• Proceedings of the PSK Conference
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• 2000.10a
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• pp.136.1-136.1
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• 2000

• Proceedings of the PSK Conference
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• 2001.04a
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• pp.120.1-120.1
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• 2001

• Asian Pacific Journal of Cancer Prevention
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• v.13 no.1
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• pp.387-390
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• 2012

A combination of 5-fluorouracil plus actinomycin D (5FU plus Act D) is the regimen that has been commonly administered to Chinese and Japanese gestational trophoblastic neoplasia patients as the first or second line of treatment with an excellent outcome. However, the efficacy of this regimen in a salvage setting was unclear. To evaluate the efficacy and safety of the 5 FU plus Act D regimen utilized in this condition, all GTN patients resistant to at least three previous chemotherapy regimens who received the 5 FU plus Act D regimen between August 2009 and January 2011 at Chiang Mai University Hospital were reviewed. There were five cases who met the criteria. Four of those patients were in FIGO stage III to IV with a WHO scoring of more than 12. The median number of cycles for each patient was two and only one case achieved remission while four of the cases were unresponsive. The toxicity was evaluated in 12 cycles. Common complications were uncomplicated myelosuppression and mucositis. In conclusion, this regimen revealed modest efficacy in a salvage setting with manageable toxicity.

• Maxillofacial Plastic and Reconstructive Surgery
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• v.33 no.3
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• pp.210-217
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• 2011

Purpose: This study was to evaluate the synergistic effects of combined therapy of steroid and anti-neoplastic drug injection on hypertrophic scars in a rabbit model. Methods: Adult male white rabbits weighing about 2.5 kg were used. After full thickness wounding (about 6 mm) over the ventral surface of each ear sized was made, either saline (control group), triamcinolone, 5-fluoruracil, and mixture of triamcinolone and 5-fluoruracil were injected once 16 days after the wound was made. Rabbits were sacrificed 2, 4 and 8 weeks after injection, and tissue specimens were prepared for histologic and histomorphometric examinations. Results: With the combined injection of triamcinolone and 5-fluoruracil, collagen fiber thickness was arranged in a somewhat irregular manner 2 weeks after injection. After 4 weeks, blood vessels and inflammatory cells were decreased, and collagen fibers were arranged in an almost parallel manner. By 8 weeks, almost same amount of connective tissue compared with adjacent normal tissue was observed. Conclusion: These results indicated that combined injection of triamcinolone and 5-fluoruracil reduced the amount of hypertrophic scars by inhibition of fibroblasts and inflammatory cells. Therefore, combined injection of triamcinolone and 5-fluoruracil is a more potent and effective treatment of hypertrophic scars compared with the single injection of either triamcinolone or 5-fluorouracil.

• Asian Pacific Journal of Cancer Prevention
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• v.17 no.11
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• pp.4991-4998
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• 2016

Objective: This research was conducted to explore mechanisms behind the potency of quercetin in inhibiting colon cancer induced in an experimental model. Materials and Methods: Forty adult male rats of Wistar strain were distributed into 4 groups; a negative control group, a colon cancer bearing group, a quercetin-treated group and a 5-fluorouracil (5-FU)-treated group. Serum TAG72 and GAL3 levels were quantified by ELISA. Colonic Wnt5a and Axin-1 gene expression was estimated by PCR. In addition, colonic tissues were subjected to immunohistochemical examination of Bax expression and histological investigation of histopathological alterations. Results: Quercetin elicited significant reduction in serum TAG72 and GAL3 levels, in addition to significant suppression of colonic Wnt5a gene expression and amplification of colonic Axin-1 gene expression. Also, it caused moderate positive reaction for Bax in mucosal epithelium. Conclusion: The present research provides experimental evidence about the activity of quercetin in the colon cancer of rats. Inhibitory effects on cancer development might be ascribable to regulatory action on Wnt signaling and induction of apoptosis.

• Bulletin of the Korean Chemical Society
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• v.31 no.8
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• pp.2235-2241
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• 2010

A reverse-phase HPLC method with detection by mass spectrometry is described for the simultaneous determination of doxifluridine and its two active metabolites, 5-fluorouracil (5-FU) and 5-fluorouridine (5-FUrd), in beagle dog plasma. The optimal chromatographic separation was achieved on a Waters $Xterra^{(R)}$ $C_{18}$ column ($4.6{\times}250\;mm$ i.d., $5\;{\mu}m$ particle size) with a mobile phase of 0.1% formic acid in a mixture of 99% methanol and purified water (99:1, v/v). The developed method was validated in beagle dog plasma with a lowest limit of quantification of $0.05\;{\mu}g/mL$ for both doxifluridine and 5-FU, and $0.2\;{\mu}g/mL$ for 5-FUrd. Doxifluridine and its two metabolites were stable under the analysis conditions, and intra- and inter-day accuracies exceeded 92.87%, with a precision variability ${\leq}11.34%$ for each analyte. Additionally, the method for quantifying doxifluridine and its two metabolites, 5-FU and 5-FUrd, in beagle dog plasma was applied successfully to the analysis of pharmacokinetic samples.

