• 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.

• Korean Journal of Microbiology
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• v.28 no.3
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• pp.210-218
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• 1990

The survival and transfer of chromosomal genes coding for the synthesis of amino acids (threonine, tryptophan, histidine, leucine, methionine) and of plasmid-borne genes coding for resistance to antibiotics (chloramphenicol, kanamycin, erythromycin) by transformation in sterile and nonsterile soil (the soil was amended to 12% vol/vol with the clay mineral, montmorillonite) was studied. In pure culture, the numbers of vegetative cells of the Bacillus subtilis strains decreased by 1 to 1.5 orders of magnitude within one week, but spores of each strain showed lesser decreases. In sterile soil, the populations of vegetative cells and spores decreased by 1.5 to 3 orders of magnitude within 2 to 4 days and then showed little additional decreased. The transformation frequencies (number of transformants/numbers of donors and recipients) of individual amino acid-genes invitro ranged from $1.3{\pm}0.6{\times}10^{-6}$ to $6.0{\pm}2.36{\times}10^{-6}$, of two amino acid-genes from $8.5{\pm}0.7{\times}10^{-8}$ to $3.1{\pm}0.6{\times}10^{-7}$, and of the antibiotic-resistance genes from $1.5{\pm} 0.2{\itmes} 10^{-7}$ to $1.4{\pm} 0.4{\times} 10^{-5}$ . In sterile soil, the frequencies of transfer of individual amino acid-genes ranged from $2.0{\times} 10^{-7}$ to $2.0{\times} 10^{-5}$ and of the antibiotic-resistance genes from $2.0{\times} 10^{-7}$ to $9.4{\pm} 4.7{\times} 10^{-6}$. The transfer of two amino acid-genes in sterile soil was detected at a frequency of $2.0{\times} 10^{-6}$ to $4.5{\times} 10^{-6}$, but only in three instances. The transformation frequencies of antibiotic-resistance genes in nonsterile soil were essentially similar to those in sterile soil. However, to detect transformants in nonsterile soil, higher concentrations of antibiotics were needed, as the result of the large numbers of indigenous soil bacteria resistant to the concentration of antibiotics used in the sterile soil and in vitro studies. The results of these studies show that genes can be transferred by transformation in soil and that this mechanism of transfer must be considered in risk assessment of the release of genetically engineered microorganisms to the environment.

• KSBB Journal
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• v.21 no.1 s.96
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• pp.72-78
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• 2006

This study was carried out to investigate the antimicrobial and antioxidative effects of mycelium cultural extract from mushroom. Mushroom mycelium was grown in a defined synthetic liquid medium and citrus extracts, and the culture extracts were examined for antioxidant and antibacterial activity. Myceliums of Phellinus linteus, Cordyceps militaris, Coriolus versicolor, Sparassic crispa, Agaricus blazei, lnonotus obliquus, Lentinus edodes, Hericium erinacium, Gonoderma lucidium in 10% citrus extract supplemented medium and synthesis medium were incubated in a shaking incubator (120 rpm, $24{\sim}30^{\circ}C$ ) for $7{\sim}15$ days. The antimicrobial activity of the culture fluid of mushroom mycelium grown in submerged liquid culture was tested against 12 microorganisms which were fish pathogens and common bacterial species. The culture extracts showed high activity against Vibrio sp. and had poor effect on Streptocouus sp., S. parauberis, S. iniae. The culture extracts obtained from the synthetic medium showed $30{\sim}93%$ of the 1,1-diphenyl-2-picrylhydrazyl radical scavenger activity, the culture extracts obtained from the citrus extracts medium exhibited antioxidant activity up to 55%.

• Tuberculosis and Respiratory Diseases
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• v.54 no.5
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• pp.495-509
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• 2003

Background : Neutrophil-mediated inflammation is usually self-limiting, because neutrophils have a remarkably short life span. Prolonged neutrophil survival, which is caused by decreased spontaneous apoptosis, leads to persistent inflammation in sepsis. Because many inflammatory cytokines, which generate signals that delay apoptosis, are regulated by nuclear factor-${\kappa}B$ transcription factor, we hypothesized that nuclear factor-${\kappa}B$ might be related to the reduced neutrophil apoptosis observed in sepsis. Methods : Neutrophils of healthy volunteers and sepsis patients were freshly isolated from venous blood. Neutrophil apoptosis was assayed with two approaches : by counting apoptotic cells under a microscope and by flow cytometry using Annexin V. The activity of nuclear factor-${\kappa}B$ was assessed by immunofluorescent staining or electrophoretic mobility shift assay. Expression of X-linked inhibitor of apoptosis was measured by western blot assay. Results : We confirmed reduced spontaneous neutrophil apoptosis in patients with sepsis. The number of apoptotic neutrophils in patients with sepsis increased to the level of that in healthy controls after cycloheximide treatment, suggesting that decreased spontaneous neutrophil apoptosis is dependent on de novo protein synthesis. In patients with sepsis, basal neutrophil nuclear factor-${\kappa}B$ was activated compared to the level in healthy controls. Moreover, a blockade of nuclear factor-${\kappa}B$ activity reversed the decreased spontaneous neutrophil apoptosis in sepsis patients. Meanwhile, X-linked inhibition of apoptosis expression, which is regulated by nuclear factor-${\kappa}B$, decreased 24 hours after incubation in healthy persons, but persisted for 24 hours in patients with sepsis. Conclusion : These observations suggest that the reduced spontaneous neutrophil apoptosis observed in patients with sepsis may be related to the induction of survival protein by nuclear factor-${\kappa}B$.

