• Nuclear Medicine and Molecular Imaging
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• v.43 no.5
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• pp.478-486
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• 2009

Purpose: 5-iododeoxyuridine analogues have been exclusively developed for the potential antiviral and antitumor therapeutic agents. In this study, we synthesized carbocyclic radioiododeoxyuridineanalogue (ddIVDU) and carbocyclic intermediate as efficient carbocyclic radiopharmaceuticals. Materials and Methods: The synthesis is LAH reduction, hetero Diels-Alder reaction as key reactions including Pd(0)-catalyzed coupling reaction together with organotin. MCA-RH7777 (MCA) and MCA-tk (HSV1-tk positive) cells were treated with various concentration of carbocyclic ddIVDU, and GCV. Cytotoxicity was measured by the MTS methods. For in vitro uptake study, MCA and MCA-tk cells were incubated with 1uCi of [$^{125}I$]carbocyclic ddIVDU. Accumulated radioactivity was measured after various incubation times. Results: The synthesis of ddIVDU and precursor for radioiodination were achieved from cyclopentadiene in good overall yield, respectively. The radioiododemetallation for radiolabeling gave more than 80% yield with > 95% radiochemical purity. GCV was more toxic than carbocyclic ddIVDU in MCA-tk cells. Accumulation of [$^{125}I$]carbocyclic ddIVDU was higher in MCA-tk cells than MCA cells. Conclusion: Biological data reveal that ddIVDU is stable in vitro, less toxic than ganciclovir (GCV), and selective in HSV1-tk expressed cells. Thus, this new carbocyclic nucleoside, referred to in this paper as carbocyclic 2',3'-didehydro-2',3'-dideoxy-5- iodovinyluridine (carbocyclic ddIVDU), is a potential imaging probe for HSV1-tk.

• Korean Journal of Plant Resources
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• v.31 no.2
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• pp.124-135
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• 2018

The study was performed to explore the molecular changes in the vegetative stage (3-and 5-leaf) of sorghum under waterlogging stress. A total of 74 differentially expressed protein spots were analyzed using LTQ-FT-ICR MS. Among them, 12 proteins were up-regulated and 3 proteins were down-regulated. Mass spectrometry (MS) results showed that about 50% of the proteins involved in various metabolic processes. The level of protein expression of malate dehydrogenase and glyceraldehyde-3-phosphate dehydrogenase related to carbohydrate metabolic process increased in both 3 and 5-leaf stage under waterlogging stress. These proteins are known to function as antistress agents against waterlogging stress. The expression of oxygen-evolving enhancer protein 1 protein related to photosynthesis was slightly increased in the treated group than in the control group, however the expression level was increased in the 5-leaf stage compared to the 3-leaf stage. Probable phospholipid hydroperoxide glutathione peroxidase protein and superoxide dismutase protein related to response to oxidative stress showed the highest expression level in 5-leaf stage treatment. This suggests that the production of reactive oxygen species by the waterlogging stress was the most abundant in the 5-leaf treatment group, and the expression of the antioxidant defense protein was increased.

• Microbiology and Biotechnology Letters
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• v.35 no.3
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• pp.238-244
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• 2007

To identify the useful biological activities and the superiority in quality of Korean traditional liquors, we prepared the alcohol-free concentrates from different types of commercial traditional liquors, Takju ($T1{\sim}T3$), Yakju/Cheongju ($Y-1{\sim}Y-5$), Fruit wine (F-1) and Soju (S-1, S-2), respectively. We investigate their compositions as well as antimicrobial, antioxidant, and anti-thrombosis activity. Among the 11 traditional liquors, Y-3, Y-4, Y-5 and F-1 showed higher total-polyphenol, total-flavonoids and reducing sugars than the others. The strong antibacterial and anti-thrombosis activities were identified in Y-3, Y-4, Y-5 and F-1, and a minor antioxidant activity was found in F-l. The antibacterial activity of the Y-3, Y-4, Y-5 and F-1 alcohol-free concentrates showed a broad-spectrum, and growth inhibition was found in gram-positive, gram-negative, and ampicillin-resistant bacteria. The sequential solvent fractionation of Y-3, Y-4, Y-5 and F-1, and following analysis showed that ethyl acetate fractions of Y-3, Y-4, Y-5 and F-1 possess strong antibacterial and anti-thrombosis activity. Especially, the ethyl acetate fractions of Y-3, Y-4 and F-1 showed superior anti-thrombosis activity compared than that of aspirin. Our results suggest that the useful substances are produced from substrates and edible plant added during the fermentation, and the Korean traditional liquors could be developed as strong antibacterial and anti-thrombosis agents.

