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

• The Korean Journal of Zoology
• /
• v.16 no.1
• /
• pp.25-41
• /
• 1973

Ultrastructural changes in the cells of the corpora allata of the pine moth, Dendrolimus spectabilis Butler, were studied by electron microscope to know the structural correlates of hormone production by the gland during the larval-pupal-adult transformations. Mitochondria are in active phases from the overwintered to the last instar larvae and from the pupae just after pupation to the 20-day old pupae, while they are in inactive phases from the making cocoon stage to the prepupae just before pupation. The peripheral allatum cells have electron dense granules in the intracellular vacuoles of smooth-surfaced endoplasmic reticulum in the larval life, particularly in the overwintered larvae and in the early adults but the swollen smooth-surfaced intracytoplasmic vacuoles made by expansion of an end of the tubular rough endoplasmic reticulum, some of which contain fibrous proteins, are observed in addition to the vacuoles in the intercellular spaces in which the vacuoles grow by fusing each other from the mature larvae to the prepupae, both of them disappearing during just before pupation. After pupation the cytolasmic vacuoles develop again in the allatum cells so that they seem to begin the secretory activity. The fact that the neurosecretory granules stored within the axons terminated in the corpus allatum are visible only from the 20-day old pupa about two days before abult emergence to the 5-day old adult means that the secretion from the allatum cells is under the control of the brain from the late pupal stage, while the secretion during from the larval to the early pupal life has no relation with the brain, because such granules are not observed within the axons. It is, therefore, suggested that at least two kinds of hormone are released with the ages as far as concerned with the production and secretion mechanisms of the allatum hormone: juvenile hormone is released until the last instar larvae without any direct stimlation of the brain and gonadotropic hormone is secreted from the late pupa to the adult by getting brain's stimulation and that the secretory phases observed from the mature larvae to prepupae are presumably concerned with the biosynthesis of protein owing to the ecdysone and those from the early pupal stage in uncontrolled condition of the brain with the prothoracotropic activity.

• Tuberculosis and Respiratory Diseases
• /
• v.50 no.4
• /
• pp.450-461
• /
• 2001

Background : The underlying pathogenesis of radiation-induced lung fibrosis (RTLF) has not been very well defined. However, the role of TGF-$\beta$ in the generation of RTLF has been a major focus because there is an increase in the expression of both the TGF-${\beta}m$-RNA and its protein preceding RTLF lesions. The down stream signal after a TGF-$\beta$ stimulated lung fibrosis includes the activation of many mediators such as Smad and c-Jun N-terminal kinase (JNK) through TAK1. It is we hypothesized that JNK activation may play a pivotal role in RTLF pathogenesis through increased transcription of the fibrogenic cytokines. The present study evaluates JNK activity in alveolar macrophages after irradiation and the relationship between JNK activity and the amount of collagen in the lung tissues. Methods : C57BL/6 mice(20-25 gr, males) received chlorotetracycline(2g/L) in their drinking water 1 week prior to irradiation and continuously there after. The mice were irradiated once with 1400 cGy of $60CO{\gamma}$-ray over the whole chest. The cellular composition of the whole lung bronchoalveoalr lavage fluids(BALF), elastin expression in the lung tissues, the level of hydroxyproline in lung tissues, and an in vitro JNK assay was measured before irradiation and one, four, and eight weeks after irradiation (RT). Results : The volumes of BALF retrieved from instilled 4 mL of saline with 2% heparin were 3.7-3.8 mL for each group. The cell numbers were similar before($4.1{\times}10^4{\pm}0.5{\times}10^4/mL$) and 1 week($3.1{\times}10^4{\pm}0.5{\times}10^4/mL$) after RT. At four and eight weeks after RT, the cell number reached to $14.0{\times}10^4{\pm}1.5{\times}10^4mL$ and $10.0{\times}10^4{\pm}1.3{\times}10^4/mL$, respectively. There we no changes in the lymphocytes and neutrophils population observed in the BALF after RT. The H-E stain of the lung tissues did not show any structural and fibrotic change in the lung tissues at 4 and 8 weeks after RT. In addition, the amount of elastin and collagen were not different on Verhoeff staining of the lung tissues before RT to eight weeks after RT. The hydroxyproine content was measured with the left lung dissected from the left main bronchus. The lung were homogenized and hydrolyzed with 6 N Hel for 12 hours at $110^{\circ}C$ then measured as previously described. The content of hydroxyproline, standardized with a lung protein concentration, reached a peak 4 weeks after RT, and thereafter showed a plateau. AnIn vitro JNK assay using c-$Jun_{1-79}$-GST sepharose beads were performed with the alveolar macrophages obtained from the BAL. JNK activity was not detected prior to RT, However, the JNK activity increased from one week after RT and reached a peak four weeks after RT. Conclusion : JNK may be involved in the pathogenesis because the JNK activity showed similar pattern observed with the hydroxyproine content. However, it is necessary to clarify that the JNK increases the transcription of fibrogenic cyiokines through the transcription factor.

