• Title/Summary/Keyword: 5-bromo-2-deoxyuridine

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Syntheses and Biological Activities of Uridine Nucleoside Derivatives (Uridine Nucleoside 유도체의 합성과 생물 활성)

  • Bong-Hun Lee;Jang-Su Park;Shin-Won Kang
    • Journal of Life Science
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    • v.9 no.1
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    • pp.63-68
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    • 1999
  • Many nucleoside compounds such as 5-halogen substituted uridine, 5'-amino-5'-deoxyuridine conjugates of amino acid, peptide, and penicillin G, 5'-monophosphate uridine derivatives and 5'-monophosphate uridine-fatty acid derivatives were chemically synthesized and their antifungal, antibacterial, and antitumor activities were tested. 5-Bromo-2',3'-O-isopropylideneuridine(6) inhibited the growth of Trichophyton rubrum at $0.2{\mu}$g/ml of MIC. 5'-Amino-5'-deoxyuridine-penicillin G(19), 5'-amino-5'-deoxyuridine-cyclo(Phe-Asp)(20), and 5-iodo-5'-amino-5'-deoxyuridine- penicillin G(22) had antibarterial activity(MIC was $6.25{\mu}$g/ml against S. aureus) and the latter two nucleoside compounds were the most antitumor derivatives(their $IC_{50}$ against L5178Y murine lymphoma cell was $6.5{\mu}$g/ml).

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A study on the Synthesis and Biological Activity of Nucleoside Chemotherapeutic Agents (핵산계 화학요법제의 합성 및 생물활성에 관한 연구)

  • 강신원;김경희;신정희;이봉헌;장태식
    • Korean Journal of Microbiology
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    • v.29 no.6
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    • pp.353-360
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    • 1991
  • 5-substituted uridine(I,Br,Cl), 5'-amino-5'-deoxyuridine conjugates of amino acid, peptide and penicillin G, 5'-monophosphate uridine derivatives and 5'-monophosphate-fatty acid detrivatives were chemically synthesized. Their biological activities were determined as MIC and IC/sub 50/ unit against various pathogenic microorganisms in vitro. 5'-amino-5'-deoxyuridine-cyclo(Phe-Asp)(23), 5-iodo-5'-amino-deoxyuridine-penicillin G(26) were the most efficient; their IC/sub 50/ against L5178Y murine lymphoma cell was 6.5 h/ml, MIC against S. aureus (+) and E. coli (-) was 6.25 g/ml. MIC of 5-bromo-2', 3'-O-isopropylideneuridine(6) against Trichophyton rubrum was 0.2 g/ml. And 5'-monophosphate derivatives are more active than simple uridine derivatives, suggesting other modified nucleoside 5'-phosphate may be worthwhile examing further as a new prodrugs.

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Effects of Ginseng radix on Alcohol-induced Decrease in New Cell Formation and Nitric Oxide Synthase Expression in Dentate Gyrus of Rats (인삼이 흰쥐의 치상회에서 알코올에 의한 새로운 신경세포 생성 및 nitric oxide synthase 발현에 미치는 영향)

