• The Korean Journal of Pharmacology
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• v.16 no.2 s.27
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• pp.55-70
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• 1980

The pharmacological and microbiological studies of Cefoperazone (T-1551, Toyama Chemical Co., Japan) were conducted in vitro and in vivo. The studies included stability and physicochemical characteristics, antimicrobial activity, animal and human pharmacokinetics, animal pharmacodynamics and safety evaluation of Cefoperazone sodium for injection. 1) Stability and physicochemical characteristics. Sodium salt of cefoperazone for injection had a general appearance of white crystalline powder which contained 0.5% water, and of which melting point was $187.2^{\circ}C$. The pH's of 10% and 25% aqueous solutions were 5.03 ana 5.16 at $25^{\circ}C$. The preparations of cefoperazone did not contain any pyrogenic substances and did not liberate histamine in cats. The drug was highly compatible with common infusion solutions including 5% Dextrose solution and no significant potency decrease was observed in 5 hours after mixing. Powdered cefoperazone sodium contained in hermetically sealed and ligt-shielded container was highly stable at $4^circ}C{\sim}37^{\circ}C$ for 12 weeks. When stored at $4^{\circ}C$ the potency was retained almost completely for up to one year. 2) Antimicrobial activity against clinical isolates. Among the 230 clinical isolates included, Salmonella typhi was the most susceptible to cefoperazone, with 100% inhibition at MIC of ${\leq}0.5{\mu}g/ml$. Cefoperazone was also highly active against Streptococcus pyogenes(group A), Kletsiella pneumoniae, Staphylococcus aureus and Shigella flexneri, with 100% inhibition at $16{\mu}g/ml$ or less. More than 80% of Escherichia coli, Enterobacter aerogenes and Salmonella paratyphi was inhibited at ${\leq}16{\mu}/ml$, while Enterobacter cloaceae, Serratia marcescens and Pseudomonas aerogenosa were somewhat less sensitive to cefoperagone, with inhibitions of 60%, 55% and 35% respectively at the same MIC. 3) Animal pharmacokinetics Serum concentration, organ distritution and excretion of cefoperazone in rats were observed after single intramuscular injections at doses of 20 mg/kg and 50 mg/kg. The extent of protein binding to human plasma protein was also measured in vitro br equilibrium dialysis method. The mean Peak serum concentrations of $7.4{\mu}g/ml$ and $16.4{\mu}/ml$ were obtained at 30 min. after administration of cefoperazone at doses of 20 mg/kg and 50 mg/kg respectively. The tissue concentrations of cefoperazone measured at 30 and 60 min. were highest in kidney. And the concentrations of the drug in kidney, liver and small intestine were much higher than in blood. Urinary and fecal excretion over 24 hours after injetcion ranged form 12.5% to 15.0% in urine and from 19.6% to 25.0% in feces, indicating that the gastrointestinal system is more important than renal system for the excretion of cefoperazone. The extent of binding to human plasma protein measured by equilibrium dialysis was $76.3%{\sim}76.9%$, which was somewhat lower than the others utilizing centrifugal ultrafiltration method. 4) Animal pharmacodynamics Central nervous system : Effects of cefoperazone on the spontaneous movement and general behavioral patterns of rats, the pentobarbital sleeping time in mice and the body temperature in rabbits were observed. Single intraperitoneal injections at doses of $500{\sim}2,000mg/kg$ in rats did not affect the spontaneous movement ana the general behavioral patterns of the animal. Doses of $125{\sim}500mg/kg$ of cefoperazone injected intraperitonealy in mice neither increased nor decreased the pentobarbital-induced sleeping time. In rabbits the normal body temperature was maintained following the single intravenous injections of $125{\sim}2,000mg/kg$ dose. Respiratory and circulatory system: Respiration rate, blood pressure, heart rate and ECG of anesthetized rabbits were monitored for 3 hours following single intravenous injections of cefoperazone at doses of $125{\sim}2,000mg/kg$. The respiration rate decreased by $3{\sim}l7%$ at all the doses of cefoperazone administered. Blood pressure did not show any changes but slight decrease from 130/113 to 125/107 by the highest dose(2,000 mg/kg) injected in this experiment. The dosages of 1,000 and 2,000 mg/kg seemed to slightly decrease the heart rate, but it was not significantly different from the normal control. All the doses of cefoperazone injected were not associated with any abnormal changes in ECG findings throughout the monitering period. Autonomic nervous system and smooth muscle: Effects of cefoperazone on the automatic movement of rabbit isolated small intestine, large intestine, stomach and uterus were observed in vitro. The autonomic movement and tonus of intestinal smooth muscle increased at dose of $40{\mu}g/ml$ in small intestine and at 0.4 mg/ml in large intestine. However, in stomach and uterine smooth muscle the autonomic movement was slightly increased by the much higher doses of 5-10 mg/ml. Blood: In vitro osmotic fragility of rabbit RBC suspension was not affected by cefoperazone of $1{\sim}10mg/ml$. Doses of 7.5 and 10 mg/ml were associated with 11.8% and 15.3% prolongation of whole blood coagulation time. Liver and kidney function: When measured at 3 hours after single intravenous injections of cefoperaonze in rabbits, the values of serum GOT, GPT, Bilirubin, TTT, BUN and creatine were not significantly different from the normal control. 5) Safety evaluation Acute toxicity: The acute toxicity of cefoperazone was studied following intraperitoneal and intravenous injections to mice(A strain, 4 week old) and rats(Sprague-Dawler, 6 week old). The LD_(50)'s of intraperitonealy injected cefoperazone were 9.7g/kg in male mice, 9.6g/kg in female mice and over 15g/kg in both male and female rats. And when administered intravenously in rats, LD_(50)'s were 5.1g/kg in male and 5.0g/kg in female. Administrations of the high doses of the drug were associated with slight inhibition of spontaneous movement and convulsion. Atdominal transudate and intestinal hyperemia were observed in animals administered intraperitonealy. In rats receiving high doses of the drug intravenously rhinorrhea and pulmonary congestion and edema were also observed. Renal proximal tubular epithelial degeneration was found in animals dosing in high concentrations of cefoperazone. Subacute toxicity: Rats(Sprague-Dawley, 6 week old) dosing 0.5, 1.0 and 2.0 g/kg/day of cefoperazone intraperitonealy were observed for one month and sacrificed at 24 hours after the last dose. In animals with a high dose, slight inhibition of spontaneous movement was observed during the experimental period. Soft stool or diarrhea appeared at first or second week of the administration in rats receiving 2.0g/kg. Daily food consumption and weekly weight gain were similar to control during the administration. Urinalysis, blood chemistry and hematology after one month administration were not different from control either. Cecal enlargement, which is an expected effect of broad spectrum antibiotic altering the normal intestinal microbial flora, was observed. Intestinal or peritoneal congestion and peritonitis were found. These findings seemed to be attributed to the local irritation following prolonged intraperitoneal injections of hypertonic and acidic cefoperazone solution. Among the histopathologic findings renal proximal tubular epithelial degeneration was characteristic in rats receiving 1 and 2g/kg/day, which were 10 and 20 times higher than the maximal clinical dose (100 mg/kg) of the drug. 6) Human pharmacokinetics Serum concentrations and urinary excretion were determined following a single intravenous injection of 1g cefoperazone in eight healthy, male volunteers. Mean serum concentrations of 89.3, 61.3, 26.6, 12.3, 2.3, and $1.8{\mu}g/ml$ occured at 1,2,4,6,8 and 12 hours after injection respectively, and the biological half-life was 108 minutes. Urinary excretion over 24 hours after injection was up to 43.5% of administered dose.

