In cancer chemotherapy, it is necessary to control the phamacokinetic behavior of an antitumor drug for effective treatment. Therefore, two 5-fluorouracil derivatives synthesize d with N-a-cyloxycarbonyl derivatives {1-(N-t-butyloxycarbonyl)leucyloxymethyl-5-FU(BLFU) and 1-(N-t-carbobenzyloxymethyl)leucyloxymethyl-5-FU(CLFU)}. prodrugs of 5-fluorouracil, antitumor agent, were loaded into liposome of different lipid compositions. After liposomal drugs were injected intramuscularly, their pharmacokinetics and tissue distribution were assessed. The $AUC_{0{\to}{\infty}$ values were 1.29, 72.50, 85.57, 66.40 and 103.60${\mu}$g.hr/ml for 5-FU, BLFU, CLFU, BLFU- and CLFU-loaded liposome, respectively. 5-FU was distributed to spleen and liver with a maximal concentration after 1 hr and eliminated after 24 hr. But both prodrugs and dimyristoylphosphatidylcholine liposome entrapped prodrugs were distributed to spleen and liver at a lower concentration but maintained for a long time with a relatively high concentration in lung. Especially, liposome-entrapped CLFU was distributed to lung with a maximal concentration after 1 hr and redistributed to spleen increasingly, while the concentration of liposome-entrapped BLFU in lung reached a maximal level after 12 hr.
In HL-60 cells, extracellular A TP increases intracellular $Ca^{2+}$ ([Ca$^{2+}$]$_{i}$) in a concentration-dependent manner with the maximal response occurring around 10 $\mu$M. However, above the maximal responsive concentration ATP elicits different patterns of $Ca^{2+}$ signaling.(omitted)d)
Maximal oxygen debt, lactate and excess lactate were measured in 13 men with low hematocrit ratio before and after maximal exercise. Maximal exercise run was performed on a treadmill and the duration of run was 2 minutes 45 seconds in each subject. Hematocrit ratio ranged between 35 and 47%, the mean being 39.8%. The following results were obtained. 1. Maximal oxygen debt expressed on basis of body weight increased as the hematocrit ratio decreased. The correlation coefficient between the two was r= -0.770. 2. The time necessary for decreasing to 50% of total maximal $O_2$ debt(half time) became longer as the hematocrit ratio decreased. In normal men the half time was about 4 minutes and at the longest it was 12 minutes in men with the lowest hematocrit ratio. 3. The lactate concentration reached its peak value after 3 minutes of recovery. Thereafter, the time course of decrease in lactate concentration coincided roughly with that of respiratory oxygen debt curve. To reach to the resting level, however, it took longer time than that of respiratory oxygen debt. 4. Resting concentrations of lactate was 1.28 mM/l, pyruvate 0.13 mM/l and L/P ratio was 9.8. Peak value of ${\Delta}L$ after exercise reached to the value of 10.4 mM/l and ${\Delta}L/P$ reached 26.0. Peak excess lactate after exercise was 6.34 mM/l. 5. The part of oxygen debt accounted for by the oxygen equivalent of excess lactate was only 38.4%. A better relationship between lactate and oxygen debt was observed and the part of oxygen debt accounted for by the oxygen equivalent of lactate was 63.3%. 6. Peak value of lactate after maximal exercise increased as the hematocrit ratio decreased. 7. Respiratory oxygen debt of 100 ml/kg was accounted for by lactate more than 60% and only 30% was by excess lactate. 8. Excess lactate was not a good index of respiratory oxygen debt.
[Purpose] The combined effect of different types of post-exercise treatment has not been fully explored. We investigated the effect of combined cold water immersion (CWI) and compression garment (CG) use after maximal eccentric exercise on maximal muscle strength, indirect muscle damage markers in the blood, muscle thickness, and muscle soreness score 24 h after exercise. [Methods] Ten men performed two trials (CWI + CG and CON) in random order. In the CWI + CG trial, the subjects performed 15 min of CWI (15℃), followed by wearing of a lower-body CG for 24 h after exercise. In the CON trial, there was no post-exercise treatment. The exercise consisted of 6 × 10 maximal isokinetic (60°·s-1) eccentric knee extensions using one lower limb. The maximal voluntary contraction (MVC) and maximal isokinetic (60°·s-1) strength during knee extension, as well as the indirect muscle damage markers, were evaluated before exercise and 24 h after exercise. [Results] The maximal muscle strength decreased in both trials (p < 0.001), with no difference between them. The exercise-induced elevation in the myoglobin concentration tended to be lower in the CWI + CG trial than in the CON trial (p = 0.060). The difference in the MVC, maximal isokinetic strength, muscle thickness, and muscle soreness score between the trials was not significant. [Conclusion] CWI followed by wearing of a CG after maximal eccentric exercise tended to attenuate the exercise-induced elevation of indirect muscle damage markers in the blood.