  • Min-Chul, Shin;Ee-Hwa, Kim;Youn-Hee, Kim
    • The Journal of Korean Medicine
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    • v.23 no.3
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    • pp.26-32
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    • 2002
  • 목적 : 본 연구에서는 알코올 독성에 대하여 흰쥐의 치상회에서 새로운 신경세포의 생성 및 nitric oxide synthase (NOS) 발현에 인삼이 미치는 영향을 5-bromo-2-deoxyuridine (BrdU) 면역 조직 화학법 및 nicotinamide adenine dinucleotide phosphate-diaphorase (NADPH-d) 조직화학법을 통해서 관찰하고자 한다. 방법 : 실험동물을 정상군, 인삼처치군, 알코올처치군 및 알코올-인삼 처치군으로 분류하여 각각의 실험군에 3일간 BrdU (50mg/kg)를 복강주사하였다. 인삼처치군은 30mg/kg 용량의 인삼 전탕액을 중완혈에 약침주사하였고, 알코올 처치군은 2 g/kg 용량의 알코올을 투여하였으며. 알코올-인삼 처치군은 2 g/kg 용량의 알코올 및 30mg/kg 용량의 인삼 전탕액을 투여한 후 각각의 BrdU 양성 세포수와 NADPH-d 양성세포수를 관찰하였다. 결과 : 알코올 투여군은 BrdU 양성세포 및 NADPH-d 양성세포 발현이 감소하였으나, 인삼 및 알코올 인삼처치군에서는 알코올 투여군에 비해서 모두 증가하였다. 결론 : 인삼은 알코올에 의해서 유발된 새로운 신경세포 생성의 감소에 대하여 보호효과가 있으며, 알코올에 의해서 부가적으로 영향 받는 산화질소는 세포생성 조절에 중요한 역할을 하는 것으로 사려된다.

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Effect of Liuweidihuang-tang on Alcohol-induced Decrease in New Cell Formation in Rat Dentate Gyrus

  • Bahn Goon Ho;Yoon Doh Joon;Park Jin Kyung;Lee Taeck Hyun;Jang Mi Hyoon;Shin Min Chul;Kim Chang Ju;Paik Eun Kyung;Park Jae Hyung;Cho Son Hae;Lee Choong Yool
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.16 no.5
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    • pp.1055-1059
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    • 2002
  • Liuweidihuang-tang has been traditionally used for the treatment of delayed mental and physical development in children, complications of diabetes. and glomerulonephritis. In the present study, the effect of Liuweidihuang-tang on cell proliferation in the dentate gyrus of alcohol-intoxicated Sprague-Dawley rats was investigated via 5-bromo-2' -deoxyuridine (BrdU) immunohistochemistry. Alcohol administration was shown to decrease the number of BrdU-positive cells in the dentate gyrus, while Liuweidihuang-tang treatment increased new cell formation in the dentate gyrus under normal conditions and alcohol intoxication. It was thus demonstrated that aqueous extract of Liuweidihuang-tang exerts a protective effect against alcohol-induced decrease in new cell formation.

Effect of bee venom on cell proliferation and cyclooxygenase 2 expression in the dentate gyrus of mice with acetic acid induced hyperalgesia (세포 증식과 COX 2 발현에 미치는 봉독의 효과)

  • Lyoo, Eun-kyoung;Choi, Do-young;Lee, Jae-dong
    • Journal of Acupuncture Research
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    • v.20 no.2
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    • pp.112-122
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    • 2003
  • 연구 배경 및 목적 : 봉독은 항염증 등의 효과를 가지고 있다고 알려져 있지만 세포 증식과 관련된 봉독의 효과에 대한 고찰을 위해 본 연구(硏究)에서는, 봉독(蜂毒) 약침(藥鍼) 자극(刺戟)이 아세트산 유발(誘發) 통각(痛覺) 과민증(過敏症)을 가진 쥐의 치상회(齒狀回)에서의 세포(細胞) 증식(增植)과 COX2 발현(發現)에 미치는 영향(影響)에 대해 알아보고자 하였다. 실험방법 : 대조군, 아세트산 처치군, 아세트산 0.1mg/kg 봉독 처치군, 아세트산 1mg/kg 봉독처치군(n=5 in each group)의 네 군으로 나누고 해당 군에 일벌 봉독(蜂毒)(Sigma Chemical Co., St. Louis, MO, USA)을 양측 족삼리 경혈(ST36)에 주입시키고 30분 후 아세트산(100% acetic acid 1% 용액의 0.5ml)을 복강내로 주입하여 복부 긴장 회수를 세었으며, BrdU 양성, COX 2 양성 세포수를 면역 화학 조직법을 수행하여 세어 보았다. 결과 : 아세트산 처치군에서는 대조군에 비해 5 bromo 2' deoxyuridine 양성 세포의 수는 감소(減少)되며, 치상회(齒狀回)에서의 COX 2의 발현(發現)은 증강(增强)되는 것으로 보여졌다. 봉독(蜂毒) 주입(注入)은 아세트산 유발(誘發) 복부(腹部) 긴장(緊張) 횟수와 치상회(齒狀回)에서의 COX2 발현(發現)을 억제(抑制)하여, 치상회(齒狀回)에서의 세포(細胞) 증식(增植)을 증가(增加)시켰다. 결론 : 이번 결과(結果)에서 보면, 치상회(齒狀回)에서의 COX 2의 발현(發現)은 세포(細胞) 증식(增植) 억제(抑制)와 관련(關聯)되며 봉독(蜂毒)은 COX 2 발현(發現) 억제(抑制)를 통해 치상회(齒狀回)에서의 새로운 세포(細胞) 형성(形成)을 증가(增加)시킨다는 것을 알 수 있다.

