• Molecules and Cells
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• v.20 no.3
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• pp.423-428
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• 2005

Immediately after fertilization, a chromatin remodeling process in the oocyte cytoplasm extracts protamine molecules from the sperm-derived DNA and loads histones onto it. We examined how the histone H3-lysine 9 methylation system is established on the remodeled sperm chromatin in mice. We found that the paternal pronucleus was not stained for dimethylated H3-K9 (H3-$m_2K9$) during pronucleus development, while the maternal genome stained intensively. Such H3-$m_2K9$ asymmetry between the parental pronuclei was independent of $HP1{\beta}$ localization and, much like DNA methylation, was preserved to the two-cell stage when the nucleus appeared to be compartmentalized for H3-$m_2K9$. A conspicuous increase in H3-$m_2K9$ level was observed at the four-cell stage, and then the level was maintained without a visible change up to the blastocyst stage. The behavior of H3-$m_2K9$ was very similar, but not identical, to that of 5-methylcytosine during preimplantation development, suggesting that there is some connection between methylation of histone and of DNA in early mouse development.

• Archives of Pharmacal Research
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• v.21 no.4
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• pp.458-464
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• 1998

Search for a new $\alpha$-methylene-$\gamma$-butyrolactone-bearing 6-substituted purine as a potental antitumor agent has led to synthesize seven, hitherto unreported, $5^1$-Methyl-$5^1$-[(6-substituted-9H-purin-9-yl)methyl]-$2^1$-oxo-$3^1$- methylenetetrahydrofurans (H, Cl, l, $CH_3$, $NH_2$, SH, >C=O) (6a-g). These include $5^1$-Methyl-$5^1$-[(9H-purin-9-yl)methyll-$2^1$-oxo-$3^1$ -methylenetetrahydrofurans (6a), $5^1$-Methyl-$5^1$-[(6-chloro-9H-purin-9-yl)methyl]-$2^1$-oxo-$3^1$-methylenetetrahydr ofurans (6b), $5^1$-Methyl-$5^1$-[(6-chloro-9H-purin-9-yl) methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6c), $5^1$-Methyl-$5^1$-[(6-methyl-9H-purin-9-yl) methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6d), $5^1$-Methyl-$5^1$-[(9H-adenin-9-yl)methyll-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6e), $5^1$-Methyl-$5^1$-[(6-mercapto-9H-purin-9-yl) methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6f) and $5^1$-Methyl-$5^1$-[(9H-hypoxanthin-9-yl)methyll-$2^1$-oxo-$3^1$-methylenetetrahydrof urans (6g) which were made by the Reformatsky-type reaction of ethyl $\alpha$-(bromomethyl) acrylate with the corresponding (6-substituted-9H-purin-9-yl)-2-propanone intermediates (5a-g). These ketone intermediates 5a-g, 1-(9H-purin-9-yl)-2-propanone (5a), 1-(6-chloro-9H-purin-9-yl)-2-propanone (5b), 1-(6-iodo-9H-purin-9-yi)-2-propanone (5c), 1-(6-methyl-9H-purin-9-yl)-2-propanone (5d), 1-(9H-adenin-9-yl)-2-propanone (Se), 1-(6-mercapto-9H-purin-9-yl)-2-propanone (5f), and 1-(9H-hypoxanthin-9-yl)-2-propanone (5g) were directly obtained by the alkylation of the 6-substituted purine bases with the chloroacetone in the presence of $K_2$$CO_3$ (or NaH) under DMF (or DMSO). The preliminary in vitro cytotoxcity assay for the synthetic .alpha.-methylene-y-butyro-lactone compounds (6a-g) were determined against three cell lines (PM-3A, P-388, and K-562) and showed the moderate antitumor activity ($IC_50$ ranged from 1.4 to 4.3 $\mu\textrm{g}$/ml) with the compound $5^1$-methyl-$5^1$ -[(9H-hypoxanthin-9-yl)methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofuran (6g) showing the least antitumor activity.

• Molecules and Cells
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• v.42 no.11
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• pp.773-782
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• 2019

Cellular senescence is an irreversible form of cell cycle arrest. Senescent cells have a unique gene expression profile that is frequently accompanied by senescence-associated heterochromatic foci (SAHFs). Protein kinase CK2 (CK2) downregulation can induce trimethylation of histone H3 Lys 9 (H3K9me3) and SAHFs formation by activating SUV39h1. Here, we present evidence that the PI3K-AKT-mTOR-reactive oxygen species-p53 pathway is necessary for CK2 downregulation-mediated H3K9me3 and SAHFs formation. CK2 downregulation promotes SUV39h1 stability by inhibiting its proteasomal degradation in a p53-dependent manner. Moreover, the dephosphorylation status of Ser 392 on p53, a possible CK2 target site, enhances the nuclear import and subsequent stabilization of SUV39h1 by inhibiting the interactions between p53, MDM2, and SUV39h1. Furthermore, $p21^{Cip1/WAF1}$ is required for CK2 downregulation-mediated H3K9me3, and dephosphorylation of Ser 392 on p53 is important for efficient transcription of $p21^{Cip1/WAF}$. Taken together, these results suggest that CK2 downregulation induces dephosphorylation of Ser 392 on p53, which subsequently increases the stability of SUV39h1 and the expression of $p21^{Cip1/WAF1}$, leading to H3K9me3 and SAHFs formation.

