• Journal of Korean Ophthalmic Optics Society
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• v.13 no.3
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• pp.1-6
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• 2008

Purpose: Plastic optical monomer materials having ultra high refractive index have an income of the whole quantity from advanced nations to domestic companies which are related to plastic optical lens. It is necessary to develop novel plastic optical lens materials in order to overcome a FTA provision and revitalize a stagnating optical lens industry in the interior optical lens industries. The new plastic optical lens materials against the substitution effect of income should be gradually demanded. This work will be synthesized novel super high refractive monomer resin materials of urethane lens series and studied the properties of optical lens using it. Methods: ETS-4 (2-(2-mercaptoethylthio)-3-{2-[3-mercapto-2-(2-mercaptoethylthio)propyl thio]ethylthio}propane -1-thiol), which is optical lens monomer resin having super high refractive index, was synthesized and identified its structure and property by elemental analysis, EI-MS, TGA, FT-IR spectroscopy, $^1H$ and $^{13}C$ NMR spectroscopies. After mixing evenly from mixed monomer resin and diisocyanate series, it was casting in glass mold. After thermal curing, the obtained optical lenses were measured and compared with the refractive index and Abbe number for studies of their optical properties. Results: We have synthesized the novel ultra high refractive index monomer resin, ETS-4, and have identified its structure and property by elemental analysis, EI-MS, TGA, FT-IR spectroscopy, $^1H$ and $^{13}C$ NMR spectroscopies. The existence of three isomers for EST-4 was identified by $^{13}C$ NMR spectroscopy. The refractive index ($N_d$ at $25^{\circ}C$) of monomer resin in liquid state obtained from the Abbe refractometer was 1.647. The refractive indexes of raw plastic optical lenses prepared from the mixed ETS-4 monomer and diisocyanate series were in the range of 1.656~1.680. Conclusions: Novel super high refractive index plastic optical lens monomer was synthesized and analysed, the optical lenses prepared using it were colorless transparency and excellent properties. It is of utility for the industrialization.

• Tuberculosis and Respiratory Diseases
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• v.44 no.6
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• pp.1296-1307
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• 1997

Background : Erdosteine is a thiol derivative developed for the treatement of chronic obstructive bronchitis, including acute infective exacerbation of chronic bronchitis. Erdosteine has mucomodulating and antioxidant properties and especially exhibits excellent gastrointestinal tolerability. Methods : The study was conducted as a prospective evaluation, with 2 comparative groups orally treated with erdosteine 300mg (bid.) or ambroxol 30mg (b.i.d.) for 7 days and the design of trial was double-blind. The treatments have been assigned randomly to patients (n=80) with acute or chronic bronchitis. The primary end-point used to determine efficacy in this study was subjective symptoms including expectorating frequence, expectoration volume, expectorating difficulty, expectoration viscosity, cough intensity and dyspnea. The secondary end-points of efficacy was the result of arterial blood gas analysis and pulmonary function test. Safety was evaluated with adverse drug reactions and laboratory tests monitoring. 61 patients was included in the efficacy analysis, due to the fact that 19 patients drop-out for different reasons. The obtained values have been analyzed with paired Hest., ANOVA test., multivariate $t^2$-test, repeated measures analysis of covariance, two sample t-test, loglinear-logit model analysis, Fisher's exact test. Results : 1) There was no significant difference on demographic data and vital signs between erdosteine and ambroxol treated groups. 2) The comparison between erdosteine and ambroxol treated groups showed no significant difference in improvement of each symptom in spite of the more favorable efficacy obtained with erdosteine. No difference on the contrary was observed for arterial blood gas analysis and pulmonary function test. 3) As safety is concerned, no clinical significant changes in laboratory test and symptom were induced in erdosteine and ambroxol treated group and two patients in ambroxol treated group drop-out for adverse reactions in symptom. 4) In the evaluation of final clinical efficacy, erdosteine improved more effectively patient's overall symptoms {very good effect (11/31), good effect (12/31), moderate effect (6/31), no effect (2/31), aggravation (0/31)} than ambroxol {very good effect (6/30), good effect (14/30), moderate effect (5/30), no effect (4/30), aggravation (2/30)}. And the probability of symptomatic improvement by erdosteine compared to ambroxol was 2.5 times. (p<0.05). Conclusion : This study showed that erdosteine was clinically effective and safe drug for treatment of acute and chronic bronchitis.

