• Macromolecular Research
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• v.9 no.5
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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.

• The Korean Journal of Physiology and Pharmacology
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• v.7 no.5
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• pp.255-259
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• 2003

Dendritic cells (DCs) play a critical role in various immune responses involving $CD4^+$ T cells and have been used to generate anti-tumor immunity. Chemotherapy induces severe side effects including immunosuppression in patients with cancer. Although immunosuppression has been studied, the effects of anticancer drugs on DCs are not fully determined. In this study, we demonstrated that CD40 activation strongly protected DCs from 5-fluorouracil (5-FU) or mitomycin C-induced apoptosis. DCspecific surface markers, including CD11c and major histocompatibility complex (MHC) class II, were used for identifying DCs. CD 40 activation with anti-CD40 mAb significantly enhanced the viability of DCs treated with 5-FU or mitomycin C, assayed by MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide). Fluorescence staining and analysis clearly confirmed the enhancing effect of anti-CD40 mAb on the viability of DCs, suggesting that CD40 activation may transduce critical signals for the viability of DCs. Annexin V staining assay showed that CD40 significantly protected DCs from 5-FU or mitomycin C-induced apoptosis. Taken together, this study shows that CD40 activation with anti-CD40 mAb has strong anti-apoptosis effect on DCs, suggesting that CD40 activation may overcome the immunosuppression, especially downregulation of number and function of DCs in chemotherapy-treated cancer patients.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.15
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• pp.6595-6597
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• 2015

Objective: To investigate short- and long-term treatment effects and side reactions of lobaplatin plus 5-Fu combined and concurrent radiotherapy in treating patients with inoperable middle-advanced stage esophageal cancer. Methods: Sixty patients with middle-advanced stage esophageal squamous cell cancer were retrospectively analyzed. All patients were administered lobaplatin (50 mg intravenously) for 2 h on day 1, and 5-Fu ($500mg/m^2$) injected intravenously from day 1 to 5 for 1 cycle, in an interval of 21 days for totally 4 cycles. At the same time, late-course accelerated hyperfractionated three-dimensional conformal radiotherapy was performed. Patients were firstly treated with conventional fractionated irradiation (1.8 Gy/d, 5 times/week, a total of 23 treatments, and DT41.4 Gy), and then treated with accelerated hyperfractionated irradiation (1.5 Gy, 2 times/d, a total of 27 Gy in 9 days, an entire course of 6-7 weeks, and DT 68.4Gy). Results: All patients completed treatment, including 10 complete response (CR), 41 partial response (PR), 7 stable disease (SD), and 2 progressive disease (PD). The total effective rate was 85.0% (51/60). Thirty-nine patients had an increased KPS score. One-, 2-, and 3-year survival rates were 85.3%, 57.5%, and 41.7%, respectively. The median survival time was 27 months. The adverse reactions included myelosuppression, which was mainly degree I and II. The occurrence rate of radiation esophagitis was 17.5%. No significant hepatic or renal toxicity was observed. Conclusion: Lobaplatin plus 5-Fu combined with concurrent radiotherapy is safe and effective in treating patients with middle-advanced stage esophageal cancer. However, this result warrants further evaluation by randomized clinical studies.

• Archives of Plastic Surgery
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• v.49 no.6
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• pp.704-709
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• 2022

