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Imidazolidine-2,4,5-trione 혹은 2-thio-imidazolidine-4,5-dione기를 포함하는 새로운 saccharin 유도체의 합성 (Synthesis of the New Saccharin Derivatives Containing Imidazolidine-2,4,5-trione or 2-Thio-imidazolidine-4, 5-dione Group)

  • Jung, Dai-Il;Byun, Suk-In;Kim, Yun-Young;Kim, Young-Hwan;Lee, Do-Hun;Song, Hyun-Ae;Lee, Yong-Gyun;Park, Yu-Mi;Choi, Soon-Kyu;Han, Jung-Tae
    • 생명과학회지
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    • 제14권2호
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    • pp.351-355
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    • 2004
  • 활성있는 새로운 농약을 창출하기 위해, saccharin 모체에 imidazolidine-2,4,5-trione과 2-thio-imidazolidine-4,5-dione 기를 도입시켰다. 각 saccharin 유도체들은 1-치환된 urea (혹은 1-치환된 thiourea)와 oxalyl chloride의 반응을 시작으로 4단계를 거쳐 합성하였다. 1-치환된 urea를 사용해서 1-치환된-3-(1,1,3-trioxo-1,3-dihydro-1$^{6}$-benzo[d]isothiazol-2- ylmethyl)-imidazolidine-2,4,5-trione 5a, 5b, 5c를 합성하였고, 1-치환된 thiourea를 사용하여 1-치환된-2-thioxo-3-(1,1,3-trioxo-1,3-dihydro-1$^{6}$-benzo[d]isothiazol-2-ylmethyl)-imidazolidine-4,5-dione 12a,12b, 12c를 합성하였다.

N-[1-(benzotriazol-1-yl)butyl]-p-nitroaniline의 구조 (Crystal Structure of N[1(benzotriazol-1-yl)butyl]-p-nitroaniline)

  • 조소라;김문집;성낙도
    • 한국결정학회지
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    • 제5권2호
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    • pp.78-84
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    • 1994
  • N-[1-(benzotriazol-1-yl)butyl]-P-nitroaniline ( BBN, C6H7N502) 의 분자 및 결정구조를 반-선 회절 법Abstract으로 연구하였다. 이 결정은 단사정계이고 공간군은 P21/n이다. 단위세포 길이는 a=17.542(2)A, b= 10.755(3)A, c=8.891(1)A 이며 a=b=r=90˚,b=104.58(1)˚,Z=4 이다.구조해석에 사용한 X-선은 CuKa선(λ:1.5418A )을 사용하였다. 분자구조는 직접법으로 풀었으며 최소자승법으로 정밀화하였 다. 최종 신뢰도 R값은 255개 파라메터, F≥4o(F)인 2248개의 회절반점에 대하여 R= 0.0411 이었다. 분자간 결합은 1개의 수소결합인 N(11)-Hll(Nll)‥‥N(3)로 결합되어 있으며, N(11)‥‥N(3)=3.136(2).1, N(11)-Hl 1 (Nl 1) ‥‥N(3) =164.1(15)˚이다.

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Susceptibility of Lung Cancer with Polymorphisms of CYP1A1, GSTM1, GSTM3, GSTT1 and GSTP1 Genotypes in the Population of Inner Mongolia Region

