• 제목/요약/키워드: fluorouracil

검색결과 365건 처리시간 0.025초

1,3-Dibenzyl-5-Fluorouracil Prevents Ovariectomy-Induced Bone Loss by Suppressing Osteoclast Differentiation

  • Hyoeun Jeon;Jungeun Yu;Jung Me Hwang;Hye-Won Park;Jiyeon Yu;Zee-Won Lee;Taesoo Kim;Jaerang Rho
    • 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.

Low-Dose Docetaxel/Cisplatin - Leucovorin and 46 Hour Infusional Fluorouracil in Metastatic Gastric Carcinoma

  • Alici, Suleyman;Buyukberber, Suleyman;Alkis, Necati;Benekli, Mustafa;Ozkan, Metin;Bilici, Ahmet;Demirci, Umut;Karaca, Halit;Arpaci, Erkan;Gumus, Mahmut;Altunbas, Mustafa;Dane, Faysal;Turk, H. Mehmet;Anatolian Society of Medical Oncology
    • Asian Pacific Journal of Cancer Prevention
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    • 제14권1호
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    • pp.423-427
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    • 2013
  • Background: Phase II and III trials of docetaxel, cisplatin and fluorouracil (DCF) have shown superior efficacy versus cisplatin and fluorouracil alone but with high rates of hematologic toxicity in metastatic gastric cancer cases. To reduce toxicity while maintaining the efficacy of DCF, we investigated low dose docetaxel (D), cispatin (C) - leucovorin and fluorouracil (De Gramont regimen). Patient and methods: Chemotherapy-naïve patients with metastatic gastric cancer (MGC) received D 60 mg/$m^2$ on day 1 and cisplatin 30 mg/$m^2$ on day 1-2 and the De Gramont regimen (Folinic acid 400 mg/m2 on day 1 and 5-FU 2400 mg/$m^2$/46h continuous infusion) every 3 weeks. The primary endpoint was response rate. Results: One hundred twenty patients with a median age of 52.5 years (range, 32-78) received a median of 6 cycles (range, 2-12 cycles). Of the 120 evaluable patients, 4 showed complete remission and 36 achieved a partial response. The overall response rate was 56.6%. Twenty eight patients (23.3%) showed stable disease and 52 (43.3%) progression. The median time to progression was 7 months (95%CI 6-7.9). The median overall survival was 15 months (95%CI 13.7-16.2). The most frequent hematological toxicity was leucopenia, which occurred at grade 3/4 intensity in 24 patients (20%). Conclusions: Low-dose DC-De Gramont regimen is active in MGC with a tolerable toxicity profile.

Selective Radiotherapy after Distant Metastasis of Nasopharyngeal Carcinoma Treated with Dose-Dense Cisplatin plus Fluorouracil

  • Liang, Yong;Bu, Jun-Guo;Cheng, Jin-ling;Gao, Wei-Wei;Xu, Yao-Can;Feng, Jian;Chen, Bo-Yu;Liang, Wei-Chao;Chen, Ke-Quan
    • Asian Pacific Journal of Cancer Prevention
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    • 제16권14호
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    • pp.6011-6017
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    • 2015
  • Purpose: To investigate the efficacy and safety of selective radiotherapy after distant metastasis of nasopharyngeal carcinoma (NPC) treated with dose-dense cisplatin plus fluorouracil. Materials and Methods: Eligible patients were randomly assigned to a study group treated with dose-dense cisplatin plus fluorouracil following selective radiotherapy and a control group receiving traditional cisplatin plus fluorouracil following selective radiotherapy according to a 1:1 distribution using a digital random table method. The primary endpoint was overall survival (OS). Secondary endpoints were progression-free survival (PFS), objective response rate, relapse or progression rate in the radiation field and treatment toxicity. Results: Of 52 patients in the study group, 20 cases underwent radiotherapy., while in the control group of 51 patients, 16 underwent radiotherapy. The median PFS, median OS, survival rates in 1, 2 and 3 years in study and control group were 20.9 vs 12.7months, 28.3 vs 18.8months, 85.2%vs 65.9%, 62.2% vs 18.3%, and 36.6%vs 5.2% (p values of 0.00, 0.00, 0.04, 0.00 and 0.00, respectively). Subgroup analysis showed that the median OS and survival rates of 1, 2, 3 years for patients undergoing radiotherapy in the study group better than that in control group( 43.2vs24.1 months, 94.1% vs 86.7%, 82.4% vs 43.3%, 64.7% vs 17.3%, (p=0.00, 0.57, 0.04 and 0.01, respectively). The complete response rate, objective response rate after chemotherapy and three months after radiotherapy, relapse or progression rate in radiation field in study group and in control group were 19.2% vs 3.9%, 86.5% vs 56.9%, 85% vs 50%, 95% vs 81.3% and 41.3% vs 66.7% (p =0.03, 0.00, 0.03,0.30, 0.01 respectively). The grade 3-4 acute adverse reactions in the study group were significantly higher than in the control group (53.8% vs 9.8%, p=0.00). Conclusions: The survival of patients benefits from selective radiotherapy after distant metastasis of NPC treated with dose-dense cisplatin plus fluorouracil.

