• Journal of Life Science
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• v.27 no.2
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• pp.139-148
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• 2017

The inhibition of tyrosinase, a key enzyme in mammalian melanin synthesis, plays an important role in preventing skin pigmentation and melanoma. Therefore, tyrosinase inhibitors are very important in the fields of medicine and cosmetics. However, only a few tyrosinase inhibitors are currently available because of their toxic effects on skin or lack of selectivity and stability. Therefore, we synthesized a novel series of (E)-2-(substituted benzylidene)-2,3-dihydro-1H-cyclopenta[a]naphthalen-1-one derivatives and evaluated their inhibitory effects on mushroom tyrosinase, with the aim of discovering a novel tyrosinase inhibitor. Among 19 derivatives, MHY3655 ($IC_{50}=0.1456{\mu}M$) showed the strongest inhibitory effect on tyrosinase activity compared to kojic acid ($IC_{50}=17.2{\mu}M$), a well-known tyrosinase inhibitor. In addition, MHY3655 showed competitive inhibition on Lineweaver-Burk plots. We confirmed that MHY3655 strongly interacts with mushroom tyrosinase residues through the docking simulation. Substitutions with a hydroxy group at both R2 and R4 in the phenyl ring indicated that these groups play a major role in the high binding affinity to tyrosinase. Further, MHY3655 did not show cytotoxicity at the concentrations tested in B16F10 melanoma cells. In conclusion, the novel compound MHY3655 potentially shows tyrosinase inhibitory activity, and it could be used as an ingredient in whitening cosmetics.

• Journal of Pharmaceutical Investigation
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• v.25 no.3
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• pp.249-264
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• 1995

Although liposome has many advantages as a pharmaceutical dosage form, its application in the industrial field has been limited because of some problems such as preparation method, reproducibility, scale-up, stability and sterilization etc. Liposomes prepared by microemulsification method had defined size, narrow size distribution, reproducibility and high entrapment efficiency. For enhancing the stability, the dry form of liposome was recommended. These types of liposome are proliposome and freeze-dried liposome. The liposome must have some properties for preparing of freeze-dried liposome; small size $(50{\sim}200\;nm)$, narrow size distribution and cryoprotectant. In this experiment, the liposomes containing 5-Fluorouracil(5-FU) and its prodrug(pentyl-5-FU-1-acetate; PFA, hexyl-5-FU-1-acetate; HFA) were made with soybean phosphatidylcholine, cholesterol, stearylamine(SA) and dicetyl phosphate(DCP) employing hydration method or microemulsification method using $Microfluidizer^{TM}$. Both or liposome types were MLV and MEL. After preparation, freeze drying and rehydration were performed. In the process of freezing, trehalose(Tr) was added as a cryoprotectant. Their evaluation methods were as follows; entrapment efficiency, mean particle size and size distribution, dissolution test, retain of entrapment efficiency and turbidity after freeze-drying. The results are summarized as belows. The entrapment efficiency of 5-FU was dependent on total lipid concentration and cholesterol content but that of PFA and HFA was decreased when cholesterol was added. When DCP and SA were added, entrapment efficiency was decreased. As the partition coefficient of drug was increased, entrapment efficiency was increased. Under the same condition, entrapment efficiency of MEL is similar to that of MLV. The mean particle size and size distribution of MEL were smaller than those of MLV. Dissolution rates of drug from both liposome types were comparatively similar. Dissolution rates of drugs with serum and liver homogenate were faster than without these material. After preparation of liposome, free drug was removed efficiency by Dowex 50W-X4. When liposome was freeze-dried and then rehydrated in the presence of Tr, characteristics of liposome were maintained well in MEL than MLV. Tr Was used successfully as a cryoprotectant in the process of freeze drying and the optimal ratio of Tr:Lipid was 4:1(g/g).

• The Korean Journal of Nuclear Medicine
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• v.36 no.2
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• pp.121-132
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• 2002

