• Biomolecules & Therapeutics
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• v.15 no.1
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• pp.40-45
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• 2007

The vascular relaxant effects on isolated rat aorta of amlodipine camsylates (S-, R-enantiomer, and R/S-racemate), were evaluated and compared with that of S-amlodipine besylate. Furthermore, antihypertensive effects were measured in spontaneously hypertensive rat (SHR). The S-amlodipine camsylate concentration-dependently inhibited $Ca^{2+}$-induced contraction of rat aorta with a very slow onset of action (reached its maximum at 3.5h; $ED_{50}:\;1.50\;{\pm}\;0.24$ nM), having a potency 2-fold higher than those of R/S-amlodipine camsylate $(ED_{50}:\;3.36\;{\pm}\;0.91\;nM)$ and similar to those of S-amlodipine besylate $(ED_{50}:\;1.44\;{\pm}\;0.14\;nM)$, whereas the R-amlodipine camsylate has 590-fold lower vasorelaxant activity $(ED_{50}:\;886.4\;{\pm}\;49.7\;nM)$. In SHR, orally administered S-amlodipine camsylate produced a dose-dependent and long-lasting (>>10 h) antihypertensive effect $(ED_{20}:\;0.89\;mg/kg)$, with a potency 2-fold higher than those of R/S-amlodipine camsylate $(ED_{20}:\;1.82\;mg/kg)$ and similar to those of S-amlodipine besylate $(ED_{20}:\;0.71\;mg/kg)$. In contrast, the R-amlodipine camsylate has no effect even-though administrated high concentration 10 mg/kg. These results suggest that S-amlodipine camsylate has the potency and long-lasting antihypertensive activity as single enantiomer drug, and its antihypertensive effect is not significantly different to that of S-amlodipine besylate.

• YAKHAK HOEJI
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• v.38 no.2
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• pp.140-148
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• 1994

${\beta}-Lactamase$ stability, chemotherapeutic activity, and pharmacokinetics of 7-[(Z)-2-(2-aminothiazole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyridyl)piperazinyl]thiocarbonylthiomethyl-3-cephem-4-carboxylic acid(CEN1), 7-[(Z)-2-(2-aminothiazole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyrimidyl)piperazinyl]thiocarbonylthiomethyl-3-cephem-4-carboxylic acid(CEN2), pivaloyloxymethyl-7-[(Z)-2-(2-aminothizaole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyridyl)piperazinyl]thiocarbonyl-thiomethyl-3-cephem-4-carboxylate(CEN1P), and pivaloyloxymethyl-7-{(Z)--2-(2-aminothizaole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyridyl)piperazinyl]thiocarbonyl-thiomethyl-3-cephem-4-carboxylate(CEN2P) were examined. CEN1, CEN2, CEN1P, and CEN2P were very stable to the ${\beta}-lactamase$ obtained from three strains(Enterobacter cloacae P99, Escherichia coli TEM, and Citrobacter freundii). Chemotherapeutic activities$(ED_{50})$ of CEN2 and CEN2P against experimental systemic infections due to Streptococcus pyogenes 77A and Escherichia coli 078 were superior to those of CEN1 and CEN1P, respectively. The $ED_{50}$ values of CEN1, CEN2 were 5.82 mg/kg, 0.89 mg/kg(s.c., S. pyogenes 77A) while those of CEN1P, CEN2P were 14.56mg/kg, 6.40mg/kg(p.o., S. pyogenes 77A), respectively. The pharmacokinetics of CEN1, CEN2, CEN1P, and CEN2P were investigated in mice and rats. In mice, peak blood levels of $1.25\;{\mu}g/ml$ were recorded within 20 min after oral administration of a single dose equivalent to 40 mg/kg CEN1P. Cmax of CEN1P was much higher than that of CEN1 in mice and rats. Oral absorption of CEN2P was much higher than that of CEN2.

• Natural Product Sciences
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• v.15 no.3
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• pp.130-133
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• 2009

The crude extract of the mycelium of Cladosporium was found to exhibit antimicrobial activity against the Staphylococcus aureus, methicillin-resistant S. aureus, and multidrug-resistant S. aureus. Bioassayguided fractionation of an organic extract led to the isolation of an acetophenone derivative, clavatol (2',4'-dihydroxy-3',5'-dimethylacetophenone) (1), and a benzodiazepine alkaloid, circumdatin A (2). Compound 1 showed moderate antibacterial activity against S. aureus, methicillin-resistant S. aureus, and multidrug-resistant S. aureus with minimum inhibitory concentration (MIC) values of 62.5, 62.5, 31.0 $\mu$g/mL, respectively, but compound 2 was inactive. Compounds 1 and 2 exhibited UV-A protection activity with ED$_{50}$ values of 227.0 and 82.0 $\mu$M, respectively, indicating that they were more potent than the positive control, oxybenzone (ED$_{50}$ 350 $\mu$M), a common sunscreen agent.

