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PubMed1981

Resistance to fluorouracil in Candida utilis: effects on the uptake of pyrimidines and amino acids.

5-Fluorouracil powerfully inhibits growth of Candida utilis. Isolates that are resistant to fluorouracil all have a reduced ability to transport uracil but most also have other defects. Their capacity to take up a wide range of amino acids is greatly reduced, as is their ability to alter rates of amino acid transport during nitrogen starvation. These isolates may be defective in the coupling of energy generation to transport systems.

Amino Acids↗
PubMed2001

Destabilizing effect of a fluorouracil extra base in a hybrid RNA duplex compared with bromo and chloro analogues.

In the presence of cobalt, rhodium or iridium hexammine salts, the RNA/DNA hybrid r-GCUUCGGC-d(X)U (with X = F, Cl or Br) crystallizes as a double-stranded helix with four consecutive G-U and C-U mismatches. The deoxy chloro- and bromouracil derivatives are isomorphous, space group C2, unit-cell parameters a = 53.80, b = 19.40, c = 50.31 A, beta = 109.9 degrees, with the same infinite helix arrangement in the packing along the c axis with one extra DNA halogenouracil base included in the stacking. However, the fluorouracil derivative, with unit-cell parameters a = 53.75, b = 19.40, c = 45.84 A, beta = 105.7 degrees, is not isomorphous. The corresponding extra DNA base d(F)U of the second strand is ejected out of the helical stack, leading to a shortening of the c axis. The specific destabilization of the fluorouracil for the duplex building is analyzed in terms of the polarization effect of the halogen atom attached to the 3'-terminal base that modulates its interactions.

Bromine↗
PubMed1979

Basal cell nevus syndrome and adenocarcinoma of the colon. Response to systemic fluorouracil.

A patient with basal nervus syndrome was found to have an adenocarcinoma of the colon. This association, probably fortuitous, made it possible to study the effect of intravenous 5-fluorouracil on the cutaneous basal cell tumors. There was no reaction to this treatment. Subsequently, all visible basal cell tumors were satisfactorily eradicated with topical 5-fluorouracil.

Adenocarcinoma↗
PubMed1994

Oral administration of BOF-A2 to rats with lung transplanted tumors results in increased 5-fluorouracil levels.

A new tumor model was developed in which solid Yoshida sarcoma tissue injected intravenously developed into tumors in the lungs of about 30% (13/42) of the inoculated rats. Histological examination revealed that alveoli were occupied with tumor cells and the tumors were similar to those obtained by subcutaneous inoculation. Using this model, the concentrations of 5-fluorouracil (5-FU) in tumor tissue 12 h after oral administration of 3-[3-(6-benzoyloxy-3-cyano-2-pyridyloxycarbonyl)-benzoyl]-1-ethoxy methyl- 5-fluorouracil (BOF-A2, 36 mumol/kg) or a combination of tegafur and uracil in a molar ratio 1 to 4 (UFT, 50 mumol/kg) were found to be 129.8 ng/g and 19.2 ng/g, respectively. Thus, compared to treatment with UFT, BOF-A2 resulted in higher levels of 5-FU in lung tumor tissues. Increased concentrations of 5-FU should have a superior anti-tumor effect and so BOF-A2 merits clinical trial in the treatment of patients with lung cancer.

Administration, Oral↗
PubMed2000

Modulation of myogenic differentiation in a human rhabdomyosarcoma cell line by a new derivative of 5-fluorouracil (QF-3602).

The in vitro study of mechanisms involved in drug-induced maturation has made it possible to use differentiation-based therapy in clinical practice. The goal of this new therapy is the development of specific agents to induce cancer cells to stop proliferating and express characteristics of normal cells. Recently, by structural modifications of 5-fluorouracil (5-FU), we synthesized a new pyrimidine acyclonucleoside-like compound, 1-¿[3-(3-chloro-2-hydroxypropoxy)-1-methoxy]propyl¿-5-fluorouracil (QF-3602), which showed in rhabdomyosarcoma cells a low toxicity and time-dependent growth inhibition. In this work, we compared the degree of myogenic differentiation of RD rhabdomyosarcoma (RMS) cells after treatment with QF-3602 and 5-FU. Scanning and transmission electron microscopy (SEM and TEM) and immunocytochemical analyses showed that QF-3602 induced the appearance of myofilaments along the myotube-like giant RD cells, an increase in fibronectin and a decrease in vimentin expression. In contrast, only minor changes were observed with 5-FU. Moreover, polymerase chain reaction (PCR) analyses showed that QF-3602 did not induce overexpression of the mdr 1 gene, a resistance mechanism that frequently appears in classical cytotoxic therapy in these tumors. Compounds obtained by structural modifications of 5-FU may be useful in differentiation therapy as a new approach to the treatment of RMS.

