• Title/Summary/Keyword: Thiouracil

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Assembly of Gold Nanoparticles on Electrospun Polymer Nanofiber Film for SERS Applications

  • Wang, Li;Sun, Yujing;Wang, Jiku;Li, Zhuang
    • Bulletin of the Korean Chemical Society
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    • v.35 no.1
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    • pp.30-34
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    • 2014
  • We report a novel approach for fabricating active surface-enhanced Raman scattering (SERS) substrate for sensitive detection. This approach is based on the assembling of gold nanoparticles (AuNPs) onto the electrospun polycaprolactone (PCL) nanofiber film. The hydrophobic surface of PCL nanofiber film was pretreated using UV-inducing graft polymerization with acrylic acid. Afterwards this PCL nanofiber film was incubated with the AuNP solution to promote the assembly of AuNPs onto the PCL nanofibers and the formation of SERS active substrate. 4-aminothiophenol (4-ATP) molecule was used as a test probe for SERS experiments, indicating that the substrate has high sensitivity to SERS response. Our method has great advantage in term of environment-friendly synthesis, large-scale, high stability and good reproducibility. This highly active SERS substrate can be employed to detect the drug molecule, 2-thiouracil.

A Facile One-pot Synthesis of Fused 2-Thiouracils: Dipyrimidinopyridine, Pyrazolopyrimidine and Pyridazinopyrimidines

  • Youssif, Shaker;EI-Bahaie, Said;Nabih, Esam
    • Bulletin of the Korean Chemical Society
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    • v.24 no.10
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    • pp.1429-1432
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    • 2003
  • A novel fused thiouracil containing a heterocyclic ring system, dipyrimidinopyridine (3), has been prepared through the cyclization of compound 2. Compound 2 was formed by the formylation of 6-amino-2-thiouracil 1, pyrazolopyrimidines 8-10 via the heating of 6-arylhydrazono-2-thiouracils 5-7, compound 11, using Vilsmeier reagent with compound 4, pyrazolylpyrimidine 12, indolodiazinopyrimidine 14 and pyridazinopyrimidine 15. Pyridazino-pyrimidine 15 was formed by the condensation of compound 4 with acetylacetone, isatin and benzyl, respectively.

Partition Property of 5-Nitrothuopyrimidine Nucleoside

  • 이봉훈;신정희;임미경;장태식;박장수;김광호;강신원
    • Bulletin of the Korean Chemical Society
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    • v.18 no.7
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    • pp.734-736
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    • 1997
  • 5-Nitrouracil and 5-nitrouridine derivatives which C-2 and C-4 oxo-groups of the pyrimidine base were replaced by thio groups were synthesized. The lipophilicities of thiopyrimidine bases were enhanced significantly as indicated by P-values. Oxygen-sulfur exchange leading to 2-thiouracil (2) and 2,4-dithiouracil (3) were associated with 1.4- and 2.6-fold increase in P-value relative to that of uracil (1). The P-values of 5-nitro-2-thiouracil (5) and 5-nitro-2,4-dithiouracil (6) were increased 13.2- and 79.8-fold relative to that of 5-nitrouracil (4). Most of the 5-nitrothiopyrimidine bases and their nucleosides were found to be moderately active against Staphylococcus aureus and Escherichia coli except 5-nitrouracil (4).

Effects of Ginseng Radix on the Rat Hypothyroidism Induced by PTU (6-n-propyl-2-thiouracil) (인삼이 PTU (6-n-propyl-2-thiouracil)로 유발된 Rat 갑상선 기능저하증에 미치는 영향)

