• Archives of Pharmacal Research
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• v.27 no.2
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• pp.265-272
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• 2004

The pharmacokinetics of CKD-732 (6-0-4-[dimethyl-aminoethoxy)cinnamoyl]-fumagillolㆍhemioxalate) was investigated in male SD rats and beagle dogs after bolus intravenous administration. The parent compound and metabolites obtained from in vitro and in vivo samples were determined by LC/MS. The main metabolite was isolated and identified as an N-oxide form of CKD-732 by NMR and LC/MS/MS. CKD-732 was metabolized into either M11 or others by rapid hydroxylation, demethylation, and hydrolysis. The blood level following the intravenous route declined in first-order kinetics with $T_{1}$2/$\beta$ values of 0.72-0.78 h for CKD-732 and 0.92-1.09 h for M11 in rats at a dose of 7.5-30 mg/kg. In dogs, $T_{1}$2/$\beta$ values of CKD-732 and M11 were 1.54 and 1.79 h, respectively. Moreover, AUC values increased dose dependently for CKD-732 and M11 in rats and dogs. The CLtot and Vdss did not change significantly with increasing dose, indicating linear pharmacokinetic patterns. The excretion patterns through the urine, bile, and feces were also examined in the animals. The total amount excreted in urine, bile, and feces was 2.13% for CKD-732 and 1.29% for M11 in rats, and 1.58% for CKD-732 and 2.28% for M11 in dogs.

• Horticultural Science & Technology
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• v.33 no.2
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• pp.186-195
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• 2015

This research was conducted to investigate effect the plant growth regulators (PGRs) on the characteristics of fruit and flesh softening, using GA3 and thidiazuron (TDZ) treatments in 'Heukboseok' grapes. The total yield obtained under PGR treatment was 88.3% lower than the target production when a single treatment with $GA_3$ of low concentrations was used, but the expected yield was recovered by combined treatment with TDZ and $GA_3$. When harvested on the basis of color, the harvest rate up to 100 days after full bloom (DAFB) was low with the $GA_3$ single treatment, but was increased by the addition of TDZ, with the second TDZ mixed treatment being particularly effective. The soluble solids content in the PGR-treated samples demonstrated no significant changes after 90 DAFB, while the acidity content decreased rapidly starting from 90 DAFB. Measured on the basis of sugar and acidity content, maturity was reached much earlier in treated fruit than in the non-treated fruit. Firmness was maintained at a higher level until the final harvest time after PGR treatment compared to untreated grapes according to epidermis thickness and flesh density increase to activity cell division and expansion by $GA_3$ and TDZ. In particular, the fruit quality was improved based on the delay of softening in primary and secondary treatments of $25mg{\cdot}L^{-1}\;GA_3+2.5mg{\cdot}L^{-1}$ TDZ. The production of seedless fruit was difficult, even with the inclusion of TDZ, reaching the highest seedless rate of only 65.5%. Fruit cracking was rare, occurring at a rate of about 0.0~0.9% in all treatments. Accordingly, 'Heukboseok' grapes should be harvested within 100 days after full bloom (DBFB) before a rapid decrease of firmness, conferred by primary and secondary treatments with $25mg{\cdot}L^{-1}\;GA_3+2.5mg{\cdot}L^{-1}$ TDZ.

• Food Science and Preservation
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• v.14 no.2
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• pp.148-153
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• 2007

The chemical components of flesh persimmon flowers (petal and calyx), and the qualify of hot-water extracts (teas) prepared from powders of these flower parts, were investigated In flesh petal and calyx, the contents of moisture, crude protein, crude lipid, and carbohydrate were 84.8% 0.4% 0.3% and 13.7% respectively. The values were not significantly different when the two tissues were compared. In petal and calyx respectively, the crude ash values were 0.5% and 1.1% of flesh weights, the vitamin C content were 192.3mg% and 392.7ng%, the flavonoid levels were 98.4 mg% and 355.2mg% and the carotenoid content were 0.8mg% and 3.8mg%. Hot air and freeze drying methods applied to petals, prior to powder preparation, did not affect the levels of soluble solids or soluble annins. Extract from calyx had higher L values, higher ${-\alpha}$ values, more soluble tannins, greater 1,1-diphenyl-2-picrylhy-drazylradical-scavenging activities, me lower pH values, than did exracts from petal. Fructose and glucose were higher in petal extract than in calyx extract, but sucrose was higher in calyx extracts. Extract of freeze-dried powdered petals had significantly higher free sugar levels than did exracts from petals dried with hot air. The major organic acids in extracts were citric acid, oxalic acid, and malic acid. The levels of organic acids were inversely related to free sugar levels in all flower parts and after all drying methods tested. Sensory tests of aroma, taste and overall acceptability yielded scores above medium for all teas, regardless of the flower part powdered, or the drying method used. The results show that the petal and calyx of persimmon may be used to make tea and perhaps other foods.