• Journal of Oral Medicine and Pain
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• v.32 no.2
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• pp.137-150
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• 2007

Trees emit phytoncide into atmosphere to protect them from predation. Phytoncide from different trees has its own unique fragrance that is referred to as forest bath. Phytoncide, which is essential oil of trees, has microbicidal, insecticidal, acaricidal, and deodorizing effect. The present study was performed to examine the effect of phytoncide on Porphyromonas gingivalis, which is one of the most important causative agents of periodontitis and halitosis. P. gingivalis 2561 was incubated with or without phytoncide extracted from Hinoki (Chamaecyparis obtusa Sieb. et Zucc.; Japanese cypress) and then changes were observed in its cell viability, antibiotic sensitivity, morphology, and biochemical/molecular biological pattern. The results were as follows: 1. The phytoncide appeared to have a strong antibacterial effect on P. gingivalis. MIC of phytoncide for the bacterium was determined to be 0.008%. The antibacterial effect was attributed to bactericidal activity against P. gingivalis. It almost completely suppressed the bacterial cell viability (>99.9%) at the concentration of 0.01%, which is the MBC for the bacterium. 2. The phytoncide failed to enhance the bacterial susceptibility to ampicillin, cefotaxime, penicillin, and tetracycline but did increase the susceptibility to amoxicillin. 3. Numbers of electron dense granules, ghost cell, and vesicles increased with increasing concentration of the phytoncide, 4. RT-PCR analysis revealed that expression of superoxide dismutase was increased in the bacterium incubated with the phytoncide. 5. No distinct difference in protein profile between the bacterium incubated with or without the phytoncide was observed as determined by SDS-PAGE and immunoblot. Overall results suggest that the phytoncide is a strong antibacterial agent that has a bactericidal action against P. gingivalis. The phytoncide does not seem to affect much the profile of the major outer membrane proteins but interferes with antioxidant activity of the bacterium. Along with this, yet unknown mechanism may cause changes in cell morphology and eventually cell death.

• The Korean Journal of Pesticide Science
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• v.19 no.1
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• pp.64-70
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• 2015

In order to control garlic white rot (Sclerotium cepivorum), which threatens garlic production in farmers fields, soil solarization (solar sterilization), sclerotia germination inducers and effective microorganisms as biological control agents, and chemical fungicides have been used. Among them, fungicide has been largely used to reduce garlic white rot. In this study, the antifungal activities of five fungicides, prochloraz(a.i. 25%, EC), tebuconazole (a.i. 25%, WP), flutolanil (a.i. 15%, EC), iminoctadine tris-albesilate (a.i. 40%, WP) and isoprothiolane (a.i. 40%, EC) with different mode of action, in mycelial growth, sclerotia germination and sclerotia production, were tested. The inhibitory effects of the 5 fungicides on the mycelial growth, and sclerotia germination and production of garlic white rot pathogen (S. cepivorum T11-2) were investigated on potato dextrose agar (PDA) and their control efficacies were evaluated on garlic flakes. There was no mycelial growth of S. cepivorum T11-2 on PDA amended with $0.8{\mu}g\;mL^{-1}$ of prochloraz or $100{\mu}g\;mL^{-1}$ of tebuconazole. Also prochloraz and tebuconazole inhibited perfectively the sclerotia germination of the pathogen at 10 and $1.0{\mu}g\;mL^{-1}$, respectively. In spite of a very low activity of isoprothiolane in mycelial growth and sclerotia germination of S. cepivorum T11-2, it showed a good inhibitory activity against sclerotia production of S. cepivorum T11-2 on PDA amended with $1.67{\mu}g\;mL^{-1}$. Prochloraz, tebuconazole and flutolanil showed above 70% of control value when they were treated at $100{\mu}g\;mL^{-1}$ using the garlic flake cutting-method.

• Applied Chemistry for Engineering
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• v.22 no.2
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• pp.178-184
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• 2011