ATP Binding Cassette Transporter, Subfamily B, Mem↗
PubMed1993

Pellagra secondary to 5-fluorouracil.

The development of pellagra in a patient treated with 5-fluorouracil for malignant disease is reported. The aetiology of pellagra in this patient is discussed, and the reasons for possible under-diagnosis of pellagra in association with malignant disease considered. We report a patient who presented with the typical skin changes of pellagra. The rash, and an associated acute deterioration in cerebral function, were exacerbated by treatment with 5-fluorouracil. The importance of considering nicotinic-acid deficiency in patients with malignant disease has not been emphasized in the literature.

Aged↗
PubMed1979

Effects of 5-fluorouracil on mouse bone marrow.

5-Fluorouracil (150 mg/kg) was injected intravenously into 11-week-old male mice. Its effects on marrow structure over the following 9 d were assessed using light microscopic examination of semi-thin transverse sections of decalcified humeri. The extravascular compartment became markedly depleted of cells and decreased in size, reaching a minimum on day 5 post-treatment. Proliferating haematopoietic cells disappeared within 2 d. Post-replicative erythrocytic cells underwent extra-vascular phagocytosis by resident macrophages, whilst mature granulocytes continued to pass into the circulation. Repopulation was underway by day 6, and re-expansion of the extravascular compartment by day 7 when megakaryocytes, of larger than normal average size, occupied most of the extravascular compartment. Megakaryocyte dominance gave way over days 8 and 9 as other haematopoietic cells proliferated and the extravascular compartment continued to enlarge. The significance of the results is discussed in relation to marrow micro-circulation, egress of haematopoietic cells into the circulation, and cell proliferation in the marrow. Endotoxin, administered 4 h after 5-fluorouracil, accelerated depletion of the marrow and recovery of haematopoiesis by about 1 d.

Animals↗
PubMed1980

Dynamic histology of a rat hepatoma and the response to 5-fluorouracil.

The cellular response of the rat hepatoma 3924A to a single intraperitoneal injection of 5-fluorouracil has been measured in respect of the spatial relationship of the cells to the tumour microvasculature. In this tumour the parenchyma is arranged in cords approximately 150 micron thick around central capillaries. For untreated tumours, those cells at distance less than 80 micron from the capillary had a mean [3HTdR labelling index of 39% and a mitotic index of 2.1%, while for those cells more than 80 micron away the values were 14% and 0.8% respectively. Two days after 150 mg/kg of 5-fluorouracil, mean cord thickness was reduced by 25% and did not recover to the control level until 11 days after treatment. This was also true for the mitotic index. Recovery of the labelling index was complete 2 days earlier. Although absolute values of parameters were different in the populations adjacent to and remote from the capillary, the time course of recovery was similar, with a 'growth spur' 7 to 9 days after treatment. The results from this histologically-based assay have been compared with those from biochemical/biophysical assays that sample the overall tumour population.

Animals↗
PubMed2004

Intralesional 5-fluorouracil in the treatment of keloid scars.

Two patients with keloid scars are described. The first patient presented with extensive keloid scarring on both cheeks secondary to acne. The second patient developed a keloid scar on her chest following excision of a mole. Both patients' scars were diagnosed clinically and treated with fortnightly injections of a mixture of 5-fluorouracil and betamethasone acetate and betamethasone sodium phosphate. At each injection session up to 1.6 mL of 5-fluorouracil at a concentration of 500 mg/10 mL and 0.4 mL of betamethasone acetate and betamethasone sodium phosphate (as betamethasone acetate 3 mg in suspension and betamethasone sodium phosphate 3.9 mg in solution) were used. Multiple treatments were required to obtain resolution of the keloid scars. Improvement was maintained in both patients at 1 year post treatment.

Acne Keloid↗
PubMed2006

Reversible findings of restricted diffusion in 5-fluorouracil neurotoxicity.

A 35-year-old woman presented with neurotoxicity correlated to an i.v. regimen of 5-fluorouracil as episodes of acute confusional state and abnormalities of symmetrically restricted diffusion in the periventricular white matter and corpus callosum. On discontinuing the medication, the areas of severely restricted diffusion had entirely resolved, with minimal residual T2 signal abnormality. In this case, immediate discontinuation of the chemotherapeutic agent apparently reversed the patient's symptoms and findings on MRI. The scant information available in the published literature regarding this phenomenon is reviewed with regard to 5-fluorouracil.

