• Title, Summary, Keyword: 5-fluorouracil

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

  • Seung Ho Jung;Yong Jin Yoon;Chong Kwang Lee
    • Journal of the Korean Chemical Society
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    • v.35 no.3
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    • pp.233-239
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    • 1991
  • $N_1-alkyl-5-fluorouracil$ derivatives from 2-chloro-ethylacrylate(CEA) were synthesized. The reaction of 5-fluorouracil(5-FU) with 2-chloroethyl acrylate gave 1-hydroxyethyl-5-fluorouracil(HEFU) in 70% yield. The treatment of HEFU with acryloyl chloride afforded 1-acryloyloxyethyl-5-fluorouracil (AOEFU). Poly(1-acryloyloxyethyl-5-fluorouracil)[Poly(AOEFU)] was also synthesized from 5-fluorouracil and Poly(CEA). The hydrolysis rates of $N_1-alkyl-5-fluorouracil$ derivatives were observed by means of UV spectrophotometer at 265 nm in ethanol-water(1 : 1); k = the constant of hydrolysis rate, $k=1.38{\times}10^{-4}$/sec for HEFU, $k=9.25{\times}10^{-5}$/sec for AOEFU, $k=4.16{\times}10^{-5}$k = 4.16 ${\times}$ $10-5}sec$ for Poly(AOEFU). The differential thermal analysis and thermogravimetry of 5-fluorouracil derivatives have been discussed.

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

  • Lee, Eun Kyung;Suh, Okkyung;Lee, Suk Hyang;Shin, Hyun Taek
    • Korean Journal of Clinical Pharmacy
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    • v.7 no.1
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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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Preparation and Evaluation of Sold Lipid Nanoparticles(SLNs) containing 5-Fluorouracil and Its Derivative (5-Fluorouracil과 그 유도체를 함유하는 Solid Lipid Nanoparticles 제조와 평가)

  • Suh, Hae-Sun;Choi, Myoeng-Sin;Han, Kyu-Won;Park, So-Min;Kim, Kil-Soo
    • Journal of Pharmaceutical Investigation
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    • v.35 no.3
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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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    • v.15 no.14
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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.

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

  • Jang, Sang-Heon
    • The journal of the Korean dental association
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    • v.14 no.3
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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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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
    • Proceedings of the PSK Conference
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    • pp.428.1-428
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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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Synthesis of Pyrimidine Nucleoside Analogues and Screening of Their Biological Effects (Pyrimidine Nucleoside 유도체들의 합성 및 약물학적 효능 검색)

  • 신혜순;이희주
    • Biomolecules & Therapeutics
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    • v.3 no.3
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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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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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    • v.1 no.4
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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.

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

  • Lee, Hee-Joo;Shin, Hae-Soon;Lee, Myung-Gull;Park, Man-Ki;Kim, Chong-Kook
    • YAKHAK HOEJI
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    • v.33 no.5
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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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Preparation and In Vitro Release of Ramose Chitosan-Based-5-Fluorouracil Microspheres

  • Li, He-Ping;Li, Hui;Wang, Zhou-Dong;Zhang, Juan-Juan;Deng, Man-Feng;Chen, San-Long
    • Journal of the Korean Chemical Society
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    • v.57 no.1
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    • pp.88-93
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    • 2013
  • In order to construct a controlled release system of drugs and to reduce toxic side effects of 5-fluorouracil, the novel ramose chitosan-based-5-fluorouracil microspheres (CS-FU-MS) were prepared. Firstly, using chitosan (CS) as carriers and 5-fluorouracil (5-FU) as a model drug, ramose chitosan-based-5-fluorouracil (CS-FU) was efciently synthesized by chemical crosslinking method through microwave irradiation, drug loading was 10.6%; Secondly, CS-FU-MS were prepared by CS-FU self-assembled under the dialysis conditions and the free 5-FU was encapsulated further at the same time. The size dispersivity of particles is uniform, and the average diameter of the CS-FU-MS was $4{\mu}m$. The drug encapsulation efficiency was 76.1%, and the drug loading was increased to 26.22%. CS-FU-MS maintain the zero-order release time in PBS (pH = 7.4) and HCl/KCl (pH = 1.2) dialysis medium was 40h and 34h respectively, and the cumulative release were 58.89% and 79.33% in 182 h. The results showed that CS-FU-MS have excellent sustained release properties.