• Archives of Pharmacal Research
• /
• v.16 no.3
• /
• pp.219-226
• /
• 1993

For the analysis of structure relationship of ar-turmerone analogues, the compounds containing the various substituents on the phenyl ring and 1(or 2)-naphthyl group in the place of phenyl of ar-turmerone were prepared and tested their cytotoxicity against HL-60, K-562, and L1210 leukemia cells in vitro. The substituents at para position are methoxy, phenoxy, methyl, trifluoromethyl, fluoro, and chloro. At meta position methoxy, methyl, trifluoromethyl, or chloro groups at ortho position mathoxy or chloro group were introduced. Against HL-60 and K-562 cells, $ED_{50}$ values of the analogues are ranged from 0.8 to $30.0\;\mu{g/ml}$. Againste L1210 cell, these are located more than $20.0\;\mu{g/ml}$. However, 5-carbone-thoxy-2-methyl-6(1-naphthyl)-2-octen-4-one (5n)possesses $ED_{50}$ valuses 0.8, 2.1, $6.5\;\mu{g/ml}$ against HL-60, L1210 cells, respectively. The electronic nature of the substituents on phenyl ring of ar-tumerone dose not affect the biological activity. Therefore the flat structure of aromatic potion of ar-tumerone analogues is the more important factor for their activity rather than its electronic nature. The potentiation of the cytotoxicity with the enlargement of aromatic ring region also supports the importance of the plane structure of this area. The restriction of the single bond rotation between C-6 and aromatic ring through the introduction of substituents at the ortho position of phenyl ring and the increment of size of alkyl group at C-6 position enhances the activity. Therefore the effective conformation should by the one having the orthogonal arrangement between the aromatic ring and the side chain.

• YAKHAK HOEJI
• /
• v.40 no.3
• /
• pp.357-368
• /
• 1996

The in vitro antibacterial activity of a novel fluoroquinolone, DWP20373(1-Cyclopropyl-6-fluoro-8-methoxy-7-(2,7-diazabicyclo[3,3,0]oct-4-ene-7-yl)-1,4-dihydro-4 oxoquino line-3carboxylic acid) was compared with those of ciprofloxacin (CPFX), sparfloxacin (SPFX) and ofloxacin (OFLX). DWP20373 was more active than SPFX and OFLX but was less potent than CPFX against gram-negative bacteria. DWP20373 showed an excellent activity against L-MRSA and H-MRSA ($MlC_{90}=0.781{\sim}1.563{\mu}g/ml$).The activity of DWP20373 decreased moderately in the presence of 5mM $Mg^{2+}$. However, pH and serum had no effect on the activity of DWP20373. DWP20373 possessed a rapid bactericidal activity against gram-positive and gram-negative strains.

• Journal of Adhesion and Interface
• /
• v.9 no.3
• /
• pp.14-19
• /
• 2008

In this study, silicone rubber (SR40) and fluororubber (FKM) mixture blends were prepared by various weight percentages, and their properties were characterized. The crosslinking rate increased as the contents of SR40 due to the crosslinking agent in SR40. As contents of FKM increase in SR40/FKM blends, thermal decomposition temperature of blends increased. When SR40/FKM blend ratio was at 50/50, the thermal decomposition stabilization was higher than that of pure SR40. The contact angle of SR40/FKM blend increased as the increase of SR40 contents in blend. All composition of SR40/FKM blends showed typical phase separation morphology. As the contents of SR40 increase in SR40/FKM blend, the degree of separation in SR40/FKM blends also increased.

• Journal of Gastric Cancer
• /
• v.17 no.4
• /
• pp.384-393
• /
• 2017

Purpose: The tumor microenvironment is known to be associated with the metabolic activity of cancer cells and local immune reactions. We hypothesized that glucose metabolism measured by 2-deoxy-2-($^{18}F$)fluoro-D-glucose ($^{18}F-FDG$) positron emission tomography (PET)-computed tomography (CT) ($^{18}F-FDG$ PET-CT) would be associated with local immune responses evaluated according to the presence of tumor infiltrating lymphocytes (TILs). Materials and Methods: We retrospectively reviewed 56 patients who underwent $^{18}F-FDG$ PET-CT prior to gastrectomy. In resected tumor specimens, TIL subsets, including cluster of differentiation (CD) 3, CD4, CD8, Forkhead box P3 (Foxp3), and granzyme B, were subjected to immunohistochemical analysis. The prognostic nutritional index (PNI) was calculated as: ($10{\times}serum$ albumin value)+($0.005{\times}peripheral$ lymphocyte counts). Additionally, the maximum standard uptake value ($SUV_{max}$) was calculated to evaluate the metabolic activity of cancer cells. Results: The $SUV_{max}$ was positively correlated with larger tumor size (R=0.293; P=0.029) and negatively correlated with PNI (R=-0.407; P=0.002). A higher $SUV_{max}$ showed a marginal association with higher CD3 (+) T lymphocyte counts (R=0.227; P=0.092) and a significant association with higher Foxp3 (+) T lymphocyte counts (R=0.431; P=0.009). No other clinicopathological characteristics were associated with $SUV_{max}$ or TILs. Survival analysis, however, indicated that neither $SUV_{max}$ nor Foxp3 held prognostic significance. Conclusions: FDG uptake on PET-CT could be associated with TILs, especially regulatory T cells, in gastric cancer. This finding may suggest that PET-CT could be of use as a non-invasive tool for monitoring the tumor microenvironment in patients with gastric cancer.

