• Journal of Radiopharmaceuticals and Molecular Probes
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• v.3 no.2
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• pp.91-97
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• 2017

$^{18}F-THK-5351$ is a PET radiotracer to image the hyperphosphorylated tau fibrillar aggregates in human brain. This protocol describes the optimized radiosynthesis of $^{18}F-THK-5351$ using a commercial GE $TRACERlab^{TM}$ $FX_{FN}$ radiosynthesis module. $^{18}F-THK-5351$ was prepared by nucleophilic [$^{18}F$]fluorination from its protected tosylate precursors, (S)-(2-(2-methylaminopyrid-5-yl)-6-[[2-(tetrahydro-2H-pyran-2-yloxy)-3-tosyloxy]propoxy] quinolone(THK-5352), at $110^{\circ}C$ for 10 min in dimethyl sulfoxide, followed by deprotection with 1 N HCl. The average radiochemical yield of $^{18}F-THK-5351$ was $31.9{\pm}6.7%$(decay-corrected, n = 10), with molar activity of $198.1{\pm}33.9GBq/{\mu}mol$($5.4{\pm}0.9Ci/{\mu}mol$, n = 10). The radiochemical purity was determined to be above 98%. The overall production time including HPLC purification is approximately 70 min. This fully-automated protocol is validated for clinical use.

• Archives of Pharmacal Research
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• v.19 no.1
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• pp.62-65
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• 1996

A homologous series of twenty, hitherto unreported, analogues of 5-halosubstituted $1, 3-Bis(\omega-cyanoalkyl)uracil$acyclic nucleosides were synthesized by the series of alkylation reactions of 5-halouracils with the corresponding chloroacetonitrile, chloropropionitrile, chlorobutyronitrile and 5-chlorovaleronitrile $(Cl-(C_ 2)_n-CN: n=l, 2, 3, 4)\; in\; anhydrous\; DMSO\; (or DMF)/K_2CO_3(or NaH)\; under\; 75^{\circ}C$ temperature. Antitumor activities for the synthesized compounds were determined against three cell lines (FM-3A cell, P-388 cell and U-938 cell lines). The compounds that exhibited moderate activity to significant activity, included la-b, 2a-b, 3a-c, and 4a, whose compounds were active against P-388, FM-3A and U-937 cell lines with the compounds la, lb, and 2a, showing significant antitumor activity (inhibitory concentrations $(IC_{50})$ ranged from 2.2 to $7.0\mug/ml$). Their strucrure-activity relationship did not show any activity differences in their effective chain length (methyl, ethyl, propyl, butyl) in 1, 3-bis(.omega.-cyanoalkyl) uracils.

• Journal of Society of Preventive Korean Medicine
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• v.13 no.2
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• pp.39-50
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• 2009

Objectives : In order to evaluate the cytotoxicity of 3,4,5-trihydroxybenzoic acid and related compounds on the growth of normal cell lines and human oral epithelioid cell line, cell viability, cell adhesion ability, and morphological changes of cells were examined. Methods : We measured the cytotoxicity of 3,4,5-trihydroxybenzoic acid and related compounds with 3-[4,5-dimethyl-thiazol-2-yl]-2,5-diphenyltetrazolium bromide-[MTT), and 2,3-bis-[2-methoxy-4-nitro-5-sulfophenyl]-2H-tetrazolium -5-caboxanilide-[XTT) methods. Results : The cytotoxicity of 3,4,5-trihydroxybenzoic acid($IC_{50}$, $2,552.40\;{\mu}M$) was low according to the toxic criteria. Cytotoxic effect of 3,4,5-trihydroxybenzoic acid and related compounds against $IC_{50}$ value in cell morphology increased in a concentration-dependent manner. In light microscopy, $100\;{\mu}M$ 3,4,5-trihydroxy-benzoic acid showed th highest cytotoxic activity. Conclusions : These results suggest that 3,4,5-trihydroxybenzoic acid may have a potential anticancer activity.

