• Archives of Pharmacal Research
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• v.25 no.5
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• pp.718-723
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• 2002

CKD-602 (7-[2-(N-isopropylamino)ethyl]-(20S)-camptothecin) is a recently-developed synthetic camptothecin analogue and currently under clinical development by Chong Kun Dang Pharm (Seoul, Korea). CKD-602 showed potent topoisomerase inhibitory activity in vitro and broad antitumor activity against various human tumor cells in vitro and in vivo in animal models. This study describes the pharmacodynamics of the immediate and delayed cytotoxicity induced by CKD-602 in a human colorectal adenocarcinoma cell line, HT-29, and its intracellular drug accumulation by HPLC. The present study was designed to address whether the higher activity of CKD-602 with prolonged exposure is due to delayed exhibition of cytotoxicity and/or an accumulation of anti proliferative effect on continuous drug exposure. The drug uptake study was performed to determine whether the delayed cytotoxicity is due to a slow drug accumulation in cells. CKD-602 produced a cytotoxicity that was exhibited immediately after treatment (immediate effect) and after treatment had been terminated (delayed effect). Both the immediate and delayed effects of CKD-602 showed a time dependent decrease in 4IC_{50}$ values. Drug uptake was biphasic and the second equilibrium level was obtained as early as at 24hr, indicating that the cumulative and delayed antitumor effects of CKD-602 were not due to slow drug uptake. On the other hand, CKD-602 treatment was sufficient to induce delayed cytotoxicity after 4hr, however, longer treatment (＞24hr) enhanced its cytotoxicity due to the intracellular accumulation of the drug, which requires 24hr to reach maximum equilibrium concentration. In addition, $C^n$$\times$T=h analysis (n=0.481) indicated that increased exposure times may contribute more to the overall antitumor activity of CKD-602 than drug concentration. Additional studies to determine the details of the intracellular uptake kinetics (e.g., concentration dependency and retention studies) are needed in order to identify the optimal treatment schedules for the successful clinical development of CKD-602.

• Journal of Oral Medicine and Pain
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• v.38 no.3
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• pp.221-233
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• 2013

Bile acids are polar derivatives of cholesterol essential for the absorption of dietary lipids and regulate the transcription of genes that control cholesterol homeostasis. Recently it have been identified the synthetic chenodeoxycholic acid (CDCA) derivatives HS-1200 and cisplatin showed apoptisis-inducing activity on various cancer cells in vivo and in vitro. This study was undertaken to investigate the synergistic apoptotic effect of co-treatment with HS-1200 and cisplatin on human tongue squamous cell carcinoma cells (SCC25 cells). To investigate whether the co-treatment with HS-1200 and cisplatin compared to each single treatment efficiently reduces the viability of SCC25 cells, MTT assay was conducted. The induction and augmentation of apoptosis were confirmed by DNA electrophoresis, Hoechst staining and an analysis DNA hypoploidy. Westen blot analysis and immunofluorescent staining were also performed to evaluate the expression levels and the translocation of apoptosis-related proteins following this co-treatment. Furthermore, proteasome activity and mitochondrial membrane potential (MMP) change were also assayed. In this study, co-treatment with HS-1200 and cisplatin on SCC25 cells showed several lines of apoptotic manifestation such as nuclear condensations, DNA fragmentation, reduction of MMP and proteasome activity, the increase of Bax and the decrease of Bcl-2, decrease of DNA content, the release of cytochrome c into cytosol, translocation of AIF and DFF40 (CAD) onto nuclei, and activation of caspase-9, caspase-7, caspase-3, PARP and DFF45 (ICAD) whereas each single treated SCC25 cells did not show these patterns. Although the single treatment of $25{\mu}M$ HS-1200 and $4{\mu}g/ml$ cisplatin for 24 h did not induce apoptosis, the co-treatment of these reagents prominently induced apoptosis. Therefore our data provide the possibility that the combination therapy with HS-1200 and cisplatin could be considered as a novel therapeutic strategy for human squamous cell carcinoma.

• Tribology and Lubricants
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• v.31 no.4
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• pp.183-188
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• 2015

This paper presents the experimental effects of lubricant with nanodiamond particles in sliding friction. In order to improve the performance of lubricants many additives are used, such as MoS₂, cadmium chloride, indium, sulfides, and phosphides. These additives are harmful to human health and to the environment, so alternatives are necessary. One such alternative is nanodiamond powder, which has a large surface area. In order to investigate the effect of nanodiamonds in lubricants under sliding friction, they are dispersed in the lubricant at a variety of concentrations (0 wt%, 0.1 wt%, 0.3 wt%, 0.5 wt%, and 1 wt%) using the matrix synthesis method. Friction and wear tests are performed according to the ASTM G99 method using a pin-on-disc tester at room temperature. The specimens used in this experiment are AISI 52100 ball bearings and AISI 1020 steel discs. During the test, lubricant mixed with nanodiamond is supplied constantly to keep the two bodies separated by a lubricant film. To maintain boundary lubrication, the speed is set to 0.18 m/s and a load of 294 N is applied to the disc through the pin. Results are recorded by using workbench software over the test duration of 10 minutes. Experimental results show that when the concentration of nanodiamond increases, the coefficient of friction decreases. However, above a nanodiamond concentration of 0.5 wt%, both the coefficient of friction and wear volume increase. From this experiment, the optimum concentration of nanodiamond showing a minimum coefficient of friction of 0.09 and minimum wear volume of 0.82 nm² was 0.5 wt%.