• Journal of the Korean Electrochemical Society
• /
• v.23 no.2
• /
• pp.39-46
• /
• 2020

Composite electrodes for rechargeable batteries generally consist of active material, electric conductor, and polymeric binder. And their composition and distribution within the composite electrode determine the electrochemical activity in the electrochemical systems. However, it is not easy to quantify the physical properties of composite electrodes themselves using conventional experimental analysis tools. So, 3D structural modeling and simulation can be an efficient design tool by looking into the contact areas between particles and electric conductivity within the composite electrode. In this study, while maintaining the composition (LiCoO₂ : Super P Li^® : Polyvinylidene Fluoride (PVdF) = 93 : 3 : 4 by wt%) and loading level (13 mg cm^-2) of the composite electrode, the effects of LiCoO₂ size (10 ㎛ and 20 ㎛) and electrode density (2.8 g cm^-3, 3.0 g cm^-3, 3.2 g cm^-3, 3.5 g cm^-3, 4.0 g cm^-3) on the physical properties are investigated using a GeoDict software. With this tool, the composite electrode can be efficiently designed to optimize the contact area and electric conductivity.

• Journal of Life Science
• /
• v.26 no.5
• /
• pp.545-554
• /
• 2016

Hyaluronic acid (HA) is an important macromolecule in medical and pharmaceutical fields. HA is a natural and linear polymer composed of repeating disaccharide units of β-1, 3-N-acetyl glucosamine and β-1, 4-glucuronic acid. This work aimed to confirm the structural characteristics and anti-inflammatory activities of HA and its chemically sulfated-HA. HA was produced from a fed-batch fermentation process using Streptococcus dysgalactiae in a 5 l bioreactor. HA was isolated water-soluble form (HA-WS) and water-insoluble form (HA-WI) from culture medium, and was obtained chemically sulfated-derivative (S-HA) that resulted in a 90% yield from HA-WI. The structural features of the sulfated- HA (S-HA) were investigated by FT-IR and ¹H-NMR spectroscopy. The FT-IR and NMR patterns revealed the similarity in both the FTIR spectrum as well as NMR spectrum of both reference standard and purified HA from S. dysgalactiae. The anti-inflammatory activities of HA and S-HA were examined on LPS-induced RAW 264.7 cells. S-HA was significantly inhibited production of pro-inflammatory mediators such as nitric oxide (NO) and PGE₂ and the gene levels of iNOS and COX-2, which are responsible for the production of NO and PGE₂, respectively. Furthermore, S-HA also suppressed the overproduction of pro-inflammatory cytokine TNF-α (<80 pg/ml) and IL-6 (<100 pg/ml) compared to that of HA-WI. The present study clearly demonstrates that HA-S exhibits anti-inflammatory activities in RAW 264.7 macrophage cells.