• Korean Chemical Engineering Research
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• v.50 no.5
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• pp.795-801
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• 2012

Nanoparticles have received significant attention because of their unusual characteristics including high surface area to volume ratios. Thiol ligand have been used as stabilizers of metal nanoparticles since Brust et al. They reported the preparation method of ligand capped metal nanoparticles by protecting the nanoparticles with a self-assembled monolayer of dodecanethiolate. In this method, volatile organic compounds (VOCs) were used as sovents. This study was carried out to replace these VOCs with room temperature ionic liquids (RTILs). We used two type of ILs to prepare metal nanoparticles. One is a hydrophobic IL, [BMIM][[$PF_6$] (1-Butyl-3-methylimidazolium hexafluorophosphate) purchased from IL maker, C-Tri from Korea and the other one is a hydrophilic one, [BMIM][Cl] (1-Buthy-3-methylimdazolium chloride) sinthesized by us. In the case of preparing Ag and Au nanoparticles using [BMIM][Cl], we didn't use phase transition reagents and ethanol because it has hydrophilic property and preparing Au, Ag nanoparticles using [BMIM][[$PF_6$] the method is as same as Brust et al.'s except using [BMIM][[$PF_6$] instead of organic solvent because it has hydrophobic property. FT-IR and UV-vis, TEM, TGA analysis have been used in an attempt to determine the particle size and verify functional groups. The particle size obtained from TEM was very similar to those obtained by Brust et al. This is a clear example of ligand capped metal nanoparticles prepared using ionic liquids. And the experimental result demonstrated ionic liquids can act as a highly effective medium for the preparation and stabilization of gold and silver metal nanoparticles.

• Journal of Life Science
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• v.14 no.3
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• pp.478-483
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• 2004

In a model reaction using lysyl oxidase purified partilally from bovine aorta, effect of L-ascorbic acid AsA on the oxidative reaction of lysine in collagen was investigated. Addition of Ash to the reaction mixture under aerobic conditions resulted in the decrease of enzymatic activity. In order to examine the specificity of AsA in the oxidative reaction of lysine, other reductants including A derivatives instead of AsA were added to the reaction mixture. Thiol such as glutathione had no effect on the activities of lysyl oxidase. on the other hand, it was observed that erythorbic acid, which was a stereoisomer of AsA, had the same inhibitory effect on this oxidative reaction as AsA. Moreover, by the addition of 3,4-dihydroxybenzoate, which was structural analog of AsA, the activities decreased in a similar manner to that of AsA. These results indicate that the regulatory effect of AsA on lysyl oxidase is attributed to characteristics of the structure. From the determination of Ash remained in the reaction mixture, it is shown that AsA concentration remarkably decreased by lysyl oxidase of the reaction mixture. It is hypothesized that endiol groups reduces the enzyme-bound $Cu^{+2}$ required for further progress of the reaction, and suggests that AsA regulates specifically the reduction of $Cu^{+2}$ required to oxidize lysyl oxidase. This findings support that AsA has an important regulatory role on the oxidative reaction of lysine and on changes of collagen cross-links with aging.

• Applied Biological Chemistry
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• v.40 no.1
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• pp.23-29
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• 1997

To develop novel cephem antibiotics, We have synthesized a new compound, named YH-487, by attaching the thiol and aminothiazole residue to $C_3$ and $C_7$ position of 7-ACA, respectively. Several characteristics such as structure, antibiotic spectrum, action mechanism, stability against ${\beta}-lactamase$ and synergistic effect were investigated. Anti-bactericidal activity of YH-487 against gram-positive and gram-negative bacteria were superior to that of the other cephem antibiotics. We have examined the action mechanisms of YH-487 using penicillin binding protein (PBP) assay, and found that the bactericidal activity was obtained by inhibiting PBP-1A, PBP-1B and PBP-3. YH-487 showed synergistic effect with gentamicin, tobramycin, and amikacin against Pseudomonas aeruginosa. In addition, YH-487 was effective against Enterobacter cloacae in combination with amikacin. Based on the above observations, YH-487 was classified as a novel third-generation ${\beta}-lactam$ antibiotics.

