• Biomolecules & Therapeutics
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• v.30 no.1
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• pp.19-27
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• 2022

Epidermal growth factor receptor (EGFR) is a receptor tyrosine kinase widely expressed in many cancers such as non-small cell lung cancer (NSCLC), pancreatic cancer, breast cancer, and head and neck cancer. Mutations such as L858R in exon 21, exon 19 truncation (Del19), exon 20 insertions, and others are responsible for aberrant activation of EGFR in NSCLC. First-generation EGFR tyrosine kinase inhibitors (TKIs) such as gefitinib and erlotinib have clinical benefits for EGFR-sensitive (L858R and Del19) NSCLC patients. However, after 10-12 months of treatment with these inhibitors, a secondary T790M mutation at the gatekeeper position in the kinase domain of EGFR was identified, which limited the clinical benefits. Second-generation EGFR irreversible inhibitors (afatinib and dacomitinib) were developed to overcome this T790M mutation. However, their lack of selectivity toward wild-type EGFR compromised their clinical benefits due to serious adverse events. Recently developed third-generation irreversible EGFR TKIs (osimertinib and lazertinib) are selective toward driving mutations and the T790M mutation, while sparing wild-type EGFR activity. The latest studies have concluded that their efficacy was also compromised by additional acquired mutations, including C797S, the key residue cysteine that forms covalent bonds with irreversible inhibitors. Because second- and third-generation EGFR TKIs are irreversible inhibitors, they are not effective against C797S containing EGFR triple mutations (Del19/T790M/C797S and L858R/T790M/C797S). Therefore, there is an urgent unmet medical need to develop next-generation EGFR TKIs that selectively inhibit EGFR triple mutations via a non-irreversible mechanism.

• Korean Journal of Veterinary Research
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• v.63 no.3
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• pp.23.1-23.9
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• 2023

This study was conducted to investigate tiamulin (TML) residues in the edible tissues of orally dosed broiler chickens and to re-establish the withdrawal time (WT). Thirty-six healthy Ross broiler chickens were administered 0.5 (TML-1) and 2.5 kg (TML-2) per ton feed, respectively, of the drug containing TML 78 g/kg for 10 days. Twenty-four tissue samples were collected from 6 chickens in each of the TML-1 and TML-2 groups on 0, 1, 3, and 5 days after drug administration, respectively. The residual concentrations of TML were measured using liquid chromatography-tandem mass spectrometry (LC-MS/MS). The correlation coefficient of the calibration curves was 0.9978 to 0.9998, and the limits of detection and the limits of quantification (LOQ) were in the range of 0.03 to 0.06, and 0.1 to 0.2 ㎍/kg, respectively. Recoveries ranged between 89.0% to 116.7%, and the coefficients of variation were less than 13.9%. After the drug administration, TML in the TML-1 and TML-2 groups was detected above the LOQ in 1 and 6 samples of liver, respectively, at day 0, and in 1 liver sample from both groups on day one. At 3 days after administration, TML was detected below the LOQ in all samples of TML-1 and TML-2. The calculated WT of TML in both TML-1 and TML-2 using the WT calculation program WT 1.4 was 0 days. In conclusion, the developed analytical method is suitable for detection, and the calculated WT of TML in poultry edible tissues is shorter than the current recommended WT of 7 days for TML in broiler chickens.

• Analytical Science and Technology
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• v.27 no.5
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• pp.234-242
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• 2014

Imicyafos which is a nematicide for controlling root-knot nematodes has been registered in the Republic of Korea in 2012, and the maximum residue limits of imicyafos are set to watermelon and korean melon as each 0.05 mg/kg. Extremely reliable and sensitive analytical method is required for ensuring food safety on imicyafos residues in agricultural commodities. Imicyafos residues in samples were extracted with acetone, partitioned with hexane and dichloromethane, and then purified with florisil. The purified samples were analyzed by HPLC-UVD and confirmed with LC-MS. Linear range was between 0.1~5 mg/kg with the correlation coefficient ($r^2$) 0.99997. Average recoveries of imicyafos ranged from 77.0 to 115.4% at the spiked levels of 0.02 and 0.05 mg/kg with the relative standard deviations of 2.2~9.6%. Limit of detection and quantification were 0.005 and 0.02 mg/kg, respectively. An inter-laboratory study was conducted to validate the determination method in depth, and the results were satisfactory. All of the validation results revealed that the developed analytical method in this study is relevant for imicyafos determination in agricultural commodities and will be used as an official analytical method.

• Analytical Science and Technology
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• v.26 no.2
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• pp.154-163
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• 2013

The maximum residue limits of pyrimisulfan is set as 0.05 mg/kg in rice in 2011, so very reliable and sensitive analytical method for pyrimisulfan residues is required for ensuring the food safety of pyrimisulfan residues in agricultural products. In this study, a rapid and sensitive analytical method was developed and validated using liquid chromatography electrospray ionization tandem mass spectrometry (LC-MS/MS) for the determination of herbicide pyrimisulfan residues in agricultural products. Average recoveries of pyrimisulfan ranged from 88.7 to 99.3% at the spiked level of 0.005 mg/kg and from 90.1 to 94.2% at the spiked level of 0.05 mg/kg, while the relative standard deviation was less than 10%. Linear range of pyrimisulfan was between 0.01~1.0 ${\mu}g/mL$ with the correlation coefficient ($r^2$) 0.999 and limit of quantification was 0.005 mg/kg. The results of method validation were satisfied Codex guideline. The results revealed that the developed and validated analytical method is possible for pyrimisulfan determination in agricultural product samples and will be used as an official analytical method.

