• Journal of Applied Biological Chemistry
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• v.66
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• pp.29-38
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• 2023

Recent studies have highlighted the link between diseases and inflammation across our lifespan. Our sedentary lifestyle, high-calorie diet, chronic stress, chronic infections, and exposure to pollutants and xenobiotics, collectively intensify the course and recurrence of infections and inflammation in our bodies, promoting the prevalence of chronic diseases and aging. Given such phenomena and considering additional factors such as the frequency of prescription, and easy access to over-the-counter drugs, the need for anti-inflammatory therapeutics is ever-increasing. However, the readily available anti-inflammatory treatment option comes with a greater risk of side effects or high cost (biologics). Therefore in this growing competition of discovering and developing new potent anti-inflammatory drugs, we focused on utilizing the established knowledge of traditional medicine to find lead compounds. Since lead optimization is an indispensable step toward drug development, we applied this concept for the production of potent anti-inflammatory compounds achieved by structural modification of flavonoids. The derivative obtained through acetylation of myricetin, 3,3',4',5,5',7-hexaacetate myricetin, showed a greater inhibitory effect in the production of pro-inflammatory mediators such as nitric oxide, Prostaglandin E₂, and pro-inflammatory cytokines like interleukin-6, interleukin1β, in lipopolysaccharide-stimulated RAW264.7 mouse macrophage cells compared to myricetin. The increased potency of inhibition was in conjunction with an increased inhibitory effect on inducible nitric oxide synthase and cyclooxygenase-2 proteins. Through such measures, this study supports lead optimization for well-established lead compounds from traditional medicine using a simpler and greener chemistry approach for the purpose of designing and developing potent anti-inflammatory therapeutics with possibly fewer side effects and increased bioavailability.

• International Journal of Advanced Culture Technology
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• v.12 no.3
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• pp.67-72
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• 2024

The algorithm is applied on the premise that the image generated by AI can be recognized and used smoothly by the user. Other assets are not exposed to the user or discarded because they are unnecessary or unfamiliar. This study aims to expand the scope of the utility of the image generated by AI, which is used as a high-level tool in the design field. To this end, we first examined human information processing and reflection in AI by the cognitive paradigm by examining previous studies and cases, and discussed the value of expansion by focusing on creativity and bottom-up processing of AI's self-organization. Considering the human recogmition process that instinctively grasps an object, the following AI usability was proposed. It is to utilize AI as a high-level tool applied appropriately to human perception, or to utilize the derivative itself by bottom-up self-organization. In addition, it is to set the algorithm to the minimum intervention so that basic elements such as shape, color, size, texture, and movement are composed of figure-ground according to the human perception process that instinctively grasps an object, and to utilize the results. Limiting the use of AI to a tool suitable for human perception and information processing or production by designers or general users is to operate only a part of the convenience and usability of AI. The image creation through AI's self-organization, as seen from the cognitive paradigm, is a step toward opening a new era of design where technical aesthetics meets devices, just as design has been constantly developing in pursuit of novelty and differentiation due to its nature.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.6
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• pp.2501-2504
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• 2014