• Korean Journal of Veterinary Research
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• v.48 no.4
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• pp.385-391
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• 2008

This study was performed to examine the effect of 2,3',4,4',5-pentachlorobiphenyl (PCB#118) on testis of male rats. PCB#118 (20 mg/kg/week) in corn oil was intraperitoneally injected to adult male rats for 2, 5, 8 weeks. The body and testicular weights were measured at 3, 6, 9 weeks of PCB treatment. The morphological changes in the rat testes were then analyzed by light microscopy (LM) and transmission electron microscopy (TEM). The results showed that PCB#118 caused significant change in the body weights and testicular weights. Moreover, the morphological studies that were conducted on the PCB-treated rats revealed that the number of spermatocytes and spermatids in their seminiferous tubules decreased than control group (LM). The nuclear membrane was damaged when PCB was administered to them for 9 weeks (TEM). These results suggest that the reproductive function of the adult male rats is sensitive to PCB#118, and that may affect the testicular morphology of adult male rats.

• BMB Reports
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• v.33 no.2
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• pp.166-171
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• 2000

Thioredoxin is a multifunctional protein that is ubiquitous in microorganisms, animals and plants. Previously, the expression of the Escherichia coli thioredoxin gene (trxA) was found to be negatively regulated by cAMP. In the present study, the effect of temperature on the expression of the E. coli trxA gene was investigated. In order to examine the temperature effect, the fusion plasmid pCL70 that harbors the E. coli trxA P1P2 promoter was used. The other two fusion plasmids, pJH3 and pMH521 that were constructed in different vectors which harbor the E. coli trxA P2 promoter, were also used. When the E. coli strain MC1061/pCL70 was grown in a rich medium at $25^{\circ}C$, $34^{\circ}C$ and $42^{\circ}C$, the cells grown at $42^{\circ}C$ gave the highest $\beta$-galactosidase activity. The E. coli MC1061/pJH3 and MC1061/pMG521 cells showed increased $\beta$-galactosidase activity after the shift of the culture temperature to $42^{\circ}C$. The wild-type trxA gene of the E. coli MC1061 cells produced much higher thioredoxin activity at the higher temperature. These results support the conclusion that the E. coli trxA gene is regulated in a temperature-dependent manner. Especially the expression from its P2 promoter appeared to be sensitive to temperature.

• Biomolecules & Therapeutics
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• v.11 no.3
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• pp.178-182
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• 2003

The clinical use of once daily aminoglycoside (ODA) dosing has been increased because of the potential therapeutic advantages of this dosing regimen. To evaluate the optimal sampling times of ODA dosing method in a clinical setting, the study was prospectively conducted in a total of 28 patients with UTI. All of the patients were intravenously administered gentamicin at a dose of 7 mg/kg over 60 minutes and randomly divided into two groups. Blood was collected at 0, 2, and 6 hours in Group A and at 1, 2, and 6 hours in Group B after the end of 1-hour infusion. The pharmacokinetic parameters (Ke, Vd and Cmax) obtained using the 0, 6 hour levels and 2, 6 hour levels in Group A were statistically different while those of 1, 6 hour levels and 2, 6 hour levels in Group B were similar. This finding indicated that the distributional phase of ODA is completed within 1 hour following the end of the I-hour infusion. If we are allowed to collect only two blood samples in ODA considering patients comfort and the analytical cost of drug, the first one should be drawn after 1 hour following the end of infusion to obtain adequate pharmacokinetic information.

• Journal of Periodontal and Implant Science
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• v.38 no.sup2
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• pp.273-298
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• 2008

Purpose: The aim of this review is to introduce a novel bone-graft material for hard-tissue regeneration based on the calcium phosphate glass(CPG). Materials and Methods: CPG was synthesized by melting and subsequent quenching process in the system of CaO-$CaF_2-P_2O_5$-MgO-ZnO having a much lower Ca/P ratio than that of conventional calcium phosphates such as HA or TCP. The biodegradability and bioactivity were performed. Effects on the proliferation, calcification and mineralization of osteoblast-like cells were examined in vitro. Influence in new bone and cementum formations was investigated in vivo using calvarial defects of Sprague-Dawley rats as well as 1-wall intrabony defect of beagle dogs. The application to the tissue-engineered macroporous scaffold and in vitro and in vivo tests was explored. Results: The extent of dissolution decreased with increasing Ca/P ratio. Exposure to either simulated body fluid or fetal bovine serum caused precipitation on the surface. The calcification and mineralization of osteoblast-like cells were enhanced by CPG. CPG promoted new bone and cementum formation in the calvarial defect of Sprague-Dawley rats after 8 weeks. The macroporous scaffolds can be fabricated with $500{\sim}800{\mu}m$ of pore size and a three-dimensionally interconnected open pore system. The stem cells were seeded continuously proliferated in CPG scaffold. Extracellular matrix and the osteocalcin were observed at the $2^{nd}$ days and $4^{th}$ week. A significant difference in new bone and cementum formations was observed in vivo (p<0.05). Conclusion: The novel calcium phosphate glass may play an integral role as potential biomaterial for regeneration of new bone and cementum.