• Journal of Pharmaceutical Investigation
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• v.33 no.3
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• pp.237-243
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• 2003

Erdosteine, the thiol derivatives chemically related to cysteine, is a mucolytic and mucoregulator agent which modulates mucus production and viscosity and increases mucociliary transport. The purpose of the present study was to evaluate the bioequivalence of two erdosteine capsules, Erdos (Dae Woong Pharmaceutical Co., Korea) and Erblon (Kuhn Il Pharmaceutical Co., Korea), according to the guidelines of Korea Food and Drug Administration (KFDA). The erdosteine release from the two erdosteine capsules in vitro was tested using KP VII Apparatus II method with various different kinds of dissolution media (pH 1.2, 4.0, 6.8 buffer solution and water). Twenty four healthy male subjects, $23.33{\pm}2.06$ years in age and $66.18{\pm}8.19\;kg$ in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After three capsules containing 300 mg as erdosteine were orally administered, blood was taken at predetermined time intervals and the concentations of erdosteine in serum were determined using HPLC method with UV detector. The dissolution profiles of two formulations were similar at all dissolution media. Besides, the pharmacokinetic parameters such as $AUC_t,\;C_{max}\;and\;T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t\;and\;C_{max}$ and untransformed $T_{max}$. The results showed that the differences between two formulations based on the Erdos were 0.20%, 1.10% and -9.44% for $AUC_t,\;C_{max}\;and\;T_{max}$, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log(0.8) to log(1.25) $(e.g.,\;log(0.94){\sim}log(1.22)\;and\;log(0.92){\sim}log(1.20)\;for\;AUC_t\;and\;C_{max},\;respectively$. Thus, the criteria of the KFDA guidelines for the bioequivalence was satisfied, indicating Erblon capsule and Erdos capsule are bioequivalent.

• Microbiology and Biotechnology Letters
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• v.35 no.4
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• pp.272-277
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• 2007

The physiological responses of microorganisms to specific nutrient limitation can be regulated at the transcriptional levels. In this study, in order to develop the Pichia pastoris-derived promoter inducible by nutrient-limited condition, we constructed cDNA libraries using RT-PCR of total RNA from P. pastoris in steady-states of phosphate-limited chemostat with different dilution rates. Various genes were detected from cDNA library. Among these genes, the gene encoding putative sodium/phosphate ($Na^+$/Pi) symporter (NPS), high affinity transporter of phosphate, was detected. It was observed that expression of NPS increased in a manner specific to phosphate-limited condition through Northern blot. Therefore, it is thought that the promoter from NPS gene may have the potential as auto-inducible promoter by phosphate-limited culture condition without inducer.

• Korean Journal of Food Science and Technology
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• v.28 no.4
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• pp.730-735
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• 1996

Antibacterial action of garlic extract against Escherichia coli was investigated. When the survival of E. cloi in tryptic soy broth (TSB) containing 50% garlic extract was compared with those of Lactobacillus plantarum, Leuconostoc mesenteroides and Staphylococcus aureus, E. coli was the most sensitive to garlic antibacterial action. When E. coli was inoculated into TSB with different concentrations of garlic extract, viable cell number decreased continuously during the test period even at 1% garlic extract. When E. coli was inoculated into pH-adjusted TSB containing 0.5% garlic extract, viable cell number of E. coli decreased continuously at initial pH of 5.2 and 6.2, while it decreased initially but increased to $8.0{\times}10^{7}\;CFU/ml at 48 hr at pH 7.2. With larger initial populations $(10^{6}\;CFU/ml), E. coli grew without apparent inhibition, while with smaller initial populations $(<10^{5}\;CFU/ml), viable cell number decreased initially but later increased. Thiol compounds like cysteine and glutathione, with free SH group (s), helped E. coli to grow or survive better in TSB with inhibitory level (5%) of garlic extract. The possibility of eliminating E. coli by using garlic extract from foods like kimchi of which garlic is one of regular ingredients is suggested.

• Bulletin of the Korean Chemical Society
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• v.31 no.9
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• pp.2497-2502
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• 2010