• Tuberculosis and Respiratory Diseases
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• v.65 no.3
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• pp.177-182
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• 2008

Background: Isoniazid (INH, H) is a key drug of the standard first-line regimen for the treatment of tuberculosis (TB), yet some reports have suggested that treatment efficacy was maintained even though INH was omitted from the treatment regimen. Methods: One hundred forty C57BL/6 mice were infected with the H37Rv strain of M. tuberculosis with using a Glas-Col aerosol generation device, and this resulted in depositing about 100 bacilli in the lung. Four weeks after infection, anti-TB treatment was initiated with varying regimens for 4-8 weeks; Group 1: no treatment (control), Group 2 (4HREZ): 4 weeks of INH, rifampicin (R), pyrazinamide (Z) and ethambutol (E), Group 3: 1HREZ/3REZ, Group 4: 4REZ, Group 5: 4HREZ/4HRE, Group 6: 1HREZ/3REZ/4RE, and Group 7: 4REZ/4RE. The lungs and spleens were harvested at several time points until 28 weeks after infection, and the colony-forming unit (CFU) counts were determined. Results: The CFU counts increased steadily after infection in the control group. In the 4-week treatment groups (Group 2-4), even though the culture was negative at treatment completion, the bacilli grew again at the 12-week and 20-week time points after completion of treatment. In the 8-week treatment groups (Groups 5-7), the bacilli did not grow in the lung at 4 weeks after treatment initiation and thereafter. In the spleens of Group 7 in which INH was omitted from the treatment regimen, the culture was negative at 4-weeks after treatment initiation and thereafter. However, in Groups 5 and 6 in which INH was taken continuously or intermittently, the bacilli grew in the spleen at some time points after completion of treatment. Conclusion: TThe exclusion of INH from the standard first-line regimen did not affect the treatment outcome in a murine model of TB in the early stage of disease. Further studies using a murine model of chronic TB are necessary to clarify the role of INH in the standard first-line regimen for treating TB.