Background The scar alopecia after cranioplasty (SAC) may decrease the patient's quality of life. We have treated SAC using follicular unit extraction (FUE). The aim of this study was to discuss that efficacy of FUE and how much hair follicular unit (FU) should be transplanted intraoperatively for the treatment of SAC. Methods We treated 10 patients (4 men and 6 women) who had SAC using FUE. Results The average age, alopecia size, and intraoperative hair density on the graft area were 29.8 ± 12.1 years, 29.8 ± 44.5 cm², and 34.6 ± 11.8 FU/cm², respectively. One year postoperatively, the average hair survival rate on the graft area was 66.3 ± 6.1%. Hair appearance was rated as good in six, fair in three, and poor in one. Among patients whose 1-year postoperative hair density was ≥ 20 FU/cm², five of six patients achieved good results. However, among patients whose 1-year postoperative hair density was < 20 FU/cm², all four patients achieved fair or poor results. The postoperative hair density was significantly higher in patients whose 1-year postoperative hair density was ≥ 20 FU/cm² than in patients whose 1-year postoperative hair density was< 20 FU/cm². The rate of achieving fair or poor results was significantly higher if the postoperative hair density was < 20 FU/cm² than if it was ≥ 20 FU/cm² (p = 0.047). Conclusions FU excision is useful for the treatment of scar alopecia after craniotomy. Our results suggest that the 1-year postoperative hair density should exceed 20 FU/cm² to achieve good outcomes.

• Applied Microscopy
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• v.40 no.4
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• pp.229-235
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• 2010

Cervical cancer is associated with low antioxidant status. It has a high prevalence especially amongst woman in Asia and is a leading cause of cancer death. Cancer chemotherapy in vivo improved in cases with high p53 expression in the tumor tissue. The restoration of p53 levels could be a potential strategy to increase chemoresponsiveness. Under circumstances where damage is extensive, p53 plays a direct role in trigering apoptosis. To investigate the effect of curcumin (CMN) as an antioxidant agent on anticancer agent 5-fluorouracil (5FU) induced apoptosis and p53 expression, HPV-18 positive HeLa cells were treated with noncytotoxic amounts of antioxidant. Curcumin induced apoptosis in cervical cancer cells. Morphological hallmarks of apoptosis such as nuclear fragmentation and internucleosomal fragmentation of DNA were observed. CMN caused upregulation of p53 expression, evident from Western blotting data and also increased the susceptibility/apoptosis induced by 5FU. These results show that increasing drug sensitivity of cervical cancer cells by upregulation of p53 using CMN is novel approach and could have a possible therapeutic potential in cervical cancer.

• Advances in Traditional Medicine
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• v.1 no.1
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• pp.45-54
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• 2000

Cannabidiol derivatives (1, 2 and 3), and 5-fluorouracil (4, 5-FU) were tested for their growth inhibitory effects against human oral epitheloid carcinoma cell lines (KB) using two different 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay and sulforhodamine B protein (SRB) assay. These compounds showed a potent inhibitory activity in vitro in the micromolar range against KB cell lines. In general, the antitumor activity of these compounds (1, 2, 3 and 4) was in a dose-dependent over the micromolar concentration ranges from $1\;{\mu}M\;to\;100\;{\mu}M$. The comparison of $IC_{50}$ values of these compounds in tumor cell lines shows that their susceptibility to these compounds decreases in the following order: CBD > 5-FU > CBDME > CBDDE by the MTT assay and SRB assay. Cannabidiol derivatives (1, 2 and 3), and 5-FU were tested for their cytotoxic effects on NIH 3T3 fibroblasts using two different MTT assay and SRB assay. These compounds exhibited potent cytotoxic activities in vitro in the micromolar range against NIH 3T3 fibroblasts. In general, the cytotoxic activities of these compounds (1, 2, 3 and 4) were in a dose-dependent over the micromolar concentration range $1\;{\mu}M\;to\;100\;{\mu}M$. The comparison of $CD_{50}$ values of these compounds on NIH 3T3 fibroblasts shows that their susceptibility to these compounds decreases in the following order; CBD > 5-FU > CBDDE > CBDME by MTT assay, CBD > 5-FU > CBDME > CBDDE by SRB assay. These results suggest that cannabidiol (1, CBD) retains the most growth-inhibitory activity against KB cell lines.