Adult↗
PubMed1991

Reducing corneal toxicity of 5-fluorouracil in the early postoperative period following glaucoma filtering surgery.

To gain a better understanding of the relationship between postoperative 5-fluorouracil administration and corneal complications associated with its use, we analysed 43 consecutive filtering procedures in which it had been employed. Nine of the 43 eyes had corneal complications during that period. At the end of the three-month period, these corneal complications had all resolved. There was no correlation between postoperative intraocular pressure lowering and incidence of corneal complications. A low dose of 5-fluorouracil, and early recognition and treatment of corneal toxicity associated with its use may reduce corneal complications while maintaining filtration in eyes with poor surgical prognosis.

Aged↗
PubMed2004

Operative revision of non-functioning filtering blebs with 5-fluorouracil to regain intraocular pressure control.

PURPOSE: To determine the efficacy of extensive microsurgical needling revision of failed filtering blebs followed by serial 5-fluorouracil subconjunctival injections. METHODS: Thirty-six eyes of 34 consecutive patients with progressive open-angle glaucoma refractory to topical therapy submitted to needling revision as a major procedure. All patients required multiple antiglaucoma medications preoperatively, and had completely flat or densely encapsulated filtering blebs. All patients underwent elaborate needling revision (limbus to superior rectus >8 mm diameter, >3 mm elevation, entry-site sutured with 8-0 vicryl and bleb reformed via paracentesis with viscoelastic) in the operating room, followed by serial 5-fluorouracil. The patients were followed for up to 6 months postoperatively. The main outcome measures were intraocular pressure (IOP) and the number of antiglaucoma medications used. RESULTS: Thirty-one eyes (86%) maintained mean IOP below 15 mmHg postneedling without medication. Overall the mean IOP postneedling was >9 mmHg lower than medicated preoperative levels (P < 0.0001). IOP reduction in encapsulated blebs was marginally superior to that in flat blebs. CONCLUSIONS: Extensive needling revision in the operating room is safe, straightforward, and produces reproducible restoration of filtering function.

Adult↗
PubMed1988

Cardiac arrest--a manifestation of 5-fluorouracil cardiotoxicity.

We report a case of cardiac arrest occurring during an infusion of 5-fluorouracil where electrocardiograms suggested coronary artery spasm as the underlying event. Treatment with vasodilators and diltiazem, proved effective. This clinical presentation of 5-fluorouracil cardiotoxicity has not previously been described.

Carcinoma, Squamous Cell↗
PubMed1997

Long-term efficacy and safety of Jessner's solution and 35% trichloroacetic acid vs 5% fluorouracil in the treatment of widespread facial actinic keratoses.

BACKGROUND: Few studies have examined the long-term efficacy of fluorouracil (FU) or chemical peels for the treatment of actinic keratoses (AK). Our earlier work examined the efficacy and safety of a medium-depth chemical peel compared with the standard regimen of topical FU in the treatment of widespread facial AK through 12 months. OBJECTIVES: To determine long-term efficacy of both treatments by extending our observations through 32 months. METHODS: Fifteen patients with severe facial actinic damage were treated on the left side with a single application of Jessner's solution and 35% trichloroacetic acid and on the right side with twice daily applications of 5% FU cream for 3 weeks. Parameters evaluated at 1, 6, 12, and 32 months included counts of visible AK, random skin biopsies from both treatment areas, development of intercurrent neoplasms, and surveys assessing sun exposure. RESULTS: Eight patients were available for reevaluation at 32 months. Both treatment sides showed a reduction in mean number of AK at 12 months followed by an increase in mean AK number between 12 and 32 months. Improvements in biopsies of clinically actinically damaged skin were seen in keratinocytic atypia, hyperkeratosis, parakeratosis, and inflammation at all treatment times during the study with both treatments. Three squamous cell carcinomas developed in the patients after initial treatment; one developed on the side treated with the peel, and two developed on the side treated with fluorouracil. Surveys failed to demonstrate an association between sun exposure and clinical response. CONCLUSION: Based on these findings, patient with widespread actinic keratoses treated with medium-depth chemical peel or with 5% FU should be reevaluated yearly or every 1.5 years for reappearance of AK and retreatment.

Administration, Topical↗
PubMed2005

Pharmacokinetics and tissue distribution of 5-fluorouracil encapsulated by galactosylceramide liposomes in mice.

