• Bulletin of the Korean Chemical Society
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• v.27 no.11
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• pp.1769-1774
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• 2006

A new liquid chromatographic chiral stationary phase based on (2S,3S)-O,O'-bis-(10-undecenoyl)-N,N'-bis-(3,5-dinitrobenzoyl)-2,3-diamino-1,4-butandiol was prepared starting from (2R,3R)-1,4-bis(benzyloxy)-2,3-butanediol. The new chiral stationary phase was applied to the resolution of racemic anilide derivatives of N-acetyl-a-amino acids, 1,1'-bi-2-naphthol and 3,3'-diaryl-1,1'-bi-2-naphthols. The CSP was also applied to the resolution of some chiral drugs including a diuretic, bendroflumethiazide, and non-steroidal anti-inflammatory agents such naproxen and alminoprofen. In every case, the chiral recognition efficiency of the new CSP was quite excellent.

• Journal of the Korea Institute of Information and Communication Engineering
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• v.10 no.11
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• pp.2039-2044
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• 2006

Since the bio-information now even exceeds the capability of human brain, the techniques of data mining and artificial intelligent are needed to deal with the information in this field. There are many researches about using DNA microarray technique which can obtain information from thousands of genes at once, for developing new methods of analyzing and predicting of diseases. Discovering the mechanisms of unknown genes by using these new method is expecting to develop the new drugs and new curing methods. In this Paper, We tested accuracy on classification of microarray in Bayesian method to compare normalization method's Performance after dividing data in two class that is a feature abstraction method through a normalization process which reduce or remove noise generating in microarray experiment by various factors. And We represented that it improve classification performance in 95.89% after Lowess normalization.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.34 no.1
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• pp.15-23
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• 2008

This study is on encapsulation of a new whitening agent, LA-PEG using solid lipid nanoparticle(SLN) method, one of nanoparticle preparation method. Classical method has high capsulation efficiency for hydrophobic compounds but has demerit of low capsulation efficiency($2{\sim}3%$) for hydrophilic compounds. Purpose of this study is preparation of SLN that has higher skin penetration effect compared with general liposome, and also has higher encapsulation efficiency of hydrophilic compounds. For SLN preparation, coconut oil, macadamia oil, and jojoba oil were used. As a result, SLN preparation using coconut oil(include LA-PEG) has the most high encapsulation efficiency and also has the smallest average particle size(270 nm). SLN prepared with macadamia oil and 1% of Tween 60 has the largest particle size. Base made with coconut oil and 2% of Tween 60 showed the fastest release and base made with macadamia oil and 2% of Tween 20 showed the latest release.

• Journal of fish pathology
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• v.9 no.2
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• pp.185-193
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• 1996

Extensive acquirement of drug resistance to traditional antibacterial agents poses a serious problem to eel aquaculturists. To collect the basic information for new drug development in the future, we assessed the in vitro antibacterial efficacy of 14 new quinolones with 75 isolates of Edwardsiella tarda from local aquaculture tanks of Anguilla japonica. Of all tested quinolones under development or marketed for human use, DU-6859 was most potent with its $MIC_{50}$ value of $0.05{\mu}g$/ml in broth microdilution assay. The drugs whose $MIC_{50}$ values ranged from 0.2 to $0.78{\mu}g$/ml were T-3762, Bay-y3118, ciprofloxacin, norfloxacin, ofloxcin and tosufloxacin. The weakest group of drugs, with their $MIC_{50}$ being 1.56-$3.13{\mu}g$/ml, were difloxacin, sparfloxacin, fleroxacin, Q-35, amifloxacin, lomefloxacin and enoxacin. The number of resistant strains, when arbitrarily defined with their MICs of $\geq6.25{\mu}g$/ml, was : 3 to T-3762, 3 to Bay-y3118, 44 to difloxacin, 16 to sparfloxacin, 13 to ciprofloxacin, 19 to fleroxacin, 36 to Q-35). 31 to amifloxacin, 5 to norfloxacin, 13 to ofloxacin, 31 to lomefloxacin, 41 to enoxacin, 12 to tosufloxacin and 0% to DU-6859, respectively. This information can be taken into consideration for the future development of fisheries antibacterial quinolones.