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Decreased Diethylnitrosamine-induced Liver Preneoplastic Lesions by Estradiol-3-benzoate Treatment

  • Kang, Jin-Seok;Park, Ki-Dae;Ahn, Byeong-Woo;Han, Beom-Seok
    • Toxicological Research
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    • v.27 no.4
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    • pp.247-251
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    • 2011
  • To clarify whether inhibitory effect of estrogen on liver tumor is associated with cell proliferation, we investigated its role in diethylnitrosamine (DEN)-induced rat preneoplastic lesions, with time sequenced manners. F344 male rats (n = 90) were divided into three groups at 5 weeks of age. The mini-osmotic pumps providing a continuous infusion of DEN was implanted into the abdominal cavity of each animal in group 1, 2 and 3 at 6 weeks of age. To see the effect of estrogen, pellet containing 1 or 10 ${\mu}g$ of estradiol-3-benzoate (EB) was implanted subcutaneously in the animals of groups 2 or 3, respectively, one week prior to DEN treatment. Ten animals of each group were euthanized at 10, 14 and 18 weeks after DEN treatment. Liver tissues at each time point were fixed in 10% phosphate-buffered formalin and were processed and embedded in paraffin and 5 ${\mu}g$ sections mounted on a silanized slide. Glutathione S-transferase placental form (GST-P) positive foci and 5-bromo-2-deoxyuridine (BrdU) labeling cells were detected at each time point. Area of GST-P positive foci in DEN+EB 1 or 10 ${\mu}g$ group was significantly decreased compared to DEN alone at 14 weeks (p < 0.01 or p < 0.05, respectively) an at 18 weeks (p < 0.05 or p < 0.01, respectively). BrdU index in DEN+EB 1 or 10 ${\mu}g$ groups was significantly decreased compared to DEN alone at 14 weeks and at 18 weeks (p < 0.01). Taken together, we conclude that EB treatment decrease the DEN-induced liver preneoplastic lesions and this may be associated with decrease of cellular proliferation.

BrdU에 의한 DNA

  • 손우찬;김형진;이영순
    • Toxicological Research
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    • v.7 no.1
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    • pp.83-92
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    • 1991
  • Complexities of testis structure and function are emphasized in morphometrical and genotoxic evaluation by statistical analysis. F-344 rats were treated with azinphos methyl, cyclophosphomide, and dichlorvos. And Brdu was injected with intrapertionially before sacrifice. The existence and degree of DNA damage were measured by Brdu labeling index which represented relative amount of Brdu incorporated in DNA, morphometric change was evaluated by the relative length of tubular diameter in circular seminiferous tubules and the number of spermatogonia per Sertoli cell in stage IX seminiferous tubules.

