• YAKHAK HOEJI
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• v.37 no.6
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• pp.638-646
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• 1993

A cepfialosporin with an aminothiazoiylmethoxyimino-type side chain at the 7 position and bicyclic quinolone dithicarbamate at the 3' position was synthesized. It has broad and potent antivacterial activity in vitro. The antibacterial spectrum reflects contributions of both the cephalosporin moiety and the quinolone moiety. Thus, this compound was named DACD implying a dualaction cephalosporin derivative. In this paper, the physicochemical proper-ties (lipid-water partition, pKa), stability and pharmacokinetics of DACD were determined and compared with cefotaxime 3'-norfloxacin dithiocarbamate (CENO). Stability tests were studied in pH 1.20, 6.80 and 8.00 buffers and in the presence of AB type human plasma, rat liver homogenate and its .betha.-lactamase. The pharmacokinetic parameters of DACD were evaluated in mice after a single intravenous dose of 40 mg/kg. The results are as follows. The lipid-water partition coefficient of DACD was higher than that of CENO. The calculated pKa values of CENO and DACD, were 6.82$\pm$0.03, 7.53$\pm$0.21, respectively. In the hydrolysis test, half-lives (t$^{1/2}$) of CENO and DACD was 66.0 hr and 80.0 hr in pH 6.80 buffer, 190 hr and 91.4 hr in pH 8.00 buffer. CENO and DACD were rapidly hydrolyzed in human plasma and in rat liver hornogenate. Half-lives (t$_{1/2}$ of CENO and DACD were 1.29 hr and 1.15 hr in hyman plasma, 0.62 hr and 0.71 hr rat liver homogenate. In $\beta$-lactamase stability test, CENO and DACD were very stable to the .betha.-lactamases obtained from three different strains. Half-life (t$_{1/2}$) and areas under the curve (AUC) in mice were 2.33 hr and 15.97 (mg.h/1), respectively.

• Korean Journal of Microbiology
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• v.54 no.3
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• pp.175-187
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• 2018

Myxobacteria produce diverse secondary metabolites for predation, self-defense, intercellular signaling, and other unknown functions. Many secondary metabolites isolated from myxobacteria show pharmaceutically useful bioactivity such as anticancer, antibacterial, and antifungal activities with a unique mechanism of action. Therefore, a large number of myxobacterial strains have been isolated globally and many bioactive compounds have been purified from them. However, 16S rRNA database analysis indicates that there are far more types of myxobacterial species in the wild than have ever been isolated, and genome sequence analysis suggests that each myxobacterium is capable of producing much more metabolites than already known. In this article, the current status of studies on the secondary metabolites from myxobacteria, their biosynthetic genes, biological functions, and transcriptional regulatory factors governing gene expression were reviewed.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.28 no.1
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• pp.99-115
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• 2002

Tests of stability and toxicity, and clinical evaluation of anti-acne activity suggest that cryptotanshinone, a constituent of the roots of Salvia miltiorrhiza Bunge, is an effective active ingredient for acne vulgaris treatments. Acne vulgaris, called acne or pimples, is the most common disease of the pilosebaceous follicle unit of the skin. It affects nearly 80% of people between the ages of 11 and 30. Approximately 30% of teenagers have acne of sufficient severity to require medical treatment. Acne is a follicular disorder of the skin. It occurs in specialized pilosebaceous units on the face and body. Acne develops when these specialized follicles undergo pathologic alterations that result in the formation of non-inflammatory lesions (comedones) and inflammatory lesions (papules, pustules and nodules). An abnormality of keratinizing epithelium of these follicles, thought to be due to the action of sebum synthesized and secreted by the androgen-sensitive sebaceous glands, leads to inflammation induced by the follicular bacterium Propionibacterium acnes. Therapy involves treatments that modify these pathogenic factors and includes drugs with antikeratinizing, antibacterial and antiseborrheic actions. Acne vulgaris is a very frequent disease, seen primarily in adolescents, involving the sebaceous follicles. Acne vulgaris is characterized by a great variety of clinical inflammatory and non-inflammatory lesions: comedones, papules, pustules, nodules, cysts and scars. Acne vulgaris is a multi-factorial disease. Although its pathogenicity is unclear, extensive studies have shown that hyperseborrhea, superinfection by P. acnes and endocrinologic androgenic changes play a role in the development of acne vulgaris.

• Analytical Science and Technology
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• v.32 no.4
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• pp.147-154
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• 2019

Ampicillin and Sulbactam (2:1, w/w) are combined in formulation to provide broader antibacterial action in treatment of many infections. The development of analytical method for simultaneouly determine these two compounds was difficult because of the differences in their chemical structures and ratio in the formulation. Current published methods still have some limitations. In this study, we developed an alternative high-performance liquid chromatography (HPLC) assay method for simultaneously determination of ampicillin sodium and sulbactam sodium in powder for injection. Method validation of HPLC method was conducted to determine linearity, precision, accuracy, system suitability, robustness. The linearity of the calibration curves in the desired concentration range was good ($r^2$> 0.9994). RSDs of intra-day and inter-day precision obtained were less than 2.00 %. Accuracy was obtained with the recoveries in range of 98.42 % and 101.36 %. As a result of system suitability, RSD of both retention time and the peak area obtained were not more than 1.0 %. The values of plate number were more than 7000 and symmetric factors obtained were 0.8. As intermediate-precision and robustness of the developed assay, it could be expected to become valuable tools for revising the Korean Pharmacopoeia (KP XI).