  • Jiang, Xue-Yan;Chang, Fu-Hou;Bai, Tu-Ya;Lv, Xiao-Li;Wang, Min-Jie;Wang, Guang
    • Asian Pacific Journal of Cancer Prevention
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    • 제15권13호
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    • pp.5207-5214
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    • 2014
  • Background: To study the relationship of susceptibility to lung cancer with the gene polymorphisms of CYP1A1, GSTM1, GSTM3, GSTT1, GSTP1 and smoking status in Han and Mongolian populations of Inner Mongolia, an autonomous region of China. Materials and Methods: PCR-RFLP, allele-specific and multiplex PCR were employed to identify the genotypes of CYP1A1, GSTM1, GSTM3, GSTT1 and GSTP1 in a case-control study of 322 lung cancer patients diagnosed by bronchoscopy and 456 controls free of malignancy. Results: There is a significant difference in genotypic frequency of GSTT1 of healthy Mongolian and Han subjects. A statistically prominent association was found between CYP1A1 Msp1 (vt/vt) (OR=4.055, 95%CI:2.107-7.578, p=0.000), GSTM1 (-) (OR=2.290, 95%CI:1.467-3.573, p=0.000) and lung cancer in Mongolians. Similarly, in the Han population, CYP1A1 Msp1 (vt/vt) (OR=3.194, 95%CI:1.893-5.390, p=0.000) and GSTM1 (-) (OR=1.884, 95%CI:1.284-2.762, p=0.001) carriers also had an elevated risk of lung cancer. The smokers were more susceptible to lung cancer 2.144 fold and 1.631 fold than non-smokers in Mongolian and Han populations, respectively. The smokers who carried with CYP1A1 Msp1 (wt/vt+vt/vt), exon7 (Val/Val+Ile /Val), GSTM1 (-), GSTM3 (AB+BB), and GSTT1 (-) respectively were found all to have a high risk of lung cancer. Conclusions: CYP1A1 Msp1 (vt/vt) and GSTM1 (-) are risk factors of lung cancer in Han and Mongolian population in the Inner Mongolia region. The smokers with CYP1A1 Msp1 (wt/vt+vt/vt), CYP1A1 exon7 (Val/Val+Ile /Val), GSTM1 (-), GSTM3 (AB+BB), and GSTT1 (-) genotypes, respectively, are at elevated risk of lung cancer.

프라바스타틴에서 $SLCO1B1^*15$의 약동학적 영향: 체계적 고찰 및 메타분석 (Effect of $SLCO1B1^*15$ on Pravastatin Pharmacokinetics: A Systematic Review and Meta-analysis)

  • 김종윤;나오토 나카가와;윤현옥;천부순;유기연
    • 한국임상약학회지
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    • 제24권4호
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    • pp.231-239
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    • 2014
  • Background and objective: Pravastatin has been shown to have favorable risk-benefit profile when it is administered to hypercholesterolemic subjects to prevent cardiovascular events. However, subjects with impaired OATP1B1 activity may be more susceptible to pravastatin-induced muscle toxicity than subjects with normal OATP1B1 activity. A systematic review was conducted to evaluate the effect of SLCO1B1 genetic polymorphism on pharmacokinetics of pravastatin. Method: Medline$^{(R)}$ and Embase$^{(R)}$ were searched for relevant studies until July 2013. The search terms used were pravastatin AND (SLCO1B1 OR OATP1B1 OR LST1 OR SLC21A6) AND (gene OR $genetic^*$ OR $genomic^*$ OR $pharmacogenet^*$ OR $pharmacogenom^*$ OR $polymorph^*$). Results: A meta-analysis of the area under the concentration-time curve (AUC) of pravastatin in $SLCO1B1^*15$ and $SLCO1B1^*1a/^*1a$ was conducted. Five studies met all the inclusion criteria and methodological requirements. There was no statistically significant difference in the AUC value between $SLCO1B1^*15$ and $SLCO1B1^*1a/^*1a$ (p=0.728). However, $SLCO1B1^*15$ participants exhibited significantly higher AUC values than $SLCO1B1^*1b/^*1b$ carriers (p<0.001). In case of $SLCO1B1^*15^*15$ carriers, they had significantly higher AUC value than $SLCO1B1^*1a/^*1a$ subjects (p=0.002). Lastly, compared with to the subjects of $SLCO1B1^*1a/^*1a$, the carriers of heterozygous $SLCO1B1^*15$ increased the AUC value of pravastatin statistically significantly in Asian population (p=0.014). Conclusion: The present meta-analysis suggests that subjects with $SLCO1B1^*15$ are associated with increased AUC of pravastatin.

경운깊이 및 퇴비 시용량이 고추 생육에 미치는 영향 (Effect of Tillage Depth and Amount of Compost on Red Pepper Growth)

