• YAKHAK HOEJI
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• v.44 no.2
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• pp.155-161
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• 2000

New cephalosporin antibiotics , 3-[(4-carboxy-5-ethylthioisothiazol-3-yl)oxymethyl]-7-[(1H-tetra-zol-1-yl)acetamido]-3-cephem-4-carboxylic acid 2, 3-[(4-carboxy-5-ethylthioisothiazol-3-yl) oxymethyl]-7-[(2-aminothiazol-4-yl)acetamido]-3-cephem-4-carboxylic acid 3, 3-[(4-carb oxy-5-ethylthioisothiazol-3-yl)-oxymethyl]-7-[5-(ethylthio-3-hydroxyisothiazol-4-yl)carboxamido]-3-cephem-4-carboxylic acid 4, 3-[(4-car-boxy-5-ethylthioisothiazo1-3-yl)oxymethy1]-7-[(Z)-2-(fur-2-yl)-2-(methoxyimino)acetamido]-3-cephem-4-carboxylic acid 5, 7-[(Z)-2-(2-aminothiazol-4-yl)-2-[(alkoxyimino)acetamido]-3-[(4-carboxy-5-ethylthioisothiazol-3-yl)oxymethyl]-3-cephem-4-carboxylic acid 6-8 were synthesized. Antibacterial activities and structure-activity relationships of these new cephalosporin derivatives were examined. Among them, 7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxyimino)acetamido]-3-[(4-carboxy-5-ethylthylth-ioisothiazol-3-yl)oxymethyl]-3-cephem-4-carboxylic acid 7 exhibited good antibacterial activities compared to cefotaxime and ceftriaxone.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.251.2-251.2
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• 2002

2-Methylaminoethyl- 4,4' -dimethoxy- 5, 5',6,6' -dimethylenedioxybiphenyl- 2' -carboxy- 2-carboxylate (DDB-S) is a synthetic compound derived from DDB. which is protects liver against carbon tetrachloride-, D-galactosamine-, thioacetamine-, and prednisolone- induced hepatic injury in experimental animals. We assessed the use of liquid chromatography/electrospray iontrap tandem mass spectrometry (LC/MS/MS) method to identify and quantify in vivo metabolites and to measure excretion. (omitted)

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.133.2-134
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• 2003

2-Methylaminoethyl-4, 4'-dimethoxy-5, 5', 6.6 -dimethylenedioxybiphenyl-2'-carboxy-2-carboxylate (DDB-S), a synthetic compound derived from DDB, has been known to protect liver against carbon tetrachloride-, D-galactosamine-, thioacetamide-, and prednisolone-induced hepatic injury in experimental animals. The metabolism of this compound has been assessed in rats by using liquid chromatography/electrospray tandem mass spectrometry (LC/MS/MS) method. (omitted)

• Food Science of Animal Resources
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• v.20 no.3
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• pp.199-206
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• 2000

축육 생산시 주요 부산물인 돼지 심장근으로부터 항산화제(0.02% propyl gallate, 0.2% asxorbic acid, 0.2% sodium tripolyphosphate) 첨가 세척액(25 mM phosphate buffer, pH 6.0)에 의해 제조된 surimi(5% protein 0.6 M NaCl, 25 mM phosphate buffer, pH 6.0)를 alginate(0.4%), calcium carbonate(0.075%) 및 lactate(0.6%) 등의 첨가에 의해 AC surimi 로 조제한 다음, CMC 또는 MC를 일정수준 (0.5%, 1.0%) 첨가하여 surimi 의 pH, 겔의 보수력과 조리 손실을 비롯하여 겔읨 루성을 비교 검톻였다. CMC 첨가시 pH는 0.2 단위씩 감소하는 경향을 보인데 비해 MC 첨가시에는 뚜렷한 변화를 보이지는 않았다. 조리 손실에 대한 영향을 살펴 본 결과 CMC와 MC 첨가구에서 0.5% CMC 첨가구를 제외하고서는 나머지 세 처리구에서 감소하는 경향이었고, 특히 MC 첨가시에는 대조구에 비해 뚜렷한 감소 경향을 나타내었으나(p<0.05) 첨가수준에 따른 차이는 나타나지 않았다 CMC나 MC의 첨가는 보수력에 대해서는 거의 영향을 미치지 않은 것으로 나타났고, 물성에 대한 측정 결과에서 CMC 첨가시에는 겔의 강도. 경도 및 탄성등은 약간 증가하였으나 유의적인 차이를 나타내지는 않았고 (P<0.05), MC 첨가시에는 뚜렷한 차이를 나타내지 않았으며, 겔 응집성에 대해서는 CMC와 MC 첨가에 의해 서로 다른 경향을 나타내었다.