Background: Capecitabine is an oral fluoropyrimidine derivative which is frequently used alone or in combination regimens for the treatment of metastatic breast cancer. Although overall and progression free survivals have increased in recent years with the use of new generation drugs, predictive factors that would further improve the outcomes are needed. Previous studies have demonstrated the relation between post-treatment increase in mean corpuscular volume (MCV) and predicting therapy response as well as survival. The present study investigated the clinical impact of MCV elevation in metastatic breast cancer patients treated with capecitabine. Materials and Methods: The data of a total of 82 patients from three centers followed between June 2005 and June 2013 were retrospectively analyzed. The demographic data and hormone receptor status of the patients, as well as initial examination before and after treatment and data concerning progression were recorded. MCV ${\geq}100$ fl was considered as macrocytosis. Capecitabine was given at a dose of $2500mg/m^2$ daily for 14 days every three weeks. Pre-treatment and post-treatment MCV and other parameters of complete blood count were recorded. Post-treatment initial evaluation was performed after 2 cycles of therapy. Results: The median age of the patients was 46.5 years (range 26-72 years) and 54% were premenopausal. Performance status was ECOG 0 and 1 in 81 (99%) patients. The median number of cycles for capecitabine therapy was 5 (min-max: 2-18). The median ${\Delta}MCV$ level (post-treatment values at sixth week - baseline) was 6.4. Whilst ${\Delta}MCV$ was ${\geq}6.4$ in 42 patients, it was <6.4 in 40 patients. Clinical benefit (complete response+partial response+stable disease) was observed in 37 (88%) of 42 patients with a median ${\Delta}MCV$ ${\geq}6.4$ and in 30 (75%) of 40 patients with ${\Delta}MCV$ <6.4 with no statistically significant difference (p=0.158). No significant difference was determined between the group with ${\Delta}MCV$ ${\geq}6.4$ and the group with ${\Delta}MCV$ <6.4 in terms of progression-free survival (11 vs 12 months) (p=0.55) and overall survival (20 months vs. 24 months) (p=0.11). Conclusions: The identification of new predictive markers in metastatic breast cancer is very important. In some recent studies, increase in MCV has been suggested as a marker in tumor response. In the present study, however, no significant difference was determined between tumor response and increase in MCV. Further studies including higher numbers of patients are needed to determine whether increase in MCV is a predictive marker or not.

• The Sea:JOURNAL OF THE KOREAN SOCIETY OF OCEANOGRAPHY
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• v.17 no.1
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• pp.9-15
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• 2012

Worldwide development of harmful algal blooms causes serious problem for public health and fisheries industries. To evaluate the algicidal impact on the harmful algae bloom species in aquatic ecosystems of coast, a new algicide thiazolidinedione derivative (TD49) were tentatively examined in the growth stages (i.e., lag, logarithmic and stationary phase) of rapidophyceae $Heterosigma$ $akashiwo$, $Chattonella$ $marina$ and $Chattonella$ sp..Three strains could easily destroy in the lag phase due to relatively weak cell walls than those of the logarithmic and stationary phase. It is thought that inoculation of TD49 substances into initial or developmental natural blooms with a threshold concentration ($2{\mu}M$) can maximize the algicidal activity. Also, bio-chemical assays revealed that the algicidal substances from all culture strains were likely to be extracellular substances because those cells have easily destroyed in cell walls. On the other hand, natural zooplankton communities were influenced within the exposure experiments of $2{\mu}M$, which is showed the maximum algcidal activity of tested organisms. These results indicate that although the TD49 substance is potential agents for the control of $H.$ $akashiwo$, $C.$ $marina$ and $Chattonella$ sp. in the enclosed eutrophic bay and coastal water, more detailed research of acute toxicity effect on high trophic organism in marine ecosystems need to be conducted.

• The Korean Journal of Nuclear Medicine Technology
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• v.12 no.3
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• pp.176-180
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• 2008

Department of Nuclear Medicine in Seoul National University Hospital (SNUH) had developed $^{18}F$-Flumazenil as Benzodiazepine receptor imaging agent for PET diagnosis of Epilepsy. But production Activity of $^{18}F$-Flumazenil is decreased owing to this method has difficult synthesis procedures and pretty long synthesis time. In this study, we can modify synthesizing method to have more simple procedure and less spend time and help to increase production Activity. Old method: Radioactivity was produced by cyclotron was captured by QMA cartridge that was activated. Captured radioactivity was eluted into the reaction vial by using kryptofix solution and delivered. After evaporation of eluent, the azeotrophic drying step repeated two times. tosylflumazenil in anhydrous Acetonitrile was added to a reaction vial while bubbling. The reaction mixture was evaporated until the mixture volume was 0.5 mL. Reaction vial washed with 20 % Acetonitrile and that solution went into the reaction vial. The reaction mixture was loaded to the HPLC loop by hand and purified $^{18}F$-Flumazenil by HPLC column. New method: We used $TBAHCO_3$ solution as a eluent. After the eluent was evaporated, tosylflumazenil in anhydrous acetonitrile was added to a reaction vial and the reaction mixture was bubbled for 15 minutes. It was evaporated until the mixture volume became 0.5 mL. It was loaded to the HPLC loop. In old method, $^{18}F$-Flumazenil was synthesized via 6 steps synthesis procedures in 105 minutes with 30~35% synthesizing yield (non-decay correction) and specific activity was about $0.5{\sim}2{\times}10^5$ Ci/mole. In new method, It had 3 steps synthesis procedures in 53 minutes with 40~45% synthesizing yield and specific activity was about $3{\sim}8{\times}10^5$ Ci/mole. This method leads to improve of minimizing synthesis time, increasing synthesis yield and specific activity. While we can load reaction mixture to the HPLC loop, we can expose high radiation field thanks to used by hand.

