The differences in pharmacokinetic behavior and tissue distribution of verapamil and its enantiomers were investigated in rats. In high-performance liquid chromatographic method, an achiral ODS column (150 mm $\times$ 4.6 mm i.d.) with the mobile phase consisting of methanol-water (73:30, v/v) was used for the determination of the concentration for racemic verapamil, and a Chiralcel OJ column (250 mm$\times$4.6 mm i.d.) with the mixture of n-haxane-ethanol-triethylamine (85:15:0.2, v/v/v) as mobile phase was used to determine the concentrations of verapamil enantiomers. A fluorescence detector in the analytical system was set at excitation and emission wavelengths of 275 nm and 315 nm. The differences between enantiomers were apparent in the pharmacokinetics in rats. The area under the concentration-time curve (AUC) of S-(-) verapamil was higher than that of R-(+) verapamil. The half-distribution time ($T_{1/2(\alpha)}$) of S-(-) verapamil which distributing to tissue from blood was shorter than that of R-(+) verapamil, but the elimination half-time ($T_{1/2(\beta)}$) was longer in rat following oral administration of racemic verapamil. At 1.3 h after oral administration of racemic verapamil, however, there were no significant differences between enantiomers for the distributions in major tissues such as heart, cerebrum, cerebellum, liver, spleen and kidney.
Objectives : Oxidative stress seems to play a major role in mechanisms by which ethanol causes liver injury. Previous studies have shown that treatment with Yinjinchunggan-tang (Yinchenqinggan-tang, YJCGT) has protective effects on alcoholic liver disease. The aim of this study was to investigate the protective effects of YJCGT on alcohol-induced oxidative stress. Materials and Methods : In vitro, we evaluated the inhibitory activities of YJCHT on DPPH(1,1-diphenyl-2-picryl-hydrazyl), xanthine oxidase, trypsin, and hyaluronidase. In a cell culture model, we measured cell viability and proliferation, and the activities of superoxide dismutase (SOD), and catalase (CAT) after YJCGT treatment in C34 and E47 cell lines, and HepG2 cells transfected with/ without cytochrome P450IIE1 (CYP2E1) gene. In vivo, we estimated serum level of hepatic biochemical markers, and alcohol concentration in the blood. Results : YJCGT showed significant free radical scavenging activity against DPPH and xanthine oxidase and decreased hyaluronidase activity effectively in vitro. YJCGT also increased cell viability, and proliferation in C34 and in E47 cell lines, and increased activities of superoxide dismutase, and catalase in C34 and in E47 cell lines. YJCGT reduced serum AST, LDH, and total cholesterol level in some of the results, and reduced blood alcohol concentration in vivo, as well. Conclusions : This study suggests that YJCGT has protective effects on oxidative stress by inhibiting alcohol-induced suppression of antioxidant enzyme activities.
Increased consumption of fresh vegetables that are high in polyphenols has been associated with a reduced risk of oxidative stress-induced disease. The present study aimed to evaluate the antioxidant effects of spinach in vitro and in vivo in hyperlipidemic rats. For measurement of in vitro antioxidant activity, spinach was subjected to hot water extraction (WE) or ethanol extraction (EE) and examined for total polyphenol content (TPC), oxygen radical absorbance capacity (ORAC), cellular antioxidant activity (CAA), and antigenotoxic activity. The in vivo antioxidant activity of spinach was assessed using blood and liver lipid profiles and antioxidant status in rats fed a high fat-cholesterol diet (HFCD) for 6 weeks. The TPC of WE and EE were shown as $1.5{\pm}0.0$ and $0.5{\pm}0.0mg$ GAE/g, respectively. Increasing the concentration of the extracts resulted in increased ORAC value, CAA, and antigenotoxic activity for all extracts tested. HFCD-fed rats displayed hyperlipidemia and increased oxidative stress, as indicated by a significant rise in blood and liver lipid profiles, an increase in plasma conjugated diene concentration, an increase in liver thiobarbituric acid reactive substances (TBARS) level, and a significant decrease in manganese superoxide dismutase (Mn-SOD) activity compared with rats fed normal diet. However, administration of 5% spinach showed a beneficial effect in HFCD rats, as indicated by decreased liver TBARS level and DNA damage in leukocyte and increased plasma conjugated dienes and Mn-SOD activity. Thus, the antioxidant activity of spinach may be an effective way to ameliorate high fat and cholesterol diet-induced oxidative stress.