• The Korean Journal of Pesticide Science
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• v.14 no.1
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• pp.21-29
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• 2010

The analytical method for bifenazate was developed using a HPLC (UVD). Also, analytical condition of LC/MS was set up for bifenazate. We validated the method for the precision and the reproducibility. The correlation coefficient of bifenazate ranged from 0.05 to 2.5 mg/kg was 1.0. Limit of quantitation (LOQ) was 0.01 mg/kg. To measure recoveries from agricultural products such as foxtail millet (cereal grains), kidney bean (beans), orange (fruits), perilla leaves (vegetables) and oak mushroom (mushrooms), bifenazate was spiked. Mean recoveries of bifenazate for each sample were 82.7~104.1% at the level of 0.1 mg/kg and 73.1~104.3% at the level of 0.5 mg/kg. The relative standard deviations (n=3) were 0.2~9.7%. Pesticide residues for bifenazate were investigated in 16 commodities (rice, foxtail millet, buckwheat, kidney bean, peanut, sesame, orange, grapefruit, kiwifruit, spinach, perilla leaves, leek, garlic stem, garlic, ginger and oak mushroom) collected from 22 provinces in 2009. Bifenazate was analyzed using analytical method by HPLC from 304 samples, and residue was not detected.

• Journal of Applied Biological Chemistry
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• v.48 no.4
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• pp.207-212
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• 2005

Prolyl endopeptidase (PEP, EC 3.4.21.26), also referred to as prolyl oligopeptidase, has been suggested to participate in learning and memory processes by cleaving peptide bonds on carboxyl side of prolyl residue within neuropeptides of less than 30 amino acids, and is abundant in brains of amnestic patients. Therefore, compounds possessing PEP inhibitory activity can be good candidate of drug against memory loss. Upon examination for PEP inhibition from traditional medicinal plants having tonic, stimulating, and anti-amnestic effects, Corni Fructus (Cornus officinallis) showed significant PEP inhibition. Ursolic and oleanolic acids, components of Corni Fructus, inhibited PEP with $IC_{50}$ values of $17.2\;{\pm}\;0.5$ and $22.5\;{\pm}\;0.7\;{\mu}M$, respectively.

• Korean Journal of Pharmacognosy
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• v.11 no.2
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• pp.69-74
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• 1980

The rhizome of Polygonatum robustum Nakai (Liliaceae) has been used as a crude drug for the purpose of tonic and thirst cure in Korea. The dried rhizomes were extracted with hot ether, then the residue was extracted with hot alcohol. 1) The three kinds of chemical constituents, substance, I, II and III were isolated by silicagel column chromatography from ether and alcohol extracts of the rhizomes. Substance I was confirmed as ${\beta}-sitosterol$, $C_{29}H_{50}O$ by mass and IR spectroscopy. Substance II was identified as stigmasterol by GLC. 2) Substance III was obtained by crystallization from the column chromatography of alcohol fraction. It was suggested as diosgenin based on chemical and spectral discussions. 3) The concentration of blood sugar was significantly decreased in the group administered the ether extract with 20% dextrose and adrenaline in comparison to that of 20% dextrose and adrenaline along.

• Food Science and Biotechnology
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• v.15 no.2
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• pp.308-311
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• 2006

Saesongi (Pleurotus eryngii) was cultivated in both potato dextrose agar (PDA) and sawdust media supplemented with Ca salts. The addition of Ca phosphate and Ca carbonate to sawdust media did not affect the growth, whereas Ca sulfate addition suppressed the mycelial growth appreciably. The efficiencies of Ca accumulation in the fruiting were studied based on mycelial growth experiments on Ca-supplemented sawdust media. Supplementation with 0.1 to 5% Ca phosphate increased the Ca content in the fruiting body by 4.5-6.5 fold, to a level of $314.6{\pm}22.7$ to $449.7{\pm}29.3$.

• Proceedings of the KSME Conference
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• 2003.11a
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• pp.905-909
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• 2003

This paper describes a shower type ultrasonic cleaning system using particle acceleration, developed for better effectiveness in washing out agricultural chemicals from fruits or vegetables, compared to the existing bath type ultrasonic cleaning system. The shower type system consists of a signal generator, a transducer, and a spouting nozzle, mainly. The system has been tested based on the method recommended by Korea Food and Drug Administration. It is found that shower type system shows better performance and cost-effectiveness than the bath type system that is commercially available .

• Korean Journal of Veterinary Research
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• v.36 no.3
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• pp.571-575
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• 1996

Sulfamethazine sodium was orally administrated to Sprague Dawley female rats(body weight: 200~250g) with the sonde caude at the dose of 20mg of sulfamethazine sodium per 100g of body weight for 3 days to investigate the depletion rate of the drug from liver, kidney and muscle of rat. The results obtained were summerized as follows; 1. The mean concentrations of sulfamethazine in liver according to the time lapsed after oral administration of the sulfamethazine sodium were decreased from 1.27ppm at day 1 to 0.28ppm at day 4. 2. Sulfamethazine concentrations in kidney according to the time lapsed after oral administration of the sulfamethazine sodium were decreased from 0.77ppm at day 1 to 0. 12ppm at day 4. 3. The mean concentration of sulfamethazine in skeletal muscle according to the time lapsed after oral administration of the sulfamethazine sodium was at or below 0.09ppm within 4 days after withdrawl of medicated solution.