• Biomolecules & Therapeutics
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• v.3 no.1
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• pp.34-37
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• 1995

Non-steroidal anti-inflammatory drugs (NSAIDs) have been known as inhibitors of the folate-requiring enzymes. In the present work, we have expanded on these observations and have investigated the inhibitory effects of NSAIDs on Lactobacillus casei thymidylate synthase expressed in E. coli. NSAIDs including sulphasalizine, salicylic acid, indomethacin and mefenamic acid were found to be competitive inhibitors with respect to folate of Lactobacillus casei thymidylate synthase. In contrast, aspirin and the antipyretic-analgesic drugs acetaminophen and antipyrine were weak inhibitors of the enzyme. Structure-activity correlation suggests that an aromatic ring with a side chain containing a carboxylic acid is a requirement for competitive inhibition of the thymidylate synthase. The results are consistent with the hypothesis that the antifolate activity of NSAIDs, and hence cytostatic consequences, are important factors in producing anti-inflammatory activity and aspirin exerts its anti-inflammatory effects after its conversion into salicylic acid, which possesses greater antifolate activity than its parent compound.

• Journal of Pharmaceutical Investigation
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• v.21 no.3
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• pp.125-132
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• 1991

Using X-ray crystallography powder diffraction, the quantitative representation method of preferred orientation of particles ill tablets was developed. Selected faces of a tablet. the upper surface and faces cut parallel and normal to the upper surface, were presented to an X-ray beam and X-ray diffraction patterns for these faces were measured. The effects of particle size. tableting pressure, and particle form on the preferred orientation were also investigated. It was also recognized that the degree of anisotropy in terms of capping tendency was influenced by the preferred orientation of particles in tablets.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.175.2-176
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• 2003

Herbal medicines are increasingly being utilized to treat a wide variety of disease processes. We previously reported that aqueous extract from the roots of Platycodon grandiflorum A. DC (Campanulaceae), Changkil (CK), had hepatoprotective effects against acetaminophen induced liver injury. In the present study, we assayed the preventive and therapeutic effects of CK on experimental hepatic fibrosis induced by dimethylnitrogamine or carbon tetrachloride in rats. (omitted)

• Archives of Pharmacal Research
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• v.15 no.1
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• pp.35-40
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• 1992

S. fradiae showed the highest acetanilide p-hydroxylation activity in the tested strains. And S. fradiae was well characterized genetically, especially with respect to tylosin production. Two mutants, which lost hydroxylation, were isolated in 140 regenerated colonies from protoplasts. In restriction enzyme digesion of total DNAs, isolation of giant linear plasmid DNA and determination of antibiotic resistances to chloramphenicol, tylosin, hygromycin B and mitomycin C, any differences among mutants and a wild type strain were not detected. These facts suggest that lesion on 6, 000 Kb chromosomal DNA was responsible for the lack of p-hydroxylation activity induced by protoplast formation and regeneration.

• Journal of Pharmaceutical Investigation
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• v.14 no.2
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• pp.76-85
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• 1984

Antibiotic activity and antipyretic effect of three synthetic prodrugs, chloramphenicol acetylsalicylate (CAF-ASP), chloramphenicol naproxenate(CAF-NAX) and chloramphenicol acetaminophen succinate (CAF-SUC-ACET), were studied in vitro and in vivo. In the experimental results, the CAF-NAX showed the moat rapid absorption and the highest blood levels, and the CAF-SUC-ACET and CAF-ASP also were more rapid absorption and higher blood levels than controls, chloramphenicol and chloramphenicol palmitate. The synthetic prodrugs also showed the antipyretic effect by modified Roszkowski method using endotoxin.