AIM: To study the pharmacokinetics and tissue distribution of 5-fluorouracil encapsulated by galactosylceramide liposomes (5-Fu-GCL) in mice. METHODS: The concentration of 5-fluorouracil (5-Fu) in serum was detected by high performance liquid chromatography after 5-Fu-GCL (80, 40, 20 mg/kg) and free 5-Fu (40 mg/kg) were injected intravenously into mice. The tissue distribution of 5-Fu-GCL (40 mg/kg) and free 5-Fu (40 mg/kg) was investigated, and concentration-time profile of the two preparations in the liver were studied. Data were analyzed by 3p97 program. RESULTS: Serum concentration-time curves of 5-Fu-GCL and free 5-Fu conformed to one compartment model of first order absorption. 5-Fu-GCL at 80, 40, and 20 mg/kg had T(1/2Ke) of 25.8+/-4.2, 27.3+/-4.4, and 28.2+/-5.6 min; C0 of 24.9+/-4.9, 17.7+/-3.6, and 11.5+/-2.7 mg/L; and AUC of 990.0+/-45.2,622.5+/-38.3, and 340.4+/-25.6 mg x min x L(-1), respectively. In contrast free 5-Fu at 40 kg/mg had T(1/2Ke) of 15.8+/-2.2 min, C0 of 35.8+/-6.2 mg/L, AUC of 639.0+/-35.9 mg x min x L(-1). The tissue distribution of 5-Fu-GCL in the liver and immune organs was significantly increased, while in heart and kidney it was remarkably decreased. The AUC of 5-Fu-GCL in the liver was 3 times higher than that of free 5-Fu. CONCLUSION: The pharmacokinetics and tissue distribution of 5-Fu-GCL appears to be linear-related and dose-dependent, and exhibits sustained-release and hepatic target characteristics.

Animals↗
PubMed2006

Inhibition of Bcl-2 expression by a novel tumor-specific RNA interference system increases chemosensitivity to 5-fluorouracil in Hela cells.

AIM: RNA interference (RNAi) has been proposed as a potential treatment for cancer, but the lack of cellular targets limits its use in cancer gene therapy. No current technology has achieved direct tumor-specific gene silencing using RNAi. In the present study we attempt to develop a tumor-specific RNAi system using the human telomerase reverse transcriptase (hTERT) promoter; furthermore, we analyzed its inhibitive effect on Bcl-2 expression. METHODS: The vectors containing a small hairpin RNA (shRNA) to target exogenous reporters [firefly luciferase and enhanced green fluorescent protein (EGFP)] and endogenous gene (Bcl-2) were constructed. Luciferase expression was determined by dual luciferase assay. Reverse transcription-polymerase chain reaction (RT-PCR), fluorescence microscopy and fluorescence-activated cell sorting (FACS) were used to measure EGFP expression. Inhibition of Bcl-2 was evaluated by RT-PCR and Western blotting. Cell proliferation and viability were measured by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay. FACS was used to analyze the cell cycle distribution profile. RESULTS: We showed that with the hTERT promoter directly driving shRNA transcription, expression of the exogenous reporters (LUC and EGFP) in tumor cells, but not normal cells, was specifically inhibited in vitro. The hTERT promoter-driven shRNA also depressed the expression of Bcl-2. Inhibition of Bcl-2 did not affect cell proliferation, but increased the chemosensitivity of HeLa cells to 5-fluorouracil. CONCLUSION: The present study describes an efficient RNAi system for gene silencing that is specific to tumor cells using the hTERT promoter. Suppression of Bcl-2 by using this system sensitized HeLa cells to 5-fluorouracil. This system may be useful for RNAi therapy.

Cell Cycle↗
PubMed1993

Intra-operative use of 5-fluorouracil in glaucoma filtering surgery.

This study reviews the outcome of 14 eyes considered to be at risk of surgical failure undergoing trabeculectomy with 5-Fluorouracil (5-FU). The antimetabolite was administered intra-operatively by placing a surgical sponge soaked in 5-FU (25 mg/ml) directly on the sclera under the conjunctival flap for 5 minutes. All eyes showed a reduction in intraocular pressure (IOP) at a mean follow-up of 18.5 weeks, and only one eye required topical antiglaucoma medication. Mean IOP reduction at final follow-up was 43.1%. No eyes showed any corneal problems associated with the intra-operative use of 5-FU. These results suggest that the intra-operative use of 5-Fluorouracil is an effective way of improving surgical success in at risk eyes. The early complications appear to be less than those associated with post-operative subconjunctival injections of 5-FU, but the long-term differences are still to be shown.

Adult↗