• The Korean Journal of Food And Nutrition
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• v.22 no.2
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• pp.252-260
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• 2009

According to Article 7 and Annex B of the World Trade Organization(WTO) Agreement on the Application of Sanitary and Phytosanitary(SPS) Measures, WTO members are required to notify their newly established or amended SPS measures that might affect international trade. This study analyzed SPS notifications from 1995 to 2008 to identify international trends for food safety measures. The notifications were collected from the SPS information management system and the official document distribution system of WTO. The 153 WTO members represented 37 developed countries, 84 developing countries and 32 least developed countries. The number of overall notifications was 9,820. The annual notifications increased from 198 in 1995 to 1,264 in 2008. The monthly average notifications were from 44.8 in December to 69.5 in June; however, there were no statistical differences among them. The six leading Members in terms of notification submissions were United States(U.S.), Brazil, New Zealand, Canada, European Community and Korea. Among the regular and emergency notifications, 62.7% notifications were concerned with food safety, followed by animal and plant protections. Among animal protection notifications, 54.8% were emergency situations. Of the 4,821 food safety notifications, 60.4% were from developed countries, and 39.3% were from developing countries. Measures concerning pesticide residues and risk assessments were mainly from developed countries. In contrast, 77.5% of the measures concerning zoonoses were from developing countries. However considering the numbers of developing and developed countries, the average number of measures for each country was similar. Food safety measures were mainly involved pesticide residues followed by food additives, zoonoses, new regulations, labeling. As the overall notifications, zoonosis measures were mainly emergency notifications. Measures concerning pesticide residues, food additives, zoonoses, new regulations, veterinary drugs, and labeling were submitted most often by the U.S., Korea, Albania, U.S., Australia, and U.S., respectively. Identifying the exact trends of food safety measures was complicated by a number of factors. However, WTO notifications might be useful tool in providing a general view of international trends.

• Biomolecules & Therapeutics
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• v.21 no.3
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• pp.190-195
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• 2013

Cisplatin is a member of platinum-containing anti-cancer drugs that causes cross-linking of DNA and ultimately cancer cell apoptosis. The therapeutic function of cisplatin on various types of cancers has been widely reported but the side effects have been discovered together and nephrotoxicity has been regarded as major side effect of cisplatin. To select candidates for new sensitive nephrotoxicity biomarker, we performed proteomic analysis using 2-DE/MALDI-TOF-MS followed by cisplatin treatment in human kidney cell line, HK-2 cells, and compared the results to the gene profile from microarray composed of genes changed in expression by cisplatin from formerly reported article. Annexin A5 has been selected to be the most potential candidate and it has been identified using Western blot, RT-PCR and cell viability assay whether annexin A5 is available to be a sensitive nephrotoxic biomarker. Treatment with cisplatin on HK-2 cells caused the increase of annexin A5 expression in protein and mRNA levels. Over-expression of annexin A5 blocked HK-2 cell proliferation, indicating correlation between annexin A5 and renal cell toxicity. Taken together, these results suggest the possibility of annexin A5 as a new biomarker for cisplatin-mediated nephrotoxicity.

• Bulletin of the Korean Chemical Society
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• v.34 no.11
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• pp.3429-3443
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• 2013

Chemokine receptor (CCR2) is a G protein-coupled receptor that contains seven transmembrane helices. Recent pharmaceutical research has focused on the antagonism of CCR2 and candidate drugs are currently undergoing clinical studies for the treatment of diseases like arthritis, multiple sclerosis, and type 2 diabetes. In this study, we analyzed the time dependent behavior of CCR2 docked with a potent 4-azetidinyl-1-aryl-cyclohexane (4AAC) derivative using molecular dynamics simulations (MDS) for 20 nanoseconds (ns). Homology modeling of CCR2 was performed and the 4AAC derivative was docked into this binding site. The docked model of selected conformations was then utilized to study the dynamic behavior of the 4AAC enzyme complexes inside lipid membrane. MDS of CCR2-16b of 4AAC complexes allowed us to refine the system since binding of an inhibitor to a receptor is a dynamic process and identify stable structures and better binding modes. Structure activity relationships (SAR) for 4AAC derivatives were investigated and reasons for the activities were determined. Probable binding pose for some CCR2 antagonists were determined from the perspectives of binding site. Initial modeling showed that Tyr49, Trp98, Ser101, Glu291, and additional residues are crucial for 4AAC binding, but MDS analysis showed that Ser101 may not be vital. 4AAC moved away from Ser101 and the hydrogen bonding between 4AAC and Ser101 vanished. The results of this study provide useful information regarding the structure-based drug design of CCR2 antagonists and additionally suggest key residues for further study by mutagenesis.

