• 제목/요약/키워드: 5-fluorouracil

검색결과 303건 처리시간 0.722초

새로운 Acyclonucloside의 합성 : 새로운 $N_1$-Substituted 5-Fluorouracil 유도체의 합성과 그 특성에 관한 연구 (Synthesis of Novel Acyclonuclosides : Study on the Synthesis and Characteristics of New $N_1$-Substituted 5-Fluorouracil)

  • 정승호;윤용진;이종광
    • 대한화학회지
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    • 제35권3호
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    • pp.233-239
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    • 1991
  • 합성된 2-chloroethyl acrylate를 출발물질로 이용하여 5-fluorouracil의 $N_1$-위치에 각각 hydroxyethyl, acryloyloxyethyl, poly(acryloyloxyethyl)기를 가진 5-fluorouracil 유도체를 높은 수율로 얻었다. 이들 유도체들과 HCl과의 가수분해속도를 물-에탄올(1:1) 혼합용매에서 UV 분광기를 이용하여 측정하였다. 1-hydroxyethyl-5-fluorouracil, 1-acryloyloxyethyl-5-fluorouracil 및 Poly(1-acryloyloxyethyl-5-fluorouracil)의 가수분해속도는 각각 $k=1.38{\times}10^{-4}$sec, $9.25{\times}10^{-5}$/sec, $4.16{\times}10^{-5}$/sec 이었다. 또한, 합성된 5-fluorouracil 유도체의 열분해성에 대해 논의하였다.

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정맥주사제 혼주시 5-fluorouracil의 차광유무에 따른 안정성에 관한 연구 (The Effect of Light on the Stability of IV admixture with 5-Fluorouracil)

  • 이은경;서옥경;이숙향;신현택
    • 한국임상약학회지
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    • 제7권1호
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    • pp.45-49
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    • 1997
  • The effect of the light on the stability of 5-fluorouracil admixture was investigated. Four sets of 5-fluorouracil admixture were prepared using 50 mg/ml injection in $5\%$ dextrose solution in PVC bags and glass bottles: (1) 5-fluorouracil 1 mg/ml concentration in glass bottles, (2) 5-fluorouracil 1 mg/ml in PVC bags, (3) 5-fluorouracil 10 mg/ml in glass bottles, and (4) 5-fluorouracil 10 mg/ml in PVC bags. In each set, one group was protected from the light (control group) and the other group was exposed to the fluorescent light (study group). All admixtures were stored at room temperature for 72 hours. Also, 5-fluorouracil injections (50 mg/ml) were prepared in plastic syringes. Half of the samples of 50 mg/ml concentration were protected from the light (control group) and the other half were exposed to the fluorescent light (study group). These were stored at room temperature for 48 hours. After visual inspection, the pHs of each admixture were determined. The 5-fluorouracil concentrations were measured by high-performance liquid chromatography with UV detection, with 5-bromouracil as an internal standard. Over the study period, no visual changes were observed. The pHs of 5-fluorouracil admixtures were in the range of $8.2\~8.5$. The peak area ratios (5-FU/5-BrU) of 5-fluorouracil admixtures protected from the light were compared with those of the admixtures exposed to the light. There was no statistically significant difference between two groups during the study period (p>0.05). In conclusion, 5-fluorouracil admixtures in $5\%$ dextrose solution exposed to the light were stable for 72 hours.

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5-Fluorouracil과 그 유도체를 함유하는 Solid Lipid Nanoparticles 제조와 평가 (Preparation and Evaluation of Sold Lipid Nanoparticles(SLNs) containing 5-Fluorouracil and Its Derivative)

  • 서혜선;최명신;한규원;박소민;김길수
    • Journal of Pharmaceutical Investigation
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    • 제35권3호
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    • pp.143-150
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    • 2005
  • Solid lipid nanoparticles(SLNs) are particulate systems for parenteral drug administration and have good biocompatibility and stability. SLNs were prepared with lauric acid, as the lipid core. Tween 20 and tween 80 were used as surfactant. 5-fluorouracil and l-benzoyl-5-fluorouracil were used as model drugs. Drug-loaded SLNs were prepared by the hot homogenization technique in order to evaluate the physical stability, entrapment efficiency of drugs as well as release profile. The particle size of SLNs was $40{\sim}600$ nm. By increasing speed, the mean particle size of SLNs was decreased. And entrapment efficiency in the case of using 1-Benzoyl-5-fluorouracil was higher than using 5-Fluorouracil. The higher surfactant concentration, the faster release rate at the range of $1.5{\sim}2.5%$.

