• Macromolecular Research
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• 제9권5호
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• pp.277-284
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• 2001

Poly(exo-3,6-epoxy-1,2,3,6-tetrahydrophthalic anhydride)s [poly(ETA)s] and poly($\alpha$-ethoxy-exo-3,6-epoxy-1,2,3,6-tetrahydrophthaloyl-5-fluorouracil)s [poly(EETFU)s ] with various average molecular weights were prepared by photopolymerizations. The number average molecular weights of the fractionated poly(ETA)s and poly(EETFU)s determined by GPC were in the range of 3,600∼21,000 and 3,600-33,400, respectively. The release rate of 5-FU from poly(EETFU) decreased with increasing average molecular weight. The in vitro cytotoxicity of poly(ETA) against a normal cell line was lower than that of 5-fluorouracil(5-FU), The in vivo antitumor activities of the synthesized samples at dosage of 0.8 mg/kg against mice bearing sarcoma 180 tumor cell line decreased in the following order: poly(EETFU) > poly(ETA) > EETFU > ETA > 5-FU. The antiangiogenic activities of the poly(ETA)s were better than those of 5-FU.

• Journal of Pharmaceutical Investigation
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• 제16권3호
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• pp.101-105
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• 1986

The changes of water absorption and surface area of polydimethylsiloxane-5-fluorouracil devices containing different water soluble additives such as sodium chloride, glycerine, poly-propylene glycol(PPG 400), and polyethylene oxide(PEO 400, 400 and 2000) were investigated. It was confirmed that carriers controlled water absorption and swelling of the devices in the aqueous solutions. The water absorption and the swelling were affected by the osmotic pressure and ionic strength of the aqueous solutions.

• Bulletin of the Korean Chemical Society
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• 제7권3호
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• pp.228-230
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• 1986

Diacetylene compound, 1,4-diphenyl-1,3-butadiyne, was photolyzed with 5-fluorouracil as a model reaction of the phototoxic conjugated poly-ynes with DNA or RNA and obtained a [2 + 2] photocycloadduct. The structure of the photoadduct was determined by spectral methods and compared with the [2 + 2] photoadducts of 1,4-diphenyl-1,3-butadiyne with tetramethylethylene and dimethyl fumarate.

• 약학회지
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• 제53권3호
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• pp.145-150
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• 2009

We evaluated cytotoxic effect based on the MTT assay and identified altered proteins in 5-FU(fluorouracil) treated HT29 cells using two-dimensional gel electrophoresis and MALDI-TOF/TOF-MS. As proteins inducing apoptosis, siah binding protein 1 and p47 protein isoform a were up-regulated and tumor protein translationally-controlled 1 was down-regulated by 5-FU treatment. And mannose 6 phosphate receptor binding protein 1 controls DNA mismatch repair system was increased. We suggest 5-FU promotes a cytotoxicity under the action of these proteins in colon cancer cells.

• Applied Microscopy
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• 제40권4호
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• pp.229-235
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• 2010

암은 전 세계적으로 사망률이 높은 질병으로 현재 자궁암 치료는 cisplatin, 5-fluorouracil (5FU) 등의 항암화학요법과 방사선 요법 등을 복합적으로 병행하고 있다. 최근 항암효과를 가지고 있는 자연식품의 섭취에 관심이 커지면서 커리의 주성분인 curcumin (CMN), 녹차의 주성분인 카테킨, 토마토의 주성분인 리코펜 등의 약리효과에 대한 연구가 활성화되고 있다. CMN은 동물실험 결과 항염증의 활성이 있고, 피부, 대장, 유방, 전립선 등에서 암으로의 진행을 억제한다는 보고가 있으나 인체 자궁암에서는 그 효과가 밝혀져 있지않다. 본 연구는 항암제 5FU와 CMN이 인체 자궁암세포 HeLa에 미치는 영향을 apoptosis의 유도로 평가하고, p53유전자 발현율과의 상관관계로 확인하고자 시행하였다. CMN은 HeLa 세포의 성장을 억제하였으며, 5FU로 유도된 apoptosis의 발생률과 p53유전자의 발현률을 현저하게 증가시키는 것으로 나타났다(p<0.05). 이러한 연구결과는 CMN이 자궁암 치료제의 가능성이 있으며, 또한 5FU와 복합적으로 사용하면 항암제를 단독으로 투여하는 경우보다 자궁암 치료에 보다 효과적임을 강력히 시사하는 것이다.

• IMMUNE NETWORK
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• 제22권5호
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• pp.43.1-43.12
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• 2022

Osteoclasts (OCs) are clinically important cells that resorb bone matrix. Accelerated bone destruction by OCs is closely linked to the development of metabolic bone diseases. In this study, we screened novel chemical inhibitors targeting OC differentiation to identify drug candidates for metabolic bone diseases. We identified that 1,3-dibenzyl-5-fluorouracil, also named OCI-101, is a novel inhibitor of osteoclastogenesis. The formation of multinucleated OCs is reduced by treatment with OCI-101 in a dose-dependent manner. OCI-101 inhibited the expression of OC markers via downregulation of receptor activator of NF-κB ligand and M-CSF signaling pathways. Finally, we showed that OCI-101 prevents ovariectomy-induced bone loss by suppressing OC differentiation in mice. Hence, these results demonstrated that OCI-101 is a good drug candidate for treating metabolic bone diseases.