  • 이경자;김영상;송인규
    • 한국토양비료학회지
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    • 제43권6호
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    • pp.798-803
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    • 2010
  • 노지 고추재배시 경운 깊이에 따른 유기물 함량을 구명하여 지속적 안전생산에 활용하고자 경운 깊이는 10, 30 및 50 cm로 하고 퇴비의 양을 1, 3 및 5 톤 $10a^{-1}$으로 처리하여 고추를 재배한 결과 다음과 같다. (1) 시험후 토양의 pH는 모든 처리에서 시험전 토양보다 낮아졌으며 EC를 비롯한 Av. $P_2O_5$, K, Ca, Mg, Na는 시험전보다 높았다. 퇴비 시용량 별로는 퇴비 1 톤 $10a^{-1}$ 및 3 톤 $10a^{-1}$ 처리에 비해 퇴비 5 톤 $10a^{-1}$에서 높았다. (2) 고추 생육은 퇴비 1 톤 $10a^{-1}$처리에 비하여 퇴비 3 톤 및 5 톤 $10a^{-1}$에서 좋았으며, 경운깊이 10 cm 및 30 cm에 비해 경운깊이 50 cm에서 좋았다. (3) 고추 수량은 경운깊이 10 cm에서는 퇴비 3 톤 $10a^{-1}$ 처리에서 5,880 kg $ha^{-1}$으로 가장 좋았고, 경운깊이 30 cm 에서는 퇴비 5 톤 $10a^{-1}$ 처리에서 5,610 kg $ha^{-1}$으로 가장 좋았다. (4) 고추식물체의 T-N 함량 및 흡수량은 퇴비 3 톤 $10a^{-1}$ 및 5 톤 $10a^{-1}$ 처리에서 1 톤 $10a^{-1}$처리에 비해 높았다.

Anti-oxidative effects of exogenous ganglioside GD1a and GT1b on embryonic developmental competence in pigs

  • Kim, Jin-Woo;Park, Hyo-Jin;Yang, Seul-Gi;Koo, Deog-Bon
    • 한국동물생명공학회지
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    • 제35권4호
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    • pp.347-356
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    • 2020
  • Gangliosides are glycolipids in which oligosaccharide is combined with sialic acids. Our previous studies have suggested an interplay between ganglioside GD1a/GT1b and meiotic maturation capacity in porcine oocyte maturation. Furthermore, ganglioside GD1a and GT1b are known for its antioxidant activity, but it is still unclear whether possible antioxidant role of GD1a and GT1b is involved in porcine embryos development competence during in vitro culture (IVC). Here, the effects of ganglioside GD1a and GT1b on the embryonic developmental competence during in vitro culture of porcine were investigated. The effects of ganglioside GD1a and GT1b on the expression of ST3GAL2 were confirmed during embryos development (2-cell, 4-cell, 8-cell and blastocyst) using immunofluorescent staining (IF). As a result, the fluorescent expression of ST3GAl2 was higher in embryos at 4-8 cells stage than blastocysts. Blastocyst development rate significantly increased in only 0.1 μM GD1a and GT1b treated groups compared with control group. To investigate the cellular apoptosis, we analyzed TUNEL assay. In case of only 0.1 μM GD1a and GT1b treated groups, the total number of cells in blastocyst compared with control group, but there was no significant difference in the rate of apoptotic cells. We identified the intracellular ROS levels using DCF-DA staining. According to the result, ROS production significantly decreased in blastocysts derived from the 0.1 μM GD1a and GT1b treated groups. These results suggest that ganglioside GD1a and GT1b improve the developmental competence of porcine embryos via reduction of intracellular ROS during preimplantation stage.

PAH가 송어 RTH-149세포에서 CYP1A1 유전자 발현에 미치는 영향 (Effect of PAH on CYP1A1 Gene Expression in Trout RTH-149 Cells)

  • 김지선;신윤용
    • 한국환경성돌연변이발암원학회지
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    • 제24권4호
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    • pp.155-162
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    • 2004
  • In mammalian, cytochrome P4501A1 (CYP1A1) is very important for metabolism of xenobiotics such as PAHs(Polycyclic aromatic hydrocarbon) and heterocyclic amine, and it is induced by environmental contaminants such as PAHs, TCDD(2,3,7,8-tetrchlorodibenzo-p-dioxin) and 3-MC (3-methylcholanthrene). In fish, like mammalian, when it is exposed to environmental contaminants, they cause specific and sensitive induction of CYP1A. Therefore, induction of CYP1A in fish and mammalian is widely used as a biomarker for exposure of environmental contaminants. In this study, to compare the function of Cyp1a1 in fish with it in mammalian, we have used rainbow trout(Oncorhynchys mykiss) hepatoma cells (RTH-149) and mouse hepatocyte (Hepa-I). in order to examine induction of Cyp1a1 by TCDD, we have used the bioassay system. We examined effects of TCDD on the Cyp1a1-luciferase reporter gene activity, 7-ethoxyresorufin O-deethylase(EROD) activity and Cypa mRNA level.

