• Archives of Pharmacal Research
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• v.28 no.1
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• pp.61-67
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• 2005

We evaluated the antiplatelet effects of two classes of ATP-sensitive potassium channel openers $(K_{ATP}\;openers)$ on washed human platelets, and the study's emphasis was on the role of mitochondrial $K_{ATP}$ in platelet aggregation. Collagen-induced platelet aggregation was inhibited in a dose dependent manner by lemakalim and SKP-450, which are potent cardio-nonselective $K_{ATP}$ openers, and also by cardioselective BMS-180448 and BMS-191095 $(IC_{50}\;:\;1,130,\;>\;1,500,\;305.3\;and\;63.9\;{\mu}M,\;respectively)$, but a significantly greater potency was noted for the cardioselective $K_{ATP}$ openers. The latter two $K_{ATP}$ openers also inhibited platelet aggregation induced by thrombin, another important blood-borne platelet activator, with similar rank order of potency $(IC_{50}\;:\;498.0\;and\;104.8{\mu}M\; for\;BMS-180448\;and\;BMS-191095,\;respectively)$. The inhibitory effects of BMS-191095 on collagen-induced platelet aggregation were significantly blocked by a 30-min pretreatment of platelets with glyburide $(1{\mu}M)$ or sodium 5-hydroxyde­canoate$(5-HD,\;100{\mu}M)$, a nonselective and selective mitochondrial $K_{ATP}$ antagonist, respectively, at similar magnitudes; this indicates the role of mitochondrial $K_{ATP}$ in the antiplatelet activity of BMS-191095. However, glyburide and 5-HD had no effect when they were added to the platelet cuvette immediately prior to the addition of BMS-191095. These findings indicate that cardioselective mitochondrial $K_{ATP}$ openers like BMS-191095 are able to exert cardioprotective effects in cardiac ischemia/reperfusion injury via dual mechanisms directed at the inhibition of platelet aggregation and the protection of cardiomyocytes, and both these mechanisms are mediated by mitochondrial$K_{ATP}$.

• Journal of Life Science
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• v.19 no.9
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• pp.1245-1250
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• 2009

Beimu (Fritillaria thunbergii Miquel), a bulbous plant of Liliaceae found in Korea, Japan and China, has been used as an antitussive and expectorant agent, and is also useful in alleviating stonsillitis and bronchiolitis. Most researches have been focused on micro-propagation and plant regeneration, component analysis, and dormancy relieving of beimu. Reports regarding the biological activity of beimu, such as anti-Helicobacter pyroli or platelet aggregation inhibition activity, are few and not widely available. In this study, methanol extract and its organic solvent fractions were prepared from Fritillaria thunbergii Miquel and their antimicrobial, antithrombin, and antioxidant activities were evaluated, respectively. The methanol extract contained lots of water-soluble materials (58.98%) and hexane-soluble oils (14.85%). The ethylacetate and butanol fraction at $500{\mu}g$/disc concentration showed strong antibacterial activity against tested bacteria, except Escherichia coli. Antifungal activity was not observed in methanol extract and its fractions. The hexane, ethylacetate and butanol fractions showed strong antithrombin activity at 4.8 mg/ml concentration. Especially, the ethylacetate fraction showed 95.4 sec of thrombin time at a concentration of 1.2 mg/ml, which is comparable to aspirin, a widely used antithrombosis agent. For antioxidation activity, the ethylacetate and butanol fraction showed good 1,1-diphenyl-2-picryl hydrazyl scavenging activity ($IC_{50}$ of $344{\sim}368{\mu}g$/ml). In superoxide dismutase-like activity and reducing power, the fractions showed $20{\sim}25%$ of vitamin C, and $51{\sim}54%$ of butyl hydroxytoluene, respectively.

