• YAKHAK HOEJI
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• v.56 no.5
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• pp.304-308
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• 2012

In vitro antibacterial activity of DW286 was tested against recently collected clinical isolates of Gram-positive strains by the two fold agar dilution method. In vivo activity of DW286 was also determined against systemic infections in mice caused by Staphylococcus aureus. DW286 showed 16~64-fold more potent in vitro activities than ciprofloxacin against Gram-positive bacteria. Against systemic infection model caused by two S. aureus strains, one being methicillin-susceptible and the other methicillin-resistant, DW286 ($ED_{50}s$, 0.16 mg/kg and 4.36 mg/kg, respectively) was more potent than gemifloxacin (1.37 mg/kg, 26.58 mg/kg, respectively).

• Archives of Pharmacal Research
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• v.21 no.5
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• pp.543-548
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• 1998

We examined the immunological properties of the recombinant hepatitis B surface antigen (r-HBsAg) which was expressed in mammalian cell (C127). The cross-immunity of r-HBsAg and plasma-derived hepatitis B surface antigen (p-HBsAg) were tested using Western blotting and ELISA with guinea pig polyclonal antibody and naturally infected human-derived antibody and the both antigens show the same results in their response pattern and intensity, which indicate they have a good cross-immunity. from the measurement of $ED_{50}$ after formalin- or heat-inactivation, both r-HBsAg and p-HBsAg and p-HBsAg showed $ED_{50}$ of 0.2-0.3 in formalin-inactivaton, while r-HBsAg was 0.05-0.09 and p-HBsAg was 0.03-0.07 in heat-inactivation, which means heat-inactivation method is 3-4 times superior in immunogenicity. In the immunopersistency test performed in guinea pig for the period of 3 months with two different adjuvants, antibody titer was 34.2 with muramyl dipeptide adjuvant, which was 1.8 times greater than the antibody titer of 18.9 with $AIPO_{4}$ adjuvant. the mutagenicity of r-HBsAg has the same cross-immunity with p-HBsAg, and heat-inactivation method and muramyl dipeptide adjuvant allow development of r-HBsAg vaccine with excellent immunogenicity.

• YAKHAK HOEJI
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• v.42 no.4
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• pp.345-352
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• 1998

Praecoxin A, an ellagitannin, purified from Alnus hirsuta var.microphlla was evaluated on the antitumor activity. Praecoxin A had the significant cytotoxicity to s ix tumor cell lines: human chronic myelogenous leukemia K-562, human promyelocytic leukemia HL-60, mouse leukemia P388, mouse lymphocytic leukemia L-1210, sarcoma-l8O, mouse lymphoma L5178Y except L-1210. And the most sensitive cell line was K-562 ($ED_{50}=2.43{\mu}g/ml$). The $ED_{50} of praecoxin A against HL-60, P388, L-1210, sarcoma7l8O and L5178Y were 6.28, 8.66, 10.00, 7.01, $9.32{\mu}g/ml$, respectively. Praecoxin A showed the increasing effect in life span by 36.8% on the 1st day after treatment of 10mg/kg in mice bearing sarcoma-180 tumor cells (ascitic form) via NCI (National Cancer Institute, U.S.A.) protocol in vivo assay. As a result, praecoxin A is considered to show the antitumor activity.

• Archives of Pharmacal Research
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• v.21 no.4
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• pp.406-410
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• 1998

Biflavonoid is one of unique classes of naturally-occurring bioflavonoids. Certain biflavonoids including amentoflavone were previously reported to have inhibitory effect on the group 11 phospholipase $A_2$ activity. Amentoflavone was also found to inhibit cyclooxygenase from guinea-pig epidermis without affecting lipoxygenase. In this study, anti-inflammatory and analgesic activities of amentoflavone were evaluated. When amentoflavone was administered intraperitoneally, it showed a potent anti-inflammatory activity as determined by amelioration of croton-oil induced mouse ear edema. It also showed a potent anti-inflammatory activity in the rat carrageenan paw edema model ($ED_{50}$=42 mg/kg) compared to the activity of prednisolone (35 mg/kg) and indomethacin (10 mg/kg). However, amentoflavone did not show a significant inhibitory activity against rat adjuvant-induced arthritis, a chronic inflammatory model. In addition, amentoflavone was found to possess a potent analgesic activity in the acetic acid writhing test ($ED_{50}$=9.6 mg/kg) compared to the activity of indomethacin (3.8 mg/kg). These results suggest that amentoflavone may be a potential lead for a new type of anti-inflammatory agents having dual inhibitory activity of group 11 phospholipase $A_2$ and cyclooxygenase.