• Nutrition Research and Practice
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• v.13 no.4
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• pp.323-332
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• 2019

BACKGROUND/OBJECTIVES: The aim of this study was to analyze specific foods influencing absolute nutrient intake and between-person variations of nutrient intake among Korean preschoolers. SUBJECTS/METHODS: This study included 2,766 participants aged 1-5 years in the 2009-2013 Korea National Health and Nutrition Examination Surveys. Dietary data were obtained from a 24-h dietary recall method. Major food sources of absolute nutrient intake were evaluated based on percent contribution of each food. To assess the contribution of specific foods to between-person variations in nutrient intake, stepwise multiple regressions were performed and cumulative $R^2$ was used. RESULTS: White rice and milk were main food sources of energy, protein, carbohydrate, phosphorus, iron, potassium, thiamin, riboflavin, and niacin. The percentage of fat contributed by milk was 21.3% which was the highest, followed by pork, soybean oil, and egg. White rice accounted for 25% and 40% of total variability in total energy and carbohydrate intakes, respectively. About 39% of variation in calcium intake was explained by milk while 40% of variation in phosphorous intake was explained by cheese. The top 10 foods contributing to between-person variations in nutrient intakes were similar with food items that mainly contributed to absolute nutrient intakes. The number of foods explaining 90% of absolute amounts of nutrient intakes varied from 28 for vitamin A to 80 for iron. CONCLUSIONS: This study identified specific foods that contributed to absolute nutrient intakes and between-person variations in nutrient intakes among Korean preschoolers. Our findings can be used to develop dietary assessment tools and establish food-based dietary guidelines for young children.

• Journal of the Korean Chemical Society
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• v.56 no.2
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• pp.236-245
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• 2012

The main mycobacterial infection in human is tuberculosis caused by Mycobacterium tuberculosis. Tuberculosis is the leading infectious cause of death in the world. Therefore there is continuing and compelling need for new and improved treatment for tuberculosis. The entire logic towards design of new compounds containing 4-hydroxy-N'-(1,3-thiazoldin- 2-yldene)benzohydrazide moiety is basically for superior antimycobacterial activity. The recent advances in QSAR and computer science have provided a systematic approach to design a structure of any compound and further, the biological activity of the compound can be predicted before synthesis. The 3D-QSAR studies for the set of 4-hydroxy-N'-(1,3-thiazoldin- 2-yldene)benzohydrazide and their derivatives were carried out by using V-life MDS (3.50). The various statistical methods such as Multiple Linear Regression (MLR), Partial Least Square Regression (PLSR), Principle Component Regression(PCR) and K nearest neighbour (kNN) were used. The kNN showed good results having cross validated $r^2$ 0.9319, $r^2$ for external test set 0.8561 and standard error of estimate 0.2195. The docking studies were carried out by using Schrodinger GLIDE module which resulted in good docking score in comparison with the standard isoniazid. The designed compounds were further subjected for synthesis and biological evaluation. Antitubercular evaluation of these compounds showed that (4.a), (4.d) and (4.g) found as potent inhibitor of H37RV.

• Restorative Dentistry and Endodontics
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• v.9 no.1
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• pp.59-68
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• 1983

The purpose of this study was to examine the influence of canal irrigants and the method of canal filling on the quality of canal obturation. Sixty extracted human teeth with single root were selected and divided into three different groups; In group I (control); 5 cc normal saline irrigated after each instrumentation In group II; 2.5 cc-3% NaOCl in combination with 2.5 cc-3% $H_2O_2$ In group III; RC-Prep in combination with 5 cc-3% NaOCl All specimens were cleaned, shaped(#50 file size), irrigated and obturated by lateral condensation and automated thermatic condensation filling method of gutta-percha and AH-26. After all the specimens were immersed in 2% methylene blue dye solution in $37^{\circ}C$ for 7 days and the degree of dye penetration into the canals observed by magnifying glass(${\times}$20) and reflected light microscope The results were as follows: 1. All the the teeth showed some degree of the dye penetration. 2. There were no significant difference among three groups in the degree of the dye penetration in each canal filling method. 3. There were no significant difference of the dye penetration between each canal filling method in group I. 4. There were no statistically significant difference of the dye penetration between each canal filling method in group II and group III, but lateral condensation group was showed slightly more than automated thermatic condensation group.