  • Kim, Seong-Mo
    • The Korea Journal of Herbology
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    • v.25 no.3
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    • pp.11-18
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    • 2010
  • Object : This study was to evaluate the effect of Ginseng Radix, aqueous extracts of the root part of Panax ginseng on the 6-n-propyl-2-thiouracil(PTU)-induced rat hypothyroidism. Methods : Aqueous extracts of Ginseng Radix(GR; yield = 11.70%) were administered, once day for 42 days from 2 weeks before start of PTU treatment as an oral dose of 300 and 150 mg/kg(body weight), and hypothyroidism was induced by daily subcutaneous treatment of PTU 10mg/kg for 28 days. The changes in the body weight, thyroid gland weights, serum levels of thyroid hormone-thyroid stimulating hormone(TSH), tri-iodothyronine(T3) and thyroxine(T4), total cholesterol, low density lipoprotein(LDL), high density lipoprotein(HDL) and triglyceride, liver antioxidant defense system-lipid peroxidation, $H_2O_2$, superoxide dismutase(SOD) and catalase(CAT) were observed with histopathology of thyroid glands. Results : Results were compared with LevoT4 0.5mg/kg treated rats. GR extracts suppressed the decreases in the body weight, thyroid gland weights, T3 and T4, TG, liver $H_2O_2$ and SOD activities as results of PTU treatment. And GR extracts suppressed the increases of HDL contents, liver CAT activities, thyroid gland weight as results of PTU treatment. In addition, marked hyperplasia of follicular cells with decreases of follicular colloid contentsand sizes were demonstrated at histopathological inspections. However, these PTU-induced histopathological changes related to hypothyroidism were dramatically decreased by treatment of both different dosages of GR extract, respectively Conclusions : This study suggest that GR extracts have favorable effects on the thyroid hormone productions with beneficial effects on the hypothyroidism mediated by the modulatory effects on the antioxidant defense system.

The Effects of Morinda Officinalis Radix on Thyroid function in Hypothyroidism Rat Model induced by 6-propyl, 2-thiouracil (PTU) (6-propyl, 2-thiouracil로 유발된 갑상선 기능저하증 동물모델에서 파극천이 갑상선 호르몬 및 갑상선 조직에 미치는 효능)

  • Kim, Young-Seok;Ahn, Se-Young;Ahn, Young-Min;Lee, Byung-Choel
    • The Journal of Internal Korean Medicine
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    • v.32 no.3
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    • pp.425-434
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    • 2011
  • Objectives : Hypothyroidism is the most common pathological disease of the endocrine system. Morinda Officinalis Radix has been used in treatment of Yang deficiency. In this study, we investigated the therapeutic effects of Morinda Officinalis Radix on a rat model of hypothyroidism induced by 6-propyl, 2-thiouracil (PTU). Methods : Two-month-old Sprague-Dawley male rats were used with injection of PTU which induced rats into hypo-thyroidism. During 2 weeks, rats were treated with Morinda Officinalis Radix and thyroxine. Body weights were checked every week, the after 4 weeks, biochemical analyses were performed. The levels of T3, T4 and TSH was measured by EILSA. Results : In the Morinda Officinalis Radix group, we could observe the level of T4 significantly increased and TSH level significantly decreased. Conclusions : Morinda Officinalis Radix could help the thyroid to produce thyroid hormones under PTU suppression. There is no harm effect on liver and kidney function, or other metabolism. According to these results it could help to treat hypothyroidism patients and relieve their symptoms.

The Effects of Epimedii Herba on a Hypothyroidism Rat Model induced by PTU(6-Propyl, 2-thiouracil) (음양곽(淫羊藿)이 실험적으로 유발된 갑상선 기능저하증 동물모델에 미치는 영향과 안전성)

  • Hong, Min-Jin;Lee, Byung-Choel;Ahn, Young-Min;Ahn, Se-Young
    • Journal of Pharmacopuncture
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    • v.14 no.4
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    • pp.13-22
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    • 2011
  • Objectives: The symptoms of hypothyroidism are fatigue, cold intolerance, arthralgia, muscle cramps, dry skin and etc. Although hypothyroidism is a relatively common endocrinical disease, we do have many difficulties treating it effectively. The symptoms of hypothyroidism are similar to those of Yang-deficiency in Oriental medicine. Epimedii Herba is a popular herb that has the effect of tonifying the kidney and strengthening Yang in Oriental medicine. In this study, we investigated the therapeutic effects of Epimedii Herba on a hypothyroidism rat model induced by PTU(6-Propyl, 2-thiouracil). Methods: 24 two-month-old Spargue-Dawley(SD) rats were divided into 4 groups: 1) normal(n=6), 2) PTU-induced hypothyroidism control(n=6), 3) hypothyroidism rat treated with Epimedii Herba(n=6), 4) hypothyroidism rat treated with levothyroxine(n=6). PTU was administered for 4 weeks, Epimedii Herba and levothyroxine was administered for 2 weeks after PTU was initiated for a total duration of 2 week. At the end of the experiment, blood samples from all the rats were taken from their hearts and were analyzed. Results: In comparison with normal group, the PTU-induced control group significantly showed hypothyroidism with low T3, T4 and high TSH. In Epimedii Herba group, T4 was significantly increased(p<0.05). There was no significant difference in TSH between the Epimedii Herba treatment group and the control group. And no significant differences were observed in biochemical labs and weight between the Epimedii Herba group and the control group. Conclusions: These results suggest that Epimedii Herba could help thyroid cells to produce thyroid hormones. And no significant side effects related with Epimedii Herba were found, suggesting that it is safe to administer. According to these results, Epimedii Herba may be a safe alternative medicine for hypothyroidism.