• Parasites, Hosts and Diseases
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• v.38 no.2
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• pp.107-110
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• 2000

We investigated the role of recombinant Toxoplasma gondii heat shock protein (rT.g.HSP) 70-full length, rT.g. HSP70-NH2-terminal region, or rT.g. HSP70-carboxy-terminal region in prophylactic immunity in C57BL/6 mice perorally infected with Fukaya cysts of T. gondii. At 3, 4, 5, and 6 weeks after infection, the number of T gondii in the brain tissue of each mouse was measured by quantitative competitive-polymerase chain reaction (QC-PCR) targeting the surface antigen (SAG) 1 gene. Immunization with rT.g.HSP70-full length or rT.g.HSP70-carboxy-terminal region increased the number of T. gondii in the brain tissue after T. gondii infection, whereas immunization with rT.g.HSP70-NHa-terminal region did not. These results suggest that T.g. HSP70-carboxy-terminal region as well as T.g.HSP70-full length may induce deleterious effects on the protective immunity of mice infected with a cyst-forming T. gondii strain, Fukaya.

• Journal of the Korean Association of Oral and Maxillofacial Surgeons
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• v.31 no.6
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• pp.461-467
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• 2005

Background. 5-(and-6)-carboxy-2',7'-dichlorofluorescein diacetate, succinimidyl ester mixed (CFSE) is the fluorescent labelling agent of living cells and used to trace the cells in vivo after transplatnation of various cells. The CFSE labelled cells can maintain fluorescence for up to 7 days after labelling. The MC3T3-E1 cell line (MC3T3) has been used for many studies about osteoblast, which is well known as a mouse preosteoblast. So the CFSE would be used to trace the transplanted MC3T3. However there are few reports about CFSE labelling of MC3T3. This study is aimed to know about adequate concenturation and incubation time of CFSE to MC3T3. Materials and methods. The MC3T3 was incubated in a humidified atmosphere of 95% air with 5% $CO_2$ at $37^{\circ}C$ using ${\alpha}$-minimal essential medium (${alpha}$-MEM) containing10% FBS and gentamycin. Ten mM CFSE solution in dimethylsulphoxide (DMSO: 1%) was diluted with phosphate buffered saline (PBS) and final concentration of culture medium was, respectively, 5, 10, 15, 20, 25 and 30 ${{\mu}M$. Then the MC3T3 was incubated with CFSE in a humidified atmosphere of 95% air with 5% $CO_2$ at $37^{\circ}C$ for 5, 10, 15, 20, 25, 30, 35, 40 and 45 minutes in each concentration. The fluorescence of CFSE labelled cells was analysed with a inverted fluorescence microscope. The duration of cell labelling was also studied. Trypan blue dye exclusion test was done for cell viability. Results. For concentration between 5 and 10 ${\mu}M$, CFSE did not significantly label the MC3T3 in vitro. The destruction of MC3T3 was observed at the concentration of 20 ${\mu}M$. In the concentration of 15 ${\mu}M$, the best labelling was obtained at an incubation period between 15 and 30 minutes. The MC3T3 labelled with an incubation period of 15 minutes at 15 ${\mu}M$ was still fluorescent 7 days after CFSE labelling. The mean cell viability was 95.93%. Conclusion. These results suggests an incubation period of 15 minutes at 15 ${\mu}M$ of CFSE provides best labelling of MC3T3 in vitro.

• Journal of the Korean Ceramic Society
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• v.33 no.8
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• pp.909-914
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• 1996

In this research [RCOOH]-$\varepsilon$-Caprolactam-Montmorillonite was synthesized by reaction between Na-Mont-morillonite (10-Carboxy-n-decyl)dimethylethylammonium (=RCCOH) ion and $\varepsilon$-Caprolactame-Motmorillonite ob-tained was 3.62$\AA$ After heat treatment of this intercalations complex at 37$^{\circ}C$ in high vacuum for 12 h 24 h, 40 h and 90 h the basal spacing was reduced to 35.8$\AA$, 34.2, 17.5 $\AA$ and 16.6$\AA$ respectively. The calculated amount of free $\varepsilon$-caprolactame included int he intercaltions complex and that of $\varepsilon$-caprolactame which is interca-lated into the interlayer space of montomorillonite and still remained after heat treatment are 4.6~4.9 and 0.5 molecules per unite cell of montmorillonite respectively.