Journal of the Korean Society of Food Science and Nutrition
/
v.22
no.6
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pp.664-672
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1993
The purpose of this study was to investigate the effect of alcohol administration on selenium concentration and cell morphology in tissurs of rats fed with the different levels of selenium (Se) and vitamin E. Seventy two male rats of Sprague-Dawley strain weighing about 58~62g were divided into 12 groups. The dietary Se levels were 0mg(L-), 0.4mg(C-) and 10mg(H-), and the dietary vitamin E levels were 0mg(-L) and 150mg(-C) per kg diet, respectively. Alcohol-adminstrated groups(--A) received the triple distilled potable water solution containing 10% of ethanol from the 3rd week of experimental periods. The obtained experimental results are summarized as follows. Se concentration in blood and urine made difference in accordance with Se level in diet and tended to be low in alcohol administrated groups. Se concentration in liver and kidney was also directly proportional to the dietary Se level, and it tended to be low in each alcohol group, but Se concentration in kidney tended to be increased by alcohol administration. Myocardium in rats showed lysosome increasing, fat droplet, mitochondrial swelling, and in particular, bad intracellular edema, in H-group fed with high Se and in L-group with low Se. It also showed such phenomena in the alcohol administrated group. In HC-group fed with excessive Se and normal vitamin E. there appeared no noticeable change in liver tissue. However, in the alcohol administrated HCA-group, there came out fat droplet. Especially, in the alcohol administrated LLA-group, not fed with sufficient Se and vitamin, E, there were found lysosome increasing and a number of fat droplet.
This study was undertaken to investigate effects of alcohol and fat content in a balanced diet on growth, hepatic function and some biochemical indices of blood in growing rats. Fourty eight male rats of Sprague-Dawley strain weighing about 160g were divided into 4 groups ; high fat diet group, alcohol-adminstered high fat diet group, low fat diet group and alcohol-administered low fat diet group. High and low fat diet supplied 30% and 12%, respectively, of total calorie intake from fat and alcohol-treated groups received water containing 10% ethanol. Diets contained adequate amounts of all nutrients required for rats, including lipotropic agents(choline and methionine) to minimize effects of factors other than alcohol on liver function. Growth rate was lowest in alcohol-administered low-fat diet group, despite that their energy intake was equivalent to the others. For a 3-week study period, 21.86% and 23.61% of total calorie intake were derived from alcohol in alcohol-adminitered high fat diet group and low fat diet group, respectively. There was no influenced on vitamin B$_1$ status by alcohol consumption. Concentration of triglyceride in plasma increased with alcohol comsumption, and the effect was greater after 6 weeks than after 3 weeks of alcohol consumption . Difference of dietary fat content did not affect the level of triglyceride . The levels of total cholesterol and HDL-cholesterol in plasma were not influenced by alcohol consumption. Serum glutamate pyruvate transaminase activity and hepatic mitochondrial respiration rate did not differ between groups. The results indicate that neither moderate alcohol drinking for 6 weeks nor fat content with a balanced diet caused any dramatic change of metabolism and liver function in rats. However they suggest that even moderate alcohol consumption can affect growth of animals dramatically and the effect may be lessened with relatively high fat content in diet.
Kim, Ah-Rong;Jeong, Soo-Mi;Kang, Min-Jung;Jang, Yang-Hee;Choi, Ha-Neul;Kim, Jung-In
Nutrition Research and Practice
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v.7
no.3
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pp.166-171
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2013
The purpose of this study was to investigate the effects of lotus leaf on hyperglycemia and dyslipidemia in animal model of diabetes. Inhibitory activity of ethanol extract of lotus leaf against yeast ${\alpha}$-glucosidase was measured in vitro. The effect of lotus leaf on the postprandial increase in blood glucose levels was assessed in streptozotocin-induced diabetic rats. A starch solution (1 g/kg) with and without lotus leaf extract (500 mg/kg) was administered to the rats after an overnight fast, and postprandial plasma glucose levels were monitored. Four-week-old db/db mice were fed a basal diet or a diet containing 1% lotus leaf extract for 7 weeks after 1 week of acclimation to study the chronic effect of lotus leaf. After sacrifice, plasma glucose, insulin, triglycerides (TG), total cholesterol (CHOL), high-density lipoprotein (HDL)-CHOL, and blood glycated hemoglobin levels were measured. Lotus leaf extract inhibited ${\alpha}$-glucosidase activity by 37.9%, which was 1.3 times stronger than inhibition by acarbose at a concentration of 0.5 mg/mL in vitro. Oral administration of lotus leaf extract significantly decreased the area under the glucose response curve by 35.1% compared with that in the control group (P < 0.01). Chronic feeding of lotus leaf extract significantly lowered plasma glucose and blood glycated hemoglobin compared with those in the control group. Lotus leaf extract significantly reduced plasma TG and total CHOL and elevated HDL-CHOL levels compared with those in the control group. Therefore, we conclude that lotus leaf is effective for controlling hyperglycemia and dyslipidemia in an animal model of diabetes mellitus.
Journal of the Korean Society of Food Science and Nutrition
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v.38
no.11
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pp.1499-1505
/
2009
This study investigated the effect of improved liver function in rats administered with ethanol by kimchi lactic acid bacteria with high GABA producing capacity. Sprague-Dawley male rats were divided into four groups; normal diet control (NC), ethanol control (EC), ethanol+Lactobacillus sp. OPK2-59 normal powder (EL1), ethanol+Lactobacillus sp. OPK2-59 GABA powder (EL2) and fed for 6 weeks. Analysis showed that there were no significant differences in body weight and feed consumption among the groups during the experimental period. Also, there were no significant differences in organ weight among the groups. The test results showed total cholesterol and triglyceride in the blood concentration that were increased by ethanol administration were significantly lowered in EL2 group. Liver triglyceride was also significantly lowered in the EL2 group compared with the EC group. Serum GOT and GPT, and liver GOT levels were significantly lower in the EL2 group compared with the EC group. Serum ethanol concentration was lower in the EL1 and EL2 groups compared with the EC group. SOD activities in liver were significantly increased in the EL1 and EL2 groups compared with the EC group. These results suggest that Lactobacillus sp. OPK2-59 GABA powder improves lipid and enzyme profiles of rats administered with ethanol.