• Journal of Periodontal and Implant Science
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• v.38 no.1
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• pp.7-14
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• 2008

Purpose: Chitosan & chitosan derivative(eg. membrane) have been studied in periodontal regeneration, and recently many studies of chitosan have reported good results. If chitosan's effects on periodontal regeneration are enhanced, we can use chitosan in many clinical and experimental fields. For this purpose, this study reviewed available literatures, evaluated comparable experimental models. Materials and Methods: Ten in vivo studies reporting chitosan's effects on periodontal tissue regeneration have been selected by use of the 'Pubmed' and hand searching. Results: 1. In Sprague Dawley rat calvarial defect models, amount of newly formed bone in defects showed significant differences between chitosan/chitosan-carrier/chitosan-membrane groups and control groups. 2. In beagle canine 1-wall intrabony defect models, amount of new cementum and new bone showed significant differences between chitosan/chitosan-membrane groups and control groups. The mean values of the above experimental groups were greater than the control groups. Conclusion: The results of this study have demonstrated that periodontal regeneration procedure using chitosan have beneficial effects, which will be substitute for various periodontal regenerative treatment area. One step forward in manufacturing process of chitosan membrane and in use in combination with other effective materials(eg. bone graft material or carrier) may bring us many chances of common use of chitosan in various periodontal area.

• The Korean Journal of Pesticide Science
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• v.9 no.4
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• pp.279-286
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• 2005

The herbicidal activities against pre-emergence barnyard grass (Echinochloa crus-galli) by a series of new 2-(4-(6-chloro-2-benzoxazolyloxy)phenoxy)-N-phenylpopionamide derivatives as substrate molecule were studied using molecular holographic (H) quantitative structure activity relationships (HQSAR) methodology. From the based on the findings, the higher herbicidal active compounds are predicted by the derived HQSAR model. The best HQSAR model (VI-1) was derived from fragment distinction combination of atoms/bonds in fragment size, $7{\sim}10$bin. The herbicidal activities from atomic contribution maps showed that the activity will be able to increased according to the R-substituents variation of the N-phenyl ring and change of 6-chloro-2-benzoxazolyloxy group. Based on the results, the statistical results of the best HQSAR model (VI-1) exhibited the best pedictability and fitness for the herbicidal activities based on the cross-validated value ($q^2=0.646$) and non cross-validated value ($r^2_{ncv.}=0.917$), respectively. From the graphical analyses of atomic contribution maps, it was revealed that the lowest herbicidal activitics depends upon the 4-(6-chloro-2-benzoxazolyloxy)phenoxy group ($pred.pI_{50}=-3.20$). Particularly, the R=4-fluoro, X=isobutoxy substituent (P2) of (X)-phenoxy-N-(R)-phenylpropionamide derivative is predicted as the highest active compound ($pred.pI_{50}=9.12$).

• Polymer(Korea)
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• v.28 no.1
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• pp.41-50
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• 2004

A new hydroxypropyl chitosan capable of forming a thermotropic liquid crystalline phase and two kinds of derivatives based on the hydroxypropyl chitosan (6-cholesteryloxycarbonylpentoxypropyl) chitosans (CHPCTs) and acrylic acid esters of CHPCT (CHPCTEs) were synthesized. The crosslinked films with liquid crystalline order were also prepared by photocrosslinking CHPCTE in mesophase. The liquid crystalline properties for all the samples and the swelling behavior of the crosslinked samples in acetone were investigated. In contrast with the hydroxypropyl chitosan, all the uncrosslinked cholesteryl-bearing samples farmed monotropic cholesteric phases with left-handed helicoidal structures and exhibited reflection colors over the full cholesteric range. This is the first report of a thermotropic cholesteric liquid crystalline chitosan derivative with reflection bands in the visible region. Both the optical pitches (λ$\_$m/'S) of CHPCT and CHPCTE decrease with temperature or with cholesteryl content at a given temperature. However, the λ$\_$m/ of CHPCT was larger than that of CHPCTE at the same temperature and at the same cholesteryl content. All the crosslinked samples did not display reflection colors, indicating that the cholesteric structure of CHPCTE significantly changes upon crosslinking. The two-dimentional anisotropic swelling characteristic of liquid crystalline networks was observed for all the crosslinked samples.