Arg13 is a conserved active-site residue in all known Pi class glutathione S-transferases (GSTs) and in most Alpha class GSTs. To evaluate its contribution to substrate binding and catalysis of this residue, three mutants (R13A, R13K, and R13L) were expressed in Escherichia coli and purified by GSH affinity chromatography. The substitutions of Arg13 significantly affected GSH-conjugation activity, while scarcely affecting glutathione peroxidase or steroid isomerase activities. Mutation of Arg13 into Ala largely reduced the GSH-conjugation activity by approximately 85 - 95%, whereas substitutions by Lys and Leu barely affected activity. These results suggest that, in the GSH-conjugation activity of hGST P1-1, the contribution of Arg13 toward catalytic activity is highly dependent on substrate specificities and the size of the side chain at position 13. From the kinetic parameters, introduction of larger side chains at position 13 results in stronger affinity (Leu > Lys, Arg > Ala) towards GSH. The substitutions of Arg13 with alanine and leucine significantly affected $k_{cat}$, whereas substitution with Lys was similar to that of the wild type, indicating the significance of a positively charged residue at position 13. From the plots of log ($k_{cat}/{K_m}^{CDNB}$) against pH, the $pK_a$ values of the thiol group of GSH bound in R13A, R13K, and R13L were estimated to be 1.8, 1.4, and 1.8 pK units higher than the $pK_a$ value of the wild-type enzyme, demonstrating the contribution of the Arg13 guanidinium group to the electrostatic field in the active site. From these results, we suggest that contribution of Arg13 in substrate binding is highly dependent on the nature of the electrophilic substrates, while in the catalytic mechanism, it stabilizes the GSH thiolate through hydrogen bonding.

• Proceedings of the Korean Society of Embryo Transfer Conference
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• 2002.11a
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• pp.81-81
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• 2002

$\beta$-Mercaptoethanol($\beta$-ME)은 일반적으로 황화합물(thiol compounds)의 일종으로, 배양액 중에서 이황화결합(disulfide bonds)을 분해하여 일정한 물질의 산화.환원반응에 관여하며, 특히 cysteine이 cystine으로 산화되는 것을 차단함으로서 cysteine의 이용능력을 증대시키고, GSH의 합성을 촉진 및 증대시키는 것으로 알려져 있고, 각종 활성산소로부터 세포를 보호하는 역할을 수행하는 것으로 보고되었다. 특히, 돼지수정란의 체외배양체계에 유의적인 영향을 미치는 것으로 보고되었다(Abebydeera 등, Theriogenol., 50:747-756, 1998). 따라서 본 실험에서는 돼지난포란의 체외성숙시 $\beta$-ME의 첨가배양이 체외수정과 배발달에 미치는 영향에 관하여 조사하였다. 돼지난포란을 10% PFF, 0.1mg/ml cysteine, 10IU/m1 PMSG, 10IU/m1 hCG 및 10ng/m1 EGF가 첨가된 NCSU23 배양액에 $\beta$-ME를 각각 0, 25, 50 및 100uM을 처리하여 22시간 동안 배양을 실시하고, 성선자극호르몬이 배제된 배양액에서 추가로 22시간을 배양하여 체외성숙을 유도하였다. 체외성숙이 유기된 난자는 난구세포를 제거하고, 2.5mM caffeine과 0.1% BSA가 첨가된 mTBM배양액에 정자를 1.25 $\times$ $10^{5}$cells/ml의 농도로 5-6시간 동안 공동배양을 실시하여 체외수정을 유도하였다. 체외수정후 일부의 수정란은 12시간에 난자 급속 염색방법으로 염색하여 다정자침입률 및 자.웅전핵형성률 등을 확인하였다. 그리고 나머지1-세포기의 수정란은 0.4mg/ml BSA가 함유된 NCSU23 배양액에 30 embryos/50ul 소적으로하여 38.8$^{\circ}C$, 5% $CO_2$의 탄산가스 배양기에서 각각 7일간 배양을 실시하였다. 조사된 결과는 SAS/STAT를 이용하여 통계분석을 실시하였다. 체외수정 12시간 후에 난자 급속 염색법으로 염색을 실시한 결과, 모든 처리구에서 핵성숙률(76.4~95.2%), 정자침투율(51.1~66.9%), 웅성전핵형성률(95.2~100%), 다정자침입률(18.2~25.6%) 및 평균침입정자수(1.2~l.4개)에서 유의적인 차이가 인정되지 않았다. 체외배양 48시간 난할률을 조사한 결과, 처리구별 차이(53.9~67.9%)는 인정되지 않았으나, 배양 7일째 배반포형성률은 각각 14.5, 25.4, 17.3 및 12.4%로서 25uM의 $\beta$-ME처리구가 유의적(P<0.05)으로 높은 배발달률을 나타내었고, 총세포수에 있어서는 대조구와 처리구간 유의적인 차이가 인정되지 않았다. 따라서 돼지 난포란을 성숙배양할 때, 25uM $\beta$-ME를 첨가배양하는 것이 양질의 돼지체외수정란을 생산하는 하나의 방법으로 조사되었다.다.