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Puerariae radix increases Alcohol-induced Suppressed Cell Proliferation and Expression of Nitric Oxide Synthase in Dentate Gyrus of Rats

  • Jang Mi Hyean;Lee Taeck Hyun;Shin Min Chul;Lim Baek Vin;Kim Hyun Bae;Lim Sabina;Kim Jin Woo;Lee Cheong Yeal;Kim Ee Hwa;Kim Chang Ju
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.16 no.1
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    • pp.192-196
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    • 2002
  • Traditionally, aqueous extracts of Puerariae radix had been used for the treatment of alcohol-related problems. In the present study, the effect of Puerariae radix on cell proliferation and expression of nitric oxide synthase (NOS) in the dentate gyrus of alcohol-intoxicated rats were investigated via 5-bromo-2' -deoxyuridine (BrdU) immunohistochemistry and nicotinamide adenine dinucleotide phosphate-diaphorase (NADPH-d) histochemistry, respectively. Sprague-Dawley rats weighing 150 ± 10 g were divided into four groups: the control group, the Puerarias radix-treated group, the alcohol-treated group, and the alcohol- and Puerariae radix-treated group. The numbers of both BrdU-positive and NADPH-d-positive cells in the dentate gyrus were inhibited significantly by alcohol administration, while Puerariae radix treatment was shown to increase those numbers. In this study, it was revealed that Puerariae radix possesses protective effect against alcohol-induced suppressed new cell formation and NOS expression in the dentate gyrus. Based on the results, it is possible that NO, which might play an important role in the regulation of cell proliferation, is a major target of the toxic effects of alcohol.

Sister Chromatid Exchanges in Lymphocytes on Normal Human Blood Culture with Mercury chloride or Methylmercury Chloride (Mercury chloride 및 Methylmercury chloride가 정상인(正常人)의 혈액배양(血液培養)에서 임파구(淋巴球)의 자매염색분체교환(姉妹染色分體交換)에 미치는 영향(影響))

  • Koh, Dai-Ha
    • Journal of Preventive Medicine and Public Health
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    • v.17 no.1
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    • pp.245-250
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    • 1984
  • Reciprocal exchanges of DNA in sister chromatids (SCEs) are induced by various carcinogens and mutagens, although the quantitative relationship between the number of mutations and SCEs induced varies among chemicals. Nevertheless, the analysis of SCEs production by various agents often proposed as a sensitive and quantitative assay for mutagenicity and cytotoxicity. Mercury, even if which has no evidences for mutagenicity and carcinogenicity, is reported to exert some cytotoxic effects, such as chromosomal aberrations or bad influences to ovulation and reproduction in experimental animals, etc.. In this study, tests for sister chromatid exchanges have been carried out on normal human lymphocytes in whole blood culture to add mercury chloride ($HgCl_2$) or methylmercury chloride ($CH_3\;HgCl$) for 72 hr. The results indicate the dose-dependent relationship between the frequencies of SCEs and the concentrations of $HgCl_2,\;CH_{3}HgCl$ and 5-bromo-2'-deoxyuridine (BrdU). Lymphocyte proliferation has depressed in the higher concentration of mercury.

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Melatonin increases cell proliferation in the dentategyrus of maternally-separated rats

  • Jung, Kyung-Hee;Jung, Eun-young;Kim, Mi-Ja;Kim, Hye-Kyung;Kim, Yong-Ok;Chang, Un-Jae;Yim, Sung-Vin
    • Proceedings of the KSCN Conference
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    • 2004.05a
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    • pp.439.2-439
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    • 2004
  • Melatonin in mammals, produced by the pineal gland and elsewhere, has shown antioxidant and neuroprotective properties in neuronal cells. We investigated whether melatonin would increase newly-born cells (cell proliferation) in the dentate gyrus of maternally-separated rats. To examine the effect of melatonin on cell proliferation of the dentate gyrus in maternally-separated rats, 5-bromo-2'-deoxyuridine (BrdU) immunohistochemistry was performed.(omitted)

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