• Korean Journal of Oriental Medicine
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• v.9 no.1
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• pp.137-144
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• 2003

The objective on this study was to investigate medicinal protection with KH-19, which was composed of 9 kinds of oriental herbs tonifying the blood, against side effect of chemotherapy in mice and its mechanism through microarray. Not only WBC (white blood cell), and PLT (platelet) as a hematopoiesis toxicity indicator but also spleen weight as an immune toxicity indicator was reduced significantly 7 day after. 5-flurouracil (FU) treatment. However, reduction of WBC, PLT, and spleen weight after 5-FU treatment was significantly recovered by KH-19. For mechanic study on KH-19 action, gene expression in mouse spleen treated 5-FU was compared with gene expression in mouse treated 5-FU and KH-19. The result indicates that 23 genes were increased. in expression level over 2 fold and 41 genes were decreased in expression level more than 2 fold at mouse spleen by KH-19 treatment. KH-19 mechanism may be complicated more than other drug which of mechanism were composed of single compound because KH-19 was composed of various compounds.

• Molecules and Cells
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• v.42 no.2
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• pp.175-182
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• 2019

microRNAs regulate a diverse spectrum of cancer biology, including tumorigenesis, metastasis, stemness, and drug resistance. To investigate miRNA-mediated regulation of drug resistance, we characterized the resistant cell lines to 5-fluorouracil by inducing stable expression of miRNAs using lenti-miRNA library. Here, we demonstrate miR-551a as a novel factor regulating cell survival after 5-FU treatment. miR-551a-expressing cells (Hep3B-lenti-miR-551a) were resistant to 5-FU-induced cell death, and after 5-FU treatment, and showed significant increases in cell viability, cell survival, and sphere formation. It was further shown that myocyte-specific factor 2C is the direct target of miR-551a. Our results suggest that miR-551a plays a novel function in regulating 5-FU-induced cell death, and targeting miR-551a might be helpful to sensitize cells to anti-cancer drugs.

• IMMUNE NETWORK
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• v.2 no.1
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• pp.60-64
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• 2002

Background: Chemotherapy with 5-fluorouracil (5-FU) has been one of the mainstay in breast cancer treatment. The effects of high dose 5-FU on cell cycle regulation were studied in breast caner cells. Methods: A breast cancer cell line MCF-7 was used. Protein expressions of G1/S cyclins, $p21^{Waf1/Cip1}$, cdk2, E2F1 and retinoblastoma were tested by western blot analysis. Immunoprecipitation and immune complex kinase assay were done for the assessment of E2F1/RB interacton and the activity of cdk2 respectively. Results: $p21^{Waf1/Cip1}$ expression was barely detectable in control cells. With addition of 5-FU level of $p21^{Waf1/Cip1}$ were induced and cyclin D3 level was decreased as cell growth decreases. In accordance with increased expression of $p21^{Waf1/Cip1}$, cyclin E-associated cdk2 kinase activity was reduced. Retinoblastoma protein (RB) became dephosphorylated and E2F-1 binding activity with RB was increased. Conclusion: In this situation of high concentration of 5-FU breast cancer cells tend to be G1/S cell cycle arrested. Overexpression of $p21^{Waf1/Cip1}$ and dephosphorylation of RB may mediate the effectss of 5-FU by inhibiting E2F-1 activity, which contributes to G1/S cell cycle arrest. These results could be an indicating landmark for further study of high dose chemotherapy with 5-FU.

• Journal of the Korean Chemical Society
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• v.57 no.4
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• pp.439-446
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• 2013

Chitosan (CS) and hydroxypropylmethyl cellulose (HPMC) blend microspheres were prepared by water-in-oil emulsion technique and were loaded with an anti-cancer drug 5-fluorouracil (5-FU). CS-HPMC microspheres were characterized by Fourier transform infrared spectroscopy to confirm the cross-linking reaction. Scanning electron microscopy (SEM) was also used to assess the surface morphology of particles prepared. The quantity of release of 5-FU from the microspheres have been studied in terms of blend composition and amount of cross-linking agent. Differential scanning calorimetry and X-ray diffraction techniques indicated a uniform distribution of 5-FU particles in microspheres, whereas SEM suggested the spherical structure of the microspheres with slight rough surface. The in vitro drug release indicated that the particle size and release kinetics depend upon blend composition, amount of cross-linking agent used and amount of 5-FU present in the microspheres.