• The Korean Journal of Pain
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• v.33 no.4
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• pp.386-394
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• 2020

Background: In the emergency department (ED), adequate pain control is essential for managing patients; however, children with pain are known to receive less analgesia than adults with pain. We introduce the Pain Passport to improve pain management in paediatric patients with suspected fractures in the ED. Methods: This was a before-and-after study. We reviewed the medical records of paediatric patients who were primarily diagnosed with fractures from May to August 2015. After the introduction of the Pain Passport, eligible children were enrolled from May to August 2016. Demographics, analgesic administration rates, time intervals between ED arrival and analgesic administration, and satisfaction scores were obtained. We compared the analgesic prescription rate between the two periods using multiple logistic regression. Results: A total of 58 patients were analysed. The baseline characteristics of subjects during the two periods were not significantly different. Before the introduction of the Pain Passport, 9 children (31.0%) were given analgesics, while after the introduction of the Pain Passport, a significantly higher percentage of patients (24/29, 82.8%) were treated with analgesics (P < 0.001). The median administration times were 112 (interquartile range [IQR], 64-150) minutes in the pre-intervention period and 24 (IQR, 20-74) minutes in the post-intervention period. The median satisfaction score for the post-intervention period was 4 (IQR, 3-5). The adjusted odds ratio for providing analgesics in the post-intervention period was 25.91 (95% confidence interval, 4.36-154.02). Conclusions: Patient-centred pain scoring with the Pain Passport improved pain management in patients with suspected fractures in the paediatric ED.

• Archives of Pharmacal Research
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• v.18 no.6
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• pp.396-401
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• 1995

As a part of trials to develop the antitumor agent from tannins isolated from plants, the antitumor activity of peduculagin, an ellagitannin, isolated from Alnus hirsuta var. microphylla was examined in vitro and in vivo. In vitro, the cytotoxicity was determined by 0.4% typanblue dye exclusion method. peduculagin showed the dose-dependent cytotoxicity against human chronic myelogenous leukemia (K-562), human promyelocytic leukemia (HL-60), mouse lymphoid neoplasm (P388), mouse lymphocytic leukemia (L1210) and mouse sarcoma 180(S180) cell lines. $ED_{50}\; values\; (ED_{50})$ of each cell line were 5.30, 0.92, 2.78, 9.35 and $1.38 \mug/ml$ respectively. The most sensitive cell line was HL-60. In vivo, pedunculagin was administered to ICR mouse with the doses of 50 and $100{\;}{\mu}g/ml$intraperitoneally once at 20 days before S180 inoculation. peduculagin showed the antitumor activity and its T/C ratio (%) was 120.82% in the group of both concentrations.

• Journal of the Korean Society of Food Science and Nutrition
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• v.23 no.5
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• pp.774-783
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• 1994

New food item numbers for each food included in Food Composition Table in Korea (4th ed) and other Food Composition Table. New Food item numbers classified to base 5-basic food groups and its classification was as follows. 1 As for the 1569 food items , they were classified as 20 food sub-groups(82 food sorts) for 5-basic food groups. 2. As for the 82 food sorts, they were individually classified with raw prepared , fat sugar content and arranged in order, ㄱ , ㄴ and ㄷ and made the item number. 3. The data set of nutritive value of food with new item numbers was accessed on computer files. 4. The Food & Description Table was drafted as 1572 food items were arranged in order, ㄱ, ㄴand ㄷ. 5. The Food Table arranged in the order or each nutrient content (energy, carbohydrate, protein , etc....) was drafted. Clipper program for computing nutritive values and tabulation of nutrients of daily diet were coded by applying new food item numbers. It is expected that should utilized as a basic data of computer program for calculating the nutritive value of diet, evaluating the nutrition and counseling the nutrition.

• Korean Journal of Microbiology
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• v.45 no.4
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• pp.404-410
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• 2009

We investigated the physicochemical stabilities and biological activities of ethanol- extracted pigment from marine bacteria Pseudoalteromonas sp. Ju11-1 and Pseudoalteromonas sp. Ju14. The bacterial pigment of strain Ju11-1 was very stable at pH 5.0 below $25^{\circ}C$. The stability of the pigment showed higher stability in the presence of metal ions such as $Cu^{2+}$ and $Mg^{2+}$. The pigment has activity of free-radical scavenging ($IC_{50}$ $95.2{\mu}g$/ml) and the protective antioxidant effect ($ED_{50}$ $82.3{\mu}g$/ml) against DNA damage in human lymphocytes. The bacterial pigment of strain Ju14 was very stable at pH range between 4.0 and 8.0 below $40^{\circ}C$. In the presence of light, the pigment was also very stable, showing more than 90 percent of remaining absorbance during 14 days at $25^{\circ}C$. The stability of the pigment, when metal ions were present, showed higher stability in all examined metal ions except for $Fe^{2+}$, $Al^{3+}$, and $Cu^{2+}$, especially in the presence of $Na^+$. The pigment has activity of freeradical scavenging ($IC_{50}$ $208.6{\mu}g$/ml) and the protective antioxidant effect ($ED_{50}$ $ 96.4{\mu}g$/m) against DNA damage in human lymphocytes. The result indicates that the bacterial pigments from marine bacteria, Pseudoalteromonas sp. Ju11-1 and Pseudoalteromonas sp. Ju14 showed higher physicochemical stability and significant effects for reduction in oxidative DNA damage. Therefore, the results suggest that these bacterial pigments could be used as a natural colorant having the advantages of antioxidant.