• Food Science of Animal Resources
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• v.25 no.3
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• pp.310-315
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• 2005

The changes in pH, temperature, R-values and ${\mu}-calpain$ and its inhibitor activity of M. longissimus from Hanwoo steer were investigated at 1, 3, 9 and 24h postmortem. The pH and temperature of M. longissimus were significantly (p<0.05) decreased during 24h postmortem time, and were 6.50 and $31.99^{\circ}C$, respectively, at 3h postmortem. $R_{248}\;and\;R_{250}$ were increased, but $R_{258}$ was decreased after 9h postmortem time (p<0.05). Calpain I and calpastatin activity were decreased after 3h and 9h postmortem time, respectively (p<0.05). pH and temperature showed high positive correlations with $R_{258}$ (r=0.967 and r=0.970, respectively), calpain I (r =0.956 and r=0.954, respectively) and calpastatin (r=0.978 and r=0.986, respectively) but had high negative correlations with $R_{248}$ (r=-0.982 and r=-0.973, respectively) and $R_{248}$ (r=-0.983 and r=-0.976, respectively). from these results, the change of postmortem metabolism of M. longissimus from Hanwoo steer likely occurred after 9h postmortem time. However, the further study on the establishment of metabolism from Hanwoo between postmortem 3h and 9h are necessary to produce Hanwoo beef with high acceptance in meat quality.

• Journal of Veterinary Clinics
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• v.31 no.4
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• pp.293-297
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• 2014

Swine influenza is an acute respiratory disease prevalent in pig-growing areas worldwide. In total, 518 gilt and sow serum samples and 14 litters (66 samples) of aborted fetuses from 37 farms (average of 14 serum samples per farm) in Gyeongbuk Province were collected between September 2010 and May 2011. All samples were examined for antibodies to swine influenza virus (SIV) H1N1 and H3N2 using enzyme-linked immunosorbent assay (ELISA). The seropositive rates of gilt and sows were 59.8% (310/518) for SIV H1N1, 78.8% (408/518) for H3N2, and 55.6% (288/518) for both subtypes tested. The rate of aborted fetuses was 13.6% (9/66) for H1N1, 9.1% (6/66) for H3N2, and 9.1% for both subtypes. The seroprevalence for H1N1 in gilts and sows was 46.6% (69/148) and 65.1% (241/370), respectively, and that for H3N2 was 78.4% (116/148) and 78.9% (292/370), respectively.

• Journal of the Korea Academia-Industrial cooperation Society
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• v.19 no.8
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• pp.378-384
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• 2018

$C_9H_7NHCrO_3Cl$ was synthesized by reacting $C_9H_7NH$ with chromium (VI) trioxide. The structure of the product was characterized by FT-IR (Fourier transform infrared) spectroscopy and elemental analysis. The oxidation of benzyl alcohol by $C_9H_7NHCrO_3Cl$ in various solvents showed that the reactivity increased with increasing dielectric constant(${\varepsilon}$) in the following order: DMF (N,N'-dimethylformamide) > acetone > chloroform > cyclohexane. The oxidation of alcohols was examined by $C_9H_7NHCrO_3Cl$ in DMF. As a result, $C_9H_7NHCrO_3Cl$ was found to be an efficient oxidizing agent that converts benzyl alcohol, allyl alcohol, primary alcohols, and secondary alcohols to the corresponding aldehydes or ketones (75%-95%). The selective oxidation of alcohols was also examined by $C_9H_7NHCrO_3Cl$ in DMF. $C_9H_7NHCrO_3Cl$ was the selective oxidizing agent of benzyl, allyl and primary alcohol in the presence of secondary ones. In the presence of DMF with an acidic catalyst, such as $H_2SO_4$, $C_9H_7NHCrO_3Cl$ oxidized benzyl alcohol (H) and its derivatives ($p-OCH_3$, $m-CH_3$, $m-OCH_3$, m-Cl, and $m-NO_2$). Electron donating substituents accelerated the reaction rate, whereas electron acceptor groups retarded the reaction rate. The Hammett reaction constant (${\rho}$) was -0.69 (308K). The observed experimental data were used to rationalize hydride ion transfer in the rate-determining step.

• YAKHAK HOEJI
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• v.41 no.2
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• pp.181-186
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• 1997

A series of 7-deazahypoxanthine and 7-deazaadenine derivatives[6,7.8.9.10,13] as purine antagonists was prepared. The pyrrolidine-5-one derivatives[4,11] were treated vith $(C_2H_5)_3OBF_4$ to give 3- aryl-5-ethoxy-2H-3,4-dihydropyrrole[5,12], which were converted to 7-aryl-7,8-dihydro-7(9H)-deazahy-poxanthine[6,7,8,9,10] and 7-phenyl-2-methyl-7,8- dihydro-7(9H)-deazaadenine[13].

