• Title/Summary/Keyword: C metabolism

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Pharmacokinetic Study of YH1885 (I): Absorption, Distribution and Excretion of $^{14)C-YH1885$ in Rats (YH1885의 체내동태(제1보):흰쥐에서 $^{14)C-YH1885$의 단회투여시 흡수, 조직분포 및 배설)

  • Ahn, Byung-Nak;Fujio, Naoki;Kusumoto, Naotoshi;Abe, Yoshifumi;Odomi, Masaaki;Lee, Jong-Wook
    • YAKHAK HOEJI
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    • v.41 no.3
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    • pp.335-344
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    • 1997
  • The absorption, distribution and excretion of $^{14}C$ labeled YH1885 {5,6-Dimethyl-2(4-fluorophenylamino)-4-(1-methyl-1,2,3,4-tetrahydroisoquinolin-2-yl)pyrimidine hydroc hloride), a new proton pumpinhibitor, were investigated in rats after a single administration of $^{14}C$-YH1885. 1. After intravenous administration of 5mg/kg, the blood level of radioactivity declined in a biphasic fashion with the mean terminal elimination half-life of 12.4hr. 2. After oral administration of 20mg/kg, the maximum blood level of radioactirity was reached at 4.0hr in female rats. The blood level of radioactivity-time profiles in male and female rats were similar, and the absorptionof $^{14}C$-YH1885 was not affected by food. 3. Appproximately 89% and 1% of radioactivity of the total dose were excreted in feces and urine, respectively. 4. Biliary excretion of radioactivity was 47.9% of the dose. Enterohepatic circulation of radioactivity was 49.6%. 5. Radioactivity was excreted maily into feces via bile. 6. The concentration of radioactivity in most tissues reached the peak level at 4.0hr after dosing, and then declined. Autoradiograms of male rats showed that the radioactivity levlels in the fat, harder's gland, liver and G-Itract were higher than those in the other tissues and the elimination of radioactivity from fat and liver was slow. 7. Autoradiograms of a pregnant rat showed that radioactivity was transferred to mammary gland, placenta and fetus. The radioactivity level in the mammary gland was higher than that in the blood.

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The Effects of Korean Safflower(Carthamus tinctorious L.) Seed Powder Supplementation Diet on Bone Metabolism Indices in Rats during the Recovery of Rib Fracture (한국산 홍화씨분말 보충식이의 급여가 골절된 흰쥐의 골대사지표에 미치는 영향)

  • 전선민;김준한;이희자;이인규;문광덕;최명숙
    • Journal of Nutrition and Health
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    • v.31 no.6
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    • pp.1049-1056
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    • 1998
  • This study was carried out to investigate the effects of Korean safflower(Carthamus. tinctorious L.) seed powder supplementation on bone metabolism during the recovery of rib-fracture induced by surgical operation in rats. Male Sprague-Dawley rats of 10 weeks old, weighing 370$\pm$5g, were divided into two groups after arrival : the control group(C group, AIN-76 semifurified diet) and safflower seed group(S group, AIN-76 semifurified diet+10% safflower seed powder). They were fed experimental diets for 12 days before the rib fracture operation and for 30 more days after the operation. A number 9 rib was fractured surgically and sham-operation was also performed. After the rib-fracture operation, rats were sacrificed on the 8th, 11th, 16th, 21st, and 30th day, respectively. The body weights were decreased on the 8th day after operation in both groups but recovered gradually thereafter. The fractured sections of the S group were more strongly adhered and more rapidly repaired than those of C group. Effects of safflower seed powder supplementation on indices of bone metabolism during the repairing of rib-fracture can be summarized as following. There were no differences between C and S group. In the levels of PTH and calcitonin, which regulate the concentration of plasma calcium. However, PTH level on the 8th day was significantly higher than that on the 16th day in control group. There were also no differences between groups or within groups in the levels of calcitonin. Osteocalcin levels, one of the bone-formation indices, were similar in two groups. Activities of total-ALP in plasma were highest at the 8th day in both groups and decreased thereafter, except on the 30th day in control group. The activities of bone-specific ALP that is directly related to bone calcification, showed higher levels in the S group than in the C group throughout the experimental period. They were significantly increased in the S group on the 11th, 16th, and 21st days. In comparisons of plasma calcium and phosphate levels, Ca levels were tended to be lower in the S group than in the C group and P levels showed the opposite trend. It seems that the fractured ribs were more rapidly repaired in rats supplemented with safflower seed powder than in control rats, possibly due to stimulation of bone calcification from increased activity of bone-specific ALP. (Korean J Nutrition 31(6) : 1049-1056, 1998)

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Effect of Phenobarbital Sodium and 3-Methylcholanthrene on Metabolism of 14C-carbofuran in Rat (쥐에서 Phenobarbital Sodium 및 3-Methylcholanthrene이 14C-carbofuran의 대사에 미치는 영향)