• KSBB Journal
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• v.23 no.6
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• pp.513-518
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• 2008

This paper described the extraction/purification of $\beta$-carotene from recombinant E.coli and evaluation of anti-wrinkle activity of purified $\beta$-carotene. No significant differences in extraction yields were observed when hexane or isobutyl acetate was used. However, extraction from wet-cell cake resulted in 2-fold higher amount of $\beta$-carotene than that from dry cells. Disruption of 5 g-wet cells by ultrasonic homogenizer, acetone dehydration, extraction with isobutyl acetate resulted in 36 mg of $\beta$-carotene corresponding to 61.2% of recovery. The formation and separation of $\beta$-carotene crystal improved the purity. 633 mg of $\beta$-carotene crystal with 93% purity was obtained from 223 g/L of wet-cell cake harvested from 2.5-L fed-batch culture broth. The cultures of normal human primary fibroblast were performed to investigate the effect of $\beta$-carotene on cytotoxicity as MTT assay and anti-wrinkle activity as collagen synthesis assays. $1.7{\mu}M$ of $\beta$-carotene was found to be optimal concentration at which 1.4-fold higher amount of collagen was synthesized than that in absence of $\beta$-carotene. This indicates that highly purified $\beta$-carotene can be obtained from recombinant E.coli by applying simple method with less toxic solvent and can be used in functional cosmetics as anti-wrinkle agent.

• Proceedings of the Korean Ceranic Society Conference
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• 2005.06a
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• pp.1-112
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• 2005

This report is results of a research on recent R&D trends in electroceramics, mainly focusing on the papers submitted to the organizing committee of the International Conference on Electroceramics 2005 (ICE-2005) which was held at Seoul on 12-15 June 2005. About 380 electroceramics researchers attended at the ICE-2005 from 17 countries including Korea, presenting and discussing their recent results. Therefore, we can easily understand the recent research trends in the field of electroceramics by analyses of the subject and contents of the submitted papers. In addition to the analyses of the papers submitted to the ICE-2005, we also collected some informations about domestic and international research trends to help readers understand this report easily. We analysed the R&D trends on the basis of four main categories, that is, informatics electroceramics, energy and environment ceramics, processing and characterization of electroceramics, and emerging fields of electroceramics. Each main category has several sub-categories again. The informatics ceramics category includes integrated dielectrics and ferroelectrics, oxide and nitride semiconductors, photonic and optoelectronic devices, multilayer electronic ceramics and devices, microwave dielectrics and high frequency devices, and piezoelectric and MEMS applications. The energy and environment ceramics category has four sub-categories, that is, rechargable battery, hydrogen storage, fuel cells, and advanced energy conversion concepts. In the processing and characterization category, there exist domain, strain, and epitaxial dynamics and engineering sub-category, innovative processing and synthesis sub-category, nanostructured materials and nanotechnology sub- category, single crystal growth and characterization sub-category, theory and modeling sub-category. Nanocrystalline electroceramics, electroceramics for smart sensors, and bioceramics sub-categories are included to the emerging fields category. We hope that this report give an opportunity to understand the international research trend, not only to Korean ceramics researchers but also to science and technology policy researchers.

• Journal of the Korean Ceramic Society
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• v.39 no.9
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• pp.857-862
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• 2002

