioxidant agents.

• 한국식품과학회지
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• 제35권3호
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• pp.483-487
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• 2003

오미자 essential oil에 존재하는 항미생물 활성물질을 분리하기 위하여 hexane-ether 용매계를 이용하여 silica gel column chromatograph를 실시하였다. 여기서 얻은 6개 획분의 S. aureus에 대한 항미생물성을 조사하였고, 항미생물성이 큰 획분의 GC-MS를 통하여 9개의 성분을 동정하였다. 한편 오미자 정유, citronellol 및 terpineol을 첨가한 배지에서 S. aureus와 E. coli의 생육억제 효과를 관할한 결과 E. coli 보다는 S. aureus에 대한 항균력이 큰 것으로 나타났다. 그리고 오미자 정유를 농도별로 첨가한 배지중에서 S. aureus와 E. coli에 대한 경시적 생육억제 효과를 조사한 결과 S. aureus의 경우 오미자 정유 첨가군에서 $6{\sim}12$시간까지 생육이 억제되었으나 E. coli의 경우에는 생육억제 효과가 거의 없었다. 따라서 citronellol과 terpineol이 오미자 정유성분 중에 존재하는 중요 항균물질임을 확인하였다.

• 대한약침학회지
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• 제24권1호
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• pp.32-40
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• 2021

Objectives: Pathogenic microbes are causal agents for various types of severe and even lethal infectious diseases. Despite of development in medication, bacterial and fungal infections still persist to be a vital problem in health care. Bacteria and several fungal species have shown resistance to antibiotics used in treatment to current medications. Therefore, it is a considerable field of interest in the design and development of novel compounds with antimicrobial activity. Methods: The compounds bearing a heterocyclic ring play an imperative role among other organic compounds with pharmacological activity used as drugs in human for control and cure of various infections. Thiadiazoles containing nitrogen-sulfur atom as part of their cyclic structure which shown wide-ranging application as structural units of biologically active molecules and are very useful intermediates in Medicinal Chemistry. Results: The effectiveness of the thiadiazole nucleus was established by the drugs currently used for the treatment of various infections. 1,3,4-Thiadiazoles and some of their derivatives are widely studied because of their broad spectrum of pharmacological activities. Conclusion: In the present work, a series of 1,3,4-Thiadiazole derivatives were synthesized by cyclization of a group of various benzaldehyde with thiosemicarbazide in the presence of various reagent like FeCl3, HCHO by losing a molecule of water. These derivatives were found to possess prominent antimicrobial activity.

• 접착 및 계면
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• 제18권1호
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• pp.13-24
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• 2017

본 연구에서는 50 wt%의 매우 높은 담지량과 70%의 높은 고형분을 가지면서도 물속이나 다양한 제품에 나노 입자 형태로 분산이 가능한 새로운 형태의 소수성 항균 물질 담지 나노 입자를 제조하였다. 실란 기능화 양친성 고분자 전구체(Alkoxysilane-functionalized Amphiphilic Polymer Precursor; 이하 AAPP)와 다양한 실란 화합물을 이용하여 전형적인 Hydrolytic Sol-Gel 공정으로 제조된 수분산 유-무기 하이브리드 나노 입자들을 제조하고, 이를 이용하여서 나노 침전법을 사용하여서 소수성 항균물질을 고함량으로 담지할 수 있는 새로운 공정으로 소수성 항균물질인 Eugenol이 담지된 유-무기 하이브리드 형태의 나노입자 제조하였다. 나노 입자 제조시 제조 조건의 변화에 따른 나노 입자들의 크기, 담지량, 항균 활성 및 방출거동 등에 영향을 미치는 인자들을 조사하였다. 나노 입자의 종류에 관계없이 Minimal Inhibitory Concentration (MIC)는 50 mg/ml로 동일하였고, 모든 균주에서 99 %에 해당하는 우수한 항균력과 Pseudomonas aeruginosa (PSE)를 제외하고는 2주 이상의 항균 지속력을 나타내었다. 특히, Tetraethoxysilane (TEOS)를 첨가한 경우에는 견고한 무기물 도메인으로 인해 가장 높은 담지량 (50 wt.%)과 서방출 (Sustained release)을 나타내었고, Hexanediol (HD)을 첨가한 경우에는 HD 자체의 항균력과 용매로서의 역할도 하였기 때문에 가장 높은 항균력과 70%의 고형분을 나타내었다.