• Natural Product Sciences
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• v.8 no.4
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• pp.165-169
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• 2002

One-hundred and twenty plant extracts were prepared from 29 Indonesian plants and were primarily tested in vitro cytotoxicity in cultured human lung (A549), colon (Col2), and stomach (SNU-638) cancer cells. As a result, the 23 extracts were found to be active in the criteria of $ED_{50}$<$20\;{\mu}g/ml$. Remarkable cytotoxicity was observed for chloroform and n-butanol extracts of Calotropis gigantea, with $ED_{50}$ values ranging from 0.25 to $0.46\;{\mu}g/ml$. Five extracts derived from Eclipta alba and Excoecaria cochinchinensis displayed potent cell-line selective cytotoxicity, while the rest of 15 extracts showed modest cytotoxic activity against all of three cancer cells. In addition, the cytotoxic potential of subfractions of Zingiber cassumunar against a panel of human cancer cell lines is presented.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.380.2-380.2
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• 2002

Peroxisome proliferator-activated receptor (PPAR)-$\gamma$ is a nuclear hormone receptor family that plays an important role in the transcriptional regulation of genes in cellular lipid and energy metabolism. In our search for Iigands for PPAR-$\gamma$ from natural resources. two phenylpropanoids. 3.4.5-Trimethoxy cinnamylalcohol (1) and 3.4.5- Trimethoxy cinnamaldehyde (2). were isolated as PPAR-$\gamma$ agonists from the MeOH extracts of Zanthoxylum schinifolium Sieb. & ZUCCo (Rutaceae) by activity-guided fractionation. These two compoundS bind and activated PPAR-$\gamma$ transcriptional activity in a dose dependent manner assessed by ligand-binding assay. While the maximum activities for PPAR-$\gamma$ of these compounds were comparable with that of rosiglitazone. which is currently used in the treatment of Type II diabetes. the potency of these compounds were much weaker than rosiglitazone ($ED_{50}$=t.2$\mu\textrm{M}$) with the $ED_{50}$ values of 9.08 and 4.08 $\mu\textrm{M}$. respectively. To examine the structure-activity relationship of phenylpropanoids. we prepared several phenylpropanoid derivatives and measured the activity. We observed that substituents at 4'- position could playa key role in determining the potency for PPAR-$\gamma$ agonistic activity .

• Journal of Nutrition and Health
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• v.36 no.2
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• pp.125-132
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• 2003

The present study was attempted to investigate and compare the antioxidant potency of several well-know flavonoids, antioxidant vitamin and commercially available popular beverages. The antioxidant potency was assessed by the effect on reducing oxidative DNA damage of human lymphocytes. Cellular oxidative DNA damage was measured by SCGE (single-cell gel electrophoresis), also known as comet assay. Lymphocytes were pre-treated for 30 minutes with wide ranges of doses of apigenin, kaempferol, luteolin, myricetin, rutin, quercetin, $\alpha$-tocopherol (10,25,50,100,200,500,1000 $\mu$M) ,green tea extract or grape juice (10,50,100,250,500,1000 $\mu$g/mL) followed by a $H_2O$$_2$(100 $\mu$M) treatment for 5 min as an oxidative stimulus. The physiological function of each antioxidant substance on oxidative DNA damage was analyzed as tail moment (tail length $\times$ percentage migrated DNA in tail) and expressed as relative DNA damage score after adjusting by the level of control treatment. Cells treated with $H_2O$$_2$alone (positive control) had an extensive DNA damage compared with cells treated with phosphate buffered saline (PBS, negative control) or pre-treated with all the tested samples. Of all the six flavonoids, quercetin was the most potent antioxidant showing the lowest $ED_{50}$/ of 8.5 $\mu$g/mL (concentration to produce 50% protection of relative DNA damage). The antoxidant potency of individual flavonoids were ranked as follows in a decreasing order; luteolin (18.4 $\mu$g/mL), myricetin (19.0 $\mu$g/mL) , rutin (22.2 $\mu$g/mL) , apigenin (24,3 $\mu$g/mL) , kaempferol (25.5 $\mu$g/mL). The protective effect of $\alpha$-tocopherol was substantially lower (highest $ED_{50}$value of 55.0 $\mu$g/mL) than all the other flavonoids, while the protective effect was highest in green tea and grape juice with low ED5O value of 7.6 and 5.3, respectively. These results suggest that flavonoids, especially quercetin, and natural compounds from food product, green tea and grape juice, produced powerful anti-oxidative activities, even stronger than $\alpha$-tocopherol. Taken together, supplementation of antioxidants to lymphocytes followed by oxidative stimulus inhibited damage to cellular DNA, supporting a protective effect against oxidative damage induced by reactive oxygen species.