Liposome-mediated Induction of Apoptosis of Human Hepatoma Cells by C-Myc Antisense Phosphorothioate Oligodeoxynucleotide and 5-Fluorouracil

  • Yuan, Yuan;Cai, Hui;Yang, Xiao-Jun;Li, Wei;He, Jin;Guo, Tian-Kang;Chen, Yi-Rong
    • Asian Pacific Journal of Cancer Prevention
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    • 제15권14호
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    • pp.5529-5533
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    • 2014
  • Background: The aim of this study was to investigate the effect of a c-myc antisense oligodeoxynucleotide and 5-fluorouracil on the expression of c-myc, invasion and proliferation of HEPG-2 liver cancer cells. Materials and Methods: HEPG-2 cells were treated with lipiosome-mediated c-myc ADSON and 5-fluorouracil. The proliferation inhibition rate and invasion were measured by MTT and invasion assay, respectively. Cell apoptosis was detected by flow cytometry and expression of c-myc by RT-PCR and immunohistochemistry. Results: The proliferation inhibition rate was significantly higher in the antisense oligodeoxynucleotide added-5-fluorouracil group than single antisense oligodeoxynucleotide or 5-fluorouracil group (p<0.05). G0/G1 cells in the antisense oligodeoxynucleotide group and S cells in the 5-fluorouracil groups were significantly increased than that in the control group, respectively (P<0.01). The amplification strips of PCR products in 5-FU, ASODN and combination groups were significantly weaker than that in the control group (P<0.01). The percentage of c-myc-protein-positive cells were significantly lower in antisense oligodeoxynucleotide, 5-fluorouracil and combination groups than that in the control group (P<0.01). Conclusions: A liposome-mediated c-myc antisense oligodeoxynucleotide and 5-fluorouracil can inhibit the proliferation and invasion of liver cancer cells by reducing the expression of c-myc. A c-myc antisense oligodeoxynucleotide can increase the sensitivity of liver cancer cells to 5-fluorouracil and decrease the dosage of the agent necessary for efficacy, providing an experimental basis for the clinical therapy of liver cancer.

Pyrimidine Nucleoside 유도체들의 합성 및 약물학적 효능 검색 (Synthesis of Pyrimidine Nucleoside Analogues and Screening of Their Biological Effects)

  • 신혜순;이희주
    • Biomolecules & Therapeutics
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    • 제3권3호
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    • pp.217-222
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    • 1995
  • Several acyclonucleoside analogues of pyrimidine base and N$^1$-derivatives of 5-fluorouracil have been synthesized and evaluated for their biological effects. When tested with in vitro Lekemia L1210 cells, the 5-fluorouracil derivatives exhibited slightly higher antitumor activity than the parent 5-fluorouracil. When tested against Herpes Simplex Virus type 1 and type 2 cultured in the Vero cell, the 5-fluorouracil derivatives showed weak antiviral activity.

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Clinical Effects of Gemcitabine and 5-Fluorouracil Combination therapy and Epirubicin. Cisplatin. and 5-Fluorouracil Combination therapy for patients with Pancreatic Cancer

  • Her, Sook;Lee, Suk-Hyung;Kang, Jin-Hyoung
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.428.1-428.1
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    • 2002
  • Gemcitabine demonstrated modest activity in locally advanced and metastatic pancreatic cancer with difficulty early diagnosis and poor prognisis. The purpose of this study was to evaluate the efficacy and toxicity of gemcitabine and 5-fluorouracil(GF) combination theraphy and epirubicin. cisplatin. and 5-fluorouracil(ECF) combination theraphy for the patients with locally advanced or metaststic pancreatic cancer. Between January 1996 and December 2001. (omitted)