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소아 Helicobacter pylori 감염에서 Clarithromycin 내성과 연관된 23S rRNA의 돌연변이 (Detection of 23S rRNA Mutation Associated with Clarithromycin Resistance in Children with Helicobacter pylori Infection)

  • 고재성;양혜란;서정기
    • Pediatric Gastroenterology, Hepatology & Nutrition
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    • 제7권2호
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    • pp.137-142
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    • 2004
  • 목적: 우리 나라 소아에 감염된 H. pylori에서 PCR RFLP를 이용하여 clarithromycin 내성의 원인으로 알려진 23S rRNA의 돌연변이를 찾아내고, cagA, vacA 유전형과 clarithromycin 내성 돌연변이 사이에 연관이 있는지 알아보고자 하였다. 방법: 서울대학교병원 소아과에서 위내시경검사를 통해 H. pylori 위염으로 진단 받은 환아 27명의 내시경 생검 조직에서 H. pylori cagA, vacA 유전자를 증폭하여 유전형을 조사하였다. H. pylori의 23 rRNA V domain을 조사하기 위해 증폭한 후, PCR 산물은 BsaI과 MboII 제한효소로 처리하여 PCR RFLP를 이용하여 돌연변이 여부를 판정하였다. 결과: A2143G 돌연변이가 1명에서, A2144G 돌연변이가 4명에서 발견되어 18.5%가 clarithromycin 내성으로 관찰되었다. cagA 양성이 25명(93%)이었고, vacA s1a/m1이 6명(22%), s1a/m2가 3명(11%), s1c/m1이 16명(59%), s1c/m2가 1명(4%)이었다. clarithromycin 내성 돌연변이를 보이는 경우는 모두 cagA 양성이었고 s1a/m1이 2명, s1c/m1이 2명으로 특정 유전형이 clarithromycin 내성 돌연변이와 연관성을 보이지 않았다. 결론: 위점막 조직에서 PCR-RFLP를 이용한 H. pylori의 clarithromycin 내성 검사는 항생제를 선택하는데 유용하다고 생각된다. Clarithromycin 내성 돌연변이는 cagA, vacA 유전형과 연관성이 없었다.

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Increased UGT1A3 and UGT1A7 Expression is Associated with Pancreatic Cancer

  • Yilmaz, Latif;Borazan, Ersin;Aytekin, Turkan;Baskonus, Ilyas;Aytekin, Alper;Oztuzcu, Serdar;Bozdag, Zehra;Balik, Ahmet
    • Asian Pacific Journal of Cancer Prevention
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    • 제16권4호
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    • pp.1651-1655
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    • 2015
  • UGT1A play important roles in the glucuronidation of a variety of endogenous and exogenous compounds. UGT1A isoforms are expressed tissue specifically. The aim of this study was to examine the relationship between UGT1A3 and UGT1A7 mRNA expression and pancreatic cancer. Paired healthy and tumor tissue samples of 43 patients with pancreatic cancer were included in this study. UGT1A3 and UGT1A7 mRNA expressions were analyzed by real time-PCR. In the result of study, UGT1A3 and UGT1A7 mRNA expressions were significantly higher in tumor tissue than normal tissue of pancreatic cancer patients (p<0.05). In addition, high mRNA expression of UGT1A3 and UGT1A7 was significantly associated with larger tumor size (p<0.05). The data suggested that UGT1A3 and UGT1A7 may play roles in the progression of pancreatic cancer. Consequently, UGT1A3 and UGT1A7 are potential prognostic indicators.

Synthesis of sulphonic acids and sultam derivatives

  • Ismail, Ibrahim-Imam
    • Archives of Pharmacal Research
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    • 제13권1호
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    • pp.1-4
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    • 1990
  • Reaction of propane-1, 3-sultone with amines gave N-substituted aminosulphonnic acids 2a-i, Dehydration of 2a-c with $POCI_3$ gave the corresponding sultams 3a-c. Propane-1, 3-sultone 1 reacted with tertury amines to give the betaiene salts 4-11. 2-4-Dimethyl-1, 3-butadiene-1, 4-sultone 12 condensed with amines to give N-substituted-2, 4-dimethyl-1, 3-butadiene-1, 4-sultames 13a and 13b. The reaction of 3a, 13a with hydrazine hydrate gave acid hydrazides 3d or 13c. Compounds 3d, 13c reacted with isocyanates to yield urea derivatives 14a-c, 15a-c.

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