The organ distribution of mercury was examined in the rat after oral administration of a single dose of red mercuric sulfide (15mg Hg/kg). The concentration of total mercury in the organs and blood after 2, 4, 6, 8, 12, 24 and 72 hours of administration was determined by Quartz Tube Combustion-Gold Amalgamation Method. It was found that the maximal concentration of total mercury was in the kidneys and muscle within 24 hours and in the brain, heart, liver and blood within 48 hours. The descending order of the maximal organ and blood concentration was: kidneys(1.08ppm)>blood> muscle>heart>liver>brain. The accumulation states of total mercury in the rat organs were investigated by continuous administration of red mercuric sulfide (5mg Hg/kg/day) for 15 days. The mercury concentration increased progressively throughout the experimental period and the descending order of the highest level of mercury after 15 days was: kidneys (1.55ppm)>blood>liver. The concentration of alkyl mercury in brain, liver and kidneys also was measured after 7 and 15 days of consecutive administration of red mercuric sulfide (5mg Hg/kg/day). The concentration in the Kidneys and the liver was very low, but was significantly different from control group. The concentration in the brain was extremely low and was not significantly different from control group.
To establish the protocol of a standardized exercise test for evaluating exercise intolerance and degree of fitness in Thoroughbred racehorses, we examined serum lactate concentrations related to exercise intensities using the high speed treadmill. Twelve clinically healthy Thoroughbred racehorses with or without previous training or racing history were assigned to two gorups, fit and unfit group, respectively. The protocol used for the standardized exercise test was consisted of two stages : stage of warm-up and that of acceleration. During the warm-up, the horses exercised 5 min at 1.8m/s and 3 min 3.4m/s without inclination. At the acceleration stage, exercise test was performed at 10% slope and the speed was increased from the initial 5m/s to the maximal speed which each tested horse could keep up with. The speed was increased with incremental steps of 1 m/s every minute. During the last 15 sec of each step, blood samples were collected for serum lactate determination. $V_{max}$(maximal treadmill speed which tested horses could keep up with) of the fit group ($10.93{\pm}0.33m/s$, mean${\pm}$SE, n = 6) was higher than that of the unfit group ($9.52{\pm}0.23m/s$, mean${\pm}$SE, n = 6). Serum lactate concentrations increased exponentially according to exercise intensities. $V_{La4}$(speed producing a serum lactate concentration of 4mmol/l) of the fit group, $6.45{\pm}0.26m/s$, was higher than that of the unfit group, $5.45{\pm}0.23m/s$. $La_{peak}$(peak plasma lactate concentration during the exercise test) was lower in the fit group ($20.34{\pm}1.62mmol/l$ at 1 min after maximal intensity exercise) than in the unfit group ($24.78{\pm}1.09mmol/l$ at 2 min after maximal exercise step). $t_{50%}$(time required for the recovery of lactate concentration to be one-half of $La_{peak}$ after maximal exercise) of the unfit group and the fit group were 40.0 and 18.0 min, respectively. Therefore, the protocol of the incremental standardized exercise test utilized in this study seems to be reliable for the assessment of fitness and exercise intolerance for the Thoroughbred racehorses.
A suitable culture method and bioreactor type for itaconic acid production were chosen by comparing the maximal concentration of itaconic acid produced in various systems. In batch culture, the maximal concentration of itaconic acid produced in a bubble column reactor was about 5% greater than that produced in stirred-tank or external-loop airlift reactor. These results were thought to be due to lower shear force and higher mass transfer efficiency in a bubble column reactor in comparison with other reactors. Moreover, the fed-batch mode in a bubble column was found to be a suitable one, producing about 25% higher concentration of itaconic acid compared to batch mode.