• Toxicological Research
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• v.23 no.3
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• pp.189-196
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• 2007

Cytochrome P450 (P450) enzymes are the major catalysts involved in the biotransformation of various drugs, pollutants, carcinogens, and many endogenous compounds. Most of chemical carcinogens are not active by themselves but they require metabolic activation. P450 isozymes playa pivotal role in the metabolic activation. The activation of arylamines and heterocyclic arylamines (HAAs) involves critical N-hydroxylation, usually by P450. CYP1A2 plays an important role in these reactions. Broad exposure to many of these compounds might cause carcinogenicity in animals and humans. On the other hand, P450s can be also involved in the bioactivation of other chemicals including alcohols, aflatoxin B1, acetaminophen, and trichloroethylene, both in humans and in experimental animals. Understanding the P450 metabolic activation of many chemicals is necessary to develop rational strategies for prevention of their toxicities in human health. An important part is the issues of extrapolation between species in predicting risks and variation of P450 enzyme activities in humans.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1993.04a
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• pp.104-104
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• 1993

시방성 제제에 대한 연구는 주로 제제학적 수단에 의한 약효의 지속화로서 제제설계상 제형개발 및 투여제형에서의 약물방출 조절로 체내의 유효 혈중농도를 유지한다. 이에 약물 방출 조절용 물질의 하나로서 체내 분해가 가능하고 독성이 없는 생체 고분자인 Chitosan이 약물방출 담체로서 양호함에 착안하여 약물의 서방화를 기하고자 본 실험에 착수 하였다. 모델 약물로서는 sulfamethoxazole, acetaminophen, sylimarin을 사용하여 chitosan gel 과 혼합비를 달리하여 고형 문산체를 조제하고 이것을 formaldehyde, glutaraldehyde, 1acetaldehyde, butylaldehyde 4종의 aldehyde를 사용하여 농도에 따른 가교화가 in vitro에서의 약물용출에 미치는 영향을 검토하였으며, 또한 위장을 거쳐 소화효소 또는 장내미생물 효소에 의한 chitosan 분해로 약물 방출의 촉진을 실험한바 지견을 얻었기에 보고한다.

• Korean Journal of Acupuncture
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• v.25 no.3
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• pp.137-146
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• 2008

Objectives : The leaves of Artemisia argyi L. have been used for the treatment of bleeding-related diseases in traditional korean medicine. But the immunological activities with macrophage have not been sufficiently reported. This study is to investigate the immunological bioactivities of the herbal acupuncture solution obtained from leaves of Artemisia argyi L. (AAAS). Methods & Results : Against Nicotine and Acetaldehyde, AAAS increased significantly the production of hydrogen peroxide (H2O2) within mouse macrophage Raw 264.7 cells above the concentration of 10 ${\mu}g/m{\ell}$. AAAS increased significantly the production of nitric oxide (NO) in Raw 264. 7 cells above the concentration of 100 ${\mu}g/m{\ell}$ against EtOH. And AAAS increased significantly the production of nitric oxide (NO) in Raw 264. 7 cells above the concentration of 200 ${\mu}g/m{\ell}$ against Nicotine, Acetaminophen, and Acetaldehyde. Conclusions : These results suggest that AAAS could be thought to have the immunological activities related with the production of hydrogen peroxide and NO in macrophage.

• YAKHAK HOEJI
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• v.41 no.5
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• pp.539-546
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• 1997

Capillary electrophoresis (CE) is perceived as an attractive tool for the analysis of pharmaceuticals and biological materials because of their high separation efficiency, easy separation and low running cost. New concept of micellar electrokinetic capillary chromatography (MECC) expanded the application of CE to the separation of neutral molecules. Validation of CE as an analytical technique for quality control of pharmaceuticals should be confirmed by quantitative analysis and the peak confirmation. In this study, the quantitative analyses of various types of neutral, acidic and basic components (acetaminophen, caffeine, ascorbic acid, riboflavin, thiamine, chlorpheniramine, phenylpropanolamine, dl-methylephedrine and dextromethorphan) in complex cold medicines have been accomplished using CE. Combined methods of MECC using SDS and capillary zone electrophoresis lowering the pH of running buffer were adopted to determine the ingredients in capsule type or liquid formula complex medicines without particular sample pretreatment. The results indicate that CE is a promising technique for quality control analysis of pharmaceuticals as a validation method.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.283.1-283.1
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• 2003

This study was designed to develop and validate an isocratic reversed phase high performance liquid chromatographic(HPLC) method for the quantitation of sobrerol in drug preparations, and obtain the data pool that can be used in the revision of pharmacopoeia. The separation of sobrerol and the other compounds (S-carboxymethylcysteine, acetaminophen, methyl paraben, propyl paraben, and sobrerol degradants) was achieved in a C18 column with an acetonitrile-methanol-water(24.5:10.5:65.0) mobile phase. (omitted)