• Title/Summary/Keyword: Thiouracil

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The Effect of Thyroxine Status on Hepatic Levels of 10-Formyltetrahydrofolate Dehydrogenase (갑상선 호르몬이 흰 쥐의 간에 있는 10-Formyltetrahydrofolate Dehydrogenase에 미치는 영향)

  • Min, Hye-Seon
    • Journal of Nutrition and Health
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    • v.24 no.4
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    • pp.350-355
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    • 1991
  • The effect of thyroid hormone on hepatic levels of 10-formyltetrahydrofolate dehydrogenase (10-formyltetrahydrofolate : NADP oxidoreductase, E.C. 1.5.1.6.) was studied using Sprague-Dawley rat. Hypothyroidism increased histidine oxidation by 5 fold and increased 10-formyltetrahydrofolate dehydrogenase activity by 142%, and also decreased methylenetetrahydrofolate reductase activity by 52%. Decreased methylenetetrahydrofolate reductase acts by decreasing synthesis of 5-methyl folate, thereby increasing the proportion of non-methyl folate required for folate-dependent reactions. Increased histidine oxidation produced by hypothyroidism may be attributed to its effect in decreasing 10-formyltetrahydrofolate dehydrogenase.

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Effects of Ukgan-san on the L-thyroxine-induced Rat Hyperthyroidism (억간산이 갑상선기능항진 유발 백서에 미치는 영향)

  • Kim, Seung Mo
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.26 no.5
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    • pp.679-686
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    • 2012
  • This study was to elucidate the effects of Ukgan-san on the hyperthyroidism induced by sodium levothyroxine. Hyperthyroidisms were induced by continuous subcutaneous treatment of LT4, 0.3 mg/kg, once a day for 27days, and 1,500, 1,000 and 500 mg/kg of Ulkansan extracts were orally administered, once a day for 15 days from 12th LT4 treatment, and the changes on the body, thyroid gland, liver and epididymal fat pad weights, serum triiodothyronine(T3), thyroxine(T4), thyroid-stimulating hormone(TSH), asparte aminotransferase (AST) and alanine aminotransferase (ALT) concentrations, hepatic lipid peroxidation(LPO), glutathione(GSH), superoxide dismutase(SOD) and catalase(CAT) activities were investigated with throid gland, liver and epididymal fat pad histopathological changes. The effects of Ukan-san extracts were compared with that of propyl thiouracil(PTU), a standard antithyroidic drug 10 mg/kg(intraperitoneally). 1,500 and 1,000 mg/kg of Ukan-san extracts reversed all LT4-induced hyperthyroidisms and these effects indicating their potential in the regulation of hyperthyroidism. Further, the Ukan-san extract normalized LT4-induced liver oxidative stresses, and also reduced liver damages and epididymal fat pad reducements suggesting its antioxidative and relative organ protective nature. However, nor favorable effects on LT4-induced hyperthyroidisms were detected in Ulkansan 500 mg/kg treated rats as compared with LT4 control rats in the present study. These effects of Ukan-san may help improvement of hyperthyroidisms and accompanied various organ damages.

How to design male hypothyroid hypogonadism model (갑상샘기능저하증에 따른 생식샘기능저하증 모델 정립을 위한 제언)

  • Yoon, Sang-Pil;Kim, Jung Woo
    • Journal of Medicine and Life Science
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    • v.16 no.1
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    • pp.34-38
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    • 2019
  • Hypogonadism is a clinical syndrome that results in hormone deficiency and can be classified as 1) primary caused by the gonadal failure and 2) secondary by the hypothalamus-pituitary gland dysfunction and/or cardiometabolic complications. Recently the presence of thyroid hormone receptors in different testicular cell types was demonstrated, and thus thyroid dysfunctions would be another cause of secondary hypogonadism. Thus, we investigated the effects of perinatal hypothyroidism on hypogonadism in male Sprague-Dawley rats. Perinatal hypothyroidism was induced by daily administration of 0.05% 6-propyl-2-thiouracil (PTU) by tap water from gestation day 15, which were compared with negative control (PTU (-)) group. At postnatal day 28, hypothyroid pups were divided into 2 groups: PTU (+) group - continued PTU treatment and PTU (+/-) group - stopped PTU until postnatal day 49. Body weights, dehydrotesosterone (DHT), and testosterone levels were checked 2 and 3 weeks after grouping. Body weights were significantly decreased in PTU(+) and PTU(+/-) groups compared with PTU (-) group at postnatal day 28. 3 weeks later, PTU (+/-) group significantly gained weight compared with PTU (+) group. DHT and testosterone levels significantly decreased with PTU treatment, but increased 3 weeks after stopping PTU administration. Perinatal PTU-induced hypothyroid hypogonadism was sustained for 2 weeks after stopping PTU administration, but restored gonadal hormone levels 3 weeks after stopping PTU. These results suggest that researchers should design an experiment on hypothyroid hypogonadism based on the estimated period.

