• 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.

• Journal of Life Science
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• v.26 no.11
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• pp.1225-1231
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• 2016

In this study, our investigated the antioxidant activities and compared other bioassay including anti-microbial, antifungal activities and total polyphenol contents of functional healthy drinks from some medicinal herbs and coffee mixture. The kind of medicinal herbs, chaga mushroom (Inonatus obliqurs), moringa (Moringa Oleifera), gravila (Anona muricata), mulberry (Morus alba), Dioscoreaceae (Dioscorea quinquelaba), Berberidaceae (Epimedii Herba), Asteraceae (Artemisia capillaries) and siberian ginseng (Acanthopanax senticous,). The functional healthy drinks, named C1, C2, C3, C4, C5, C6 and C7 were summered in Table 1. The in vitro antimicrobial activity was examined against Gram positive bacteria, Gram negative bacteria and a fungus. The functional healthy drinks were broad spectrum of anti-microbial activity without antifungal activity against Candida albicans KCTC7965. In particularly, the C7 showed strong activity against Methicillin Resistant Staphylococcus aureus CCARM3089, CCARM 3115 and CCARM3561. And, the C7 showed 88% of free radical scavenging effect on 0.5 mg/ml using 1,1-diphenyl-2-picrylhydrazyl (DPPH) method. Functional healthy drink C7 was mulberry extracts from Morus alba, chaga mushroom from Inonatus obliqurs and moringa from Moringa olifera in additionally coffee extracts. Its results confirm that the potential use of mulberry extracts as a good source of antibacterial compounds or as a health promoting food and health drinks.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.18 no.1
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• pp.42-63
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• 1992

In order to investigate the effect of nonionic surfactants on the antimicrobial activity of preservatives in the presence and absence of p.0.E(20) Sorbitan fatty acid ester commonly used in cosmetics and pharmaceutical systems, these experiments were carried out by determining Minimum Inhibitory Concentration(MIC) values and MIC values of adaptation against test organisms. And also the inactivation of the preservative against each microorganism in formula added with various concentrations of P.0.E(20) Sorbitan monostearate were measured by use of a preservative death time curve The results obtained were as fort low : 1) Nonionic surfactant inactivated Methylparaben to varying extents, but not Imidazolidinyl urea. 2) A combined preservative system was inactivated to a little extent (range of 0.16-0.20% Conc.), no adaptation was observed for the 5. aureus ATCC 6538. Imidazolidinyl urea complex combined with Methylparaben had a broad antibacterial spectrum against the Gram(.) and the Gram(-) bacteria It was found that preservatives had a synergistic effect by use of mixed form of preservatives, 3) In formula preserved with 0.2% Methylparaben containing 0.5, 1.0 and 2.0% P.0.E(20) Sorbitan monostearate, E. coli ATCC 10s36 and P. aeruginosa NCTC 10490 died quickly within in 2hr 4) However, from Fig.5, S. aereus ATCC 6538 died more slowly within increasing surfactant concentration and the D-values(Decimal reduction time) were 5.2, 8 and 14 hr. for samples containing 0.5, 1 0 and 2.0% P 0. E(20) Sorbitan monostearate, respectively. 5) In the case of Methylparaben, no adaptation for the E. coli ATCC 10536 6) All of the nonionic surfactant, p.0. E(20) Sorbitan fatty acid ester used in the experiments decreased the effectiveness of Methylparaben, but not of Imidazolidinyl urea.

• Microbiology and Biotechnology Letters
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• v.38 no.3
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• pp.255-262
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• 2010

Strain BCNU 2001 was isolated from soil samples collected from Tea-baek Mountain area. The biochemical characteristics and 16S ribosomal RNA gene sequences of the isolate revealed that the strain belonged to the Pseudomonas aeruginosa. The supernatants had an antimicrobial effect on various kind of bacteria and fungi. Especially BCNU 2001 was able to greatly inhibit the growth of Micrococcus luteus, Proteus mirabilis, Proteus vulgaris, and Aspergillus niger, and its inhibition zone was measured as 18.5 mm against Micrococcus luteus, 19.0mm against Proteus mirabilis, 17.0mm against Proteus vulgaris, and 13.5 mm against Aspergillus niger, respectively. Hexane and dichloromethane extracts of BCNU 2001 exhibited significant activity against bacteria, and dichloromethane and ethylacetate extracts showed significant activity against fungi. Pseudomonas strain BCNU 2001 was also determined to have antimicrobial peptide against various microorganisms including Gram positive bacteria, Gram negative bacteria and fungi. The obtained results may provide preliminary support for the usefulness of Pseudomonas strain BCNU 2001.