• The Korean Journal of Physiology and Pharmacology
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• v.18 no.5
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• pp.411-418
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• 2014

Vascular remodelling is an adaptive mechanism, which counteracts pressure changes in blood circulation. Nicotine content in cigarette increases the risk of hypertension. The exact relationship between nicotine and vascular remodelling still remain unknown. Current study was aimed to determine the effect of clinically relevant dosage of nicotine (equivalent to light smoker) on aortic reactivity, oxidative stress markers and histomorphological changes. Twelve age-matched male Sprague-Dawley rats were randomly divided into two groups, i.e.: normal saline as control or 0.6 mg/kg nicotine for 28 days (i.p., n=6 per group). On day-29, the rats were sacrificed and the thoracic aorta was dissected immediately for further studies. Mean arterial pressure (MAP) and pulse pressure (PP) of nicotine-treated vs. control were significantly increased (p<0.05). Nicotine-treated group showed significant (p<0.05) increase tunica media thickness, and decrease in lumen diameter, suggesting vascular remodelling which lead to prior hypertension state. The phenylephrine (PE)-induced contractile response in nicotine group was significantly higher than control group ($ED_{50}=1.44{\times}10^5M$ vs. $4.9{\times}10^6M$) (p<0.05~0.001). However, nicotine-treated rat showed significantly lower endothelium-dependent relaxation response to acetylcholine (ACh) than in control group ($ED_{50}=6.17{\times}10^7M$ vs. $2.82{\times}10^7M$) (p<0.05), indicating loss of primary vascular function. Malondialdehyde (MDA), a lipid peroxidation marker was significantly higher in nicotine group. Superoxide dismutase (SOD) enzymatic activity and glutathione (GSH) were all reduced in nicotine group (p<0.05) vs. control, suggesting nicotine induces oxidative imbalance. In short, chronic nicotine administration impaired aortic reactivity, probably via redox imbalance and vascular remodelling mechanism.

• Journal of Medicine and Life Science
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• v.17 no.1
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• pp.7-15
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• 2020

The field triage guidelines have been widely implemented in the Korean trauma system. This study aimed to evaluate and validate whether it is reliable to use the field triage guidelines for predicting severe traumatic brain injury (TBI) and traumatic spinal injury (TSI) patients. This study retrospectively analyzed in-hospital cohort registries of all TBI and TSI patients, who visited the emergency department (ED) of the Jeju National University Hospital from 1 January 2013 to 31 December 2015. The primary outcome was defined as TBI and TSI patients with an injury severity score (ISS)>15. Secondary outcomes were defined as cases in which one or more of the following conditions: in-hospital death, ISS>15, admission to the intensive care unit, emergency surgery. We enrolled 14,889 TBI and TSI patients who visited ED, of which 7,966 (53.5%) were triage positive. The overall sensitivity, specificity and area under the curve (AUC) of the full cumulative field triage guidelines step's model (Step 1+3+4 criteria) for primary outcome were 82.8%, 47.0%, and 0.646, respectively. In the results for secondary outcomes, the specificity did not show a significant difference, but the sensitivity decreased to 66.5% and AUC to 0.568. The results of this study suggest that further optimization of the field triage guidelines is needed to identify high-risk TBI and TSI patients.

• The Plant Pathology Journal
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• v.30 no.1
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• pp.82-89
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• 2014

In 2009-2010, unusual symptoms were observed on Pleurotus eryngii grown in mushroom farms in Gyeongnam Province, Republic of Korea. One of the main symptoms was a cobweb-like growth of fungal mycelia over the surface of the mushroom. The colonies on the surface rapidly overwhelmed the mushrooms and developed several spores within 3-4 days. The colonized surface turned pale brown or yellow. The fruit body eventually turned dark brown and became rancid. Koch's postulates were completed by spraying and spotting using isolated strains. The phylogenetic tree obtained from the internal transcribed spacer sequence analysis showed that the isolated fungal pathogen corresponded to Cladobotryum mycophilum (99.5%). In the fungicide sensitivity tests, the $ED_{50}$ values for the isolate with respect to benomyl and carbendazim were from 0.29 to 0.31 ppm. Benzimidazole fungicides were most effective against C. mycophilum, a causal agent of cobweb disease in P. eryngii.