  • Rim, Yo-Sup;Han, Seong-Soo
    • Korean Journal of Environmental Agriculture
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    • v.21 no.1
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    • pp.57-68
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    • 2002
  • In order to elucidate the effect of phenobarbital sodium (PB) and 3-methylcholanthrene (3-MC) on metabolism of insecticide carbofuran in rat. Carbofuran metabolites and its formation rates were determined when orally administered $^{14}C$-carbofuran alone and its combination with PB or 3-MC to rat. $^{14}C$-carbofuran administered orally, alone or in combination with PB or 3-MC, was secreted rapidly within 48 hrs. That is, 79.9 to 81.1% of the original radioactivity was secreted into the urine and 5.7 to 6.5% into the feces. The secretion rate was faster in the combined administration than that in carbofuran alone. Metabolites of carbofuran in main organs, urine, feces and blood of rat were largely 3-hydroxycarbofuran, 3-ketocarbofuran, 3-hydroxycarbofuran phenol, 3-ketocarbofuran phenol, and carbofuran phenol, the major ones being 3-hydroxycarbofuran and 3-ketocarbofuran, respectively, in all administrations of carbofuran alone, carbofuran+PB and carbofuran+3-MC. In addition, formation rate of the two major metabolites detected in the urine was 17.4% and 12.8%, respectively, when carbofuran alone was administered. Meanwhile, when carbofuran was administered with PB or 3-MC, they were 8.6% and 23.5, repectively. These results indicate that the oral administration of PB or 3-MC can reduce carbofuran toxicity by fastening and stimulating the carbofuran metabolism in rat.

Effects of quercetin on the improvement of lipid metabolism through regulating hepatic AMPK and microRNA-21 in high cholesterol diet-fed mice (고콜레스테롤 식이 섭취 쥐에서 quercetin의 간 AMPK 및 microRNA-21 조절을 통한 지질대사 개선 효과)

  • Lee, Mak-Soon;Kim, Yangha
    • Journal of Nutrition and Health
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    • v.55 no.1
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    • pp.36-46
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    • 2022
  • Purpose: Quercetin is a polyphenolic flavonoid abundant in many fruits and vegetables. It has potential health-beneficial properties, such as antioxidant, anti-obesity, anti-cancer, anti-diabetic and anti-inflammatory effects. The purpose of this study was to investigate whether the lipid metabolism improvement effect of quercetin affected the regulation of AMP-activated protein kinase (AMPK) activity and microRNA (miR)-21 expression in the liver of mice fed a high-cholesterol diet. Methods: Male C57BL/6J mice were fed with normal diet, quercetin-free diet and diets containing 0.05% or 0.1% quercetin for six weeks. Hypercholesterolemia was induced by adding 1% cholesterol and 0.5% cholic acid to all diets. Serum and liver triglyceride (TG), and total cholesterol (TC) concentrations were analyzed using a commercial enzymatic colorimetric kit. AMPK activity was quantified using an AMPK kinase assay kit. The levels of miR-21 and genes involved in lipid metabolism were measured by real-time quantitative polymerase chain reaction. Results: Supplementation of quercetin reduced serum and hepatic TG and TC levels without changing body weight and food intake. Dietary quercetin significantly inhibited the mRNA levels of hepatic sterol-regulatory element binding protein-1c, acetyl-CoA carboxylase 1 and fatty acid synthesis, which are involved in hepatic lipogenesis. Dietary quercetin enhanced AMPK activity and suppressed miR-21 expression, promoting hepatic lipid accumulation. Conclusion: These results suggest that the lipid-lowering effect of quercetin on the serum and liver of mice may be partially mediated by the regulation of lipogenic gene expression, AMPK activity and miR-21 expression in the liver of mice fed a high-cholesterol diet.

Pharmacokinetics of Omeprazole from Rectal Suppositories (오메프라졸 함유 직장좌제의 약물속도론적 연구)

  • 이창현;황성주;권광일;이계주
    • YAKHAK HOEJI
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    • v.37 no.5
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    • pp.427-436
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    • 1993
  • The pharmacokinetics and relationship between in vitro dissolution and in vivo fraction absorbed were investigated after intravenous(iv) injection of omeprazole(OMZ), oral administration of OMZ capsules and rectal administration of 8 types of suppositories. The plasma concentration of OMZ (C$_{p}$)-time (t) curve after iv. administration fitted a two-compartment open model and the equation which best fitted the pharmacokinetics of OMZ was $C_{p}$ = 13.936 $e^{-8.78t}$+2.973 $e^{-0.716t}$. The bioavailabilities of OMZ in Witepsol H15 base (Supp-2) and PEG 4000 base (Supp-6) suppositories were 40.7% and 33.4%, respectively, which are higher(p<0.001) than 13% of oral administration of capsule. The avoidance fractions of the first-pass metabolism for Supp-2 and Supp-6 suppositiories were 31.8% and 23.4%, respectively, suggesting that the rectal application of OMZ may be a more adequate route of administration than oral one.

