• Archives of Pharmacal Research
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• v.19 no.5
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• pp.359-367
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• 1996

The pharmacokinetics of LB20304 was investigated following intravenous (IV) and oral administration to rats and dogs. Additionally, in vitro metabolism and serum protein binding studies were also conducted. The total body clearance, apparent volume of distribution, terminal half-life, and extent of bioavailability were 21.8 ml/min/kg, 2265 ml/kg, 93.6 min, and 30.8% for rats; and 7.95 ml/min/kg, 4144 ml/kg, 363 min, and 81.1% for dogs, respectively. LB20304 was stable in the liver microsome containing NADPH generating system and its serum protein binding was 58.5-65.8% for rats, 19.1-29.6% for dogs, and 56.9-59.6% for humans. Its tissue concentration levels in lever, stomach, small intestine, and kidney were 9.5 to 26.1 times greater than plasma level, but the concentration in testis was quite low and that in brain was negligible in rats. The 48 hr urinary recovery of the dose was 44% for IV dosing and 14% for oral dosing, shereas the 48 hr biliary recovery of the dose was 6.4% for IV dosing and 4.5% for oral dosing in rats. In summary, the pharmacokinetic properties of LB20304 were characterized by its good oral absorption, long plasma half-life, and good tissue distribution.

• Journal of Life Science
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• v.18 no.4
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• pp.503-508
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• 2008

Deep sea water from the East sea was tested for breast cancer chemoprevention and metastasis by measuring the activities of cytochrome P450 1A1 and aromatase, invasiveness, and activity and expression of matrix metalloproteinase (MMP)-9 in breast MDA-MB-231 cancer cell. The in vitro incubation of rat liver microsome with deep sea water (a hardness range of $100{\sim}1,000$) showed a hardness-dependent inhibition of 7,12-dimethylbenz[a]anthracene (DMBA)-induced cytochrome P450 1A1 activity. Deep sea water showed 27.1, 45.4 and 51.9% inhibition of microsomal aromatase activity at the hardness of 600, 800 and 1,000, respectively. In addition deep sea water inhibited not only the invasiveness of 12-O-tetradecanoylphorbol-13-acetate (TPA)-treated MDA-MB-231 cells through matrigel-coated membrane in a hardness-dependent manner but also the activity and expression of MMP-9 in MDA-MB-231 cell.

• Journal of Life Science
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• v.23 no.7
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• pp.904-912
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• 2013

This study aimed to evaluate the protective effect of cordycepin-increased Cordyceps militaris strain on carbon tetrachloride ($CCl_4$)-induced hepatotoxicity and oxidative stress in rats. Male Sprague-Dawley rats were randomly divided into five groups (n=6) based on six dietary categories: normal (N), $CCl_4$ control (C), $CCl_4$ plus Paecilomyces japonica (CPJ) (3%, w/w), $CCl_4$ plus C. militaris (CCM) (3%, w/w), and $CCl_4$ plus cordycepin-increased C. militaris ($CCM{\alpha}$) (3%, w/w). The activities of the liver marker enzymes ALT, AST, and LDH and the levels of lipid peroxidation were increased in the $CCl_4$-treated groups, but these parameters were significantly decreased in the $CCM{\alpha}$ group. The TBARS content in the liver homogenate, microsome, and mitochondrial fractions of the C group was significantly elevated compared with the N group. However, in the $CCl_4$-treated groups, $CCM{\alpha}$ group was significantly lowered in the TBARS levels of hepatic homogenate and microsomal fractions. The C group showed a significant decrease in the levels of plasma and hepatic glutathione, whereas they were significantly increased in the $CCM{\alpha}$ group. Accordingly, cordycepin-increased C. militaris may be an ideal animal model for studying hepatoprotective effects.

• Journal of the Korean Society of Food Science and Nutrition
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• v.25 no.5
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• pp.839-845
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• 1996

To investigate effects of Jujube methanol extract on the carbon tetrachloride-induced liver damage in rats, experimental animals were divided into 4 groups; control group(CON), Jujube methanol extracttreated group(JME), $CCl_4$- treated groups(CCl), and Jujube methanol extract and $CCl_4$-treated group (JMC). Each group was sacrificed after 2 or 4week feeding and determined the activities of serum transaminase(GOT, GPT) and hepatic xanthine oxidase, superoxide dismutase(SOD), catalase and glutathione peroxidase(GSH-Px), and hepatic contents of thiobarbituric acid-reactants(TBARS) and glutathione in liver. The activities of sGOT and sGPT, and the hepatic content of TBARS after $CCl_4$-treatment were markedly increased, compared to CON, but those levels were significantly decreased by the pretreatment of Jujube methanol extract, especially in sGOT after 2 and 4 week and TBARS after 4week respectively. Xanthine oxidase activity was increased by $CCl_4$- treatment as compared to CON, but it was also inhibited by the pretreatment of Jujube methanol extract for 2 and 4 week. The activities of SOD, catalase and GSH-Px were elevated by $CCl_4$-treatment, compared to CON, but those elevated activities were showed significant decreasing effect by pretreatment of Jujube methanol extract after 2 and 4week as compared to CON, however, hepatic catalase activity was not affected significantly. These results suggest that Jujube methanol extract is believed to be a possible protective effect for the carbon tetrachloride-induced hepatotoxicity in rats.