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A Unique Gene Expression Signature of 5-fluorouracil

  • Kim, Ja-Eun;Yoo, Chang-Hyuk;Park, Dong-Yoon;Lee, Han-Yong;Yoon, Jeong-Ho;Kim, Se-Nyun
    • Molecular & Cellular Toxicology
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    • 제1권4호
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    • pp.248-255
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    • 2005
  • To understand the response of cancer cells to anticancer drugs at the gene expression level, we examined the gene expression changes in response to five anticancer drugs, 5-fluorouracil, cytarabine, cisplatin, paclitaxel, and cytochalasin D in NCI-H460 human lung cancer cells. Of the five drugs, 5-fluorouracil had the most distinctive gene expression signature. By clustering genes whose expression changed significantly, we identified three clusters with unique gene expression patterns. The first cluster reflected the up-regulation of gene expression by cisplatin, and included genes involved in cell death and DNA repair. The second cluster pointed to a general reduction of gene expression by most of the anticancer drugs tested. A number of genes in this cluster are involved in signal transduction that is important for communication between cells and reception of extracellular signals. The last cluster represented reduced gene expression in response to 5-fluorouracil, the genes involved being implicated in DNA metabolism, the cell cycle, and RNA processing. Since the gene expression signature of 5-fluorouracil was unique, we investigated it in more detail. Significance analysis of microarray data (SAM) identified 808 genes whose expression was significantly altered by 5-fluorouracil. Among the up-regulated genes, those affecting apoptosis were the most noteworthy. The down-regulated genes were mainly associated with transcription-and translation-related processes which are known targets of 5-fluorouracil. These results suggest that the gene expression signature of an anticancer drug is closely related to its physiological action and the response of caner cells.

A RADIOAUTOGRAPHIC STUDY OF POSTNATAL DEVELOPMENT OF THE TONGUE FOLLOWING 5-FLUOROURACIL ADMINSTRATION IN MICE

  • 장상헌
    • 대한치과의사협회지
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    • 제14권3호
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    • pp.297-305
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    • 1976
  • 신생의 Balb/C strain 백서20두를 사용하였고, 실험군과 대조군으로 구분하여 실험군에는 5-fluorouracil의 체중 25 mg/kg씩 2회를 복강내주사하였다. 실험군가 대조군에 모두 희생 2시간전에 체중그람당 5μ Ci의 thymidine-H³ (Specific activity는 9.0 Ci/mM 이상)를 복강내 주사하였다. 각군은 5-fluorouracil 최종 주사후 1, 3, 7, 14, 21일 간격으로 희생시키고, 두부를 4% formalin에 고정하였다. 조직을 0.5M EDTA에 탈회하고 parlodion과 paraplast에 이중 매몰을 하여 Parasagittal serial section 을 10μ의 절편을 만든 후 자기방사용표본을 제작하였다. 그 결과는 다음과 같다. 1. 5-fluorouracil이 백서설의 기저세포층의 핵산합성 및 단백합성에 미치는 영향은 실험초일인 제 1일부터 억제하기 시작하여 (80.9%) 제3일 76.9%이고, 제 7일이 가장 극심하고 (66.2%) 그후부터는 다소회복되기 시작하여 제14일이 92/3%이고, 제21일인 98.9%로서 서의 대조군수치에 접근하였다. 2. 5-fluorouracil은 설유두중 nallate papillae 성장에 가장 억제적 현상을 보였고, 그 다음이 fungiform papillae, filiform papillae의 순위였다. 3. 5-fluorouracil 이 백서설의 기저세포층의 핵산합성을 억제함을 알 수 있고, 아울러 백서설의 조기정상 발육에 영향을 줌울 알 수 있다.