• Journal of the Korean Society of Food Science and Nutrition
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• v.41 no.11
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• pp.1528-1533
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• 2012

This study examined the protective effects of ginger and processed (Beopje) ginger extracts on gastritis induced by HCl-ethanol in SD-rats. Beopje (or Poje) is a branch of herbal medicines processed using a Korean traditional method to achieve specific pharmacological effects. Gastric lesions were induced in the rats by a treatment of 1 mL of HCl-ethanol (60% ethanol＋150 mM HCl). The rats were divided into seven groups: Normal (1 mL of saline without HCl-ethanol treated group), Control (HCl-ethanol treated group), GL (35 mg/kg of ginger treated group), BGL (35 mg/kg of Beopje ginger treated group), GH (350 mg/kg of ginger treated group), BGH (350 mg/kg of Beopje ginger treated group) and Cimetidine (80 mg/kg of cimetidine treated group). The gastric injury inhibition rate was 40.2% and 64.9% in GL and BGL and 68.4% and 99.6% in GH and BGH respectively, showing significantly lower rates than the control (p<0.05). The level of gastric juice secretion decreased significantly in all ginger administered groups. The pH of the gastric juices of BGH increased and the acidity of BGH and cimetidine decreased significantly (p<0.05) compared to the other groups. Beopje ginger had stronger inhibitory effects on gastritis than ginger without the Beopje process. The protective effect on gastritis by the ginger and Beopje ginger extracts increased in a dose-dependent manner (p<0.05). These results suggest that ginger has inhibitory effects on HCl-ethanol induced gastritis in rats that can be improved through the Beopje process.

• Preventive Nutrition and Food Science
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• v.11 no.1
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• pp.31-35
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• 2006

In order to improve the antiobesity effect of Kochujang, 1% of sea tangle powder, alginic acid extract, and fucoidan extract were added to Kochujang. Sea tangle powder-added Kochujang decreased leptin secretion by only 12% compared to Kochujang, whereas alginic acid or fucoidan-added Kochujang significantly decreased leptin secretion by more than 60% in 3T3-L1 adipocytes. Fucoidan, one of the active components of sea tangle, decreased leptin secretion by 56%, 60%, and 60% compared to the control in the concentrations of $1{\mu}M,\;2.5{\mu}M,\;and\;5{\mu}M$, respectively. To see the effect of fucoidan on TG formation during adipocyte differentiation, 3T3-L1 cells were treated with $1{\mu}M\;and\;5{\mu}M$ concentrations of fucoidan during adipocyte differentiation (from 'day 0' to 'day 6'). Oil red O staining showed fucoidan decreased the amount of TG droplets and $5{\mu}M$ fucoidan potently inhibited TG formation. To see the effect of fucoidan on lipolysis, differentiated 3T3-L1 adipocytes were treated with fucoidan. The secretion of glycerol, which is used to measure lipolytic activity, was increased by 21%, 37%, and 53% compared to the control in the concentrations of $1{\mu}M,\;2.5{\mu}M,\;and\;5{\mu}M$, respectively. Oil red O staining showed fucoidan decreased TG amount at $1{\mu}M\;and\;5{\mu}M$ concentrations. These results suggest that fucoidan decreases leptin secretion and TG accumulation by inhibition of adipocyte differentiation and induction of lipolysis. Since fucoidan is reported to have various biological activities in addition to an anti-adipogenic effect, it seems valuable to develop fucoidan-added Kochujang as a multi-functional Kochujang.

• Journal of Radiation Protection and Research
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• v.24 no.3
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• pp.123-129
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• 1999

Tomato (Lycopericum esculentum $M_{ILL}$ cv. Seokwang and cv. Housemomotaro) seeds were irradiated with the doses of $1{\sim}20$ Gy from $^{60}Co$ $\gamma$-ray source to investigate the effect of the low dose $\gamma$-ray radiation on the early growth and resistance to subsequent high dose of radiation. Germination rate of seeds irradiated with low dose $\gamma$-ray was enhanced in Seokwang cultivar but not in Housemomotaro cultivar. Seedling height increased in 4 Gy and 8 Gy irradiation group of both cultivars. Plant height of Seokwang cultivar was depressed in low dose irradiation group but fresh weight was increased in 2 Gy and 4 Gy irradiation group. In Housemomotaro cultivar, plant height increased in 12 Gy and 20 Gy irradiation group and fresh weight increased in 4 Gy and 20 Gy irradiation group. Growth inhibition of tomato plants by high dose radiation was noticeably reduced by pre-irradiation of low dose radiation. Resistance to subsequent high dose of radiation was enhanced in 2 Gy and 8 Gy Irradiation group of Seokwang cultivar and in 2 Gy and 12 Gy irradiation group of Housemomotaro cultivar.