In this study, the antibacterial, antioxidative and inhibitory effects of Allium cepa peel extracts on tyrosinase and elastase were investigated. MIC values of the ethyl acetate fraction of Allium cepa peel on especially, S. aureus among the skin resident flora (Staphylococcus aureus, S. aureus; Propionibacterium acnes, P. acnes; Pityrosporum ovale, P. ovale; Escherichia coli, E. coli) were 0.06%. The aglycone fraction showed more excellent free radical (1,1-diphenyl-2-picrylhydrazyl radical, DPPH) scavenging activity ($FSC_{50}=5.05{\mu}g/mL$). Reactive oxygen species (ROS) scavenging activities ($OSC_{50}$) of the ethyl acetate fraction and aglycone fraction in the luminol-dependent $Fe^{3+}-EDTA/H_2O_2$ system were 0.05 and $0.03{\mu}g/mL$, respectively. The cellular protective effect of the aglycone fraction on the rose-bengal sensitized photohemolysis of human erythrocytes exhibited more prominent (${\tau}_{50}$, 480 min at $25{\mu}g/mL$). The inhibitory effects ($IC_{50}$) of the ethyl acetate fraction and aglycone fraction on tyrosinase were 9.16 and $8.68{\mu}g/mL$, the inhibitory effect ($IC_{50}$) of the aglycone fraction on elastase was $14.12{\mu}g/mL$ The transepidermal water loss of the cream containing 0.1% ethyl acetate fraction was decreased from $8.3g/m^2h$ in control to $6.8g/m^2h$ in the subjects applied with cream containing the ethyl acetate fraction. These results indicate that extract/fractions of Allium cepa peel can function as antioxidant in biological systems, particularly skin exposed to UV radiation by scavenging $^1O_2$ and other ROS, and protect cellular membranes against ROS, and possibly as antiaging agents. Allium cepa peel extract could be used as a new cosmeceutical for whitening and anti-wrinkle products.

• Journal of Life Science
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• v.32 no.1
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• pp.1-10
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• 2022

Natural products have gained increasing attention due to their advantage of long-term safety and low toxicity for a very long time. Torreya nucifera is widespread in southern Korea and Jeju Island and its seeds are commonly used as edible food. Oriental ingredients have often been reported for their insecticidal, antioxidant and antibacterial properties, but there have not yet been any studies on their antidiabetic effect. In this study, we investigated several biological activities of T. nucifera pericarp (TNP) and seeds (TNS) extracts and proceeded to characterize the antidiabetic compounds of TNS. The initial results suggested that TNS extract at 15 and 10 ㎍/ml concentration has inhibitory effects on α-glucosidase and protein tyrosine phosphatase 1B, that is 14.5 and 4.35 times higher than TNP, respectively. Thus, the stronger antidiabetic TNS was selected for the subsequent experiments to characterize its active compounds. Ultrafiltration was used to determine the apparent molecular weight of the active compounds, showing 300 kDa or more. Finally the mixture was then partially purified using Diaion HP-20 column chromatography by eluting with 50~100% methanol. Therefore we concluded that the active compounds of TNS have potential as therapeutic agents in functional food or supplemental treatment to improve diabetic diseases.

• Journal of Microbiology and Biotechnology
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• v.9 no.1
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• pp.106-112
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• 1999

The therapeutic potential of phosphodiesterase 4(PDE4) inhibitors in inflammatory diseases including some autoimmune diseases has been explored recently with some hopeful results. These PDE4 inhibitors are thought to show their anti-inflammatory effect by down-regulating tumor necrosis factor-a (TNF-$\alpha$) production in lymphocytes and macrophages. A high concentration of TNF-$\alpha$has been found in rheumatoid arthritis (RA) synovium and reducing TNF-$\alpha$using biological agents was proven to be an effective RA treatment. To test the possibility of using PDE4 inhibitors for RA treatment, the effects of a newly synthesized PDE4 inhibitor, DWP205505, on TNF-$\alpha$ and IL-10 production was tested in cells isolated from normal peripheral blood and rheumatoid arthritis synovial fluid. Cytokine production was assayed at the protein level by sandwich enzyme-linked immunosorbent assay (ELISA) and at the mRNA expression level by semi-quantitative RT-PCR. Another PDE4 inhibitor, RP73401, was used for comparison. DWP205505 and RP73401 had no harmful effect on cell viability up to 10 $\mu$M concentration during the 24 h culture period. DWP205505 as well as RP73401 significantly reduced TNF-$\alpha$ secretion from lipopolysaccharide (LPS)-stimulated peripheral blood mononuclear cells (pBMC) and synovial fluid mononuclear cells (SFMC). The effect of DWP205505 or RP73401 treatment on the mRNA expression of TNF-$\alpha$ was also studied in LPS-stimulated PBMC and SFMC. TNF-$\alpha$ mRNA expression was increased by LPS stimulation and both of the PDE4 inhibitors suppressed TNF-$\alpha$ mRNA expression. For interleukin-l0 (IL-l0), a little different results were obtained from PBMC and SFMC; IL-l0 secretion was unaffected by LPS stimulation and only minimally affected by both of the PDE4 inhibitors in PBMC. In unstimulated SFMC, DWP205505 and RP73401 slightly enhanced IL-10 secretion, while they reduced IL-l0 secretion from LPS-stimulated SFMC where IL-l0 secretion was a lot higher than unstimulated SFMC. These results suggest that the newly synthesized PDE4 inhibitor DWP205505 may have anti-rheumatoid arthritis activity.