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약물-고분자물질 결합체 합성연구 : 5-Fluorouracil과 사람의 혈청 Albumin 및 Poly-L-lysine 결합체 합성 (Syntheses of Drug-macromolecule Conjugates: Conjugations of 5-Fluorouracil to Human Serum Albumin and Poly-L-lysine)

  • 이희주;신혜순;이명걸;박만기;김종국
    • 약학회지
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    • 제33권5호
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    • pp.267-272
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    • 1989
  • The durg-macromolecule conjugates i.e. 5-fluorouracil-1-acetyl-human serum albumin(FU-AA-HSA, 8) and 5-fluorouracil-1-acetyl-poly-L-lysine(FU-AA-polylys, 9) have been synthesized and purified by sephadex G-25 gel filtration with 0.05M phosphate buffer(pH 7.5). The analyses of conjugates gave the molar ratio of FU-AA : HSA of 70-100:1 and FU-AA: poly-L-lysine of 109:1. The weight percent of FU-AA(as $FU-CH_2CO-$) in FU-AA-HSA conjugate was 16-22% and the one in FU-AA-polylys was 22.4%.

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5-Fluorouracil 및 Mitomycin C 투여후 생쥐 콩팥소체의 미세구조 변화 (Fine Structural Changes of the Renal Corpuscle of the Mice following the Administration of 5-Fluorouracil or Mitomycin C)

  • 고정식;오원영;김진국;박경호;안의태
    • Applied Microscopy
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    • 제29권1호
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    • pp.25-41
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    • 1999
  • 종양의 치료제로 많이 사용되고 있는 대표적인 항암제 가운데 대사길항제인 5-fluorouracil과 항암항생제인 mitomycin C가 콩팥토리에 미치는 영향을 미세구조적으로 비교 관찰하고자 이 실험을 시행하였다. Mitomycin C는 $LD_{50}$의 1/20 이하인 $400{\mu}g/kg$를, 5-fluorouracil는 $LD_{50}$의 1/4 정도인 60mg/kg를 격일 간격으로 계속 투여하였다. 각 항암제투여군은 처음 주사후 4일 (2회 투여)과 7일 (3회 투여) 째에 희생시킨 후 콩괄겉질부위의 조직을 메어 JEM 100CX-II 전자 현미경으로 관찰하였다. 1. 5-fluorouracil 및 mitomycin C 투여후 4일군에서는 다같이 혈관사이막이 증가하여 모세혈관과 주머니공간이 매우 좁아 보이는 부분이 많았는데, 그 현상은 mitomycin C 투여군에서 더 심했다. 2. 5-fluorouracil 투여 7일군은 토리의 미세구조가 거의 정상군의 모습과 비슷하게 회복되어 보였으나 mitomycin C 투여 7일군은 토리의 미세구조가 정상군의 모습과 비슷하게 회복된 모습을 거의 관찰할 수 없었다. 3. Mitomycin C 투여 4일군과 7일군에서는 내피세포의 종창현상(swelling) 이 심해서 내강으로 돌출되었을 뿐만 아니라 혈관사이세포가 모세혈관내강으로 돌출되어 내강을 거의 막고 있는 경우가 자주 관찰되었다. 4. Mitomycin C 투여 4일군에서는 토리모세혈관바닥막의 속투명판과 바깥투명판의 전자밀도가 높아서 치밀판과의 경계가 뚜렷하지 못한 부분이 많았는데, 부위에 따라서는 속투명판이 넓어진 부분이 관찰되기도 하였다. 이상의 결과를 종합해 보면 mitomycin C를 투여하였을 경우에는 마우스의 콩팥토리는 모세혈관의 내강이 좁아지고 혈관사이막이 증가하며 내피세포는 종창현상을 보이는 등의 미세구조적 변화를 보였다. 그러나 5-fluorouracil을 투여하였을 경우, 초기 (4일)에는 발세포와 혈관사이막의 경우 mitomycin C 투여군에서와 비슷한 미세구조적 변화를 보였으나, 7일군에서는 거의 정상군의 소견과 비슷한 모습을 보였다. 이와 같은 결과는 콩팥토리를 비롯한 콩팥조직에 미치는 세포독성은 mitomycin C가 5-fluorouracil에 비하여 훨씬 더 강하기 때문이라고 생각된다.

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