Purpose : Taxol(Paclitaxel), an antineoplastic agent, has been used in the treatment of ovarian and breast cancers. The determination of optimal Taxol concentrations in human serum was required for enhancing therapeutic effect and maintaining the appropriate Taxol level in blood. This study was aimed to synthesizeradiolabeled Taxol derivatives as radiotracer in competitive radioimmunoassay for monitoring Taxol concentrations in blood and to determine the usefulness of its derivatives. Materials and Methods : Hemisucdcinyltaxol(HT) was synthesized by esterification of Taxol with succinic anhydride. Tyraminehemisuccinyltaxol(THT) was synthesized by coupling of HT with tyramine using isobutylchlormate as coupling agent and purified by HPLC. By using chloramine-T($5.25mg/ml,\;10{\mu}{\ell}$) as oxidant agent, THT($4mg/ml,\;30{\mu}{\ell}$) was labeled wity $^{125}I\;(37MBq,\;1mCi)$. To estimate the stability of purified THT, $^{125}I-iodotyraminehemisuccinyltaxol(^125}ITHT)$ was dissolved in 80% acetonitrile aqueous solution, and the solution was incubated at $4^{\circ}C\;and\;37^{\circ}C$ for 7 days. At various time intervals, the stability of THT and $^{125}ITHT$ was monitored. The titer of Taxol monoclonal antibody, 3G5A7, was determined by competitive radioimmunoassay using $^{125}ITHT$ as a labeled antigen. A standard dose-response curve was demonstated by Taxol competitive radioimmunoassay. Resulls : HT and THT were synthesized with 79.9% and 19.5% yield, respectively. The labeling yield of $^{125}ITHT$ was 93%. After 7 days, the chemical purity of THT was 96.5% at $4^{\circ}C$, and 97.5% at $37^{\circ}C$. After 3 days, $^{125}ITHT$ was stable with 94.7% at $4^{\circ}C$ and 93.4% at $37^{\circ}C$. After 7 days, fadiochemical purity was diminished to 88.1% at $37^{\circ}C$. The titer of Taxol monoclonal antibody, 3G5A7, was determined to 1:256. A standard dose-response curve demonstated good collinearity ($R^2=0.971$) as Taxol concentration-dependent manner. Conclusion : Competitive radioimmunoassay using $^{125}I-iodotyraminehemisuccinytaxol$ as radiotracer could be used to monitor for concentration of Taxol in the human serum.

• Applied Chemistry for Engineering
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• v.27 no.6
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• pp.583-589
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• 2016

Lubricant additives including zinc dialkyldithiophosphate (ZDDP) containing metal have been widely used due to the advantage of very low cost, but they can generate impurities such as ash. In this work, ZDDP containing metals was partially replaced with bis[3-(dialkyloxyphosphorothionyl) thio-2-methylpropanyloxy] butane (BAP4s) which was synthesized conveniently and effectively from alkanediol without any metal components. Also, the wear resistance property of synthesized BAP4s were studied. Wear scar diameter (WSD) values of BAP4s with butyl, octyl, decyl, dodecyl or tetradecyl groups were also measured by four-ball test. As the length of the alkyl group increased from 4 to 8, the WSD value of BAP4s decreased rapidly from 0.59 to 0.45 mm, but from 8 to 14, the value increased very slowly from 0.45 to 0.50 mm. Thus, among all BAP4s, B8P4 having BAP4 with the octyl group, showed the lowest WSD value. Furthermore, the WSD values were measured in a lubricant base oil mixed with a 0.50 percent concentration (w/w) of either BAP4 or ZDDP. The former was 0.55 mm, and the latter was 0.45 mm. The thermal stability and tribofilm formation peroperty were also measured by thermogravimetric analyzer (TGA) and energy-dispersive X-rays spectroscopy (EDS), respectively.

• Korean Journal of Food Science and Technology
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• v.37 no.3
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• pp.504-507
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• 2005

Trichoderma reesei KCTC 6952 possesses cellulase system consisting of three enzymatic components necessary to synergistically hydrolyze crystalline cellulose, among which ${\beta}$-glucosidase effectively releases glucose from glycoside derivatives. ${\beta}$-Glucosidase of T. reesei KCTC 6952 grown in modified Mandels' medium showed maximum activity(1.33 unit/mL) 4 days after initiation of growth. Optimal reaction conditions of the enzyme were 50 mM sodium acetate (pH 5) at $70^{\circ}C$ for 10 min. Enzymatic activities stabilized below $50^{\circ}C$ at pH range of 4-5. Results show ${\beta}$-glucosidase exerted its catalytic activities at relatively high temperatures and broad pH range.

• Analytical Science and Technology
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• v.18 no.1
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• pp.43-50
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• 2005

A number of carbonyl compounds including formaldehyde and acetaldehyde are well known for their toxicity and irritancy. Hence, acquisition of both qualitative and quantitative tool for their analysis is essential to resolve issues associated with malodor or indoor pollution. Using HPLC/UV method, we examined various aspects involved in the measurements of formaldehyde in environmental samples. The results of our analysis indicated that its detection was made as low as 0.5 ppb (assuming 5 L of sample volume), while its precision was maintained near 2% in terms of relative standard error (RSE). When the stability of calibration was checked by variability of slope values obtained over long-term period (e.g., one month), its values were found to remain constantly with RSE values of 3%. It was also found that liquid-phase reaction between formaldehyde and DNPH proceed very slowly to attain equilibrium (one and half hour), while requiring adequate amount of DNPH to form their derivatives. The overall results of our study thus suggest that there are a number of factors to consider for the accurate analysis of formaldehyde in ambient air.