The regulation of actin gene expression during the differentiation of Naegleria gruberi was examined. Actin mRNA concentration was maximal in amoebae and decreased rapidly after the initiation of differentiation. At 20 min after initiation, the concentration of actin mRNA decreased to 55% of the maximal value. The actin mRNA concentration decreased to the minimum at 80 min (15% of the maximum), and then began to increase slightly at the end of differentiation. This decrease of actin mRNA concentration was regulated by the repression of actin gene transcription based on nuclear run-on transcription experiments. The rates of transcription of actin gene in nuclei prepared at 40 and 80 min after the initiation of differentiation were 50 and 28% of that of nuclei prepared at the beginning of differentiation, respectively. The addition of cycloheximide at the initiation of differentiation inhibited both the rapid decrease in the concentration of actin mRNA and the repression of actin gene transcription. These results suggest that the rapid decrease in the concentration of actin mRNA during the differentiation of N. gruberi is accomplished by the repression of actin gene transcription and this transcriptional regulation requires continuous protein synthesis during the differentiation.
Proceedings of the National Institute of Ecology of the Republic of Korea
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제4권1호
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pp.49-62
/
2023
Phthalates are animal carcinogens. Potassium hydrogen phthalate (KHP), which has the least complicated structure among phthalates, is used for the analysis of total organic carbon and formaldehyde. However, its toxicity has not been confirmed. A 24-hour acute toxicity test was performed using Daphnia magna, a water flea used to evaluate aquatic toxicity owing to its high sensitivity. The lowest observed effect concentration of KHP was found to be 240 mg/L. The effects of phosphorus, nitrogen, and Cr(6+), which are able to be discharged along with KHP, were also confirmed using tests. At 240 mg/L KHP, toxicity increased as phosphorus, nitrogen, and Cr(6+) increased. In addition, tests were performed to confirm the half maximal effective concentration of KHP. Through 10 test repetitions, the average ecotoxicity value was found to be 0.3, the average half maximal effective concentration was 327.75 mg/L, and the coefficient of variation (%) was 3.16%; because the latter value is lower than 25%, which is what is generally suggested for the water pollution standard method, the reproducibility of the tests is sufficient to replace the existing standard reference toxicity test that uses potassium dichromate. In addition, the half maximum effective concentration of potassium hydrogen phthalate is approximately 218 times more than that of potassium dichromate; therefore, toxicity is relatively low. In conclusion, KHP is a feasible alternative to the highly toxic potassium dichromate for performing the standard reference toxicity test.
To evaluate training effect, aerobic dance was performed by eight female collegestudents for 8 weeks. Body composition, cardiopulmonary function at rest and during maximal exercise, blood cholesterol concentration at rest were determined before and after 8weeks of aerobic dance training. Maximal exercise was performed on the treadmill according of Bruce protocol. Pre to post training differences were evaluated. The results obtained were as follows : 1. After the training, skinfold thickness and total body fat decreased significantly(p<0.1) while lean body mass increased with significance (p<0.1). 2. Heart rate and arterial blood pressure at rest decreased without sinificance after the training. 3. As a result of training, forced vital capacity and forced expiratory volume for a second increased significantly (p<0.01, p<0.1). 4. After the training period, heart rate at 3, 6, and 9 min. during treadmill exercise was significantly lower than those of pretraining (p<0.05). 5. After the training, systolic and diastolic blood pressure at 6 and 9 min during the exercise was significantly lower than those of pretraining (p<0.025, p<0.1). 6. After the training, oxygen uptake at 3 and 6 min during the exercise was significantly greater than those of pretraining (p<0.05). 7. As a result of training, the maximal oxygen uptake increased significantly during the exercise (p<0.1). 8. After the training, expired air volume for a minute at 3 and 6 min during the exercise was signigicantly grerter than those of pretraining (p<0.1). 9. After the training, repiratory quotient during the exercise was lower than pretaining without significance. 10. After the training, blood HDL -cholesterol concentration incereased with significance, (p<0.1) blood total cholesterol and triglycerids concentration decreasedsignificantly (p<0.1). From these results, it may be concluded that 8 week aerobic dance training reduces skinfold thickness and body fat contents, improves the cardiopulmonary function and tissue oxygen utilization, reduces blood cholesterol and triglyceride concentration and brings about the increase of blood HDL-cholesterol concentriation.
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