• Journal of the korean academy of Pediatric Dentistry
• /
• v.29 no.1
• /
• pp.11-18
• /
• 2002

Compomer, like resin composite, undergoes shrinkage during setting. But, due to the structure of glass ionomers and their hydrophilic nature, water sorption and subsequent expansion may lead to compensation of the shrinkage. The purpose of this study was to, evaluate the change of mliroleakage after 30day-water-storage of compomer and composite resin. 40 sound third molars were used for the microleakage test. Z-100 resin was used for the control groups(Group I and III), Dyract AP for the experimental groups(Group II and IV). The storage time was 1 day in Group I, II and 30days in Group III, IV. The result from the this study can be summarized as follows; 1. No significant difference could be found in microleakage of occlusal margin between each group(p>0.05). 2. In microleakage of gingival margin, no significant difference could be found between group I and II, and between group I and III (p>0.05). 3. Group IV was showed less microleakage than group II and group III in gingival margin(p<0.05).

• Elastomers and Composites
• /
• v.36 no.2
• /
• pp.102-110
• /
• 2001

The three types of surfactants such as nonylphenoxy poly(ethylene) ethanol homologues, caster oil poly(ethylene) ethanol homologues, and sodium perfluoroalkyl carboxylates are used to improve the wettability of rubber impression material. Among the surfactants, the usage of sodium perfluoroalkyl carboxylates containing fluoro group resulted in the lowest surface energy of impression material and the result gave the positive effect on the wettability of rubber impression material to teeth. Also, the anti-foaming agents were used to reduce or remove the hydrogen gas generating on the impression material by reaction. In the case of rubber impression material containing sodium perfluoroalkyl carboxylate as a surfactant, it was found that the tear strength of rubber impression material increased over 3 N/mm with the addition of anti-forming agent. Therefore, the anti-foaming agent could contribute to the mechanical property of rubber impression material without the change of surface property.

• Elastomers and Composites
• /
• v.45 no.3
• /
• pp.212-216
• /
• 2010

The materials of the lithium ion battery gasket require chemical resistance to the electrolyte, electrical insulating, compression set, anti-contamination and heat resistance. To estimate suitability for rubber which has better performance to compression set than PFA, each compound were made with various rubbers, such as EPDM, NBR, FKM, FVMQ, VMQ and we checked the characteristics of each compound. Samples from each compound was deposited in Propylene Carbonate and tested for changing of Hardness and Volume during 1,000 hr with $80^{\circ}C$. EPDM and VMQ showed good performance to chemical resistance to the electrolyte, and also we could get the values over $10^{10}{\Omega}cm$ on volume resistance basis in electrical insulating. EPDM and VMQ were judged as the most suitable material.

• Clean Technology
• /
• v.14 no.3
• /
• pp.193-203
• /
• 2008

A surfactant is used to assist the effect of cleaning, dispersibility and adhesion during leather manufacturing process. Existing surfactant for that process includes many hydrophilic groups that may cause problem such as stain, bad water resistance and poor durability, etc. It is potential problem to make high-performance property for future leather market. In this study, we have synthesized the fluorinated surfactant of which property decreases surface tension, increases dispersion, cleaning effect and the better chrome absorption by the high bond energy of C-F to complement weakness that the present alkyl derivative surfactants have. Using fluorinated surfactant, we can confirm that dispersion is increased, chrome absorption ratio is augmented with high osmosis and coherence, chrome content in the tanning waste water is reduced, BOD and COD contents are diminished and physical characteristics are improved.

• KSBB Journal
• /
• v.22 no.6
• /
• pp.426-432
• /
• 2007

We have developed a sensitive, one-step, homogeneous open sandwich fluoroimmunoassay (OsFIA) based on fluorescence resonance energy transfer (FRET) and luminescent semiconductor quantum dots (QDs). In this FRET assay, estrogen receptor-$\beta$ (ER-$\beta$) antigen was incubated with QD-labeled anti-ER-$\beta$ monoclonal antibody and AF (Alexa Fluoro)-labeled anti-ER polyclonal antibody for 30 minutes, followed by FRET measurement. The dye separation distance was estimated to be between $80\sim90\;{\AA}$. The present method is rapid, simple and highly sensitive, and did not require the bound/free reagent separation steps and solid-phase carriers. A concentration as low as 0.05 nM (2.65 ng/ml) receptor was detected with linearity ($R^2$ > 0.990). In addition, the assay was performed with commercial antibodies. This assay provides a convenient alternative to conventional, laborious sandwich immunoassays.

• The Korean Journal of Physiology and Pharmacology
• /
• v.13 no.2
• /
• pp.71-78
• /
• 2009

(S)-Carbamic acid 2-[4-(4-fluoro-benzoyl)-piperidin-1-yl]-1-phenyl-ethyl ester hydrochloride (YKP1447) is a novel "atypical" antipsychotic drug which selectively binds to serotonin (5-$HT_{2A}$, Ki=0.61 nM, 5-$HT_{2C}$, Ki=20.7 nM) and dopamine ($D_2$, Ki=45.9 nM, $D_3$, Ki=42.1 nM) receptors with over $10\sim100$-fold selectivity over the various receptors which exist in the brain. In the behavioral studies using mice, YKP1447 antagonized the apomorphine-induced cage climbing ($ED_{50}$=0.93 mg/kg) and DOI-induced head twitch ($ED_{50}$=0.18 mg/kg) behavior. In the dextroamphetamine-induced hyperactivity and conditioned avoidance response (CAR) paradigm in rats, YKP1447 inhibited the hyperactivity induced by amphetamine ($ED_{50}$=0.54 mg/kg) and the avoidance response ($ED_{50}$=0.48 mg/kg); however, unlike other antipsychotic drugs, catalepsy was observed only at much higher dose ($ED_{50}$=68.6 mg/kg). Based on the CAR and catalepsy results, the therapeutic index (TI) value for YKP1447 is over 100 (i.p.). These results indicate that YKP1447 has an atypical profile and less undesirable side effects than currently available drugs.