• Asian-Australasian Journal of Animal Sciences
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• v.16 no.11
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• pp.1619-1624
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• 2003

The effect of maize hybrid (Suco and Dekalb 765, DK 765), maturity stage (milk, $R_3$ and 1/2 milk line, $R_5$) and animal diet (Diet 1: 70% lucerne hay+30% maize silage; Diet 2: 50% maize silage+20% sunflower meal+30% maize grain) on ruminal stover dry matter (DM) degradability was studied. Additionally, morphological and chemical plant composition was evaluated. Fodder samples ground at 2 mm were incubated in three Holstein steers (400 kg body weight) using the in situ technique. Ruminal degradation kinetics was studied and the effective degradability (ED) was estimated for an assumed kp of 5%/h. The in situ data was analyzed in a complete randomized block design with the animals as blocks. Significant interactions between hybrid${\times}$diet and maturity${\times}$diet on kinetic digestion parameters were detected. In Diet 1, hybrids did not differ in degradable fraction, kd or ED, although a minor difference (p<0.05) in the soluble fraction was found (25.5 and 23.2% for Suco and DK 765, respectively). In Diet 2, the DK 765 had greater degradable fraction (p<0.001) but smaller (p<0.01) kd than Suco, without differences in the soluble fraction or in ED. Anticipating the harvest increased ED of stover from 37.5% in $R_5$ to 44.6% in $R_3$ (average values across hybrids and diets) due to the increase (p<0.001) in the soluble fraction ($R_5$: 22.6%, $R_3$: 28.8%). It is concluded that hybrids had similar stover in situ DM degradability and that soluble fraction represent the main proportion of degradable substrates. Advancing the date of harvesting may not improve the in situ DM degradability of whole maize plant silage since the increase in stover quality is counteracted by the depression in the grain-to-stover ratio. The diet of the animal consuming silage might not improve stover utilization either.

• Journal of The Korean Society of Clinical Toxicology
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• v.14 no.1
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• pp.9-15
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• 2016

Purpose: In most emergency department (ED), sedation is required before carrying out an invasive procedure on a pediatric patient. In the ED setting, it is essential to determine the optimal dose and administration route of CH for successful sedation. The aim of this study was to determine the optimal dose of CH for an invasive procedure and to examine the effectiveness of the drug's different administration routes. Furthermore, in this study, we performed simple survey using questionnaire which composed of Likert-scale to evaluate satisfaction of medical staffs in ED with administration routes. Methods: This study was conducted prospectively. The study participants were pediatric patients under 8 years old who visited the ED in two tertiary hospitals in South Korea within a period of 12 months. Results: Overall, 300 patients were included in this study. The age, sex, and weight of the patients were not shown to influence the sedation time. Chloral hydrate dosage is the independent factor to influence the both sedation and discharge time (p<0.01). In the comparison of the groups, groups 1, 2, and 5 showed no significant difference. On the other hand, groups 3 and 4 were shown to be statistically significantly different from group 1. Conclusion: Up to 100 mg/kg CH is safe to use in the emergency department for pediatric patients, but the initial dose of 50 mg/kg for oral administration should be considered in advance because it can provide safe and effective sedation with a lower possibility of causing an adverse effect.

• Journal of Animal Science and Technology
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• v.47 no.1
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• pp.83-90
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• 2005

ACE-inhibitory peptides derived from goat's whey hydrolyzed by various proteolytic enzymes were separated and purified for antihypertension materials. The highest ACE-inhibitory activity of goat's whey hydrolysates was 85.5 % by pepsin for 72 hrs. Also the highest ACE-inhibitory activity of goat's whey hydrolysates was F-4 by pepsin for 72 hrs by Sephadex G-25 gel chromatograms. F-4e and F-4ed from F-4 by RP-HPLC to first and second purification were the highest in ACE-inhibitory activity, respectively. The most abundant amino acid was leucine(I 8.54 %) in F-4ed of ACE-inhibitory peptides after second purification. Amino acid sequence of F-4ed of ACE-inhibitory peptides showed Leu-Lys-Asp-Tyr-Gly-GlyVal- Ser-Leu and Leu-Gly-Asp-Gly-Ala-Gly- Asp-Val-Ala-Phe. $IC_{50}$ calibrated in peptic hydrolysates(72 hrs), F-4, F-4e and F-4ed from goat's whey hydrolysates by pepsin for 72 hrs were 33.93, 28.75, 11.74 and 1.09 mg/ml, respectively. From the results of this experiment, goat's whey hydrolysate by pepsin was shown to have ACE-inhibitory activity.