• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1993년도 제2회 신약개발 연구발표회 초록집
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• pp.39-39
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• 1993

To find out the novel anticancer agent for the treatment of solid tumors, 1-arylsulfonyl-2-alkoxy-4-arylimidazolines were designed and prepared from substituted styrenes through three steps. Compared to 5-fluorouracil, these analogues exhibit moderate cytotoxicity against human solid tumor cell lines, A-549(lung carcinoma) and SK-Mel-2(malignant melanoma). The structure-activity relationship indicates the high potential of this series for the development of novel antineoplastic agent.

• 한국독성학회:학술대회논문집
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• 한국독성학회 2005년도 춘계 국제심포지엄 및 학술대회
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• pp.209-209
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• 2005

• 대한약학회:학술대회논문집
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• 대한약학회 2000년도 NEW STRATEGY FOR DRUG DEVELOPMENT IN POST-GENOMIC ERA(대한약학회)
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• pp.134.1-134.1
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• 2000

• 동의생리병리학회지
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• 제26권2호
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• pp.155-159
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• 2012

The purpose of this study was to investigate the anti-cancer effects of Sophorae Radix and the effects of 5-Fluorouracil (5-FU) in human colorectal adenocarcinoma cells (HT-29). We used human colorectal adenocarcinoma cell line, HT-29 cells. We examined cell death by MTT assay and caspase 3 assay with Sophorae Radix. To examine the inhibitory effects of Sophorae Radix, cell cycle (sub G1) analysis was done the HT-29 cells after three days with Sophorae Radix. The reversibility of Sophorae Radix was examined on one day to five days treatment with $150{\mu}g$ Sophorae Radix. Sophorae Radix inhibited the growth of HT-29 cells in a dose-dependent fashion. Also we showed that Sophorae Radix induced apoptosis in HT-29 cells by MTT assay, caspase 3 assay and sub-G1 analysis. Sophorae Radix combined with 5-FU markedly inhibited the growth of HT-29 cells compared to Sophorae Radix or 5-FU alone. After 3 days treatment of HT-29 cells with Sophorae Radix, the fraction of cells in sub-G1 phase was much higher than that of the control group. Our findings provide insight into unraveling the effects of Sophorae Radix in human colorectal adenocarcinoma cells and developing therapeutic agents against colorectal cancer.

• Asian Pacific Journal of Cancer Prevention
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• 제15권9호
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• pp.4039-4044
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• 2014

Background: The aim of this study was to investigate the anti-cancer effects and mechanisms of immunochemotherapy of 5-fluorouracil (5-FU) and interleukin-2 (IL-2) on non-small cell lung cancer (NSCLC) A549 cells. Materials and Methods: In order to detect whether 5-FU+IL-2 could effectively inhibit tumor growth in vivo, we established an A549-bearing nude mouse model. The cytotoxicity of natural killer (NK) cells was evaluated using a standard chromium release assay. To evaluate the relevance of NK cells in 5-FU+IL-2-mediated tumor inhibitory effects, we depleted NK cells in A549-bearing mice by injecting anti-asialo-GM-1 antibodies. Effects of 5-FU+IL-2 on the expression and promoter activity of NKG2D ligands (MICA/MICB) in A549 cells in vitro were also assessed. Results: In A549-bearing nude mice, combination therapy significantly inhibited tumor growth in comparison with monotherapy with 5-FU or IL-2 and enhanced the recognition and lysis of tumor cells by NK cells. Further study of mechanisms showed that NK cells played a vital role in the anticancer immune response of 5-FU+IL-2 immunochemotherapy. In addition, the combination therapy synergistically stimulated the expression and promoter activity of MICA/MICB. Conclusions: 5-FU and IL-2 immunochemotherapy significantly inhibited tumor growth and activated NK cytotoxicity in vivo, and these effects were partly impaired after depleting NK cells in tumor-bearing mice. Combination treatment of 5-FU and IL-2 upregulated the expression and the promoter activity of MICA/MICB in A549 cells, which enhanced the recognition of A549 cells by NK cells. All of the data indicated that immunochemotherapy of 5-FU and IL-2 may provide a new treatment option for patients with lung cancer.

• 대한암한의학회지
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• 제20권1호
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• pp.31-44
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• 2015

Background : The purpose of this study is to investigate the efficacy and safety of the circadian delivery schedule of fluorouracil or capecitabine based chemotherapy for advanced colorectal cancer. Patients and methods : A meta-analysis was performed using individual data from eight international randomized clinical trials, especially phase II or III trials, comparing 5-fluorouracil, or capeticabine in chronomodulated or conventional schedule. The data from 8 studies was composed of 692 patients receiving chronomodulated chemotheray and 684 patients receiving conventional chemotherapy. The main end point was response rate. Results : Response rate was insignificantly different from each group (RR 1.14, 95%CI 0.74-1.74, p=0.55). Overall survival and progresseion-free survival were not significant either. Chemotherapy induced anemia, diarrhea, and nausea/vomiting were worse in the chronotherapy group, with statistic significance respectively. On the other hand, chemotherapy induced thrombocytopenia, stomatitis, peripheral neuropathy, and dermatotoxicity were better but they were not statistically significant results. Conclusions : Patients lived longer but not significantly on chronomodulated chemotherapy rather than on conventional chemotherapy. Patients on chronomodulated chemotherapy experienced adverse events more. The chronomodulated chemotherapy schedule needs adjustment of its delivery schedule and further research is required.