Porous ceramic supports with immobilized microorganisms for the water purifier were synthesized by firing green compacts of mixed powder comprising of fly ash, bentonite and an additive of yeast powder at 800∼1,000$^{\circ}C$ for 1h and the pore and mechanical properties of specimens were investigated. The compressive strength was increased in FB (Fly Ash + Bentonite) specimens while pore properties was decreased with increasing the bentonite content and sintering temperature. The compressive strength, bulk density, apparent density, porosity, mean pore size, pore volume and specific surface area of FB specimens at 800∼1,000$^{\circ}C$ were 89.6∼128.9 kgf/$cm^2$, 1.25∼1.43, 1.61∼1.78, 27.2∼62.2%, 7.9∼25.6 ${\mu}m$, 8.9∼$22.2{\times}10^{-5}\;cm^3/g$ and 35.2∼134.3 $m^2/g$, respectively. The pore properties of FBY (FB+yeast powder) specimens were superior to that of FB specimens, however compressive strength was decreased with increasing yeast powder content. The overall properties of 9F1B1Y (9F1B+10% of yeast powder) specimens at 900$^{\circ}C$ for 1 h were 98.7 kgf/$cm^2$, 1.20, 1.67, 68.1%, 48.9 ${\mu}m$, $29.5{\times}10^{-5}\;cm^3/g$ and 152.2 $m^2/g$, respectively. In this study, it was revealed that 9F1B1Y specimen demonstrated better S. saprophyticus adherence properties n their surface pores. Consequently, the microorganisms immobilized on porous ceramic supports showed better water purifying performance with many pores and adequate strength.

• The Korean Journal of Nuclear Medicine
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• v.34 no.5
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• pp.410-417
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• 2000

Purpose: Idoxifene is currently entering phase II clinical trials for the treatment of advanced breast cancer. The radiolabeled idoxifene using $[^{123}I]$ provides an opportunity for clinical pharmacology with single photon emission computed tomography (SPECT). The purpose of this study was to prepare radiolabeled idoxifene using $[^{123}I]$ and to determine its cell uptake of breast cancer cell line. Materials and Methods: With a view to evaluating new anticancer drugs, we are investigating the novel antiestrogen pyrrolidino-4-iodotamoxifen (idoxifene). $[^{123}I]$Idoxifene has been prepared in no-carrier-added form using a tributyl stannylated precursor which has been synthesized by means of (2-chloroethoxy)benzene with (${\pm}$)-2-phenylbutanoic acid on the basis of previously reported standard methods. The biodistribution and dynamic behavior of the compound were investigated using the comparative breast cancer cell line, MCF-7 (estrogen receptor-positive) and MDA-MB-468 (non-estrogen receptor). Results and Conclusion: Acylation of (2-chloroethoxy)benzene with (${\pm}$)-2-phenylbutanoic acid gave the versatile ketone (81%) which reacted with 1,4-diiodobenzene to give triphenylethylene as a mixture of E and Z geometric isomers, which were separated by the recrystallization in ethanol. The E-isomer was treated with pyrrolidine to give idoxifene (67%). In order to incorporate radioactive iodine into the 4-position, the 4-stannylated precursor was prepared (30%). The yield of radioiodination was 90-92% with a high radiochemical purity greater than 98%. The ratio of tumor uptake of the breast cancer cell line between MCF-7 and MDA-MB-468 was about 1.7.

• Proceedings of the Korean Institute of Surface Engineering Conference
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• 2000.11a
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• pp.3-4
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• 2000

Many researchers are interested in the synthesis and characterization of carbon nitride and diamond-like carbon (DLq because they show excellent mechanical properties such as low friction and high wear resistance and excellent electrical properties such as controllable electical resistivity and good field electron emission. We have deposited amorphous carbon nitride (a-C:N) thin films and DLC thin films by shielded arc ion plating (SAIP) and evaluated the structural and tribological properties. The application of appropriate negative bias on substrates is effective to increase the film hardness and wear resistance. This paper reports on the deposition and tribological OLC films in relation to the substrate bias voltage (Vs). films are compared with those of the OLC films. A high purity sintered graphite target was mounted on a cathode as a carbon source. Nitrogen or argon was introduced into a deposition chamber through each mass flow controller. After the initiation of an arc plasma at 60 A and 1 Pa, the target surface was heated and evaporated by the plasma. Carbon atoms and clusters evaporated from the target were ionized partially and reacted with activated nitrogen species, and a carbon nitride film was deposited onto a Si (100) substrate when we used nitrogen as a reactant gas. The surface of the growing film also reacted with activated nitrogen species. Carbon macropartic1es (0.1 -100 maicro-m) evaporated from the target at the same time were not ionized and did not react fully with nitrogen species. These macroparticles interfered with the formation of the carbon nitride film. Therefore we set a shielding plate made of stainless steel between the target and the substrate to trap the macropartic1es. This shielding method is very effective to prepare smooth a-CN films. We, therefore, call this method "shielded arc ion plating (SAIP)". For the deposition of DLC films we used argon instead of nitrogen. Films of about 150 nm in thickness were deposited onto Si substrates. Their structures, chemical compositions and chemical bonding states were analyzed by using X-ray diffraction, Raman spectroscopy, X-ray photoelectron spectroscopy and infrared spectroscopy. Hardness of the films was measured with a nanointender interfaced with an atomic force microscope (AFM). A Berkovich-type diamond tip whose radius was less than 100 nm was used for the measurement. A force-displacement curve of each film was measured at a peak load force of 250 maicro-N. Load, hold and unload times for each indentation were 2.5, 0 and 2.5 s, respectively. Hardness of each film was determined from five force-displacement curves. Wear resistance of the films was analyzed as follows. First, each film surface was scanned with the diamond tip at a constant load force of 20 maicro-N. The tip scanning was repeated 30 times in a 1 urn-square region with 512 lines at a scanning rate of 2 um/ s. After this tip-scanning, the film surface was observed in the AFM mode at a constant force of 5 maicro-N with the same Berkovich-type tip. The hardness of a-CN films was less dependent on Vs. The hardness of the film deposited at Vs=O V in a nitrogen plasma was about 10 GPa and almost similar to that of Si. It slightly increased to 12 - 15 GPa when a bias voltage of -100 - -500 V was applied to the substrate with showing its maximum at Vs=-300 V. The film deposited at Vs=O V was least wear resistant which was consistent with its lowest hardness. The biased films became more wear resistant. Particularly the film deposited at Vs=-300 V showed remarkable wear resistance. Its wear depth was too shallow to be measured with AFM. On the other hand, the DLC film, deposited at Vs=-l00 V in an argon plasma, whose hardness was 35 GPa was obviously worn under the same wear test conditions. The a-C:N films show higher wear resistance than DLC films and are useful for wear resistant coatings on various mechanical and electronic parts.nic parts.