Effects of Bupleuri Radix on the Rat Hypothyroidism Induced by PTU (6-n-propyl-2-thiouracil) (시호가 PTU (6-n-propyl-2-thiouracil)로 유발된 Rat 갑상샘 기능저하증에 미치는 영향)

  • Kim, Seong Mo;Ku, Sae Kwang;Cho, Su Yeon;Park, Soo Jin
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.26 no.5
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    • pp.714-723
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    • 2012
  • The object of this study was to evaluate the effect of Bupleuri Radix, aqueous extracts of the root part of Bupleurum falcatum on the 6-n-propyl-2-thiouracil (PTU)-induced rat hypothyroidism. Aqueous extracts of Bupleuri Radix (BR; yield = 11.73%) were administered, once day for 42 days from 2 weeks before start of PTU treatment as an oral dose of 300 and 150 mg/kg (body weight), and hypothyroidism was induced by daily subcutaneous treatment of PTU 10 mg/kg for 28 days. The changes on the body weight, thyroid gland weights, serum thyroid hormone - thyroid stimulating hormone (TSH), triiodothyronine ($T_3$) and thyroxine ($T_4$), serum lipid profiles - total cholesterol, low density lipoprotein (LDL), high density lipoprotein (HDL) and triglyceride, liver antioxidant defense system - lipid peroxidation, $H_2O_2$, superoxide dismutase (SOD) and catalase (CAT), serum aspartate aminotransferase (AST) and alanine aminotransferase (ALT) were observed with histopathology of thyroid glands. Results were compared with $LevoT_4$ 0.5 mg/kg treated rats. As results of PTU treatment, marked decreases of body weights, triglyceride contents, liver CAT activities and changes of serum thyroid hormone levels were observed with increases of serum AST, HDL contents, liver $H_2O_2$ and SOD activities and thyroid gland weight. In addition, marked hyperplasia of follicular cells with decreases of follicular colloid contents and sizes were demonstrated at histopathological inspections. However, these PTU induced hypothyroidism were dose-dependently inhibited by treatment of BR extracts, and BR extracts effectively regulated the hypothyroidism related changes on the antioxidant defense system. The results obtained in this study suggest that BR extracts have favorable effects on the thyroid hormone productions with beneficial effects on the hypothyroidism mediated by the modulatory effects on the antioxidant defense system.

Effects of Lonicerae Flos on the 6-n-propyl-2-thiouracil (PTU)-induced Rat Hypothyroidism (금은화가 6-n-propyl-2-thiouracil (PTU) 로 유발된 흰쥐의 갑상샘 기능저하증에 미치는 영향)

  • Ku, Sae-Kwang;Lee, Young-Joon
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.24 no.4
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    • pp.630-637
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    • 2010
  • The object of this study was to evaluate the effect of Lonicerae Flos, aqueous extracts of the dried flower bud part of Lonicera japonica on the 6-n-propyl-2-thiouracil (PTU)-induced rat hypothyroidism. Aqueous extracts of Lonicerae Flos (LF yield = 23.80%) were administered, once day for 42 days from 2 weeks before start of PTU treatment as an oral dose of 500 and 250 mg/kg (body weight), and hypothyroidism was induced by daily subcutaneous treatment of PTU 10 mg/kg for 28 days. The changes on the body weight, thyroid gland weights, serum thyroid hormone - thyroid stimulating hormone (TSH), tri-iodothyronine ($T_3$) and thyroxine ($T_4$), serum lipid profiles - total cholesterol, low density lipoprotein (LDL), high density lipoprotein (HDL) and triglyceride were observed with liver antioxidant defense system - lipid peroxidation, $H_2O_2$, superoxide dismutase (SOD) and catalase (CAT) and serum asparte aminotransferase (AST) and alanine aminotransferase (ALT) analysis. Results were compared with Levothyroxine ($LT_4$) 0.5 mg/kg treated rats. As results of PTU treatment, marked decreases of body weights, serum thyroid hormone levels and triglyceride contents, liver $H_2O_2_3$ and SOD activities were observed with increases of serum AST and HDL contents, liver CAT activities, thyroid gland weight. However, these PTU induced hypothyroidism were dose-dependently inhibited by treatment of LF extracts, and LF extracts effectively regulated the hypothyroidism related changes on the antioxidant defense system. The results obtained in this study suggest that LF extracts have favorable effects on the thyroid hormone productions with beneficial effects on the hypothyroidism mediated by the modulatory effects on the antioxidant defense system.