• Bulletin of the Korean Chemical Society
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• 제35권8호
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• pp.2391-2399
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• 2014

Novel dual responsive pectin hydrogels composed from poly(acrylamidoglycolic acid-co-vinylcaprolactam)/Pectin (PAV-PC) and also PAV-PC hydrogels are used as templates for the production of silver nanoparticles. 5-Fluorouracil is an anticancer drug and has been loaded in situ into PAV-PC hydrogels. Structure and morphology characterization of PAV-PC hydrogels were investigated by fourier transform infrared spectroscopy, differential scanning calorimetry, thermo gravimetric analysis, X-ray diffraction studies, scanning electron microscopy and transmission electron microscopy. The results revealed a molecular level dispersion of the drug in PAV-PC hydrogels. In vitro release of 5-fluorouracil from the PAV-PC hydrogels has been carried out in GIT fluids as well as in various temperatures. 5-Fluorouracil released from PAV-PC hydrogels was 50% at pH 1.2, and 85% at pH 7.4 within 24 h. The release profile was characterized with PAV-PC hydrogels and initial burst effect was significantly reduced in two buffer media (1.2 and 7.4), followed by a continuous and controlled release phase, the drug release mechanism from polymer was due to Fickian diffusion. In situ fabrication of silver nanoparticles inside the hydrogel network via the reduction of sodium borohydrate by PAV-PC chains led to hydrogel nanocomposites. The diameter of the nanocomposites was about 50-100 nm, suitable for uptake within the gastrointestinal tract due to their nanosize range and mucoadhesive properties. These nanocomposite PAV-PC hydrogels showed strong antimicrobial activity towards Bacillus subtilis (G+ve) and Escherichia coli (G-ve).

• 대한수의학회지
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• 제62권3호
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• pp.20.1-20.8
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• 2022

5-Fluorouracil, doxorubicin, and vincristine are chemotherapy agents used to treat various cancers, such as breast cancer and lymphoma for decades, and their effects on cancer have been proven. On the other hand, these anti-cancer drugs cause fatal side effects, including immunosuppression. This study investigated whether sonicated Bordetella bronchiseptica bacterin (B. bronchiseptica) can attenuate the immunosuppression of spleen cells induced by these chemotherapy agents and which subsets of spleen cells were affected. B. bronchiseptica increased the metabolic activity of spleen cells treated with 3 anti-cancer drugs. Cell death analysis using Annexin V/propidium iodide showed that B. bronchiseptica markedly decreased the death of spleen cells. The subsets of spleen cells were analyzed by flow cytometry using a surface marker-specific antibody. B. bronchiseptica increased nitric oxide production in the spleen cells treated with anti-cancer drugs (p < 0.0001). Despite the pharmacological effects of anti-cancer drugs, many patients suffer from the fatal side effects of immunosuppression. This study provides valuable information on how to overcome chemotherapy-induced immunosuppression.

• Molecules and Cells
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• 제26권4호
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• pp.344-349
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• 2008

5-Fluorouracil (5-FU), a pyrimidine antagonist, has a long history in cancer treatment. The targeted pyrimidine biosynthesis pathway includes dihydropyrimidine dehydrogenase (DPD), which converts 5-FU to an inactive metabolite, and thymidylate synthase (TS), which is a major target of 5-FU. Using Caenorhabditis elegans as a model system to study the functional and resistance mechanisms of anti-cancer drugs, we examined these two genes in order to determine the extent of molecular conservation between C. elegans and humans. Overexpression of the worm DPD and TS homologs (DPYD-1 and Y110A7A.4, respectively) suppressed germ cell death following 5-FU exposure. In addition, DPYD-1 depletion by RNAi resulted in 5-FU sensitivity, while treatment with Y110A7A.4 RNAi and 5-FU resulted in similar patterns of embryonic death. Thus, the pathway of 5-FU function appears to be highly conserved between C. elegans and humans at the molecular level.

• 대한치과교정학회지
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• 제5권1호
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• pp.43-50
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• 1975

항암화학요법제인 5-FUR이 백서의 구개발육에 미치는 영향을 연구코자 20수의 신생백서를 반씩 나누어 실험군에는 체중kg당 25mg의 동 약제를 2회 복강내 주사하고 대조군에는 생리적 식염수만을 주사한 후 제 1, 3, 7, 14 및 21일에 각각 2수씩 도살하였다. 또한 도살 2시간전에 체중 gm당 $5{\mu}Ci$의 $H^3-TDR$을 주사하여 자기방사법적으로 처리 관찰하였다. 결과는 다음과 같다. 1. labeling index는 실험일자의 경과에 따라 점차 감소하였다. 2. 5-FUR의 억제작용이 골아세포층과 경구개의 상피층에서 제 7일에 가장 강하게 나타났고 제 14일부터는 감소되는 경향을 나타내었다. 3. 연구개의상피층과 glandular gene에서는 5-FUH의 억제효과가 제 3일에 가장 심히 나타났으며 제 7일부터는 감소되었다. 4. 5-FUR의 억제효과는 점차 감소되어 제21일에는 대조군과의 차이가 현저히 감소하였다. 5. 골아세포층이 5-FUR의 영향을 가장 심하게 받는 반면에 그 회복도 가장 빨랐다.