• Journal of Korea Foresty Energy
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• v.21 no.2
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• pp.25-33
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• 2002

One of the critical problems to preserve books and documents in libraries and archives is the deterioration. Some of previous results showed that the major cause of paper deterioration was the acid-catalyzed hydrolysis of the cellulose in paper fibres and aging rate of acidic paper was faster than that of alkaline paper. Therefore, It is necessary to remove the acid in the paper for reducing the rate of paper deterioration. It has been reported to extend the useful life of acidic paper by three to five times. Recently, It has been recognized the need for an effective method of deacidifying large quantities of books and document. However, in the previous many reports little attention was paid to the effect of paper additives. In this paper, We carried out experiment about the effect of additives on paper aging and the effect of deacidification by the gaseous ethanolamines (monoehtanolamine, diethanolamine, triehtanolamine). In result, it was found that the strength of aging was in the order of the alum＋rosin＞alum ＞AKD＞ control and the rate of deacidification was in the order of the monoethanolamine＞diethanolamine＞triethanolamine. The treatment with the gaseous ethanolamines caused decreasing of brightness and dropping of fold endurances. However, deacidification by combination treatment of the various gaseous ehtnaolamines prevented from decreasing of brightness and dropping of folding endurances.

• Journal of the korean academy of Pediatric Dentistry
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• v.36 no.2
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• pp.237-244
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• 2009

When the symptom of periapical infection is not released by mechanical instrumentation. anti-microbial agents including antibiosis become necessary in order to remove microorganisms from the root canal. Since anti-microbial agents of natural origins are currently popular, more natural remedies are being sought out. As it turns out, it is well known isothiocyanates (ITCs) in horseradish root extract have anti-microbial activity from many studies. In this research, anti-microbial effects of horseradish root extract and chlorhexidine, a typical anti-microbial agent, were investigated and compared against two kinds of obligate anaerobes. Fusobacterium nucleatum and Prevotella nigrescens, that are often discovered in infected root canal, and Clostridium perfringens, which is resistant to antibiotics and frequently used as a control strain for antibacterial studies 1. The MIC and MBC of horseradish root extract were ranged from 87 to 470 ppm and from 156 to 625 ppm against three kinds of obligate anaerobes, respectively. Horseradish root extract showed the strongest anti-bacterial activity (MBC, 156 ppm) against F. nucleatum and also showed anti-bacterial activity against antibiotic resistant obligate anaerobes. C. perfringens. 2. The MIC and MBC of chlorhexidine were ranged from 3.12 to 6.25 ppm and 10.94 ppm against three kinds of obligate anaerobes, respectively. 3. The MIC with 87-470 ppm of horseradish root exact has the same growth inhibiting effect as the one of 3.12-6.25 ppm of chlorhexidine. Likewise, the MBC with 156-625 ppm of horseradish has the similar bactericidal effect as 10.94 ppm of chlorhexidine.