• Journal of Environmental Health Sciences
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• v.42 no.2
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• pp.112-117
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• 2016

Objectives: In this study, we investigated the biodegradation rates of 8 perfluorooctanesulfonate (PFOS) alternatives synthesized at the at Changwon National University in comparison to those of PFOS potassium salt and PFOS sodium salt. Methods: A biodegradability test was performed for 28 days with microorganisms cultured in the good laboratory practice laboratory at the Korea Environment Corporation following the OECD Guidelines for the testing of chemicals, Test No. 301 C Results: While $C_5H_8F_3SO_3K$, $C_8F_{17}SO_3K$ and $C_8F_{17}SO_3Na$ were not degraded after 28 days, the 3 alternatives were biodegraded at the rates of 31.4% for $C_8H_8F_9SO_3K$, 25.6% for $C_{10}H_8F_{13}SO_3K$, 23.6% for $C_{25}F_{17}H_{32}S_3O_{13}Na_3$, 20.9% for $C_{15}F_9H_{21}S_2O_8Na_2$, 15.5% for $C_{23}F_{18}H_{28}S_2O_8Na_2$, 8.5% for $C_{17}F_9H_{25}S_2O_8Na_2$ and 4.8% for $C_6H_8F_5SO_3K$. When the concentration was the same(500 mg/L), $C_{23}F_{18}H_{28}S_2O_8Na_2$ had the lowest tension with 20.94 mN/m, which was followed by $C_{15}F_9H_{21}S_2O_8Na_2$ (23.36 mN/m), $C_{17}F_9H_{25}S_2O_8Na_2$ (27.31 mN/m), $C_{25}F_{17}H_{32}S_3O_{13}Na_3$ (28.17 mN/m), $C_{10}H_8F_{13}SO_3K$ (29.77 mN/m) and $C_8H_8F_9SO_3K$ (33.89 mN/m). Having higher surface tension of 57.64 mN/m and 67.57 mN/m, respectively, than those of the two types of PFOS salts, $C_6H_8F_5SO_3K$ and $C_5H_8F_3SO_3K$ were found valueless as substitute for PFOS. Conclusion: The biodegradation test suggest that 6 compounds could be used as substitutes for PFOS. $C_{23}F_{18}H_{28}S_2O_8Na_2$ and $C_{15}F_9H_{21}S_2O_8Na_2$ were found to be the best substitutes based on biodegradation rate and surface tension, followed by $C_{25}F_{17}H_{32}S_3O_{13}Na_3$, $C_8H_8F_9SO_3K$ and $C_{10}H_8F_{13}SO_3K$. $C_{17}F_9H_{25}S_2O_8Na_2$ was found to have relatively low value as an alternative but it still had a potential to substitute the conventional PFOS.

• Journal of Microbiology and Biotechnology
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• v.25 no.3
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• pp.343-352
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• 2015

H9 is an ethanol extract prepared from nine traditional/medicinal herbs. This study was focused on the anticancer effect of H9 in non-small-cell lung cancer cells. The effects of H9 on cell viability, apoptosis, mitochondrial membrane potential (MMP; ${\Delta}\psi_{m}$), and apoptosisrelated protein expression were investigated in A549 human lung cancer cells. In this study, H9-induced apoptosis was confirmed by propidium iodide staining, expression levels of mRNA were determined by reverse transcriptase polymerase chain reaction, protein expression levels were checked by western blot analysis, and MMP (${\Delta}\psi_{m}$) was measured by JC-1 staining. Our results indicated that H9 decreased the viability of A549 cells and induced cell morphological changes in a dose-dependent manner. H9 also altered expression levels of molecules involved in the intrinsic signaling pathway. H9 inhibited Bcl-xL expression, whereas Bax expression was enhanced and cytochrome C was released. Furthermore, H9 treatment led to the activation of caspase-3/caspase-9 and proteolytic cleavage of poly(ADP-ribose) polymerase; the MMP was collapsed by H9. However, the expression levels of extrinsic pathway molecules such as Fas/FasL, TRAIL/TRAIL-R, DR5, and Fas-associated death receptor were downregulated by H9. These results indicated that H9 inhibited proliferation and induced apoptosis by activating intrinsic pathways but not extrinsic pathways in human lung cancer cells. Our results suggest that H9 can be used as an alternative remedy for human non-small-cell lung cancer.

• Archives of Pharmacal Research
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• v.26 no.1
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• pp.1-8
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• 2003

In this study, a series of new $N^2$ substituted 1,2-dihydro-3H-indazol-3-ones (3a-d) as well as their condensed pyrazolo, pyridazino derivatives such as pyridazino[1,2-a]indazole-6,9,11-triones (4a-h) and 3,9-dioxo-3H,9H-pyrazolo[1,2-a]indazole (7) were synthesized. The antiinflammatory activity of some synthesized compounds was determined by carrageenan-induced rat paw edema technique using diclofenac as reference drug. The pharmacological data showed that most of the tested compounds exhibited a significant long lasting antiinflammatory activity, which in the case of compound 3b was superior to that of diclofenac.