5-fluorouracil과 curcumin의 복합투여에 의한 자궁암세포의 성장억제와 p53유전자 발현의 상승 효과 (Synergistic Effects of 5-Fluorouracil (FU) and Curcumin on Human Cervical Cancer Cells)

  • 안성호;김동희;강정훈;이명선
    • 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.

Cytokine production profiles of a model for fluorouracil and UVB-induced discoid lupus erythematosus in TCR $\alpha$ chain knockout mouse

  • Yoshimasu, Takashi;Hiroi, Akihisa;Ohtani, Toshio;Uede, Koji;Furukawa, Fukumi
    • Journal of Photoscience
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    • 제9권2호
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    • pp.494-496
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    • 2002
  • Fluorouracil (FU) is well known to induce discoid lupus-like eruption at the sun exposure sites in Japan. It means the associations of UVB with drug induced DLE. It is still obscure which cytokines are involved in the development of DLE. To address the issue, we established a murine model of FU and UVB-induced discoid lupus and could show the Th1 dominant cytokine profiles in DLE model of TCR $\alpha$ chain KO mice treated with FU and UVB.

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Antitumor Evaluation of Cannabidiol and Its Derivatives by Colorimetric Methods

  • Baek, Seung-Hwa;Shin, Ji-Hee;Chung, Woo-Young;Han, Du-Seok
    • Toxicological Research
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    • 제16권2호
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    • pp.101-107
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    • 2000
  • Cannabidiol derivatives (1, 2 and 3), 5-fluorouracil (4, 5-FU) and adriamycin (5, AM) were tested for their growth inhibitory effects against human tumor cell lines using two different 3-{4,5-dimeth-ylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay and sulforhodamine B protein (SRB) assay. The light microscopic study showed morphological changes of the treated cells. Disruptions in cell organelles were determined by colorimetric methods; MTT assay and STB assay. These results suggest that cannabidiol (1, CBD) retains the most growth-inhibitory activity against human tumor cell lines.

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Poly($\tau$-benzy1 L-glutamate)와 polyoxpropylene으로 된 블록 공중합체의 합성 및 약물방출특성 (Synthesis of Block Copdymers Consistin(3 of Poly($\tau$-benzy1 L-glutamate) and Polyoxpropylene and Their Drug Release Behsviours)

  • 강인규;김우식
    • 대한의용생체공학회:의공학회지
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    • 제13권1호
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    • pp.55-64
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    • 1992
  • AB -type block copolymers of poly($\tau$-benzyl L-glutamate) (PBLG, a segment) and polyoxypropylene (POP, Bsegment) were synthesized and they were reacted with polyoxypropylene his(6-aminohexyl) (POE) to enhance the hydrophilicity of the poly- mers. The degree of swelling of the POE -crosslinked block copolymers (CPB -2) was higher than that of the block dopolymers (PB). The amount of 5-fluorouracil re- leased from CPB-2 block copolymers was greater than that from the PB block copol- ymers when they were incubated in the same period. These results indicate that the amount of 5-fluorouracil released from the matrices is proportional to the hydrophilicity of the polymers. Observing polymer surfaces by scanning electron mi- croscope, pores (diameter ; $0.5-1.5{\mu}$m) were appeared on the surface of CPB-2

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6-Fluorouracil이 핵서의 구개발육에 미치는 영향에 대한 자기방사법적 연구 (RADIOAUTOGRAPHIC STUDY OF THE POSTNATAL DEVELOPMENT OF THE PALATE FOLLOWING 5-FLUOROURACIL ADMINISTRATION IN MICE)

  • 남동석
    • 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$$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.

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