• 제목/요약/키워드: coupling assay

검색결과 33건 처리시간 0.027초

Synthesis of Benzoxazole and Bezothiazole-linked TZD Analogs as PPARν Specific Ligands

  • Kim, Hae-Sung;Park, So-Yeon;Raok Jeon
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 2003년도 Annual Meeting of KSAP : International Symposium on Pharmaceutical and Biomedical Sciences on Obesity
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    • pp.117-117
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    • 2003
  • PPARs (peroxisome proliferator activated receptors) are member of nuclear hormone receptors superfamily. Activations of PPARs upon binding with ligands modulate glucose metabolite, differentiation of adipocyte, inflammation response, and so on. Thiazolidinedione analog is one of potential antidiabetic drug that binds and activates PPARν selectively and enhances insulin sensitivity. In an effort to develop novel and effective antidiabetic thiazolidindione analogs, syntheses of benzoxazole and benzothiazole-linked thiazolidinedione analogs were performed via coupling reaction of benzoxazolylalkylaminoethanol with hydroxybenzylthiazolidinedione to develop novel and effective antidiabetic thiazolidindiones. All compounds were evaluated their biological potency by PPARν transactivation assay and revealed the similar potency with Troglitazone. However, lengthening of N-alkyl substituent did not seem to be beneficial for the activity.

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Development of an ELISA for the Organophosphorus Insecticide Chlorpyrifos

  • Cho, Young Ae;Lee, Hye-Sung;Park, Eun-Yeong;Lee, Yong-Tae;Hammock, Bruce D.;Ahn, Ki-Chang;Lee, Jae-Koo
    • Bulletin of the Korean Chemical Society
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    • 제23권3호
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    • pp.481-487
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    • 2002
  • A selective enzyme-linked immunosorbent assay (ELISA) for the insecticide chlorpyrifos was developed. Four haptens for chlorpyrifos were synthesized and two of them were used as immunogens after coupling to keyhole limpet hemocyanin by two differe nt approaches. Rabbits were immunized with either of them and the sera were screened against 4 haptens coupled to ovalbumin (OVA). Using the sera of highest specificity, an antigencoated ELISA was developed, which shows an I50 of 160 ppb with a detection limit of 10 ppb. An antibody-coated ELISA was also developed, which shows an $I_{50}$ of 20 ppb with a detection limit of 0.1 ppb. The antibodies showed negligible cross-reactivity with other organophosphorus pesticides except for insecticides chlorpyrifos-methyl and bromophos-ethyl, which makes these assays suitable for the selective detection of chlorpyrifos.

Two New Scalaranes from a Korean Marine Sponge Spongia sp.

  • Yang, Inho;Nam, Sang-Jip;Kang, Heonjoong
    • Natural Product Sciences
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    • 제21권4호
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    • pp.289-292
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    • 2015
  • Intensive chemical investigation of Korean marine sponge Spongia sp. has led to the isolation of two new scalaranes. The planar structures of the new compounds 1 and 2 were determined through 1D and 2D NMR spectral data analysis, while the relative stereochemistry of the compounds was determined based on the analysis of $^1H-^1H$ coupling constants and NOESY spectroscopic data. Compounds 1 and 2 did not display any significant biological activities on farnesoid X-activated receptor (FXR) in co-transfection assay.

Stereoselective Syntheses of ($\pm$)-Epibatidine Analogues

  • Kim, Yong-Hyun;Won, Do-Youn;Oh, Chang-Young;Lee, Kee-Young;Lee, Yiu-Suk;Woo, Nam-Tae;Park, Young-Ho;Park, Hyun-Ju;Ham, Won-Hun
    • Archives of Pharmacal Research
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    • 제25권1호
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    • pp.45-48
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    • 2002
  • Stereoselective syntheses of ($\pm$)-epibatidine analogues 2, which contain the 8-azabicyclo[3.2.1]octane ring system, were achieved by using palladium-catalyzed cross-coupling reaction from 4 and the analgesic activity was tested by Mouse writhing antinociceptive assay.