• Microbiology and Biotechnology Letters
• /
• v.39 no.1
• /
• pp.29-36
• /
• 2011

Pseudomonas aeruginosa is an opportunistic pathogen that causes various infections on urinary track, cornea, respiratory track, and burn wound site, and mainly relies on quorum sensing (QS) for its virulence. To control the infectivity of P. aeruginosa, we previously synthesized the structural analogues of a major QS signal, N-3-oxododecanoyl homoserine lactone (3OC12-HSL) to use as a QS inhibitor. Two of them (5b and 5f) had been confirmed to have an inhibitory effect on LasR, a major QS signal receptor of P. aeruginosa in the screening by the recombinant Escherichia coli reporter. To further evaluate these compounds, we tested their efficacy to control the QS and virulence of P. aeruginosa. Unlike the result from E. coli reporter, both 5b and 5f failed to affect the LasR activity in P. aeruginosa, but instead they selectively affected the activity of QscR, another 3OC12-HSL receptor of P. aeruginosa. Interestingly, their effect on QscR was complex and opposite to what we obtained with E. coli system. Both 5b and 5f enhanced the QscR activity at the low concentration range (< 10 ${\mu}m$), but high concentration of 5f (${\approx}$1 mM) strongly inhibited QscR. While 5b and 5f didn't affect the production of proteases, the key virulence factor, they significantly reduced the biofilm formation that is important in mediating chronic infections. Especially, 5f inhibited the initial attachment of P. aeruginosa, rather than the biofilm maturation. Based on our results, we suggest that 5f can be applied for an anti-biofilm agent without increasing virulence of P. aeruginosa.

• Journal of the Korean Crystal Growth and Crystal Technology
• /
• v.23 no.6
• /
• pp.320-324
• /
• 2013

The effects of $CeO_2$ on catalytic activity of $CeO_2-TiO_2$ for the selective catalytic reduction (SCR) of $NO_x$ were investigated in terms of structural, morphological, and physico-chemical analyseis. $CeO_2-TiO_2$ catalysts were synthesized with three different additions, 10, 20, and 30 wt% of $CeO_2$, by the sol-gel method. The XRD peaks of all specimens were assigned to a $TiO_2$ phase (anatase) and the peaks became broader with the addition of $CeO_2$ because it was dispersed as an amorphous phase on the surface of $TiO_2$ particles. The specific surface area of $TiO_2$ increased with the addition of $CeO_2$ from $60.6306m^2/g$ to $116.2791m^2/g$ due to suppression of $TiO_2$ grain growth by $CeO_2$. The 30 wt% $CeO_2-TiO_2$ catalyst, having the strongest catalytic acid sites ($Br{\Phi}nsted$ and Lewis), showed the highest $NO_x$ conversion efficiency of 98 % at $300^{\circ}C$ among the specimens. It was considered that $CeO_2$ contributes to the improvement of the $NO_x$ conversion of $CeO_2-TiO_2$ catalyst by increasing specific surface area and catalytic acid sites.

• Journal of Applied Biological Chemistry
• /
• v.53 no.1
• /
• pp.1-7
• /
• 2010

xylA promoter is a major promoter in xylose operon of Escherichia coli. xylA promoter is sufficient as the promoter for the construction of new expression vector because this promoter was tightly controlled and induced by the addition of xylose. For the construction of xylose-inducible expression vector, 600 bp of xylA promoter was ligated between AatII and HindIII of pUC18, named pXA600. In order to investigate the effect of XylR protein encoded by xylR gene on the xylA promoter, 1,988 bp of xylR gene including its promoter was ligated into downstream of multiple cloning site to the opposite direction of xylA promoter in pXA600, named pXAR600. For the measurement of expression level, 3,048 bp of lacZ structural gene was fused into xylA promoter in both plasmids pXA600 and pXAR600 as a reporter gene, named pXA600-lacZ and pXAR600-lacZ, respectively. The $\beta$-galactosidase activity of pXA600-lacZ and pXAR600-lacZ in E. coli JM109 was determined to be 1,641 and 2,304 unit by the induction with xylose in LB medium, respectively. The $\beta$-galactosidase activity of pXAR600-lacZ/JM109 was about 1.4 times higher by the induction with xylose than that of pXA600-lacZ/JM109. The $\beta$-galactosidase activity of pXA600-lacZ and pXAR600-lacZ in E.coli JM109 showed 6,282 and 9,320 unit by the induction with xylose in DM minimal medium, respectively. A regulator, xylR protein works as an activator for the gene expression by the addition of xylose in the xylose-inducible vectors because the level of gene expression in pXA600 is increased by the insertion of xylR gene into the same vector. The xynA gene of Streptomyces thermocyaneoviolaceus cloned in pXA600 and pXAR600 was successfully expressed in E. coli BLR(DE3). As a result, plasmids pXA600 and pXAR600 using xylA promoter are sufficient as new expression system to produce a foreign protein in E. coli.