Journal of the Korea Academia-Industrial cooperation Society
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v.18
no.2
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pp.218-225
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2017
To investigate the anti-hangover effects of Cudrania tricuspidata root extract (CTE), the blood alcohol metabolism and blood gas imbalance of CTE in rats treated with 10 ml/kg alcohol were examined. CTE (500 mg/kg and 750 mg/kg) was administrated after 30 minutes of alcohol consumption (10 ml/kg). Blood collection was implemented from the tails of the animals after 1, 3, and 5 hours post alcohol consumption. The Condition drink (a commercial anti-hangover beverage) was used as a positive control. Single administration by the oral route was performed. The consumption of CTE (500 mg/kg and 750 mg/kg) decreased the serum alcohol concentration by increasing and maintaining both the alcohol dehydrogenase (ADH) and acetaldehyde dehydrogenase (ALDH) enzyme activity levels in the blood and liver. In addition, CTE led to recovery from the imbalances in the blood gas levels, including carbon dioxide ($CO_2$) and changes in pH, bicarbonate ($HCO_3{^-}$) and lactic acid levels due to alcohol ingestion. In conclusion, CTE exerted a more pronounced anti-hangover effect than a commercial anti-hangover drink. Therefore, CTE can be a novel and safe anti-hangover natural product agent for the prevention or treatment of symptoms caused by excessive alcohol consumption.
Radiotherapy is an irreplaceable method of cancer treatment but, it has various side effects, especially damage to the hemopoietic system. A lot of radioprotectors have been found but they also have toxic effects. Many kinds of crude drugs(Oriental Chinese medicine)with low toxicity have been reported to promote the recovery from radiation damage. Recently, the trial to combine radiotherapy with herbal treatment of cancer patients shows a desirable result, an enhancement in recovery of the blood system.. This study was performed to determine whether prescriptions to support the healthy energy and strengthen the body resistence, Buzhongyiqi-tang and Siliu-tang, promote the recovery of splenocytes of N:GP(s) mice from radiation damage. We investigated the proliferative effect of Buzhongyiqi-tang, Siliu-tang and EIB(ethanol insoluble fraction of Buzhongyiqi-tang) on N:GP(S)mice splenocytes before or after ${\gamma}$-irradiation. We also investigated the morphology of splenocytes cultured with these herbs. Buzhongyiqi-tang and Siliu-tang promoted the proliferation of splenocytes in a concentration of 0.1 mg/ml compared with normal control(p<0.001). After 1-5Gy of ${\gamma}$-irradiation they also showed the effect of recovery of hemopoietic cells, especially in Buzhongyiqi-tang(4Gy:p<0.005; 5Gy:p<0.05). In addition, EIB(ethanol insoluble fraction of Buzhongyiqi-tang) showed the highest proliferative effect of all agents suggesting that more effective fractions could be found from crude herbs or prescriptions. These results suggest that it is possible to make use of Buzhongyiqi-tang, Siliu-tang or EIB as radio-protective agents.
Ganoderma lucidum has been traditionally used as a medicine for treatment of bronchitis, arthritis, and high blood pressure, and it has been reported to display many biological activities including anticancer and immune activities. Since mushroom mycelium is known to have excellent biological activities together with mushroom fruiting body, studies on biological activities of mushroom mycelium have been actively conducted. Thus, the present study compared the biological activities before and after the cultivation of Ganoderma lucidum mycelium on Atractylodes rhizoma. When the radical scavenging activity was assessed by the DPPH assay, ARGL (ethanol extract of Atractylodes rhizoma mycelium fermented with Ganoderma lucidum) showed radical scavenging activity of 5.58~82.56% at concentrations of $10{\sim}500{\mu}g/assay$, while AR (ethanol extract of Atractylodes rhizoma) showed radical scavenging activity of 5.27~72.08% at the same concentrations. When measured by using the ABTS assay, ARGL showed higher radical scavenging activity than AR, which was consistent with the result obtained by the DPPH assay. In the MTT assay, the cytotoxicity of ARGL against all cell lines was higher than that of AR. In particular, the cytotoxicities of AR and ARGL against Hep3B at a concentration of $400{\mu}g/assay$ were 71.81% and 86.40%, respectively. In addition, the result obtained by the SRB assay was consistent with the result obtained by the MTT assay. According to the results mentioned above, there is a high probability that medicinal herb cultures using mycelium can be used as sources of functional foods since the cytotoxicities against cancer cells and antioxidant activities increased when the mycelium was fermented with Atractylodes rhizoma.
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