• Journal of Food Hygiene and Safety
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• v.34 no.4
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• pp.388-395
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• 2019

The object of the present study was to examine the effect of selenium-treated Spinacia oleracea L. on antioxidative defense system and oxidative damage in rats fed high-fat and high-cholesterol diets. Experimental rats were divided into six groups which were composed of normal diet group (N), high-fat and high-cholesterol diet group (HF), high-fat and high-cholesterol diet with 5% or 10% non-treated spinach supplemented group (SPA or SPB) and high-fat and high-cholesterol diet with 5% or 10% selenium-treated spinach-supplemented group (SSA or SSB). In the antioxidant enzyme activities of hepatic glutathione peroxidase and superoxide dismutase, activities increased in supplementation of non-treated or selenium-treated spinach groups compared to HF group. However, there was no significant difference in the activity of hepatic catalase among all experimental groups. The microsomal superoxide radical content of the SSB group was significantly reduced compared to the HF group. The mitochondrial carbonyl values of the SSB group were significantly reduced compared to the HF group. Thiobarbituric acid reaction substance (TBARS) values in RBC and liver were also reduced in non-treated or selenium-treated spinach-supplemented groups compared to the HF group. The hepatic TBARS values of the supplementation of selenium-treated spinach groups significantly decreased compared to the supplementation of non-treated spinach groups. These results suggest that selenium-treated spinach may reduce oxidative damage by the activation of antioxidative defense system in rats fed high-fat and high-cholesterol diets.

• Journal of Nutrition and Health
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• v.42 no.5
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• pp.415-422
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• 2009

The present study was conducted to investigate the effect of dietary supplementation of grape pomace on lipid peroxidation and related enzyme activities of rats fed high fat diet. Male Sprague-Dawley rats weighing about 90 g were assigned to 4 experimental groups of 8 rats on the basis of their body weight. The high fat diet contained additional 15% lard to AIN 93-based diet. Rats were fed experimental diets containing 5% grape pomace for 4 weeks. Dietary supplementation of grape pomace reduced serum concentration of lipid peroxide in rats fed high fat diet. Hepatic concentration of lipid peroxide tended to be lower by feeding grape pomace. Hepatic total glutathione content and GSH/GSSG ratio were increased by grape pomace feeding in normal or high fat diet groups. Hepatic superoxide dismutase activity of grape pomace group with high fat diet was induced significantly compared with high fat diet group without grape pomace. Hepatic catalase activity of high fat fed rats was induced by feeding grape pomace. Grape pomace diet increased glutathione-S-transferase and glutathione peroxidase activities in rat liver fed high fat. Hepatic glucose-6-phosphatase activity was not affected by dietary supplementation of grape pomace in rats fed high fat. These results suggest that dietary supplementation of grape pomace may alleviate lipid peroxidation through antioxidant effect in rats fed high fat.

• Journal of Nutrition and Health
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• v.23 no.1
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• pp.11-18
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• 1990

Sprague-Dawley male rats were fed the diet of p/s 4.0(soybean oil : I), p/s 0.08(Beef tallow : II) at the level of 15% fat until 8 weeks after weaning. I & II groups were divided into 4 sub-groups by diets with or without 0.3% butylated hydroxytoluene(BHT). 2-AAF was injected at the age of $5_{1/2}$, 6, $5_{1/2}$, 7 weeks. MFO system enzyme(cytochrome p-450, cytochrome p-450 reductase, cytochrome b5) activities and lipid peroxide were determined from isolated liver microsome. 2-AAF injected young rats had growth retardatiion. Lipid peroxide values were not influenced greatly by dietary fat, 2-AAF and BHT. Cytochrome p-450 contents were increased in I-BHT-AAF & II-AAF groups by 2-AAF and its contents were not affected by BHT. But cytochrome p-450 and cytochrome p-450 reductase were not increased in soybean oil diet ybean oil groups. Cytochrome b5 was not influenced by dietary fat, 2-AAF and BHT. Cytochrome p-450 and lipid peroxide, cytochrome p-450 reductase and cytochrome b5, which transfer to MFO system, appeared to have positive correlations(r=0.2474, r=0.2475, p<0.05) each other. This result suggests that MFO system metabolizing 2-AAF was influenced by dietary fats and BHT. 2-AAF induced growth retardation in young rats.