• Asian Pacific Journal of Cancer Prevention
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• 제15권1호
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• pp.407-411
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• 2014

Objective: To observe local and systemic toxicity after sustained-release 5-fluorouracil (5-Fu) implantation in canine peritoneum and para-aortic abdominalis and the changes of drug concentration in the local implanted tissue with time. Methods: 300 mg sustained-release 5-Fu was implanted into canine peritoneum and para-aorta abdominalis. Samples were taken 3, 5, 7 and 10 days after implantation for assessment of changes and systemic reactions. High performance liquid chromatography was applied to detect the drug concentrations of peritoneal tissue at different distances from the implanted site, lymphatic tissue of para-aortic abdominalis, peripheral blood and portal venous blood. Results: 10 days after implantation, the drug concentrations in the peritoneum, lymphatic tissue and portal vein remained relatively high within 5 cm of the implanted site. There appeared inflammatory reaction in the local implanted tissue, but no visible pathological changes such as cell degeneration and necrosis, and systemic reaction like anorexia, nausea, vomiting and fever. Conclusions: Sustained-release 5-Fu implantation in canine peritoneum and para-aortic abdominalis can maintain a relatively high tumour-inhibiting concentration for a longer time in the local implanted area and portal vein, and has mild local and systemic reactions. Besides, it is safe and effective to prevent or treat recurrence of gastrointestinal tumours and liver metastasis.

• Asian Pacific Journal of Cancer Prevention
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• 제15권22호
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• pp.9687-9692
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• 2014

Background: Biliary tract cancers are rare, and surgical resection is the standard treatment at early stages. However, reports on the benefits of adjuvant treatment following surgical resection are conflicting. This study aimed to evaluate the factors affecting survival and adjuvant treatments in patients with surgically treated biliary tract cancers. Materials and Methods: Patient clinical features, adjuvant treatments, and efficacy and prognostic factor data were evaluated. Survival analyses were performed using SPSS 15.0. Results: The median overall survival was 30.7 months (95% confidence interval [CI], 18.4-42.9 months). Median survival was 19 months (95% CI, 6-33) for patients treated with fluorouracil based chemotherapy and 53 months (95% CI, 33.2-78.8) with gemcitabine based chemotherapy(p=0.033). On univariate analysis, poor prognostic factors for survival were galbladder localization, perineural invasion, hepatic invasion, a lack of adjuvant chemoradiotherapy treatment, and a lack of lymph node dissection. On multivariate analysis, perineural invasion was a poor prognostic factor (p=0.008). Conclusions: Biliary tract cancers generally have poor prognoses. The main factors affecting survival are tumour localization, perineural invasion, hepatic invasion, adjuvant chemoradiotherapy, and lymph node dissection. Gemcitabine-based adjuvant chemotherapy is more effective than 5-fluorouracil-based chemotherapy.

• 한국자원식물학회:학술대회논문집
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• 한국자원식물학회 2018년도 추계학술대회
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• pp.101-101
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• 2018

Resveratrol is a polyphenolic compound, which is a naturally occurring phytochemical and is found in a variety of plants, including food such as grapes, berries and peanuts. Although several studies have demonstrated that resveratrol possesses anti-cancer activity against various types of human cancer, the molecular mechanisms of resveratrol-mediated overcome drug resistance potential are unclear. In this study, we determined whether resveratrol attenuates drug resistance responses in 5-fluorouracil-resistant colon cancer (SNUC5/5-FUR) cells. Treatment with resveratrol significantly enhanced apoptosis in a concentration-dependent manner, which was associated with the modulation of anti- and/or pro-apoptotic protein expression, activation of caspases and activation of AMP-activated protein kinase. Resveratrol treatment also increased the induction of autophagy through up-regulation of autophagy-related genes such as Microtubule-associated protein 1A/1B-light chain 3, P62 and beclin-1. However, blocking of autophagy by bafilomycin A1 reduced apoptotic cell death, suggesting that resveratrol-induced autophagy functions as a cell death mechanism in SNUC5/5-FU cells. Although the further studies are needed, these findings suggest that resveratrol may have therapeutic potential to overcome drug resistance in colon cancer patients.

• 한국한의학연구원논문집
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• 제18권1호
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• pp.85-92
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• 2012

Objective : The purpose of this study was to investigate the anti-cancer effects of Sophorae Radix and the effects of 5-Fluorouracil (5-FU) in human gastric adenocarcinoma cells (AGS). Method : We used human gastric adenocarcinoma cell line, AGS cells. We examined cell death by MTT assay and caspase 3 assay with Sophorae Radix. To examine the inhibitory effects of Sophorae Radix, cell cycle (sub G1) analysis was done the AGS cells after three days with Sophorae Radix. The reversibility of Sophorae Radix was examined on one day to five days treatment with 100 ${\mu}g/ml$ Sophorae Radix. Result : Sophorae Radix inhibited the growth of AGS cells in a dose-dependent fashion. Also we showed that Sophorae Radix induced apoptosis in AGS cells by MTT assay, caspase 3 assay and sub-G1 analysis. Sophorae Radix combined with 5-FU markedly inhibited the growth of AGS cells compared to Sophorae Radix or 5-FU alone. After 3 days treatment of AGS cells with Sophorae Radix, the fraction of cells in sub-G1 phase was much higher than that of the control group. Conclusion : Our findings provide insight into unraveling the effects of Sophorae Radix in human gastric adenocarcinoma cells and developing therapeutic agents against gastric cancer.