• Journal of the Korea Academia-Industrial cooperation Society
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• v.13 no.7
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• pp.3252-3260
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• 2012

2,2'-Bipyridinium chlorochromate[$C_{10}H_8N_2HCrO_3Cl$] was synthesized by the reaction of 2,2'- bipyridine with chromium(VI) trioxide in 6M HCl. The structure was characterized by IR and ICP analysis. The oxidation of benzyl alcohol using 2,2'-bipyridinium chlorochromate in various solvents showed that the reactivity increased with the increase in the order of the dielectric constant(${\varepsilon}$), in the order: cyclohexene< chloroform$p-CH_3$, H, m-Br, $m-NO_2$) in N,N'-dimethylformamide. Electron-donating substituents accelerated the reaction, whereas electron acceptor groups retarded the reaction. The Hammett reaction constant(${\rho}$) was -0.64(303K). The oxidation reactivity of alcohols can be a useful factor to study about physical properties such as thermal stability, when the polysilsesquioxane solution is ready for an applying coating agent. The observed experimental data was used to rationalized the hydride ion transfer in the rate-determining step.

• Korean journal of applied entomology
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• v.10 no.2
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• pp.77-83
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• 1971

In order to find out the decomposing factors of Sumithion in mineral diluents, the physical and chemical properties of the diluents such as talcs, bentonites, diatomaceous earth and other clay minerals was studied in relation to the decomposition rate of Sumithion in dust formulations. The total base, moisture adsorption capacity, pH, specific surface, water contents, active $Fe^{++}$, ignition loss and cation exchange capacity were analysed as the properties of mineral diluents, and these properties were correlated with the stability of Sumithion in dust formulations. And in hope of finding out the main factors among those properties of diluents, the decomposed products of Sumithion in dust formulations prepared with standard Sumithion were separated by the methods of column chromatography and investigated by thin layer chromatography. The following results were otbained; 1. The total base, moisture adsorption capacity, specific surface, water contents, active $Fe^{++}$ and cation exchange capacity of mineral diluents were found to be highly effective on the rate of decomposition of Sumithion in dust formulations. 2. Decomposed products of Sumithion in dust formulations were found to be dimethylphosphorothionate, 3-methyl-4-nitro phenol and its derivatives. And one fraction was not dissolved in n-hexane and ethylether, but was soluble in methylalcohol and ethylalcohol. 3. The moat highly correlated properties of diluents with the decomposition rate of Sumithion in dust were found to be the total base and water contents. 4. In regard to the kind of diluents, it was found that the rate of decomposition of Sumithion in dust formulations was higher in order of bentonite, diatomaceous earth, kaolin and talc.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.32 no.1 s.55
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• pp.35-44
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• 2006

Recently, encapsulation studies have been tarried out to protect active agents using shell materials such as polymers, lipids, inorganic materials and the other protective materials. We have prepared copolymers of methylmethacrylate (MMA) and trimethoxysilylpropylmethacrylate (TMPMA), and the copolymers as shell materials were used for encapsulating active agents. Poly(MMA-co-TMPMA) spheres were very efficient for encapsulating active agents such as vitamin derivatives (such as retinol, retinyl palmitate, tocopheryl acetate and ascorbyl tetraisopalmitate) and oil soluble licorice extract etc. Mean diameters of poly(MMA-co-TMPMA) core-shell spheres containing active agents varied between about 0.1 to $10{\mu}m$ according to the experimental conditions. The loading amount of encapsulating active agents was 15 to 25% (w/w) and the loading yield was above 90%. The stability of active agents in poly(MMA-co-TMPMA) core-shell spheres prepared with an UV absorbing precursor increased by 25% compared with that of active agents in spheres prepared without an UV absorbing precursor.

• Polymer(Korea)
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• v.33 no.3
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• pp.207-212
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• 2009

The precursor polyimide of the photoreactive polyimides(PI-SP6 and PI-SP12) was prepared from a derivative of 2, 2, 2-trifluoroethane dianhydride and 3,3'-dihydroxy-4,4'-diaminobiphenyl. PI-SP6 and PI-SP12 were then prepared by the polymer reactions of the precursor polyimide with photoreactive 2-styrylpyridine alkylene (hexylene and dodecylene) derivatives, respectively. The photoreactive polymers were soluble in organic solvents. The polymers showed the initial decomposition temperatures around $350^{\circ}C$. The glass transition temperatures of PI-SP6 and PI-SP12 were found to be $130^{\circ}C$ and $85^{\circ}C$, respectively. This result means that the latter polymer is more flexible than the former polymer. Their transmittance in the film state was 90% at $250^{\circ}C$, which indicates that the photosensitive polyimides with thermal stability have high optical transparency even at the high temperature. The respective dichroic ratios of PI-SP6 and PI-SP12 were found to be 0.01 and 0.03 at an exposure energy of $1.5\;J/cm^2$. This result suggests that the latter polymer with larger flexibility compared to the former polymer is more effective for the photoalignment.