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Health Promoting Effects of Lactoferrin from Milk

  • Shimizu, Hirohiko;Ando, Kunio;Hoshino, Tatsuo
    • Journal of Dairy Science and Biotechnology
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    • v.24 no.2
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    • pp.21-24
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    • 2006
  • The ubiquitous presence of lactoferrin(LF) receptor in human as reported by the research group of Prof. Bo Lonnerdal, Univ. California (Suzuki, Y. A.,2001) encouraged us to search for the unknown physiological roles of Lf. Under the collaboration with Prof. Etsumori Harada, Tottori Univ., and his research group, we have found two novel biological activities of LF as the control of the lipid metabolism and the effect on the central nervous system. Relating to the lipid metabolism, LF could, in animal experiments, reduce triglyceride and total cholesterol both in blood and liver (Takeuchi, T et αl., 2003). LF increased plasms HDL-C and lowered LDL-C. In the central nervous system, LF showed anti-nociceptive activity mediated by ${\mu}$-opioid receptor in the rat spinal cord (Hayashida, K. et al., 2003). LF enhanced analgesic action of morphine synergistically via nitric oxide synthesis (Hayashida, K., et al., 2003) LF showed opioid-mediated suppressive effect on distress induced by maternal separation in rat pups (Takeuchi, T., et al., 2003).

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STUDIES ON METHIONINE METABOLISM IN THE RUMEN BACTERIA OF GOATS

  • Muramatsu, T.;Numa, M.;Ueda, Y.;Furuse, M.;Okumura, J.;Samukawa, K.
    • Asian-Australasian Journal of Animal Sciences
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    • v.7 no.2
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    • pp.223-229
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    • 1994
  • The metabolic fate of methionine in rumen bacteria was studied by intraruminal administration of $^{15}N$ and $1-^{13}C$ labeled methionine in goats. Time course changes in isotopic abundance of amino acids in the rumen bacteria were determined with a computer-controlled gas-chromatograph mass spectrometer. The results from the transition of peak isotopic abundance in amino acids indicated that in rumen bacteria the $^{15}N$ or $^{13}C$ isotope in the methionine molecule was transferred rapidly to into bacteria, methionine administered intraruminally may not be retained as it is, but would be converted quickly to other metabolites in the bacteria.

Health Promoting Effect of Lactoferrin from Milk

  • Hoshino, Tatsuo;Shimizu, Hirohiko;Ando, Kunio
    • 한국유가공학회:학술대회논문집
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    • 2005.10a
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    • pp.1-9
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    • 2005
  • The ubiquitous presence of lactoferrin (LF) receptor in human as reported by the research group of Prof, Bo Lonnerdal, Univ. California, encouraged us to search for the unknown physiological roles of LF. Under the collaboration with Prof. Etsumori Harada, Tottori Univ., and his research group, we have found two novel biological activities of LF as the control of the lipid metabolism and the effect on the central nervous system. Relating to the lipid metabolism, LF could, in animal experiments, reduce triglyceride and total cholesterol both in blood and liver. LF increased plasma HDL-C and lowered LDL-C. In the central nervous system, LF showed anti-nociceptive activity mediated by ${\mu}$-opioid receptor in the rat spinal cord. LF enhanced analgesic action of morphine synergistically via nitric oxide synthesis. LF showed opioid-mediated suppressive effect on distress induced by maternal separation in rat pups.

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Hepatoprotective activity of Indigofera aspalathoides extract against CCl4-induced liver damage

  • Gupta, M.;Mazumder, U.K.;Haldar, P.K.;Manikandan, L.;Senthilkumar, G.P.;Kander, C.C.
    • Advances in Traditional Medicine
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    • v.4 no.2
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    • pp.100-103
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    • 2004
  • The plant Indigofera aspalathoides are used by a large number of tribes in India for the treatment of various hepatic disorder. The methanol extract of Indigofera aspalathoides (MEIA) was evaluated for its effect on carbontetrachloride $(CCl_{4})$ induced liver damage. Biochemical parameters such as serum glutamine oxaloacetate trasaminase (SGOT), serum glutamine pyruvate transaminase (SGPT), serum alkaline phosphatase (ALP), total serum protein (TP), thiobarbituric acid reactive substances (TBRS) and glutathione content of the liver were estimated to assess liver function and metabolism. Biochemical observations suggest that methanol extract of Indigofera aspalathoides (MEIA) significantly restored the liver function and metabolism towards normal condition in $CCl_{4}$-induced hepatic damage.

Nitrogen Control in Corynebacterium glutamicum: Proteins, Mechanisms, Signals

  • Burkovski, Burkovski;Andreas, Andreas
    • Journal of Microbiology and Biotechnology
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    • v.17 no.2
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    • pp.187-194
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    • 2007
  • In order to utilize different nitrogen sources and to survive in a situation of nitrogen limitation, microorganisms have developed sophisticated mechanisms to adapt their metabolism to a changing nitrogen supply. In this communication, the recent knowledge of nitrogen regulation in the amino acid producer Corynebacterium glutamicum is summarized. The core adaptations of C. glutamicum to nitrogen limitation on the level of transcription are controlled by the global regulator AmtR. Further components of the signal pathway are GlnK, a $P_{II}-type$ signal transduction protein, and GlnD. Mechanisms involved in nitrogen control in C. glutamicum regulating gene expression and protein activity are repression of transcription, protein-complex formation, protein modification by adenylylation, change of intracellular localization, and proteolysis.