Effects of Sipjeondaebotang on the white rat Hypothyroidism Induced by PTU(6-n-propyl-2-thiouracil) (PTU로 유발된 흰쥐의 갑상선 기능저하증에 미치는 십전대보탕(十全大補湯)의 효과)

  • Choi, Jae Young;Seo, Bu Il
    • Herbal Formula Science
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    • v.24 no.3
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    • pp.131-152
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    • 2016
  • Objectives : This study was to evaluate Sibjeondaebo-tang’s(Shiquan dabutang) effect to rat hypothyroidism which induced by 6-n-propyl-2-thiouracil(PTU)Methods : Aqueous extracts of Sibjeondaebo-tang(Shiquan dabutang)(21.29%) were administered by oral dose of 300 and 150 mg/kg(rat’s body weight) for 42 days from 2 weeks before start of PTU treatment. During this moment the body weight, thyroid gland weights, liver weight, serum thyroid hormone, lipid content and liver antioxidant defense system were measured with histopathological changes of thyroid glands, Liver and these result were compared with LevoT4 0.5mg/kg treated ratsResults : As a result of PTU treatment, marked decreases of body weight, liver weight, serum thyroid hormone levels of T3, T4, triglyceride content and liver CAT activation were observed with marked increases of thyroid gland weight, thyroid gland hormone TSH, activate liver H2O2 and SOD, serum Total cholesterol, HDL and AST amount were admitted. In addition, marked hyperplasia of follicular cells with reduce of follicular colloid contents and sizes were showed at histopathological inspections. These PTU-induces histopathological changes related to hypothyroidism were significantly reduced by treatment of both different dosages of Sibjeondaebo-tang(Shiquan dabutang).Conclusions: This study suggest that Sibjeondaebo-tang(Shiquan dabutang) extracts have favorable effect on the thyroid hormone productions with beneficial effect on hypothyroidism medicated by modulatory effects on antioxidant defense system.

Effects of Mume Fructus on the Rat Hypothyroidism Induced by PTU(6-n-propyl-2-thiouracil) (PTU(6-n-propyl-2-thiouracil)로 유발된 Rat 갑상선 기능저하증에 미치는 烏梅의 효과)

  • Choi, Jae Young;Roh, Seong Soo;Park, Ji Ha;Koo, Jin Suk;Seo, Bu Il
    • The Korea Journal of Herbology
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    • v.30 no.4
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    • pp.109-119
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    • 2015
  • Objectives : The aim of this study was to evaluate the effect of aqueous extracts of Mume Fructus(MF) on the 6-n-propyl-2-thiouracil(PTU)-induced rat hypothyroidism.Methods : Aqueous extracts of MF(yield = 19.38%) were administered, once per day for 42 days from 2 weeks before starting of PTU treatment as an oral dose of 300 and 150 ㎎/㎏(body weight), and hypothyroidism was induced by daily subcutaneous treatment of PTU 10 ㎎/㎏ for 28 days. The changes in the body weight, thyroid gland weights, liver weight, serum levels of thyroid hormone-thyroid stimulating hormone(TSH), tri-iodothyronine(T3) and thyroxine(T4), total cholesterol, low density lipoprotein(LDL), high density lipoprotein(HDL) and triglyceride (TG), aspartate aminotransferase(AST), alanine aminotransferase(ALT), liver antioxidant defense system-lipid peroxidation, H2O2, superoxide dismutase(SOD) and catalase(CAT) were examined with histopathology of thyroid glands and liver.Results : Results were compared with LevoT40.5 ㎎/㎏ treated rats. MF extracts recovered from the decreases in the body weight, liver weight, T3and T4, TG, liver CAT activities as results of PTU treatment. And MF extracts recovered from the increases of thyroid gland weights, TSH, HDL contents, liver H2O2, AST as results of PTU treatment. In addition, these PTU-induced histopathological changes in thyroid glands and liver related to hypothyroidism were dramatically decreased by treatment of both different dosages of MF extract, respectively.Conclusions : According to the above results, it is suggested that MF extracts have advantageous effects on the thyroid hormone productions with beneficial effects on the hypothyroidism related liver injuries mediated by the modulation on the antioxidant system.