• 제목/요약/키워드: 2-thiouracil

검색결과 29건 처리시간 0.021초

New Strategy for the Synthesis of 5-Aryl-1H,1'H-spiro[furo[2,3-d]pyrimidine-6,5'-pyrimidine]2,2',4,4',6'(3H,3'H,5H)-pentaones and Their Sulfur Analogues

  • Jalilzadeh, Mohammad;Pesyan, Nader Noroozi
    • Bulletin of the Korean Chemical Society
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    • 제32권9호
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    • pp.3382-3388
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    • 2011
  • Reaction of barbituric acid (BA), 1,3-dimethyl barbituric acid (DMBA) and 2-thiobarbituric acid (TBA) with cyanogen bromide and aldehydes in the presence of L-(+)-tartaric acid afforded a new route for the synthesis of stable heterocyclic 5-aryl-1H,1'H-spiro[furo[2,3-d]pyrimidine-6,5'-pyrimidine]2,2',4,4',6'(3H,3'H,5H)-pentaones which is a dimeric form of barbiturate (uracil and thiouracil derivative). In the reaction of 1,3-diethyl thiobarbituric acid (DETBA) the Knoevenagel condensation and then Michael adducts were obtained under the same condition. Structure elucidation is carried out by $^1H$ NMR, $^{13}C$ NMR, FT-IR and Mass analyses. Mechanism of the formation is discussed.

Synthesis of Silver Nanoplates with Fibronectin Nanofibril Template and Their SERS Applications

  • Wang, Li;Sun, Yujing;Cui, Yuncheng;Wang, Jiku;Li, Zhuang
    • Bulletin of the Korean Chemical Society
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    • 제34권2호
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    • pp.443-446
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    • 2013
  • In this work, a novel strategy is provided to prepare silver nanoplates by a fibronectin (Fn) nanofibril template. First, Fn molecules were controlled to assemble into amyloid-like nanofibrils in highly concentrated ethanol aqueous solution. The resultant nanofibrils could serve as a soft template to direct the formation of silver nanoplates. It is worth noting that the silver nanoplates are excellent surface-enhanced Raman scattering (SERS) substrate with 4-aminothiophenol (4-ATP) molecule as a test probe. This high active SERS substrate can also be used to detect drug molecule, 2-thiouracil with high sensitivity.

식물 바이러스병의 감염기구 및 증식억제에 관한 연구 1 (Studies on the Infection Mechanism and Inhibition of Multiplication in Plant Virus Diseases(I))

  • 이정호;오정행;박찬걸;권신한
    • 미생물학회지
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    • 제12권2호
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    • pp.53-58
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    • 1974
  • A number of antibiotics and organic compounds were tested for their effect on the multoplication of tobacco mosaic virus(TMV) in floating leaf discs. 1)Among six antibiotics tested, kanamycin sulfate showed 24% or more inhibition to TMV multiplication under these experimental conditions. Aureomycin hydrochloride and chloramphenicol showed 19% and 14% inhibition respectively. 2)For screening of organic compounds two environments were used, a diffuse day- light environment (25 foot-candles and laboratory temperature) and an artificial light environment for 12 hours per day(300 foot-candles at 4 to $5^{\circ}C above laboratory temperature). A wide range of organic compounds increased virus multoplication in the diffuse daylight environment but had less effect, or ingibited virus multiplication, in the artificial light environment. 3)The following compounds were among the most effective in increasing TMV multiplication: glucose-1-phosphate, L-aspartic acid, glucose, and 5-bromouracil. The following compoumds were most effective in inhibiting TMT multiplication: thiouracil, uracil, DL-isoleucine, L-leucine, and zinc chloride.

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오수과(吳茱菓)가 PTU로 유발된 갑상선기능저하증 Rat의 갑상선기능 및 조직학적 변화에 미치는 영향 (The Effects of Evodiae fructus on Thyroid Function and Histological Modification in Hypothyroidism Rat Model Induced by PTU.)

  • 강철호;송문구;강지석;이병철;안영민;두호경;안세영
    • 대한한방내과학회지
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    • 제29권4호
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    • pp.1000-1010
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    • 2008
  • Objective : Hypothyroidism is a syndrome characterized by symptoms such as cold intolerance, or weight gain. Because of side effects of Western medicine treatment, interest in oriental medicine has been increasing. In this study, we examined the therapeutic effects of Evodiae fructus and histological modification in hypothyroidism rat model induced by PTU(6-propyl, 2-thiouracil). Methods : After inducing hypothyroidism in the rats by PTU injections, we divided the rats into four groups, the Evodiae fructus 100 500, control, and $LT_4$ (levothyroxine) groups. After 2 weeks Evodiae fructus and $LT_4$ were administered, respectively. The weight was measured once a week. After sampling the blood for biochemical analysis to check the levels of $T_3$, $T_4$ and TSH, the thyroid tissue was removed, stained with H&E, and an image was obtained using an optical microscope. Results : Compared with normals, controls showed low $T_4$ and high TSH. The Evodiae fructus group showed a statistically meaningful $T_3$ increase to be dose related. But the levels of TSH showed no meaningful difference between the Evodiae fructus group and normals. About the biochemical tests(liver, kidney etc) and weight change, there was no meaningful difference between the Evodiae fructus group and controls. In the biopsy, the Evodiae fructus group showed thyroid tissue improvement compared to controls. Conclusions : These results show that Evodiae fructus stimulates the decreased functions of the thyroid, and also has thyroid cell protecting effects. The lab results also showed that Evodiae fructus is a safe substance that doesn't cause hepatotoxicity or nephrotoxicity. Therefore it is an effective substance in the treatment of hypothyroidism.

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

  • 윤상필;김정우
    • Journal of Medicine and Life Science
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    • 제16권1호
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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.

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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    • 제14권6호
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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.

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

  • 이승진;백선호;안세영;이병철;안영민
    • 동의생리병리학회지
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    • 제25권6호
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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.

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

  • 김종명;윤성철;최수봉;이현우;김경동;김정숙;남혜주;최원희;이태숙
    • Journal of Yeungnam Medical Science
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    • 제5권1호
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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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토사자가 PTU로 유발된 갑상선기능저하증 Rat에 미치는 영향 (The Effects of Cuscuta Semen on a Hypothyroidism Rat Model induced by Propylthiouracil(PTU))

  • 강지석;박성환;한수련;안영민;안세영;이병철
    • 대한한방내과학회지
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    • 제31권3호
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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.