• Korean Journal of Food Science and Technology
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• v.41 no.6
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• pp.681-686
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• 2009

Cronobacter spp. (Enterobacter sakazakii) is known to be highly resistant to dry conditions than any other Enterobacteriaeae. In this study, one hundred and ten Korean Cronobacter isolates were characterized to find out their survival characteristics under conditions of desiccation and humidity. Thirty percentage strains of the isolates showed high resistance to desiccation exposed on the metal surface for eight hours by half survival of the initial number, whileas less than 10% strains showed dry sensitivity by less one log scale survival among seven log scales. Finally, more than 90% of the strains consisted of dry-resistant and dry-intermediate groups. The same tendencies were evident in a 15-day exposure. Dry-resistant and intermediate strain groups showed 3 log scale survival among 5 log initial numbers in the powdered infant formula for 30 days, which were more resistant than on the above metal surface exposed. So, almost the isolate strains showed high resistance to dry condition. Dry-resistant and intermediate groups exposed on the metal surface formed a biofilm at the beginning, and the dry-sensitive group showed biofilm formation mainly only after a 7-day exposure. However, without a time difference in formation of biofilm, the dry-resistant and sensitive isolates seemed to similar biofilm formation activity. Most of the isolates showed very low survival at 75% relative humidity in 48 hours; however, they showed high resistance by 60% survival at 40% relative humidity. The Cronobacter isolates showed high resistance to desiccation on the metal surface and in the powdered infant formula, but low survival at high relative humidity. Therefore, high humidity may be a control method for Cronobacter in food processing environments.

• Journal of Life Science
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• v.20 no.12
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• pp.1851-1858
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• 2010

Estrogen deficiency in peri- and postmenopausal women results in variety of neurovegetative, psychic and somatic symptoms, and may contribute to severe diseases within the aged female population. Ecklonia stolonifera (ES) is an edible brown algae traditionally used in fishery towns in Far East Asia. This study was performed to investigate the effects of ES extracts on blood flow and serum lipid concentration in ovariectomized rats. Weight-matched female Sprague-Dawley strain rats were assigned to four groups. Three groups were surgically ovariectomized (OVX). The fourth group was sham operated. Rats were randomly assigned to the following groups: sham-operated rats (Sham), ovariectomized control rats (OVX-CON), ovariectomized rats supplemented with ES extract at 50 mg/kg bw/day (OVX-ES50) and ovariectomized rats supplemented with ES extract at 200 mg/kg bw/day (OVX-ES200). Serum total cholesterol and triglyceride contents decreased in the sham group compared to the OVX-CON group. Six weeks feeding of ES extract resulted in a significant (p<0.05) lowering of serum triglyceride and a lowering tendency of total cholesterol level. The level of Hdl-cholesterol in serum increased by supplementation of ES extracts at 50 mg/kg and 200 mg/kg bw/day (p<0.05). Blood passage time of the ES extracts-supplemented group was higher than the OVX-CON group. The ability of platelet aggregation of groups treated with ES extracts was less than that of the OVX-CON group. These results suggest that the beneficial effects of ES extract may be used to possibly improve on the metabolic syndrome of menopausal women.

• Journal of Preventive Medicine and Public Health
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• v.21 no.1 s.23
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• pp.183-194
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• 1988

This study was carried out to investigate for resistance of V. parahaemolyticus that isolated from patients of food poisoning and fish and shellfish, captured in east coast of Kyungpook province of Korea from 1985 to 1986. VP ATCC 17802 and NAG V. ATCC 6538 were used as control. In fish, shellfish and seaweed, the more temperature increased, the shorter survival time was. In case of sea-water, the more temperature rose up, the longer survival time was, particularly in $37^{\circ}C$ and $25^{\circ}C$, the strains had survived after 6 months. And in tapwater, it was sterilized in 150 mins. and survived for 11.5 days on maximum in ground water. In kimchi, at room temperature, germicidal time was shorter more than 6 times compared with that which had been kept in refrigerator. It survived for 57.1 days in milk, 49.2 mins. in yougurt. Strains had been surviving in frozen condition at $-70^{\circ}C$ even after 6 months, present study time. In resistance test in water bath at several degrees of temperature, all the strains were sterilized in 20 mins. with $60^{\circ}C$. In resistance test to driness, number of surviving strains dropped rapidly in 10-11%) water contents. In UV $2538{\AA}$, strains were sterilized in 20 mins. In resistance test to alcohol, strains had survived for 0.1-4 mins. in fermentative wine of below than 25% and distilled wine of over than 25% in alcohol concentration. The bactericidal concentration of disinfectant was 1% in phenol and 3% in cresol. In 0.1M acetic acid and 0.1M lactic acid, number of surviving colonies decreased rapidly but not in citric acid. The more NaCl concentration rose up, the lower decreasing rate of number of surviving colonies was. The strains had showed sensitive response to vancomycin, chloramphenicol, gentamicin, and resisted to carbenicillin, ampicillin and kanamycin. When one day culture strain was cultured till 25th day, resistant strains to tetracycline and cephalothin were changed to sensitive.