• Journal of Microbiology and Biotechnology
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• v.31 no.1
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• pp.25-32
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• 2021

Inflammatory reactions activated by lipopolysaccharide (LPS) of gram-negative bacteria can lead to severe septic shock. With the recent emergence of multidrug-resistant gram-negative bacteria and a lack of efficient ways to treat resulting infections, there is a need to develop novel anti-endotoxin agents. Antimicrobial peptides have been noticed as potential therapeutic molecules for bacterial infection and as candidates for new antibiotic drugs. We previously designed the 9-meric antimicrobial peptide Pro9-3 and it showed high antimicrobial activity against gram-negative bacteria. Here, to further examine its potency as an anti-endotoxin agent, we examined the anti-endotoxin activities of Pro9-3 and elucidated its mechanism of action. We performed a dye-leakage experiment and BODIPY-TR cadaverine and limulus amebocyte lysate assays for Pro9-3 as well as its lysine-substituted analogue and their enantiomers. The results confirmed that Pro9-3 targets the bacterial membrane and the arginine residues play key roles in its antimicrobial activity. Pro9-3 showed excellent LPS-neutralizing activity and LPS-binding properties, which were superior to those of other peptides. Saturation transfer difference-nuclear magnetic resonance experiments to explore the interaction between LPS and Pro9-3 revealed that Trp3 and Tlr7 in Pro9-3 are critical for attracting Pro9-3 to the LPS in the gram-negative bacterial membrane. Moreover, the anti-septic effect of Pro9-3 in vivo was investigated using an LPS-induced endotoxemia mouse model, demonstrating its dual activities: antibacterial activity against gram-negative bacteria and immunosuppressive effect preventing LPS-induced endotoxemia. Collectively, these results confirmed the therapeutic potential of Pro9-3 against infection of gram-negative bacteria.

• Journal of the FoodService Safety
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• v.2 no.1
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• pp.44-50
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• 2021

Physicochemical and antioxidant properties of the three different calorie types of HMR curry rice using fermented turmeric were analyzed in this study. The general tumeric added sample groups showed significantly higher carbohydrate content than the fermented turmeric sample group. In all sample groups, the ratio of protein, fat, and carbohydrate was found to be appropriate according to the nutritional composition ratio as one meal recommended by the Ministry of Health and Welfare. The brightness L value of the general turmeric-added sample group was measured to be significantly brighter than the fermented turmeric-added sample group. The fermented turmeric sample group showed a slightly lower pH value than the general sample group due to organic acids generated during fermentation. As a result of analyzing the radical scavenging activity of ABTS, LFTC, MFTC, and HFTC of the fermented turmeric group were 40.20, 40.46, and 36.16%, respectively, compared to those 32.41, 37.75, and 36.16% of LNTC, MNTC and FNTC of the general sample groups, respectively, consistently indicating that more free radicals were generated in the fermented sample group (p<0.01). Relatively unstable to heat and acid, DPPH scavenged radicals showed similar results to those of ABTS radical scavenging activity in terms of activity. Similar results were also shown in the measurement of total flavonoid and phenol content, which are known to have antioxidant antiviral and anticancer effects. Thus we could conclude that pilot products of the high quality varied calorie levels of HMR Bibimbap set with tumeric, which is helpful for antioxidant action have been developed to meet various customer needs.

• The Korean Journal of Food And Nutrition
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• v.17 no.3
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• pp.237-245
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• 2004

The physicochemical and physiological activities of domestic garlic from 3 different areas (Namhae, Jeju and Uiseong) were analyzed. The contents of moisture, ash, crude protein and crude fiber in garlic were little different in 3 kinds of area. Total sugar and water soluble phenolic compounds were higher in garlic from Namhae. The free sugars found in garlic were fructose, sucrose and lactose. Five kinds of organic acids were determined. Malonic acid and citric acid contents in garlic from Namhae were 23.7${\pm}$1.16 mg% and 22.1${\pm}$0.82 mg%, respectively. Total mineral content of garlic samples were in a range of 7112.6～9067.3 mg%, the potassium content showed the highest concentration (4117.3${\pm}$7.19～5175.3${\pm}$9.61 mg%). The electron donating abilities in 0.2% of garlic from Namhae and Uiseong showed 46.2${\pm}$1.25% and 37.0${\pm}$1.l6%, respectively. The nitrite scavenging effect was measured at different conditions (pH 1.2 and 4.2). The nitrite scavenging effects were higher at pH 1.2, and reached more than 95% by adding 0.2% and 0.1 % of garlic juice at pH 1.2. Addition 0.02～0.001 % garlic juice in showed the SOD-like activities. Its activity of garlic from Namhae. was a range of 6.0${\pm}$0.37～14.4～0.69%. It was found that 0.2% and 0.1% garlic showed strong antimicrobial action against growth of all the tested bacteria. Antimicrobial action. was showed 74.7${\pm}$0.70% and 51.7${\pm}$1.l1% on Sal. typhimurium in 0.2% of garlic from Namhae and Uiseong and 28.6${\pm}$0.90% on B. subtilis in garlic from Jeju.