• Journal of Korean Society of Forest Science
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• v.99 no.6
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• pp.885-890
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• 2010

This study was conducted to confirm the application as ingredients of cosmetics through an examination of the function for anti-oxidant activity of the fraction isolated from Pyrus ussuriensis leaves. The dried leaf of Pyrus ussuriensis were extracted with acetone-$H_2O$ (6:4, v/v), concentrated and fractionated with the upper layer of acetone on a separatory funnel. Each fraction was freeze dried, then a portion of acetone soluble powder was chromatographed on a Sephadex LH-20 column using a series of aqueous methanol as eluents and also used the MIC-gel using a series of aqueous methanol as developing solvent. The isolated compounds were identified by silica-gel TLC. The concentration of total phenolic compound of Pyrus ussuriensis acetate soluble fraction was high, 914 mg/g. The results obtained from the analyses of the anti-oxidanat effects of Pyrus ussuriensis acetate fraction can be summarized as follows: In the result of DPPH scavenging radical activity, Pyrus ussuriensis acetate soluble fraction showed more than 80% at 100 ppm. SOD-like activity of one of Pyrus ussuriensis acetate soluble fractions was 77% at 1000 ppm. Xanthine oxidase inhibition of Pyrus ussuriensis acetate soluble fraction was 38% at 100 ppm. From these results, we confirmed that acetate fraction of Pyrus ussuriensis has a great potential as a natural ingredients with a natural antioxidant and antimicrobial source.

• Journal of the Korean Society of Food Science and Nutrition
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• v.38 no.12
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• pp.1724-1731
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• 2009

This study was aimed to investigate the effect of phyto-extract fermented mixture (MP119) on the male sexual functions. The MP119 was evaluated for anti-impotency and anti-hypertensive effects via ACE (angiotensin converting enzyme) or PDE (phosphodiesterase) inhibition assay. $IC_{50}$ values of MP119 against ACE and PDE were 241.3${\pm}$35.5 ppm and 372.2${\pm}$33.8 ppm, respectively. To investigate the effect of testosterone expression by MP119, we performed cell media test using mouse Leydig-derived TM3 cells. Production of testosterone in TM3 cell was increased by MP119. Also, NO (nitric oxide) production of HUVEC (human umbilical vein endothelial cell) was increased when MP119 was added to the cultures. Forty male ICR mice were divided into 4 groups. MP119 was orally intubated for 7 days to group 1 and 3, and same volume of vehicle to group 2 and 4 as controls. After that, group 3 and 4 were intraperitoneally injected cadmium chloride at a single dose of 2 mg/kg. On the 8th experimental day, weights of testis, epididymis and seminal vesicle, number of sperm, concentrations of serum testosterone and cGMP were determined. The number of sperm, the concentrations of testosterone and cGMP were significantly increased in two experimental groups (group 1, 3). These results suggest that MP119 enhanced the sexual function of male mice, and could protect the sexual organs from the cadmium chloride as one of the endocrine disrupters.

• Korean Journal of Food Science and Technology
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• v.28 no.4
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• pp.730-735
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• 1996

Antibacterial action of garlic extract against Escherichia coli was investigated. When the survival of E. cloi in tryptic soy broth (TSB) containing 50% garlic extract was compared with those of Lactobacillus plantarum, Leuconostoc mesenteroides and Staphylococcus aureus, E. coli was the most sensitive to garlic antibacterial action. When E. coli was inoculated into TSB with different concentrations of garlic extract, viable cell number decreased continuously during the test period even at 1% garlic extract. When E. coli was inoculated into pH-adjusted TSB containing 0.5% garlic extract, viable cell number of E. coli decreased continuously at initial pH of 5.2 and 6.2, while it decreased initially but increased to $8.0{\times}10^{7}\;CFU/ml at 48 hr at pH 7.2. With larger initial populations $(10^{6}\;CFU/ml), E. coli grew without apparent inhibition, while with smaller initial populations $(<10^{5}\;CFU/ml), viable cell number decreased initially but later increased. Thiol compounds like cysteine and glutathione, with free SH group (s), helped E. coli to grow or survive better in TSB with inhibitory level (5%) of garlic extract. The possibility of eliminating E. coli by using garlic extract from foods like kimchi of which garlic is one of regular ingredients is suggested.

