• Biomolecules & Therapeutics
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• v.23 no.2
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• pp.201-206
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• 2015

Scutellaria baicalensis is one of the most widely used herbal medicines in East Asia. Because baicalein and baicalin are major components of this herb, it is important to understand the effects of these compounds on drug metabolizing enzymes, such as cytochrome P450 (CYP), for evaluating herb-drug interaction. The effects of baicalin and baicalein on activities of ethoxyresorufin O-deethylase (EROD), methoxyresorufin O-demethylase (MROD), benzyloxyresorufin O-debenzylase (BROD), p-nitrophenol hydroxylase and erythromycin N-demethylase were assessed in rat liver microsomes in the present study. In addition, the pharmacokinetics of caffeine and its three metabolites (i.e., paraxanthine, theobromine and theophylline) in baicalin-treated rats were compared with untreated control. As results, EROD, MROD and BROD activities were inhibited by both baicalin and baicalein. However, there were no significant differences in the pharmacokinetic parameters of oral caffeine and its three metabolites between control and baicalin-treated rats. When the plasma concentration of baicalin was determined, the maximum concentration of baicalin was below the estimated $IC_{50}$ values observed in vitro. In conclusion, baicalin had no effects on the pharmacokinetics of caffeine and its metabolites in vivo, following single oral administration in rats.

• Journal of the Korean Society of Food Science and Nutrition
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• v.46 no.9
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• pp.1128-1136
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• 2017

Previous studies of the caffeine consumption pattern were limited primarily to beverages containing caffeine. Therefore, this study examined the caffeine consumption patterns and levels in beverages and foods containing caffeine among high school students (n=310) in the Yongin region. The participants included 171 boys (55.2%) and 139 girls (44.8%). The daily mean caffeine intake of the respondents was 41.27 mg (0.651 mg/kg) and 36.47 mg (0.696 mg/kg) in boys and girls, respectively. Among the caffeinated food groups, coffee had the highest caffeine intake group in both boys (18.95 mg) and girls (26.28 mg). Girls consumed large amounts of caffeine in the form of Americano-style coffee (20.04 mg), whereas boys consumed more canned coffee (6.77 mg) than girls (2.43 mg, P<0.01). Carbonated soft drinks were the second most prevalent source of caffeine intake in both groups, even though boys (14.29 mg) consumed larger amounts of caffeine than girls (5.85 mg, P<0.001). Multiple regression analysis investigating the major contributing food group to daily total caffeine intake also showed that the highest standardized coefficient was in coffee regardless of gender (boys 0.492, P<0.001 and girls 0.944, P<0.001), followed by carbonated soft drinks and energy drinks. Approximately 95% of high school students consumed normal levels of caffeine, whereas 3.5% of boys and 5.8% of girls consumed excessive amounts based on the standard limit of Korea Food and Drug Administration (<2.5 mg/kg/d) for adolescents. The daily mean caffeine intake of the excess group was 5.38 mg/kg and 6.96 mg/kg in boys and girls, respectively. Consequently, safe daily caffeine intake needs to be determined throughout continuous national management guidelines and nutritional education.

• The Journal of Pediatrics of Korean Medicine
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• v.9 no.1
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• pp.221-236
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• 1995

In order to investigate the anticonvulsive effect of Jinkyungondamtang, the experiment were performed in mice. After solid exract of Jinkyungondamtang was orally administered to mice, four types of convulsion were induced in mice by electric shock, strychnine, picrotoxin, and caffeine. Each of the time to elicit the convulsion and to die was observed. Results were as follows: 1. In the case of convulsion induced by electric shock, the lapse of the time to elicit convulsion and the time to die were delayed by oral administration of Jinkyungondam-tang(P<0.05, P<0.025). 2. The solid extracts of Jinkyungondamtang were revealed rem- arkable effect in delaying the time to die induced by stry-chnine (P<0.05). 3. By oral administration of Jinkyungondamtang, the lapse of the time to elicit convulsion and to die were delayed significantly to elicit convulsion inducing by picrotoxin (P<0.05, P<0.05). 4. Considerable prolongation of the lapse of the time to elicit the convulsion was observed in convulsion induced caffeine due to the anticonvulsive effects of Jinkyungondamtang (P<0.05).

• Journal of Ginseng Research
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• v.40 no.4
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• pp.375-381
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• 2016