Syntheses of ($\pm$)-Homoepibatidine Analogues

  • Kim, Yong-Hyun;Oh, Chang-Young;Lee, Kee-Young;Lee, Yiu-Suk;Jung, Young-Hoon;Park, Hyun-Ju;Ham, Won-Hun
    • Archives of Pharmacal Research
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    • 제25권1호
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    • pp.49-52
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    • 2002
  • Syntheses of ($\pm$)-homoepibatidine analogues (2), which contain the 8-azabicyclo [3.2.1 ]octane ring system, were achieved by using palladium-catalyzed reductive-coupling reaction from 3 and the analgesic activity was tested by Mouse writhing antinociceptive assay

Rhodomine B dye removal and inhibitory effect on B. subtilis and S. aureus by WOx nanoparticles

  • Ying, Yuet Lee;Pung, Swee Yong;Ong, Ming Thong;Pung, Yuh Fen
    • Journal of Industrial and Engineering Chemistry
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    • 제67권
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    • pp.437-447
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    • 2018
  • Visible-light-driven wide bandgap semiconductor photocatalysts were commonly developed via doping or coupling with another narrow bandgap metal oxide. However, these approaches required extra processing. The aim of study was to evaluate the photocatalytic performance of narrow bandgap $WO_x$ nanoparticles. A mixture of $WO_2$ and $WO_3$ nanoparticles were synthesized using solution precipitation technique. The photodegradation of RhB by these nanoparticles more effective in UV light than in visible light. In antibacterial susceptibility assay, $WO_x$ nanoparticles demonstrated good antibacterial against Gram-positive bacteria. The cell wall of bacterial was the main determinant in antibacterial effect other than $W^{4+}/W^{6+}$ ions and ROS.

폴리디아세틸렌 리포좀 표면에 저분자량의 폴리에틸렌이민을 연결한 새로운 유전자 전달체 합성 및 특징 연구 (Synthesis and Characterization of Polyethylenimine-conjugated Polydiacetylene Liposome as a Gene Delivery Carrier)

  • 이영화;임강혁;허정석;최준식
    • 폴리머
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    • 제38권1호
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    • pp.43-48
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    • 2014
  • 본 논문은 저분자량의 폴리에틸렌이민을 폴리디아세틸렌 리포좀 표면에 연결하여 유전자를 세포 내로 전달할 수 있는 새로운 양이온성 고분자 리포좀 유전자 전달체 개발에 대한 결과이다. 폴리디아세틸렌 리포좀 제조 후에 자외선을 조사하여 고분자성 리포좀을 제조한 후, 유전자의 전달 효율을 높이기 위해 폴리에틸렌이민을 리포좀 표면에 커플링제를 이용하여 공유결합시켜서 PCDA-PEI 리포좀을 합성하였다. 제조한 고분자 리포좀을 이용하여 동물세포 내에서의 유전자 전달 및 발현 효율과 그에 따른 독성을 확인하는 연구를 수행하였다. 사용한 폴리에틸렌이민은 가지형이고 분자량은 2 kD인 것을 사용하였다. DNA와의 복합체 형성을 알아보기 위하여 전기영동 방법과 피코그린 형광 염색 시약을 사용하였으며 효율적으로 복합체를 형성하는 것을 확인하였다. 전달체의 효율과 독성을 확인하기 위하여 HEK 293 및 HeLa 세포를 사용하여 확인하였다. 실험 결과 PCDA-PEI 리포좀은 세포 내에서 비율이 높아질수록 유전자 전달 효율이 증가하는 경향을 보였고, 세포에 대한 독성도 상대적으로 낮음을 확인하였다. 이러한 결과는 PCDA-PEI 리포좀이 효율적인 유전자 혹은 약물 전달체로 사용될 수 있음을 보여주었다.