• Korean Journal of Veterinary Research
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• v.44 no.1
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• pp.15-21
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• 2004

This paper describes the development of $^{99m}Tc$ tricarbonyl cysteine as potential renal function diagnostic radiopharmaceutical and evaluation of its biological characteristics using experimental animals. l-Cysteine was labeled efficiently with $^{99m}Tc$ tricarbonyl precursor $([^{99m}Tc(CO)_3(H_2O)_3)]^{+})$ under 30 min heating at ${75^{\circ}C}$. Labeling yield and stability were analyzed by high performance liquid chromatography (HPLC). The biodistribution property of $^{99m}Tc$ tricarbonyl cysteine in mice and its dynamic imaging profiles in rabbits were carried out. To investigate the excretion mechanism of $^{99m}Tc$ tricarbonyl cysteine, tubular transport inhibition test with probenecid was adopted. $^{99m}Tc$ tricarbonyl cysteine was obtained with a high labeling yield under the moderate condition. The results of biodistribution experiments of $^{99m}Tc$ tricarbonyl cysteine in ICR mice at 3 and 90 min provided that $^{99m}Tc$ tricarbonyl cysteine was very highly accumulated in the kidney and bladder, thereby almost 99% of $^{99m}Tc$ tricarbonyl cysteine was excreted within 90 min post injection. The same results were confirmed by the whole body dynamic images for 30 minutes and static images in rabbits at given time intervals after injection. Renogram of $^{99m}Tc$ tricarbonyl cysteine in rabbits showed that its $T_{max}$ and $T_{1/2}$ of $^{99m}Tc$ tricarbonyl cysteine were $2.33{\pm}0.56$ and $4.30{\pm}0.79$ min, respectively. The $T_{max}$ of $^{99m}Tc$ tricarbonyl cysteine with probenecid pretreatment was $2.30{\pm}0.17$ min, whereas $T_{1/2}$ of that with probenecid pretreatment was $17.0{\pm}32.47$ min. $T_{1/2}$ of $^{99m}Tc$ tricarbonyl cysteine with probenecid pretreatment was significantly different, as compared to the result without probenecid (p<0.0001). The results showed that the excretion of $^{99m}Tc$ tricarbonyl cysteine was extremely affected by probenecid. Therefore, $^{99m}Tc$ tricarbonyl cysteine was rapidly excreted from the kidney principally by the tubular secretion.

• Microbiology and Biotechnology Letters
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• v.13 no.3
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• pp.245-250
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• 1985

In order to increase citric acid productivity. several attempts were made; isolation and characterization of the mutant strain produced citric acid in a high yield, citric acid fermentation in a medium containing relatively higher amount of glucose and citric acid production by the use of semicontinuous ceil recycle system. By the treatment of Candide lipolytica S-109 with NTG, a mutant J-24 was selected as the highest producer of citric acid among the strains formed larger CaCO$_3$ lytic zone. it produced 72g/1 citric acid in 10％ glucose medium. Because mutant J-24 produced 85g/l citric acid and showed 53％ yield in 16％ glucose medium, several factors were adjusted to increase the yield in 16％ glucose medium. 0.8-1.0$\times$10$^{-3}$ P/C ratio, 0.15％ urea, 0.25％ yeast extract were suitable at citric acid production in 16％ glucose medium. Under this condition, J-24 strain produced 93g/l citric acid and showed 58％ yield. Semicontinuous cell recycle system was used to protons the effective production phase, to minimize the product inhibition and to shorten the lag phase. The productivity of semicontinuous cell recycle system was 0.79g/l h while that of batch system was 0.53g/l.h