• The Korean Journal of Physiology
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• v.22 no.1
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• pp.63-77
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• 1988

This study was carried out to investigate relationships between maximal running time (MRT) and glycogen supercompensation in fast twitch white fibers (white vastus, WV), fast twitch red fibers (red vastus, RV) and slow twitch red fibers (soleus muscle, SM) of endurance-trained rats. Male rats of a Sprague-Dawley strain were divided into the trained groups and untrained groups. Untrained groups were acquired to run on the treadmill 10 minutes for 3 days and remained rest and maintained with mixed diet for 4 weeks. For last 10 days of resting period, the untrained rats were divided into 3 groups i.e. mixed diet (untrained control), high and low carbohydrate (CHO) diet groups. And each group was subdivided into 2 groups, one group was tested for the MRT and the other was sacrificed to measure the blood glucose, blood lactate, glycogen contents of liver and muscles. The experimental groups were trained on treadmill by a modified method of Constable et al. (1984) maintained with mixed diet for 4 weeks. After measurement of MRT of this group, they were also divided into high and low CHO groups and fed with these diet for 2 days and MRT of each group was measured again to see the effect of high or low CHO feeding on the MRT. Each group was maintained with the same diet for next 2 days during which some of the rats were sacrificed at given time intervals for the measurements of blood glucose and lactate, liver and the muscles glycogen. The results were summarized as follows; 1) In the untrained group, there were no significant differences between subgroups in MRT, glycogen conent of SM, RV and WV. But blood glucose concentration and glycogen content of liver of low CHO group were significantly lower than those of mixed diet group. 2) The MRT and glycogen content of SM, RV and WV of trained mixed diet group were significantly increased compared to those of untrained mixed diet group, but there was no significant difference in glycogen content of liver. 3) MRT of trained mixed, high CHO and low CHO groups were $137{\pm}9.8,\;176{\pm}9.8\;and\;129{\pm}7.3\;min$ respectively with the significant difference between them. 4) There were no differences in blood lactate concentrations between the trained high and low CHO groups immediately after maximal running and during recovery period. 5) Glycogen contents in RV and SM of trained high CHO group were significantly increased, and glycogen contents in RV, WV and liver of trained low CHO group were significantly decreased compared to those of trained mixed diet group. 6) Immediately after maximal running, the blood glucose concentrations of trained high CHO and low CHO groups were $73{\pm}4.0\;and\;67{\pm}6.9mg%$ respecitively. The blood glucose of the trained high CHO group was fully recovered within one hour by feeding. But blood glucose concentration of low CHO group was slowly recovered up to $114{\pm}4.1mg%$ after two hours of feeding and maintained. Those values were still significantly lower than that of trained mixed diet group. The synthetic rates of glycogen in liver and muscles during the recovery period followed the similar time course of the blood glucose recoveries in each group. These results suggest that an increase in MRT of trained high CHO group was attributed to the glycogen supercompensation in slow twitch muscle fibers. And a decrease in MRT of trained low CHO may be due to decreased glycogen contents of liver and muscles. The results also suggest that glycogen supercompensation was more evident in slow twitch red fibers of endurance-trained rats and blood glucose is one of the limiting factors of glycogen synthesis.