Effects of Cistanche Deserticola on Thyroid Function in Hypothyroidism Rat Model Induced by PTU(6-Propyl, 2-thiouracil) (육종용이 PTU로 유발된 갑상선 기능저하증 동물모델에 미치는 영향)

  • Lee, Seung-Jin;Paik, Sun-Ho;Ahn, Se-Young;Lee, Byung-Choel;Ahn, Young-Min
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.25 no.6
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    • pp.989-995
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    • 2011
  • Hypothyroidism is the most common disease in the endocrine system. Cistanche Deserticola has been used traditionally in the treatment of kidney deficiency and Yang deficiency syndrome. In this study, we investigated the therapeutic effects of Cistanche Deserticola on Hypothyroidism rat model induced by PTU. 24 Two-month-old Sprague-Dawley male rats were divided into 4 groups : 1) normal(n=6), 2) PTU-induced hypothyroidism control(n=6), 3) hypothyroidism rat treated with Cistanche Deserticola(n=6), 4) hypothyroidism rat treated with levothyroxine(n=6). PTU was administered for 4 weeks. Cistanche Deserticola and levothyroxine was administered 2 weeks after PTU was initiated for a total duration of 2 week. Body weights were checked every week and after 4 weeks, biochemical analysis was performed and T3, T4 and TSH were measured by ELISA kits. In comparison with the normal group, the control group showed hypothyroidism with lower T3, T4 level and higher TSH level. In the Cistanche group the level of T4 was significantly increased and TSH level was significantly decreased. There was no significant difference in biochemical labs and weight between the Cistanche group and the control group. These findings suggest that Cistanche Deserticola could help the production of thyroid hormones under PTU suppression. And there is no harmful effect on liver and kidney function, and other metabolism. According to these results Cistanche Deserticola could be an useful agent for treating hypothyroidism.

Purification and Properties of Intracellular Cytosine Deaminase from Chromobacterium violaceum YK 391

  • KIM , JUNG;YU, TAE-SHICK
    • Journal of Microbiology and Biotechnology
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    • v.14 no.6
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    • pp.1182-1189
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    • 2004
  • Cytosine deaminase (cytosine aminohydrolase, EC 3.5.4.1) stoichiometrically catalyzes the hydrolytic deamination of cytosine and 5-fluorocytosine to uracil and 5-fluorouracil, respectively. The intracellular cytosine deaminase from Chromobacterium violaceum YK 391 was purified to apparent homogeneity with 272.9-fold purification with an overall yield of $13.8\%$. The enzyme consisted of dimeric polypeptides of 63 kDa, and the total molecular mass was calculated to be approximately 126 kDa. Besides cytosine, the enzyme deaminated 5-fluorocytosine, cytidine, 6-azacytosine, and 5-methylcytosine, but not 5-azacytosine. Optimum pH and temperature for the enzyme reaction were 7.5 and $30^{\circ}C$, respectively. The enzyme was stable at pH 6.0 to 8.0, and at 30T for a week. About $70\%$ of the enzyme activity was retained at $60^{\circ}C$ for 5 min. The apparent $K_{m}$ values for cytosine, 5-fluorocytosine, and 5-methylcytosine were calculated to be 0.38 mM, 0.87 mM, and 2.32 mM, respectively. The enzyme activity was strongly inhibited by 1 mM $Hg^{2+},\;Zn^{2+},\;Cu^{2+},\;Pb^{2+},\;and\;Fe^{3+}$, and by o-phenanthroline, $\alpha,\;{\alpha}'$-dipyridyl, p-choromercuribenzoate, N-bromosuccinimide, and cWoramine­T. In addition, the enzyme activity was strongly inhibited by I mM 2-thiouracil, and weakly inhibited by 2-thiocytosine, or 5-azacytosine. Finally, intracellular and extracellular cytosine deaminases from Chromobacterium violaceum YK 391 were found to have a different optimum temperature, apparent $K_{m}$ value, and molecular mass.