• Journal of Pharmaceutical Investigation
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• v.34 no.3
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• pp.161-168
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• 2004

5-Fluorouracil (5-FU) is an antimetabolite anticancer agent active against many types of solid tumors. Tegafur (TF), a prodrug of 5-FU, is frequently used in combination with uracil as dihydropyrimidine dehydrogenase (DPD) inhibitory fluoropyrimidine. We studied the stability of 5-FU and TF in biological fluids of rats and determined their bioavailability (BA) and excretion into bile, and urine. The drug concentrations were analyzed by an HPLC method. At room temperature, there was a 14-30% decrease in the concentration of 5-FU and TF in bile, urine, and plasma specimen at 10 and $100\;{\mu}g/ml$ over 240 min. No significant difference was noted among the sample types or between two different concentrations of 10 and $100{\mu}g/ml$. The decrease in drug concentration was significantly less in samples kept on ice (6-12%) for both drugs. These data indicate that biological fluid samples containing 5-FU or TF in plasma, urine, or bile should be placed on ice during the sample collection. Following these storage guidelines, samples were collected after administration 50 mg/kg of each drug via i.v. or oral route. BA was 1.5 folds greater for TF (60%) than that of 5-FU (42%). Approximately 0.52 and 3.3% of the i.v. doses of 5-FU and TF was excreted into bile, respectively. Renal clearance of 5-FU was about 16% of its total body clearance. These results suggest that instability of 5-FU and TF in biological fluids should be considered in pharmacokinetic or pharmacogenomic studies.

• Archives of Pharmacal Research
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• v.29 no.1
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• pp.26-33
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• 2006

Some new derivatives of 1,2,4-triazolo[2,3-a]benzimidazoles were synthesized through the reaction of 1,2-diaminobenzimidazole with carbon disulfide. The resulting 1,2,4-triazolo-[2,3a]benzimidazole-2-thione intermediate was reacted with one equivalent of alkyl halides to give the corresponding 2-alkylthio derivatives, which were further alkylated through the reaction with another one equivalent of different alkyl halides to afford the target compounds; 1-alkyl-2alkylthio-1,2,4-traizolo[2,3-a]benzimidazoles. On the other hand, the 1,2-disubstituted derivatives with two identical alkyl substituents were prepared by the reaction of 1,2,4-triazolo[2,3-a]benzimidazole-2-thione with two equivalents of the alkyl halides. The structures of the new compounds were assigned by spectral and elemental methods of analyses. The synthesized compounds were tested for their antibacterial and antifungal activities. Most of the tested compounds proved comparable results with those of ampicillin and fluconazole reference drugs. The study indicated that, the antibacterial as well as the antifungal activities of the test compounds were improved with increase in the bulkiness of the introduced alkyl groups. Also, some active antibacterial compounds were tested for their antimycobacterial activity. All the test compounds showed equipotent antitubercular activity as that of INH as a reference drug.

• Archives of Pharmacal Research
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• v.28 no.7
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• pp.848-853
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• 2005

Synurus deltoides was previously found to possess significant anti-inflammatory activity especially against chronic inflammation, and strong analgesic activity in vivo. In this study, new anti-inflammatory formulation containing S. deltoides extract as a major ingredient was prepared and in vivo activity was evaluated. The plausible action mechanism was also investigated. The new formulation (SAG) contains 1 part of S. deltoides extract, 0.9 part of Angelica gigas extract and 0.9 part of glucosamine sulfate (w/w). SAG inhibited dose-dependently edematic response of arachidonic acid (AA)- and 12-O-tetradecanoyl 13-acetate (TPA)-induced ear edema in mice, which is an animal model of acute inflammation. SAG showed 44.1 % inhibition of AA-induced ear edema at an oral dose of 50 mg/kg. In an animal model of chronic inflammation, SAG clearly reduced the edematic response of 7 -day model of multiple treatment of TPA (38.1 % inhibition at 200 mg/kg/day). Furthermore, SAG (50-800 mg/kg/day) as well as S. deltoides extract (285 mg/kg/day) significantly inhibited prostaglandin $E_2$ production from the skin lesion of the animals of 7-day model. These results were well correlated with in vitro finding that SAG as well as S. deltoides extract reduced cyclooxygenase (COX)-1- and COX-2-induced prostanoid production, measured in mouse bone marrow-derived mast cells. Therefore, these results suggest that SAG possesses anti-inflammatory activity in vivo against acute as well as chronic inflammatory animal models at least in part by inhibition of prostaglandin production through COX-1/COX-2 inhibition. And COX inhibition of SAG is possibly contributed by S. deltoides extract among the ingredients. Although the anti-inflammatory potencies of SAG were less than those of currently used anti-inflammatory drugs, this formulation may have beneficial effect on inflammatory disorders as a neutraceutical.