• Korean Journal of Pharmacognosy
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• v.25 no.2
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• pp.144-152
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• 1994

The combined effects of Ulmi Cortex and some anti-cancer drugs on the proliferation of HeLa cells, Hep G2 cells and S 180 cells were estimated by MTT calorimetric assay. The n-BuOH fraction(UBF) of Ulmi Cortex inhibited the proliferation of HeLa cell at $10^{-3}\;g/ml$, Hep G2 cell at $10^{-5}\;g/ml$ and S 180 cell at $10^{-3}\;g/ml$. The inhibitory effects of mitomycin C(MMC), cisplatin(CPT) and 5-fluorouracil (5-FU), respectively, on Hep G2 cell was increased by the UBF. The UBF did not influence the proliferation of Balb/c 3T3 cells at concentrations of $10^{-6}$ to $10^{-4}\;g/ml$, but increased the proliferation of T cells at concentrations of $10^{-5}$ to $10^{-4}\;g/ml$. The UBF did not influence the number of leukocyte, and on the thymus weight of mice. The UBF increased the number of total-peritoreal cells of mice. In conclusion, the results suggest that the UBF have anti-cancer activity without the side effect, such as leukopenia and immunosuppresion, and increase the inhibitory activity of the anti-cancer drugs on Hep G2 cells.

• Korean Journal of Veterinary Research
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• v.37 no.3
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• pp.509-523
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• 1997

This study was carried out for investigating antitumor effects of 5-fluorouracil(5-FU), methotrexate(MTX) and retinoic acid(RA) on hepatocellular carcinoma induced in Sprague-Dawley rat. Antitumor effects were examined a flow cytometric DNA distributions by flow cytometry and stuied ATP/Pi using nuclear magnetic resorance, and the enzymatic activity of thymidylate synthetase and dihydrofolate reductase as well as contents of total collagen and sialic acid were measured with spectrophotometer. In this study, S phase fraction, contents of sialic acid and total collagen were decreased in the induced hepatocellular carcinoma treated with 5-FU and MTX, and synergistic effects of anticancer drugs were exhibited in the hepatocellular carcinoma treated with 5-FU and MTX simultaneously, and the inhibition of thymidylate synthetic and dihydrofolate reductase activity were shown in the hepatocellular carcinoma treated with 5-FU, MTX, and 5-FU and MTX simultaneously. On the other hand, the ratio of ATP/Pi were increased in all groups except group treated with RA. The experimental results suggest that above method may be valuable for evaluating antitumor effect of anticancer drugs.

• KSBB Journal
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• v.13 no.6
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• pp.669-674
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• 1998

This study was carried out particularly focusing on he antitumor effect in combination with 5-fluorocytosine(5-FC), antifungal agent, and extracellular cytosine deaminase from Chromobacterium violaceum YK 391 against U-937, K-562 and SNU-C4 cells. While the addition of 10$\mu\textrm{g}$/100 ${\mu}\ell$ of anticancer agent, 5-fluorouracil(5-FU), to U-937, K-562 and SNU-C4 caused the decrease of proliferation 90%, 75% and 93% respectively, the addition of 20 $\mu\textrm{g}$/100 ${\mu}\ell$ of the extracellular cytosine deaminase and 10 $\mu\textrm{g}$/100 ${\mu}\ell$ of antifungal agent 5-FC caused the decrease of proliferation 80%, 70% and 90%, respectively. These results, therefore, reveal that this enzyme has the similar clinical effect for considering of adjuvant antitumor effect. From the above results, the treatment of 5-FC and the cytosine deaminase was very effective and showed the possibility to remove side effects which easily occur by the treatment of 5-FU only. An extracellular cytosine deaminase.

• Archives of Pharmacal Research
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• v.26 no.12
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• pp.1096-1101
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• 2003

To enhance the liver targeting and reduce the side effects of 5-fluorouracil (5-Fu), it was acylated by stearyl chloride to obtain .$\b{N}_{\b{1}}$stearyl-5-Fu (5-FuS). The chemical structure of the prodrug was confirmed by Nuclear Magnetic Resonance and Infrared Spectrometry. 5-FuS was incorporated into solid lipid nanoparticles (SLN), which were prepared by the physical agglomeration method. The mean diameter of 5-FuS-SLN was 240.19 nm and the drug loading was 20.53%. The release characteristics in vitro of 5-FuS-SLN were fitted to the first-order pharmacokinetic model. Compared with 5-Fu injection, a study on the distribution of 5-FuS-SLN in mice showed that 5-FuS-SLN could double 5-Fu concentration in mice livers. The main pharmacokinetic parameters of 5-FuS-SLN in rabbits is shown as follows: $V_d$=0.04336L/kg, $T_{1/2} \beta$=1.2834h, CL=0.1632 L/h. In conclusion, 5-FuS-SLN has significant liver targeting properties. The employment of a prodrug to enhance drug liposoluble properties and the preparation method presented in this paper, seem to be an alternative strategy to the traditional colloidal delivery system.