Graves' disease Associated with Idiopathic Thrombocytopenic Purpura and Iron Deficiency Anemia (특발성 혈소판 감소성 자반증 및 철 결핍성 빈혈을 동반한 Graves 씨병 1례)

  • Kim, Jong-Myung;Yun, Sung-Chul;Choi, Soo-Bong;Lee, Hyun-Woo;Kim, Kyeong-Dong;Kim, Chung-Sook;Nam, Hei-Ju;Choi, Won-Hee;Lee, Tae-Sook
    • Journal of Yeungnam Medical Science
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    • v.5 no.1
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    • pp.173-179
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    • 1988
  • Since 1931, sporadic reports have appeared noting an apparent association between hyperthyroidism and idiopathic thrombocytopenic purpura. Recent various studies suggested that these two diseases may share a similar immunologic background, but the the exact mechanism is still a matter of speculation. This 22-year old female patient visisted this hospital because of general weakness and purpura of legs for 2 months. The laboratory findings were compatible with Graves' disease associated with idiopathic thrombocytopenic purpura. The palatclet count was 16000/$mm^3$, hemoglobulin was 10.9g/dl and MCV was 60.1tL. T3 was 490.53ng/dL, T4 was 24ug/dL and free T4 was 5.66ng/dL. Antiplatelet antibody and anti-microsomal antibody were positive. The bone marrow findings were compatible with tron deficiency anemia and idiopathic thrombocytopenic purpura. The thyroid biopsy showed adenomatous goiter. She was administered with propyl thiouracil, Beta-blocker, iron and prednisolon. On the 10th hospital day, platelet count was 184000/$mm^3$, hemoglobulin was 12.0gm/dL and MCV was 67.5fL. On the 20th hospital day, T4 was 10.35ug/dL and free T4 was 2.30ng/dL. Therefore she was discharged and followed up.

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Synergistic interactions of Aegle marmelos leaf, Emblica officinalis fruit and Ocimum sanctum leaf extracts in the regulation of hyperthyroidism and / or hyperglycaemia

  • Panda, Sunanda;Kar, Anand
    • Advances in Traditional Medicine
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    • v.4 no.1
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    • pp.37-43
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    • 2004
  • The effects of Aegle marmelos (Rutaceae) leaf, Emblica officinalis (Euphorbiaceae) fruit and Ocimum sanctum. (Labiateae) leaf extracts were studied in L-thyroxine (0.5 mg/kg) induced hyperthyroidic mice. Separately combined effects of these three plant extracts and of a commonly used antithyroidic drug, Propyl thiouracil (PTU) were investigated for comparison. Serum concentration of thyroxine $(T_4)$, triiodothyronine $(T_3)$, glucose and the activity of hepatic Glucose 6-Phosphatase (G-6-Pase) were considered as main parameters. Hepatic lipid peroxidation (LPO), superoxide dismutase (SOD) and Catalase (CAT) activities were also studied to reveal the toxic effect of the plant extracts, if any. While exogenous $T_4$ enhanced serum concentration of $T_4$, $T_3$, glucose and the activity of hepatic G-6-Pase, a simultaneous administration of either A. marmelos leaf (1.0 mg/kg), E. officinalis fruit( 30 mg/kg) and O. sanctum leaf (50 mg/kg) extracts, to hyperthyroidic animals decreased all these parameters. However, the effects were more pronounced, as nearly normal thyroid function and serum glucose concentration were exhibited when all three plant extracts were administered together. A decrease in LPO and a concomitant increase in SOD and the CAT activities indicated the safe and antiperoxidative nature of the plant extracts, administered either alone or in combination. Our findings reveal that the three test plant materials exhibit synergistic effects without any hepatotoxicity, suggesting their potential use in the amelioration of hyperthyroidism and/ or hyperglycaemia.