• Journal of Life Science
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• v.31 no.5
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• pp.475-480
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• 2021

Interest in edible insects such as Protaetia brevitarsis has increased rapidly, and several insect producers use these insects in industrialized mass production. However, mass rearing of insects can cause insect diseases. Sprouted barley is a valuable source of nutrients and has antioxidant, antimicrobial, anti-inflammatory, and anti-cancer effects. This study was conducted to investigate the effect of sprouted barley as a feed additive for producing healthy P. brevitarsis larvae. P. brevitarsis larvae were fed feeds with or without sprouted barley, and their body weight and larval period wewe checked weekly. To confirm the antibacterial effects of sprouted barley, in vitro bioassays were performed by counting Serratia marcescens colonies, and in vivo bioassays were performed by determining the survival rate and body weights of the S. marcescens-infected larvae. Larvae fed different feeds were analyzed for their nutrient compositions (i.e., such as proximate composition, minerals, amino acids, and heavy metals). Larvae fed 5% and 10% sprouted barley had maximum weight increases of 19.2% and 23.1%, respectively. Both treatment groups had significantly shorter larval periods than those of the control group. Sprouted barley markedly inhibited the growth of entomopathogenic S. marcescens. Furthermore, larvae fed sprouted barley exhibited higher Cu, Zn, and K levels. Seventeen amino acids were present in larvae fed sprouted barley, of which, tyrosine and glutamic acid were predominant. No heavy metals were detected in any of the investigated groups. Therefore, sprouted barley may be a suitable feed additive for producing high-quality P. brevitarsis larvae.

• Horticultural Science & Technology
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• v.34 no.2
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• pp.331-341
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• 2016

We analyzed the functional fragrant components of three species of Cymbidium oriental orchids using gas chromatography-mass spectrometry (GC/MS). For the comparative analysis, C. goeringii 'Minchunran', 'Jugeumhwa', C. forrestii 'Chwigae', 'Songmae', 'Yongja', and C. faberi 'Choemae', 'Namyangmae', 'Hwaja' were investigated. Major fragrant components detected by GC/MS were selected on the basis of more than 3% value according to the analysis of peak area (%). We found that ${\alpha}$-bergamotene, which has a cytotoxic effect on breast cancer, cervical cancer, and glioblastoma, and nerolidol, which induces apoptosis of human hepatoma cells (HepG2), inhibits the growth of Streptococcus mutans and babesiosis, and has antibacterial properties, are common substances produced by C. goeringii L. Nerolidol and ${\beta}$-bisabolene, which is cytotoxic and suppresses the growth of malignant melanoma cells (B16-F10), HepG2, and leukemia cells (HL-60, K562), are major substances in C. forrestii R. Furthermore, ${\alpha}$-pinene, which inhibits the growth of gliobastoma cells (SF-767) and inhibits the anti-inflammatory action of hepatoma cells (BEL-7402); 1,8-cineole, which is a potential therapeutic agent for the treatment of gastric ulcers; and 1,3,7-octatriene, which functions as a pheromone, are the most common substances in C. faveri R. Thus, substances identified as major fragrant components in oriental orchid species have multiple beneficial applications in human health. This research forms the basis for further studies of the roles of major fragrant components in oriental orchids.

• Korean Journal of Microbiology
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• v.49 no.3
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• pp.245-252
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• 2013

Pseudomonas aeruginosa and Acinetobacter baumannii are significant opportunistic pathogens in hospitals and are resistant to most antibiotics. Multidrug-resistant P. aeruginosa (MDRPA) and A. baumannii (MDRAB) cause severe human nosocomial infections and are more difficult to treat than methicillin-resistant Staphylococcus aureus (MRSA). Bifidobacteria are among of the most beneficial probiotics and have been widely studied for their antimicrobial activities. The present study explored the antimicrobial activity of Bifidobacterium sp. isolated from healthy Koreans against MDRPA and MDRAB. The antimicrobial activity of the isolates against MDRPA and MDRAB, which are resistant to ciprofloxacin, tobramycin, gentamicin, meropenem, and ceftazidime, was determined by modified broth microdilution methods using absorbance. Among all tested bifidobacteria isolates (nine B. adolescentis, three B. longum, and two B. pseudocatenulatum), the culture supernatant of B. pseudocatenulatum SPM1309 showed a strong growth inhibitory effect against MDRPA and MDRAB. No change in the turbidity of the mixture was observed during incubation, and its inhibitory effect occurred through bacteriostastic action. Moreover, the antibacterial activity was observed in the fraction with molecular weights <10 kDa of bifidobacteria culture supernatant, and the active fraction was heat-stable because it maintained its activity when heated at $70^{\circ}C$ for 10 min. The results suggest that this Bifidobacterium strain could have potential applications for alternative therapy in MDRPA and MDRAB infections.