• Korean Journal of Soil Science and Fertilizer
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• v.26 no.4
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• pp.271-277
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• 1993

An antagonistic bacteria was isolated from rhiaosphere of pepper and corn and identified as Bacillus (B.) subtilis. These B. subtilis B-5 was transformed and marked with the plasmid pCPP4 which possess neomycine resistan. gene. The marked stranins showed growth inhibition to Rhizoctonia (R.) solani, Fusarium (F.) solani, and F. oxysporum in vitro, and were used in studying growth promoting effects on sesame and cabbage. All the identified strains utilize glucose, sucrose, fructose, lactose, mannitol and sorbitol as carbon source, but not rhamnose, and the marked strains also showed characteristics similar to wild-type strains. Germination rate of chinese cabbage and sesame seeds was increased by about 10% or more in the plot to which these strains were inoculated and the effect was higher in soil than in petri dish. The early growth promoting effects of these strains appeared higher, as compared with control plot, in the plots to which B. subtilis B-5 and pathogenic fungi was inoculated together. When the marked strains, B. subtilis B-5NEOr, were inoculated in the rhizosphere of chinese cabbage and sesame with $1.1{\times}10^8CFU/g$ dry soil, the number of inoculated strain was decreased slowly to the level of $10^5{\sim}10^6CFU/g$ dry soil after 4 weeks and the number of Pseudomonas spp. maintanied the level of $10^5CFU/g$ dry soil throught total period, but the number of fungi was decreased rapidly from the early level of $10^8CFU/g$ dry soil to $10^3CFU/g$ dry soil after 4 weeks.

• Korean Journal of Poultry Science
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• v.40 no.4
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• pp.299-304
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• 2013

Tracheal epithelial cells (TECs) are an important tool for studies of viral respiratory diseases. Primary TECs have been cultured from human, mouse and hamster. It is also necessary to diagnose viral respiratory disease and reveal infection mechanisms in chicken. In this study, we isolated tracheal epithelial layers from tracheal of 20-day-old chicks and cultured primary TECs from the isolated layers. Ciliated cells which were a typical morphology of TECs were observed in cultured primary TECs and maintained until cell passage 5 (15 to 20 days). When we analyzed expression patterns of epithelial marker genes (retinoic acid responder, FGF-binding protein, virus activating protease (VAP) in TECs compared to immortalized chicken embryonic fibroblast cell line (DF-1), all the marker genes are highly expressed in TECs than in DF-1. When TECs were cultured with 0.1 and 1 MOI of ND virus (rNDV-GFP strain) to test the susceptibility of TECs for ND virus, 12.6% and 48.2% of the incubated TECs were infected respectively. In addition, when DF-1 was incubated with 1 MOI of ND virus, the virus infection rate of DF-1 was three times lower than the virus infection rate of TECs. These data could contribute to study infection mechanisms of viral respiratory diseases and control them in chicken.

• Journal of Mushroom
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• v.15 no.4
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• pp.183-189
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• 2017

This study investigated the synergistic effect of single inoculation and co-inoculation of phosphate-solubilizing bacteria (PSB) Burkholderia metallica JH-7 and Burkholderia contaminans JH-15. Phosphate-solubilizing abilities of these strains were assessed by measuring phosphorus content in culture media that were singly inoculated or co-inoculated with these strains for 7 days. B. metallica JH-7 was found to release the highest content of soluble phosphorus ($140.80{\mu}g\;mL^{-1}$ ) into the medium, followed by single inoculation of B. contaminans JH-15 ($135.95{\mu}g\;mL^{-1}$ ) and co-inoculation of two strains ($134.84{\mu}g\;mL^{-1}$ ). The highest pH reduction, organic acid production, and glucose consumption were observed in the medium inoculated with B. metallica JH-7 alone compared with that in the medium co-inoculated with both the strains. Results of a plant growth promotion bioassay showed 17.4% and 7.48% higher leaf and root growth, respectively, in romaine lettuce inoculated with B. metallica JH-7 alone than in romaine lettuce inoculated with a control strain. However, no significant difference was observed between single inoculation and co-inoculation of these strains with respect to phosphorus release and plant growth. Although the results of the present study did not show the synergistic effect of phosphate solubilization by the PSB strains examined, these results indicate that treatment with PSB exerts a beneficial effect on crop growth.