• Proceedings of the SAREK Conference
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• 2008.06a
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• pp.1392-1397
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• 2008

This study is to measure the change of the $CO_2$ and floating dust concentration depending on the volume of the ventilation and the state of on/off the ventilation for the estimation of the air pollution in classroom. The results could be summarized as follows: the test cell was the two full scaled model and the one is set up with ventilation system another was not. the volume of classroom is 170.1m3 and the number of persons are 35. 1)when the ventilation system was not installed, The experimental results of the $CO_2$ concentration showed the average of 2,150ppm and the maximum of 2,740ppm in the classroom. This was the higher than 1,000ppm, the standard value of ASHRAE and the enforcement regulations of School Sanitation Code in Ministry of Education & Human Resources Development, 1000ppm. The $CO_2$ concentration was relatively increasing during school hours. 3)In case of the volume of ventilation of $800m^3$/h, the $CO_2$ concentration of classroom showed the average of 962 ppm and the maximum of 1,380 ppm. This was higher than 1,000ppm, the standard of ASHRAE and the enforcement regulations of School Sanitation Code in Ministry of Education & Human Resources Development. 4)The floating dust(PM10) was the maximum of 0.52 mg/$m^3$, the minimum of 0.25 mg/$m^3$, and the average of 0.32 mg/$m^3$ in case of the ventilation system off. Those were higher than the standard value 0.15 mg/$m^3$. In case of the ventilation system on, the floating dust(PM10) was the maximum of 0.174 mg/$m^3$ , the minimum of 0.048 mg/$m^3$, and the average of 0.078 mg/$m^3$. These were the lower than 0.15 mg/$m^3$, the standard of the enforcement regulations of School Sanitation Code in Ministry of Education & Human Resources Development. 5)The concentrations of $CO_2$ and PM10 were largely depending on the number of students and the ventilation system, The installation of the ventilation system is necessary for the amenity environment and the management of the indoor air quality.

• Journal of Applied Biological Chemistry
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• v.65 no.4
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• pp.405-412
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• 2022

Echinodorus cordifolius (L.) is an aquatic plant in the family Alismataceae. The anti-skin aging activity of E. cordifolius (L.) has not been yet reported. Therefore, the objective of the present study was to prepare 70% ethanol extract (ECEE) from E. cordifolius (L.) and investigate their antioxidant and anti-hyaluronidase activities for confirm the potential of anti-skin aging. ECEE showed good activities of DPPH, hydrogen peroxide scavenging, and hyaluronidase inhibition, with EC₅₀ and IC₅₀ values of 31.4, 300, and 450 ㎍/mL, respectively. ECEE also significantly improved cell viability and inhibited intracellular reactive oxygen species dose-dependently against 1 mM hydrogen peroxide-induced oxidative stress in immortalized human keratinocytes (HaCaT cells). Furthermore, ECEE upregulated hyaluronic acid (HA)-synthesizing enzyme hyaluronan synthase 2 (HAS2) expression level, but downregulated expression level of HA-degrading enzyme hyaluronidase 2, resulting in increased HA production in HaCaT cells. Taken together, these results suggest that ECEE shows antioxidant and anti-hyaluronidase potential and could be a functional cosmetic ingredients for anti-skin aging.

• Journal of Physiology & Pathology in Korean Medicine
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• v.24 no.6
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• pp.956-961
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• 2010

Tumor necrosis factor-alpha (TNF-${\alpha}$) is a major mediator of immuno-inflammatory activity. The purpose of this study is to investigate whether TNF-${\alpha}$ productions of mouse macrophage RAW 264.7 and human hepatocyte HepG2 are modulated by Artemisiae argi Folium water extract (AW), Lactobacillus pentosus-fermented Artemisiae argi Folium water extract (AFL), and Saccharomyces cerevisiae-fermented Artemisiae argi Folium water extract (AFS) for 3 h of incubation. Effect of AW on cell viability of HepG2 was also investigated. TNF-${\alpha}$ productions were measured by Enzyme-Linked Immnunosorbent Assay method and cell viability was measured by MTT assay. Both AFL and AFS significantly increased TNF-${\alpha}$ productions of RAW 264.7 at the concentration of 50, 100, and 200 ${\mu}g$/mL (p<0.05). Also, AFL and AFS significantly increased TNF-${\alpha}$ productions of HepG2 at the concentration of 50, 100, and 200 ${\mu}g$/mL (p<0.05). AW significantly increased TNF-${\alpha}$ production of HepG2 at the concentration of 100 and 200 ${\mu}g$/mL (p<0.05). AW did not show any cytotoxicity on HepG2 cells for 3 h. These results suggest that AFL, AFS, and AW have the immune-enhancing property related with its increasing effect on TNF-${\alpha}$ production of macrophage and hepatocyte.