• Journal of Microbiology and Biotechnology
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• v.19 no.9
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• pp.922-931
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• 2009

Screening-scale studies were performed with 26 fungal cultures for their ability to transform the anti-inflammatory drug meloxicam. Among the different fungi screened, a filamentous fungus, Cunninghamella blakesleeana NCIM 687, transformed meloxicam to three metabolites in significant quantities. The transformation of meloxicam was confirmed by high-performance liquid chromatography (HPLC). Based on the liquid chromatography-tandem mass spectrometry (LC-MS/MS) data, two metabolites were predicted to be 5-hydroxymethyl meloxicam and 5-carboxy meloxicam, the major mammalian metabolites reported previously. A new metabolite was produced, which is not detected in mammalian systems. Glucose medium, pH of 6.0, temperature of $27^{\circ}C$, 5-day incubation period, dimethylformamide as solvent, and glucose concentration of 2.0% were found to be suitable for maximum transformation of meloxicam when studied separately. It is concluded that C. blakesleeana can be employed for biotransformation of drugs for production of novel metabolites.

• YAKHAK HOEJI
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• v.37 no.2
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• pp.136-142
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• 1993

To a suspension of 1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-{3,7-diazabicyclo[3.3.0]oct-1(5)-en-3-yl}-4-oxo-3-quinoline carboxylic acid(C1) in sodium hydroxide solution and water is added dropwise with stirring carbon disulfide. [6R-[6$\alpha$, 7$\beta$(Z)]]-7-[[[2-Amino-4-thiazoly)methoxyimino]-acetyl]amino]-3-[[[[7-( 3-carboxy-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-7-guinolonyl)-3,7-diazabicyclo[3.3.0]oct-1(5)-en-3-yl]thioxomethyl]thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-2-carboxylic acid (DACD) was synthesized from 1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-[7-(mercapto) thioxomethyl-[3,7-dia zabicyclo[3.3.0]oct-1(5)-en-3-yl}]-4-oxo-3-quinoline carboxylic acid disodium salt(C2) and cefotaxime. The invitro activity of novel dual-action cephalosporin, DACD, was compared with the in vitro activities of CENO(cefotaxime 3'-norfloxacin dithiocarbamate), cefotaxime, and norfloxacin against a variety of bacterial species. In vitro activity of DACD was superior to that of norfloxacin against Streptococcus pyogenes. Against Gram-positive and Gram-negative bacteria, its activity was almost equal to that of CENO.

• Archives of Pharmacal Research
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• v.18 no.6
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• pp.449-453
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• 1995

The search for patinum (II)-based compounds with improved therapeutic properties was prompted to design and synthesize a new family of water-soluble, third generation cis-diamminedichlorplatinum (II) complexes linked to uracil and uridine. Six heretofore undescribed uracil and uridine-platinum (II) complexes are ; [N-(2-aminoethyl)uracil-5-carboxamide]dichloroplatinum (II)(3a), [N-2(2-aminoethyl)uracil-6-carboxmide]dichloroplatinum (II) (3b),[5-(2-aminorthyl)carbamoyl-2',3',5',-tri-O-acetyluridine] dichloroplatinum (II) (6b), [5-(2-aminoethyl)-carbamoyl]-2',3',5',-tri-O-acetyluridine] dichloroplatinum (II) (6b), [5-(2-aminoethyl)carbamoylu-ridine]dihloroplatinum (II) (7a), [6-(2-aminoethyl)carbamoyluridine]dichloroplatinum (II) (7b). These analogues were prepared from the key starting materials, 5-carboxyuracil (1a) and 6-carboxyuracil (1b) which were reacted with ethylenediamine to afford the respective N-(2-aminoethyl)uracil-5-carboxmide (2a) land N-(2-aminoethyl)uracil-6-carboxamide (2b). The cisplatin complexes 3a and 3b were obtained through the reaction of the respective 2a and 2b ficiently introduced on the .betha.-D-ribose ring via a Vorbruggen-type nucleoside coupling procedure with hexamethyldisilazane, trimethylchlorosilane and stannicchloride under anhydrous acetonitfile to yield the sterospecific .betha.-anomeric 5-carboxy-2',3',5'-tri-O-acetyluridine (4a) and 6-carboxy-2',3',5'-tri-O-acetyluridine (4b), respective 5-(2-aminoethyl)carbamoyl-2',3',5'-tri-O-acetyluridine (5a) and 6-(2-aminoethyl)carbamoyl-2',3',5'-tri-O-acetyluridine (5b). The diamino-uridines 5a and 5b were reacted with potassium tetrachloroplatinate (II) to give the novel nucleoside complexes, 6a and 6b respectively which were deacetylated into the free nucleosides, 7a and 7b by the treatment with CH/sub 3/ONa. The antitumor activities were evaluated against three cell lines (K-562, FM-3A and P-388).