Metalaxyl의 다클론 항체생산과 최적 ELISA 조건 (Production of Polycolonal Antibody and Optimum Conditions in ELISA for Metalaxyl)

  • 이강봉;임건재;정영호;서용택
    • 한국환경농학회지
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    • 제13권1호
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    • pp.76-82
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    • 1994
  • Metalaxyl을 ELISA기법을 이용하여 분석하기 위하여 metalaxyl-HSA를 합성하고 이에 대한 항체를 생산하여 competitive indirect ELISA를 위한 최적조건을 조사하였다. Metalaxyl-protein conjugate는 metalaxyl을 가수분해시켜 생성된 metalaxyl acid에 단백질(HSA, OA)을 mixed anhydride방법이나 EDC 첨가방법으로 조제하였고 생성된 항체의 역가는 1:16,000으로 나타났다. Coating Ag의 최적농도는 $8\;{\mu}g/ml$, 배양시간은 $4\;^{\circ}C$에서 1시간 이상, $20\;^{\circ}C$$37\;^{\circ}C$에서는 4시간으로 나타났으며 항체의 희석배수는 1:2,000이 최적으로 나타났다. 항원과 항체의 혼합비율은 0.5 ml의 항원에 대해 1 ml의 항체가 최적이었으며 이 혼합액의 배양시간은 1시간, antirabbit Ig G-peroxidase conjugate의 배양시간은 30분이 최적으로 나타났다.

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Characterization of Dephosphocoenzyme A Kinase from Streptomyces peucetius ATCC27952, and Its Application for Doxorubicin Overproduction

  • Lee, Na-Rae;Rimal, Hemraj;Lee, Joo-Ho;Oh, Tae-Jin
    • Journal of Microbiology and Biotechnology
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    • 제24권9호
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    • pp.1238-1244
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    • 2014
  • Dephosphocoenzyme A (CoaE) catalyzes the last step in the biosynthesis of the cofactor coenzyme A. In this study, we report the identification and application of CoaE from Stretomyces peucetius ATCC27952. After expression of coaE, the protein was found to have a molecular mass of 28.6 kDa. Purification of the His-tagged fused CoaE protein was done by immobilized metal-affinity chromatography, and then in vitro enzymatic coupling assay was performed. The increasing NADH consumption with time shed light on the phosphorylating activity of CoaE. Furthermore, the overexpression of coaA and coaE independently under the $ermE^*$ promoter in the doxorubicin -producing wild type strain, resulted in 1.4- and 1.5-fold enhancements in doxorubicin production, respectively. In addition, the overexpression of both genes together showed a 2.1-fold increase in doxorubicin production. These results established a positive role for secondary metabolite production from Streptomyces peucetius.

Benzimidazole을 함유한 [1,2,4]-Triazole 유도체의 합성 및 생물학적 활성 (Synthesis of [1,2,4]-Triazole Derivatives Containing Benzimidazole and Biological Activities)

  • 이소하;전제호;임혜원;배애님
    • 한국응용과학기술학회지
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    • 제23권4호
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    • pp.355-361
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    • 2006
  • [1,2,4]-Triazole derivatives were synthesized by 5 steps. Benzimidazole was refluxed with ethyl chloroacetate to give 1H-benzimidazole-acetic acid ethyl ester (1) over 52% yield. Ester (1) was refluxed with hydrazine hydrate in the presence of ethanol to afford 1H-benzimidazole-1-acetic acid, hydrazide (2). 5-Benzoimidazol-1-ylmethyl-4H-[1,2,4]triazole-3-thiol (4) was made via coupling of compound (2) with methyl isothiocyanate, followed by cyclization of 1H-benzimidazole-1-acetic acid, 2-[(methylamino) thioxomethyl]hydrazide (3) on reflux, and finally the target compounds (6a-6v) were synthesized by general substitution reaction. Compounds (6a-6v) were screened for T-type calcium channel blocker using the fluorescence assay by FDSS6000. All compounds (6a-6v) did not show better activities than control compound, mibefradil.