• Analytical Science and Technology
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• v.36 no.1
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• pp.53-58
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• 2023

2'-Hydroxy-3',4'-methylenedioxy-3,4,5-trimethoxychalcone (HMTC) is a newly synthesized chalcone that affects proliferation, cytotoxic potential and apoptosis in human leukemia cells. However, no validated determination method has been described so far for HMTC in biological samples. Thus, we developed a liquid chromatographic method using a tandem mass spectrometry to determine HMTC in rat plasma. Liquid-liquid extraction with ethyl acetate was used for the clean-up procedure. The analyte was separated on a reversedphase column with mobile phase of distilled water and acetonitrile (2:8, v/v, including 0.1 % formic acid). The ion transition of the precursor to the product ion was principally deprotonated ions [M-H]^- at m/z 356.8 → 327.2 for HMTC. This analytical method was successfully applied in pharmacokinetic study of HMTC after intravenous administration in rats.

• Biomolecules & Therapeutics
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• v.21 no.2
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• pp.170-172
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• 2013

The pyrimidine nucleoside uridine has recently been reported to have a protective effect on cultured human corneal epithelial cells, in an animal model of dry eye and in patients. In this study, we investigate the pharmacokinetic profile of uridine in rabbits, following topical ocular (8 mg/eye), oral (450 mg/kg) and intravenous (100 mg/kg) administration. Blood and urine samples were serially taken, and uridine was measured by high-performance liquid chromatography-tandem mass spectrometry. No symptoms were noted in the animals after uridine treatment. Uridine was not detected in either plasma or urine after topical ocular administration, indicating no systemic exposure to uridine with this treatment route. Following a single intravenous dose, the plasma concentration of uridine showed a bi-exponential decay, with a rapid decline over 10 min, followed by a slow decay with a terminal half-life of $0.36{\pm}0.05$ h. Clearance and volume of distribution were $1.8{\pm}0.6$ L/h/kg and $0.58{\pm}0.32$ L/kg, respectively. The area under the plasma concentration-time curves (AUC) was $59.7{\pm}18.2{\mu}g{\cdot}hr/ml$, and urinary excretion up to 12 hr was ~7.7% of the dose. Plasma uridine reached a peak of $25.8{\pm}4.1{\mu}g/ml$ at $2.3{\pm}0.8$ hr after oral administration. The AUC was $79.0{\pm}13.9{\mu}g{\cdot}hr/ml$, representing ~29.4% of absolute bioavailability. About 1% of the oral dose was excreted in the urine. These results should prove useful in the design of future clinical and nonclinical studies conducted with uridine.

• Korean journal of food and cookery science
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• v.26 no.2
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• pp.214-219
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• 2010

In this study, phytoestrogen for the industrial production of soybean probiotics by lactic acid bacteria (LAB) was studied in a soybean extract. Soybean was fermented with LAB, Lactobacillus plantarum KCTC 3108 and Bifidobacterum longum ATCC 15707. The change in the content of various isoflavones (aglycone and glucoside) and the $\beta$-glucosidase activity in soybean during fermentation were investigated and shown to be dependent on the starter organism. Soybean extract powder fermented with L. plantarum showed the highest $\beta$-glucosidase activity and the greatest increase in the aglycone content. After 48h of fermentation, the contents of daidzin, genistin and glycitin in L. plantarum decreased from a mean initial levels of $83.03{\pm}2.17$, $168.13{\pm}8.17$ and $20.02{\pm}1.07$, respectively, to mean levels of $5.34{\pm}3.24$, $3.79{\pm}0.57$ and $1.87{\pm}1.09\;mg$/100 g. Whereas, after 48h fermentation, the contents of daidzein, genistein and glycitein increased from a mean initial levels of $8.09{\pm}0.78$, $11.20{\pm}0.84$ and $4.71{\pm}0.46$, respectively, to mean levels of $85.76{\pm}0.84$, $175.87{\pm}2.21$ and $22.41{\pm}0.91\;mg$/100 g. Taken together, these results suggested an increase of aglycones and decrease of glucoside in isoflavones occurred during fermentation, which coincided with an increase of $\beta$-glucosidase activity in the fermented soybean extract powder.

• Analytical Science and Technology
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• v.7 no.4
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• pp.455-460
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• 1994

A selective extraction-spectrophotometric method for the determination of mercury(II) with nocotinaldehyde-4-phenyl-3-thiosemicarbazone(NPS) was described. The method is based on the formation of an insoluble mercury-NPS complex, which is extratable into chloroform from an aqueous solution at pH 3.5 by shaking for 3 min. The absorbance is measured at 365nm and the molar absorptivity is $2.45{\times}10^4L\;mol^{-1}\;cm^{-1}$. The complex system conforms to Beer's law for up to $18{\mu}g\;mL^{-1}$ of mercury(II). The proposed method is simple and selective and has been satisfactorily applied to the determination of mercury in standard human hair sample.