• Korean Journal of Food Science and Technology
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• v.31 no.3
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• pp.831-837
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• 1999

Ochratoxin A (OA), a naturally occurring mycotoxin, has been known to cause renal and hepatic lesion in human and animals. This study was carried out to investigate the modulation effects of antioxidant vitamins on OA-induced lipid peroxidation associated with oxidative damage. Vitamin C (10 mg/kg/day) and vitamin E (63.8 mg/kg/day) were administered by intraperitoneal (i.p.) injection to male ICR mice, and 1 hr later, OA which was dissolved in 0.1 M $NaHCO_3$, treated 4 mg/kg/day by i.p. injection. During 4 days repeated, and then measured superoxide dismutase (SOD) activity, catalase activity and malondialdehyde (MDA) formation in microsomes of liver and kidney. Additionally, the relationship between cell damage and modulation effects of antioxidant vitamins was evaluated by comet assay. Results were as followed; i) SOD, catalase activity and MDA level were significantly increased by OA treated, ii) SOD, catalase activity and MDA formation were significantly decreased by antioxidant vitamins combine treated, iii) blood cell damage associated with lipid peroxidation, induced by OA, also modulated by antioxidant vitamins. These results indicated that antioxidant vitamins might be used for prevention of renal and hepatic damage due to ochratoxicosis.

• Applied Biological Chemistry
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• v.46 no.3
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• pp.165-170
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• 2003

The antioxidative activity of antioxidative substances produced from several bacterial strains isolated from fermented foods were tested by $DPPH\;({\alpha},{\alpha}'-diphenyl-{\beta}-picrylhydrazyl)$ free radical scavenging activity. One of the strains showing the highest antioxidative activity was identified as Bacillus sp. based on the morphological, biochemical, physiological characteristics, and 16S rRNA sequence, and named FF-7. The most optimal medium condition for the production of antioxidative substance from Bacillus sp. FF-7 was 2% galactose as carbon source and l% tryptone as nitrogen source. The antioxidative substance produced from FF-7 in these cultural medium was also tested by in vitro experimental models, the peruxidation of linoleic acid and the peroxidation of rat tissues microsomes by using thiobarbituric acid (TBA) for assay of free malondialdehyde production. The antioxidative activity against lipid peroxidation of rat tissues microsomes was shown in the following order; brain 97.50% > heart 79.95% > kidney 77.84% > spleen 77.47% > testis 69.96% > liver 62.45%. The antioxidative substance produced from FF-7 on linoleic acid peroxidation by IBA method was effectively inhibited during four days, and 0.05% BHT (butylated hydroxytoluene) used comparative control was also effectively inhibited. Results showed that the highest antioxidative activity by DPPH method of antioxidative substance produced from Bacillus sp. FF-7 was obtained by supplementing 2% galactose as carton source and l% tryptone as nitrogen source in cultured medium, this substance effectively inhibited the formation of TBARS in brain microsome in vit개 system and in linoleic acid peroxidation.

• Journal of Life Science
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• v.25 no.5
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• pp.577-584
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• 2015

Orostachys malacophyllus grow on the old roofing tile or on the rock of mountain and is belong to Crassulaceae family. After air drying for Orostachys malacophyllus (OM), using the mixture of lactic acid bacteria (Lactobacillus bulgaricus, Streptococcus thermophilus, Lactobacillus acidophilus) was fermented (FOM). OM and FOM extracted using water (W), ethanol (E) and methanol (M) and were measured extracts yield, pH and Brix. Extracted OM and FOM were tested by in vitro experimental models of α,α´-diphenyl-β-picrylhydrazyl (DPPH) radical scavenging activity, Fe/Cu reducing power, linoleic acid peroxidation using ferric thiocyanate and thiobarbituric acid (TBA) methods and peroxidation of rat liver homogenate. In addition, the bioactive materials (phenolic compounds, flavonoids and minerals) were measured. The highest phenolic compounds and flavonoids were OME 122.2 mg/100 g and OME 84.0 mg/100 g. OM and FOM′s major minerals were K, Ca and Mg. The highest free radical scavenging activity showed in FOMM (93.9%), OMM (93.4%), FOME (92.1%) and OME (91.9%) at 0.5% additional level. Fe reducing powers were strong in FOME and FOMM and Cu reducing powers were strong in OME and FOMM. Antioxidant activities on lipid peroxidation using rat homogenate as measured by TBARS method showed strong in FOME and on lipid peroxidation of linoleic acid as measured by ferric TBA method showed strong in OME and FOME and measured by ferric thiocyanate showed strong in FOME and FOMM.