• Journal of Periodontal and Implant Science
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• v.38 no.sup2
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• pp.343-354
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• 2008

Purpose: Aggregatibacter actinomycetemcomitans is associated with localized aggressive periodontitis. It produces cytolethal distending toxin (CDT), which induces cell cycle arrest in the G2/M phase. The CDT holotoxin is composed of CdtA, CdtB, and CdtC. CdtB has structural homology to human DNase I and is an active component of the CDT complex acting as a DNase. In particular, the pattern homology seen in the CdtB subunit has been associated with specific DNase I residues involved in enzyme catalysis, DNA binding, and metal ion binding. So, to study the functions and regulation of recombinant CdtB, we made up a quantity of functional recombinant CdtB and tested it in relation to the metal ion effect. Materials and Methods: We constructed the pET28a-cdtB plasmid from A. actinomycetemcomitans Y4 by genomic DNA PCR and expressed it in the BL21 (DE3) Escherichia coli system. We obtained the functional recombinant CdtB by the refolding system using the dialysis method and then analyzed the DNase activity and investigated the metal ion effect from plasmid digestion. Results: The recombinant CdtB subunit was expressed as the inclusion bodies. We were able to obtain functional recombinant CdtB subunit using refolding system. We confirmed that our refolded recombinant CdtB had DNase activity and was influenced by the metal ions $Mg^{2+}$ and $Ca^{2+}$. Conclusion: We suggest that the factors influencing recombinant CdtB may contribute to CDT associated diseases, such as periodontitis, endocarditic, meningitis, and osteomyelitis.

• Journal of Plant Biotechnology
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• v.49 no.3
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• pp.250-256
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• 2022

This study was conducted to measure changes in polyphenol components and antioxidant effects of Cirsium Lineare (Thunb.) after fermentation by lactic acid bacteria. First, Cirsium Lineare (Thunb.) extract (CE, unfermented) and Cirsium Lineare (Thunb.) extract fermented with Lactobacillus paracasei (FCE) were prepared. Changes in components resulting from fermentation were confirmed through changes in polyphenol compound content and silymarin derivative pattern, and antioxidant activity was confirmed using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity, 2,2'azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) radical scavenging activity, and ferric reducing antioxidant power (FRAP) analyses. As a result, polyphenol contents of CE and FCE were confirmed as 21.94 ± 1.15 and 67.90 ± 4.48 mg GAE/g, respectively. Both values were increased approximately three times by fermentation, and there was also a change in the silymarin derivative pattern. In the case of DPPH radical RC₅₀ values in particular, CE and FCE were confirmed to inhibit DPPH radicals by 50% at concentrations of 129.44 ± 5.85 and 50.00 ± 3.47 ㎍/mL, respectively, with the FCE value approximately 2.5 times lower than that of CE. In addition, ABTS radical scavenging and FRAP activity were confirmed to share similar trends as DPPH radical scavenging activity. When CE and FCE were compared, FCE showed a better antioxidant effect overall. In conclusion, this study suggested that FCE prepared through lactic acid bacteria fermentation may be utilized as a powerful antioxidant material.

• Food Engineering Progress
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• v.21 no.2
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• pp.143-149
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• 2017

This study was carried out to investigate antimicrobial activity and characteristics of Asparagus cochinchinenesis which was steamed and fermented with lactic acid bacteria. A. cochinchinensis was prepared to steaming process which was washed and freeze dried. A. cochinchinensis was steamed at $95^{\circ}C$ for 12 h and dried by hot air at $50^{\circ}C$ for 24 h. After steaming process, A. cochinchinensis was fermented with lactic acid bacteria (Leuconostoc mesenteroides 4395, Lactobacillus sakei 383 and Lactobacillus plantarum KCCM 11322). Ethyl acetate extracts of fermented A. cochinchinensis had antimicrobial activities for the respiratory disease bacteria (Staphylococcus aureus, Staphylococcus epidermidis, Pseudomonas aeruginosa and Escherichia coli). A. cochinchinensis had highest antimicrobial activity for the P. aeruginosa which fermented with L. mesenteroides 4395. The minimum inhibition concentration (MIC) of A. cochinchinensis fermented with L. mesenteroides 4395 was 10 mg/mL for S. aureus, S. epidermidis, E. coli and 5 mg/mL for P. aeruginosa. The MIC of A. cochinchinensis fermented with L. sakei 383 and A. cochinchinensis fermented with L. plantarum KCCM 11322 were the same. Total sugar was decreased from $863.33{\pm}17.47mg/mL$ to $722.67{\pm}5.51mg/mL$ during the steaming process. But reducing sugar was increased from $99.36{\pm}1.32mg/mL$ to $109.29{\pm}2.71mg/mL$ during the steaming process. Total sugar was decreased to 301.50-361.42 mg/mL and reducing sugar was decreased to 27.39-62.20 mg/mL during the fermentation process.