Background: We evaluated the drug interaction profile of Red Ginseng (RG) with respect to the activities of major cytochrome P450 (CYP) enzymes and the drug transporter P-glycoprotein (P-gp) in healthy Korean volunteers. Methods: This article describes an open-label, crossover study. CYP probe cocktail drugs, caffeine, losartan, dextromethorphan, omeprazole, midazolam, and fexofenadine were administered before and after RG supplementation for 2 wk. Plasma samples were collected, and tolerability was assessed. Pharmacokinetic parameters were calculated, and 90% confidence intervals (CIs) of the geometric mean ratios of the parameters were determined from logarithmically transformed data using analysis of variance after RG administration versus before RG administration. Results: Fourteen healthy male participants were evaluated, none of whom were genetically defined as poor CYP2C9, 2C19, and CYP2D6 metabolizers based on genotyping. Before and after RG administration, the geometric least-square mean metabolic ratio (90% CI) was 0.870 (0.805-0.940) for caffeine to paraxanthine (CYP1A2), 0.871 (0.800-0.947) for losartan (CYP2C9) to EXP3174, 1.027 (0.938-1.123) for omeprazole (CYP2C19) to 5-hydroxyomeprazole, 1.373 (0.864-2.180) for dextromethorphan to dextrorphan (CYP2D6), and 0.824 (0.658-1.032) for midazolam (CYP3A4) to 1-hydroxymidazolam. The geometric mean ratio of the area under the curve of the last sampling time ($AUC_{last}$) for fexofenadine (P-gp) was 0.963 (0.845-1.098). Administration of concentrated RG for 2 wk weakly inhibited CYP2C9 and CYP3A4 and weakly induced CYP2D6. However, no clinically significant drug interactions were observed between RG and CYP and P-gp probe substrates. Conclusion: RG has no relevant potential to cause CYP enzyme- or P-gp-related interactions.

• Journal of the Korean Home Economics Association
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• v.25 no.1
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• pp.51-58
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• 1987

This study was undertaken to investigate changes in blood pressure and heart rate in normal cats by administration of Korean native green tea. The chemical components of Korean native green tea which determined are water(2.2%), water extract(32.7%), vitamin C(480%), caffeine(2.6%), tannin(32.7%) and amino acid of water soluble content 5.8%. Effect on blood pressure in administration 100mg/kg, 300mg/kg, 500mg/kg of extract of green tea, the mean depressor response is 44.8$\pm$3.3mmHg, 60.5$\pm$3.6mmHg, and 65.0$\pm$3.3mmHg in normal cats. Effect on heart rate in administration 100mg/kg, 300mg/kg of extract of Korean native green tea, the mean decreased heart rate is 2.8$\pm$4.5 beats/min, 15.2$\pm$6.4beats/min and 19.1$\pm$4.0 beats/min.

• Journal of Physiology & Pathology in Korean Medicine
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• v.30 no.2
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• pp.88-94
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• 2016

The study was carried out to examine the anti-obesity effects of 40% ethanol extract from green tea seed (GS) and quantitative determination of caffeine as its major compound. The specificity was satisfied with retention time and UV spectrum by analysis of caffeine using HPLC and comparison with standard compound. It showed a high linearity in the calibration curve with a coefficient of correlation (R²) of 0.9974. The amount of caffeine in GS was about 4.649 mg/g (0.465%) in the three times analysis, and relative standard deviation (RSD) was less than 0.452% by the validated method. The anti-obesity effects of GS were evaluated by using Oil Red O staining in 3T3-L1 adipocytes and body weight, visceral fat and lipid profiles in high fat diet (HFD)-induced C57BL/6 obese mice. Our results indicated that treatment with GS dose-dependently decreased lipid accumulation contents (p<0.001). Moreover, after oral administration for 30 days feeding with HFD-induced obses mice, GS (100 and 300 mg/kg/day) produced a significant decrease in serum total cholesterol (TC), glutamic oxaloacetic transaminase (GOT), glutamic pyruvic transaminase (GPT) and visceral fat. Thus, the result of this study indicate that the GS may be a useful resource for the management of obesity.

• The Korean Journal of Physiology and Pharmacology
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• v.1 no.3
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• pp.325-335
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• 1997

Evidence for the existance of at least two subclasses of renal adenosine receptors has been presented. N-6-cyclohexyladenosine (CHA) is a relatively selective $A_1$ adenosine agonists, whereas 5'-N-ethylcarboxamidoadenosine (NECA) acts as a preferential agonist of $A_2$ adenoisne receptor. N6-(L-2-phenylisoproryl)-adenosine (PIA) almost unselectively activates both $A_1\;and\;A_2$ adenosine receptors at micromolar concentrations. During the characterization of adenosine receptor in the kidney, we have discovered a novel phenomenon, that is, an intramuscular administration of CHA for 3 days caused a diuresis and a suppression of urinary concentrating ability. To further characterize this novel phenomenon, an intramuscular administration of adenosine and other adenosine angonists, PIA and NECA, and prior treatment of adenosine antagonists, caffeine, theophylline and 1,3-diethyl-8-phenyl-xanthine (DPX) were performed. Systemic administration of CHA, PIA, and NECA for 3 days caused a suppression in heart rate, blood pressure and general motor activity without change in rectal temperature. Systemic administration of CHA, 0.5, 1 and 2 mg/kg/day, for 3 days caused a dose-dependent increase in urine volume and decrease in urinary osmolarity and free water reabsorption. This phenomenon was reversible and repeatable. Administration of adenosine (40 mg/kg/day) produced no apparent effect on the renal function, whereas PIA (2 mg/kg/day) produced an similar effect to CHA on the renal function. Systemic adminstration of NECA, 0.025, 0.05 and 0.25 mg/kg/day, for 3 days caused a dose-dependent increase in urine volume and dose-dependent increases in excreted amount of creatinine, urinary osmolarity and free water reabsorption. These renal effects of adenosine agonist were maximum at second day during the drug administration. In terms of increase in urine volume and the suppression of urinary concentrating ability, NECA was potent than CHA. Prior treatment of caffeine (50 mg/kg/day) or theophylline (50 mg/kg/day) abolished the diuretic effect of CHA, whereas DPX (50 mg/kg/day) did not affect the CHA effect. CHA, 0.5 mg/kg/day, produced no change in plasma renin activity and plasma levels of aldosterone, epinephrine, and norepinephrine. These results suggest that this novel phenomenon produced by an activation of renal adenosine receptors plays an important role in urinary concentrating mechanism.