• Journal of Pharmaceutical Investigation
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• v.32 no.3
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• pp.215-221
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• 2002

Cephradine is a first generation cephalosporin and has broad spectrum antibacterial activity against gram-positive and gram-negative microorganisms, through inhibition of bacterial cell wall synthesis. Cephradine is useful for treatment of infections of the urinary and respiratory tract, skin and soft tissues. The purpose of the present study was to evaluate the bioequivalence of two cephradine capsules, Cefradine Yuhan (YuHan Corporation) and Broadcef (Ilsung Pharmaceuticals Co. Ltd.), according to the guidelines of Korea Food and Drug Administration (KFDA). The cephradine release from the two cephradine capsules in vitro was tested using KP VII Apparatus II method with various different kinds of dissolution media (pH 1.2, 4.0, 6.8 buffer solution and water). Twenty normal male volunteers, $23.10{\pm}2.90$ years in age and $67.69{\pm}8.04\;kg$ in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After one capsule containing 500 mg as cephradine was orally administered, blood was taken at predetermined time intervals and the concentrations of cephradine in serum were determined using HPLC method with UV detector. The dissolution profiles of two cephradine capsules were very similar at all dissolution media. Besides, the pharmacokinetic parameters such as $AVC_t,\;C_{max}\;and\;T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed $AVC_t\;and\;C_{max}$ and untransformed $T_{max}$. The results showed that the differences in $AVC_t,\;C_{max}\;and\;T_{max}$ between two capsules based on the Cefradine Yuhan were -2.87%, -0.96% and -4.85%, respectively. There were no sequence effects between two capsules in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of 1og(0.8) to log(1.25) $(e.g.,\;log(0.93){\sim}log(1.02)\;and\;log(0.88){\sim}log(1.13)\;for \;AVC_t\;and\;C_{max},\;respectively)$. The 90% confidence interval using untransformed data was within ${\pm}20%$ $(e.g., \;-17.54{\sim}7.78\;for\;T_{max})$. All parameters met the criteria of KFDA guideline for bioequivalence, indicating that Broadcef capsule is bioequivalent to Cefradine Yuhan capsule.

• Microbiology and Biotechnology Letters
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• v.42 no.4
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• pp.317-323
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• 2014

Violacein has received much attention due to its various important biological activities, including broad-spectrum antibacterial and antifungal activity, anti-malarial, anti-tumoral, anti-oxidant, and anti-diarrheal activities. EP15224 strain isolated from forest soils in Korea was found to be a new species belonged to the genus Massilia based on its 16S ribosomal DNA sequences. The 16S ribosomal DNA of strain EP15224 displayed 97% homology with Massilia sp. BS-1, the nearest violacein-producing bacterium. Strain EP15224 produced bluish-purple pigment well in a synthetic MM2 medium containing glucose, $(NH_4)_2SO_4$, $Na_2HPO_4{\cdot}7H_2O$, $KH_2PO_4$, $MgSO_4{\cdot}7H_2O$, and 1 mM $\small{L}$-tryptophan. The chemical analysis of the pigment by LC/MS/MS showed that it is violacein with molecular weight of 343.34. This is the second report on the production of violacein by a Massilia species. In this study, the optimal culture conditions for violacein production were established under which 280 mg/l crude violacein was produced : glucose 2 g/l, $(NH_4)_2SO_4$ 1 g/l, $Na_2HPO_4{\cdot}7H_2O$ 2 g/l, $KH_2PO_4$ 1 g/l, $MgSO_4{\cdot}7H_2O$ 0.1 g/l, L-tryptophan 0.24 g/l, 25 ml medium in a 250 ml flask, with an inoculumn size of 10% (v/v), 72 h of cultivation with 250 rpm at $25^{\circ}C$.