• Journal of Ginseng Research
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• v.44 no.2
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• pp.215-221
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• 2020

Background: Panax ginseng has been used for a variety of medical purposes in eastern countries for more than two thousand years. From the extensive experiences accumulated in its long medication use history and the substantial strong evidence in modern research studies, we know that ginseng has various pharmacological activities, such as antitumor, antidiabetic, antioxidant, and cardiovascular system-protective effects. The active chemical constituents of ginseng, ginsenosides, are rich in structural diversity and exhibit a wide range of biological activities. Methods: Ginsenoside constituents from P. ginseng flower buds were isolated and purified by various chromatographic methods, and their structures were identified by spectroscopic analysis and comparison with the reported data. The 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H- tetrazolium bromide method was used to test their cytotoxic effects on three human cancer cell lines. Results: Six ginsenosides, namely 6'-malonyl formyl ginsenoside F₁ (1), 3β-acetoxyl ginsenoside F₁ (2), ginsenoside Rh₂₄ (6), ginsenoside Rh₂₅ (7), 7β-hydroxyl ginsenoside Rd (8) and ginsenoside Rh₂₆ (10) were isolated and elucidated as new compounds, together with four known compounds (3-5 and 9). In addition, the cytotoxicity of these isolated compounds was shown as half inhibitory concentration values, a tentative structure-activity relationship was also discussed based on the results of our bioassay. Conclusion: The study of chemical constituents was useful for the quality control of P. ginseng flower buds. The study on antitumor activities showed that new Compound 1 exhibited moderate cytotoxic activities against HL-60, MGC80-3 and Hep-G2 with half inhibitory concentration values of 16.74, 29.51 and 20.48 μM, respectively.

• Journal of Microbiology and Biotechnology
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• v.27 no.4
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• pp.785-790
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• 2017

Two piloquinone derivatives isolated from Streptomyces sp. CNQ-027 were tested for the inhibitory activities of two isoforms of monoamine oxidase (MAO), which catalyzes monoamine neurotransmitters. The piloquinone 4,7-dihydroxy-3-methyl-2-(4-methyl-1-oxopentyl)-6H-dibenzo[b,d]pyran-6-one (1) was found to be a highly potent inhibitor of human MAO-B, with an $IC_{50}$ value of $1.21{\mu}M$; in addition, it was found to be highly effective against MAO-A, with an $IC_{50}$ value of $6.47{\mu}M$. Compound 1 was selective, but not extremely so, for MAO-B compared with MAO-A, with a selectivity index value of 5.35. Compound 1,8-dihydroxy-2-methyl-3-(4-methyl-1-oxopentyl)-9,10-phenanthrenedione (2) was moderately effective for the inhibition of MAO-B ($IC_{50}=14.50{\mu}M$) but not for MAO-A ($IC_{50}$ > $80{\mu}M$). There was no time-dependency in inhibition of MAO-A or -B by compound 1, and the MAO-A and -B activities were almost completely recovered in the dilution experiments with an excess amount of compound 1. Compound 1 showed competitive inhibition for MAO-A and -B, with $K_i$ values of 0.573 and $0.248{\mu}M$, respectively. These results suggest that piloquinones from a microbial source could be potent reversible MAO inhibitors and may be useful lead compounds for developing MAO enzyme inhibitors to treat related disorders, such as depression, Parkinson's disease, and Alzheimer's disease.

• Spatial Information Research
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• v.15 no.1
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• pp.67-80
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• 2007

The land cover map represent the state of earth surfaces. It can be used as basic data to explore present conditions of earth surfaces and develop future plans for local areas. To produce the land cover map with efficiency, gathering geographic information from satellite images is important. Exporting, building, and managing processes on the land cover information are needed as well. In this study we aim to review the producing process of the level-2 land cover map in detail and enhance it. h present status of the producing process of the land cover map in Korea is reviewed, problems of the process are explored, and measures for improving it are proposed. The criteria for fixing boundaries and providing attributes for the land cover map are proposed. This proposed criteria may solve problems in a present producing process. The improving measures proposed in this study should be continuously revised in future studies.

• Journal of Biomedical Engineering Research
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• v.31 no.1
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• pp.67-73
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• 2010

The foot performs an important function in supporting the body and keeping body balance. An abnormal walking habit breaks the balance of the human body as well as the normal function of the foot. The influence of a flatfoot(pes planus) occupies a considerable portion of the various causes resulting in the wrong walking habit. But, little studies has been done by the functional foot orthotics for the flat foot. The object of this study, therefore, is to propose a new approach method to reveal the effects of the improvement of the foot function by using orthotics. The essential point of this study is to measure and analyze the change of ankle angle in the sagittal plane for flat foot subjects wearing the orthotics. Before and after wearing the functional orthotics, the gait analysis of flat foot subjects was conducted in three experimental aspects : the change of ankle angle, the change of the total Ankle ROM and the difference of left & right ankle angle in the sagittal plane. 1. The average ankle angle differences of before-and-after wearing the orthotics have declined like this; left : $2.71^{\circ}$, right: $1.91^{\circ}$ (p<0.05). 2. Total ankle ROM also showed decrease in both sides while the left side's is rather slight; left : $0.57^{\circ}$, right : $2.07^{\circ}$ (p<0.05). 3. The difference of left and right ankle angle in the sagittal plane decreased by $0.71^{\circ}$ (p<0.05). In result, it is confirmed that the functional foot orthotics have a significant effect on mechanical movement of ankle joint for flat foot. it is expected that this paper will be further studied and improved as a practical estimation method in the research on the effect of foot-orthotics.