• Biomolecules & Therapeutics
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• v.25 no.4
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• pp.390-395
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• 2017

The present study investigated the sedative effects of Sophora flavescens (SF) and its bioactive compound, matrine through performing locomotor activity test and the electroencephalography (EEG) analysis in the rat. The underlying neural mechanism of their beneficial effects was determined by assessing c-Fos immunoreactivity and serotonin (5-HT) in the brain utilizing immunohistochemical method and enzyme-linked immunosorbent assay. The results showed that SF and matrine administration had an effect on normalization of caffeine-induced hyperactivity and promoting a shift toward non-rapid eye movement (NREM) sleep. c-Fos-immunoreactivity and 5-HT level in the ventrolateral preoptic nucleus (VLPO), a sleep promoting region, were increased in the both SF and matrine-injected groups. In conclusion, SF and its bioactive compound, matrine alleviated caffeine-induced hyperactivity and promoted NREM sleep by activating VLPO neurons and modulating serotonergic transmission. It is suggested that SF might be a useful natural alternatives for hypnotic medicine.

• Journal of Pharmaceutical Investigation
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• v.27 no.3
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• pp.181-187
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• 1997

The purpose of this work was to investigate pharmacokinetics of alcohol as a function of dose and time of administration of ethanol. The pharmacokinetics of alcohol 15 min after and before oral administration of aspartate-containing compositions to rats were also evaluated. The retention time of acetaldehyde, alcohol and isopropyl alcohol an internal standard in gas chromatogram was 3.6, 6.0 and 10.5 min, respectively. The maximum concentration of alcohol $(C_{max})$ and area under the blood concentration (AUC) were significanly increased as a function of ethanol dose in a nonlinear fashion. The significant diurnal variation of alcohol pharmacokinetics was also noted, showing fast metabolism and elimination when given orally in the night time. When APAP was given after administration alcohol (1g/kg) to rats, AUC and $C_{max}$ were increased when compared to alcohol only. However, AUC and $C_{max}$ were decreased when aspartate or standard complex compositions containing aceaminophen (APAP, 250mg). sodium L-aspartate(25 mg), dl-methionine (125 mg) and anhydrous caffeine (25 mg) was orally given by coupling malate/asparate shuttle in hepatocyte. The blood alcohol concentration profiles between aspartate and standard complex compositions were similar when given before or after administration alcohol (1g/kg) to rats. No significant difference of administration sequence was observed. However, it was noted that AUC and $C_{max}$ of standard complex compositions given before alcohol administration were significantly lower when compared with alcohol only. Based on these findings, dose, time of administration and composition of drugs to improve alcohol metabolism and elimination were considered to be important in the pharmacokinetics of alcohol. The administration sequence of drug compositions and alcohol might be also considerd.

• Nutrition Research and Practice
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• v.13 no.1
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• pp.70-75
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• 2019

BACKGROUND/OBJECTIVES: Association between the consumption of sugar-sweetened beverages (SSBs) and obesity is universally a controversial issue. This study was undertaken to examine the beverage consumption pattern of Korean adolescents. SUBJECTS/METHODS: Data was collected from the 2016 Korea Youth Risk Behavior Survey involving 65,528 adolescent respondents. A list of the most frequently consumed beverages was analyzed, and the consumption frequency of carbonated beverages, SSBs, and energy drinks during the past seven-days was assessed. The main reasons for the adolescents to consume the beverages were also determined. RESULTS: The beverage preference of adolescents were carbonated beverages (31.0%), 'fruit and vegetable beverages (17.7%)', 'milk (13.6%)', and 'coffee (12.7%)'. Carbonated beverages and SSBs were consumed more than three times a week by 27.1% and 41.1% of the respondents, respectively. About 86.2% of adolescents did not take of any energy drinks during the last seven-days. Taste was the most common reason that adolescents considered when choosing a drink. Carbonated beverages consumed more frequently by boys than girls, and high school students drank coffee more frequently than middle school students. CONCLUSIONS: Boys had a higher preference for unhealthy beverages than girls, whereas consumption of high-caffeine drinks was greater amongst high-school students than middle school students.