• Horticultural Science & Technology
• /
• v.28 no.4
• /
• pp.648-655
• /
• 2010

This study is the first comprehensive report on the molecular cloning, structural characterization, sequence comparison between wild and mutant types, copy number in the genome, expression features and activities of a gene encoding 5-enolpyruvylshikimate-3-phosphate synthase (EPSPS) in Korean lawn grass ($Zoysia$ $japonica$). The full length cDNA of the EPSPS from Korean lawn grass ($zj$EPSPS) obtained from a 3' and 5' RACE method was 1540 bp, containing a 1176 bp ORF, a 144 bp leader sequence (5' UTR) and a 220 bp 3' UTR, which was eventually decoded 391 amino acid residues with a molecular mass of 41.74 kDa. The Southern blot detection of the $zj$EPSPS showed that the gene exists as a single copy in the Korean lawn grass genome. Sequence comparison of the $zj$EPSPS gene demonstrated that the glyphosate-tolerant mutant (GT) having a Pro-53 to Ser substitution in the gene seems to have a preferred binding activity of the enzyme to phosphoenol pyruvate(PEP) over glyphosate, which allows the continuous synthesis of aromatic amino acids in the shikimate pathway. From the Northern blotting analysis, the $zj$EPSPS was found to be highly expressed, with continuous increase until 36 hours after 0.5% glyphosate treatment in both wild and mutant samples, but 1.5-fold higher EPSP synthase activity was observed in the tolerant mutant when exposed to the glyphosate treatment. The molecular information of the $zj$EPSPS gene obtained from this study needs to be further dissected to be more effectively applied to the development of gene-specific DNA markers and zoysiagrass cultivars; nevertheless, the glyphosate-tolerant mutant having the featured $zj$EPSPS gene can be provided to turfgrass managers for weed problems with timely adoptable management options.

• Korean Journal of Food Science and Technology
• /
• v.17 no.2
• /
• pp.121-127
• /
• 1985

In studying the structural work on ciguatoxin, parrot fish collected were identified as Scarus sordidus, S. frenatus, S. scaber and S. pectarlis, in which only S. sordidus contained toxic materials. Crude toxins obtained by silicic acid column chromatography, could be separated on a DEAE-cellulose column into two fractions, ST-1(less polar) and ST-2(polar) eluted with chloroform and chloroform-methanol(1:1). Furthermore ST-1 could be changed into ST-2 by repeated chromatography on DEAE-cellulose. Rf values of ST-1 and ST-2 were 0.60-0.75 and 0.30-0.54 on TLC coated with silica gel 60F-254 developed by chloroform-methanol-water-acetic acid (90:9.5:0.2:0.3) mixture. The peaks of ST-1 and ST-2 were not observed on each HPLC chromatogram at low sensitivity(2X), but by bioassay they were detected in the fraction of 24-27ml(less polar toxin, 120ng) and 22-27 ml (polar toxin, 150 ng). Less polar ciguatoxin from morey eel viscera also showed its peak in the same elution volume(25ml). Being subjected to chromatography on basic aluminum oxide (activity grade I) or to alkaline treatment, followed by basic aluminum oxide (activity grade I) chromatography ST-1 toxin was remarkably converted into the polar toxic component supposed to be polar ciguatoxin in both cases. In the latter case, approximately 74% of the residual toxicity was changed into the polar component, accompanied by about 50% loss of the initial toxicity. More than 26% of ST-2 toxicity was transformed into the less polar toxic component supposed to be less polar ciguatoxin on a deactivated aluminum oxide (activity grade V) column.