• Journal of the Korean Chemical Society
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• v.42 no.3
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• pp.306-314
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• 1998

Acetolactate synthase (ALS) is the common enzyme in the biosynthesis of branched chain amino acids, Val, Leu, and Ile in bacteria, yeast, and higher plants. The enzyme is target site of several classes of structually diverse herbicides, including the sulfonylureas, the imidazolinones, the triazolopyrimidines, and the primidyl-oxy-benzoates. We have synthesized new triazolopyrimidine (TP) derivatives, and determined their inhibitory activities on barley ALS. $lC_{50}$ values for the active compounds were 3.2 nM-0.62 mM, and some of them appeared to be potent inhibitors. The progress curves for inhibition of ALS by TP4, a representative derivative, indicated that the extent of inhibition increased with incubation time. The inhibition of ALS by TP4 showed mixed-type inhibition with respect to pyruvate. Dual inhibition analyses of TP4 versus imidazolinone Cadre and feedback inhibitor Leu suggested that three different classes of inhibitors bind to ALS in a mutually exclusive manner. Chemical modification of tyrosyl residues of ALS decreased sensitivity of ALS to TP4, while modification of tryptophan and cysteine did not affect the sensitivity.

• Proceedings of the Korean Society of Near Infrared Spectroscopy Conference
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• 2001.06a
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• pp.1247-1247
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• 2001

Constituents of animal biofluids such as milk, blood and urine contain information specifically related to metabolic and health status of the ruminant animals. Some changes in composition of biofluids can be attributed to disease response of the animals. Mastitis is a major problem for the global dairy industry and causes substantial economic losses from decreasing milk production and reducing milk quality. The purpose of this study was to investigate potential of NIRS combined with multivariate analysis for cow's mastitis diagnosis based on NIR spectra of milk, blood and urine. A total of 112 bulk milk, urine and blood samples from 4 Holstein cows were analyzed. The milk samples were collected from morning milking. The urine samples were collected before morning milking and stored at -35$^{\circ}C$ until spectral analysis. The blood samples were collected before morning milking using a catheter inserted into the carotid vein. Heparin was added to blood samples to prevent coagulation. All milk samples were analyzed for somatic cell count (SCC). The SCC content in milk was used as indicator of mastitis and as quantitative parameter for respective urine and blood samples collected at same time. NIR spectra of blood and milk samples were obtained by InfraAlyzer 500 spectrophotometer, using a transflectance mode. NIR spectra of urine samples were obtained by NIR System 6500 spectrophotometer, using 1 mm sample thickness. All samples were divided into calibration set and test set. Class variable was assigned for each sample as follow: healthy (class 1) and mastitic (class 2), based on milk SCC content. SIMCA was implemented to create models of the respective classes based on NIR spectra of milk, blood or urine. For the calibration set of samples, SIMCA models (model for samples from healthy cows and model for samples from mastitic cows), correctly classified from 97.33 to 98.67% of milk samples, from 97.33 to 98.61% of urine samples and from 96.00 to 94.67% of blood samples. From samples in the test set, the percent of correctly classified samples varied from 70.27 to 89.19, depending mainly on spectral data pretreatment. The best results for all data sets were obtained when first derivative spectral data pretreatment was used. The incorrect classified samples were 5 from milk samples,5 and 4 from urine and blood samples, respectively. The analysis of changes in the loading of first PC factor for group of samples from healthy cows and group of samples from mastitic cows showed, that separation between classes was indirect and based on influence of mastitis on the milk, blood and urine components. Results from the present investigation showed that the changes that occur when a cow gets mastitis influence her milk, urine and blood spectra in a specific way. SIMCA allowed extraction of available spectral information from the milk, urine and blood spectra connected with mastitis. The obtained results could be used for development of a new method for mastitis detection.