The Effects of Cuscuta Semen on a Hypothyroidism Rat Model induced by Propylthiouracil(PTU) (토사자가 PTU로 유발된 갑상선기능저하증 Rat에 미치는 영향)

  • Kang, Ji-Suck;Park, Sung-Hwan;Han, Su-Ryun;Ahn, Young-Min;Ahn, Se-Young;Lee, Byung-Cheol
    • The Journal of Internal Korean Medicine
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    • v.31 no.3
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    • pp.425-436
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    • 2010
  • Objectives : Hypothyroidism is a relatively common endocrinologic disease, especially among older women. Western medical doctors treat hypothyroidism with levothyroxine, however there are several side effects, including thyrotoxicosis, atrial fibrillation, osteoporosis, etc. Therefore, traditional Korean medicine(TKM) offers an appealing alternative therapy for hypothyroidism. In this study, Cuscuta Semen was used to analyze its possible effect on a hypothyroidism rat model induced by propylthiouracil(PTU). Methods : 24 two-month-old Sprague-Dawley(SD) rats were divided into 4 groups: normal (n=6), PTU-induced hypothyroidism control(n=6), hypothyroidism rat treated with Cuscuta Semen (n=6), and hypothyroidism rat treated with levothyroxine(n=6). PTU was administered for 4 weeks, Cuscuta Semen and levothyroxine was administered 2 weeks after PTU was initiated for a total duration of 2 weeks. Blood samples from all the rats were taken from their hearts and analyzed. Results : When compared to the normal group, the PTU-induced control group showed significantly lower $T_4$, $T_3$ levels and significantly higher TSH level, which is indicative of hypothyroidism. The Cuscuta Semen group had significantly higher $T_4$ and significantly lower TSH than the control group(p<0.05). There was no significant difference in biochemical labs and weight between the Cuscuta Semen and control groups. Conclusions : These results suggest that Cuscuta Semen could be effective in increasing thyroid hormone production, and be powerful enough to affect the hypothalamus-pituitary-thyroid axis. Also, no adverse effects related with Cuscuta Semen were found, suggesting that it is relatively safe to administer. In conclusion, it seems that Cuscuta Semen is a safe alternative medicine for hypothyroidism.

Microwave Assisted Synthesis of New N1-Substituted 5-Cyano-pyrimidine Derivatives as Potent Antimicrobial Agents (마이크로파를 이용한 강한 항균제인 새로운 N1-치환된 5-Cyano-pyrimidine 유도체의 합성)

  • Pore, Yogesh;Patil, Gaurav;Tamboli, Ijaj;Chavan, Vaibhav;Kamble, Kirti;Nikam, Shital;Kuchekar, Bhanudas
    • Journal of the Korean Chemical Society
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    • v.52 no.1
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    • pp.30-35
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    • 2008
  • purpose of the study was to synthesize new series of 5-cyano substituted pyrimidine analogues with different substitutions at N1 and 6 positions and to evaluate them for antibacterial and antifungal activities. The desired compounds were synthesized by tertiary condensation of ethylcyanoacetate, substituted thioureas and suitable aldehyde in presence of potassium carbonate using MORE technique. The antibacterial and antifungal activities were evaluated by cup plate method in the concentration of 25 mg. The zone of inhibition was measured in mm. All the compounds have shown significant antibacterial and antifungal activities. The maximum activity was shown by P1 and P5 against S.aureus and E.coli respectively, while P6 has shown significant activity against all types of microorganisms. The compound P8 has been found to be significantly effective against C. albicans. Norfloxacin and griseofulvin were used as standards to compare the activites of synthesized compounds. It is concluded that analogues containing p-hydroxy, p-methoxy substituted phenyl moiety at 6 position have been found to be more potent against gram-positive microorganisms, while analogues lacking these substituents on phenyl moiety possessed gram-negative activity. The compounds having p-dimethylamino substituent on phenyl moiety at 6 positions have shown moderate activity. Further, only fluorine containing analogue at N1 position was found to possess appreciable antifungal activity. This suggests that electron donating substituent on aryl moiety as well as electron withdrawing substituent at N1 plays important role in determining potency of the compounds.