• Title/Summary/Keyword: fluorouracil

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Cytotoxicity of Water Fraction of Artemisia argyi against L1210 Cells and Antioxidant Enzyme Activities (황해쪽 물분획물의 L1210세포에 대한 세포독성과 항산화효소 활성변화)

  • 박시원;정대영
    • YAKHAK HOEJI
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    • v.46 no.1
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    • pp.39-46
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    • 2002
  • The water fraction exhibiting anticancer activity was prepared from 70% methanol extract of Artemisis argyi by stepwise solvent partioning. This water fraction(5 $\mu$g/ml concentration) showed a considerable cytotoxicity against leukemic L1210 cells with a maximal value of 92% for 3 days culture. Contrastingly to such substantial anticancer activities the identical fraction showed far low toxicity against normal lymphocytes than chloroform fraction of Artemisia argyi mitomycine and 5-fluorouracil at every concentration ranging 0.01$\mu$g/ml~10.00$\mu$g/ml. The cytotoxicity displayed against L1210 cells by the water fraction of Artemisia was found to be proportinal to the decrease of viability of L1210 cells. On the other hand, $O_2$ion generation in L1210 cells appeared to be elevated in accordance to cytotoxicity by the water fraction with concurrent increases of superoxide dismuatse (SOD) and glutathione peroxidase (GPx) which are responsible for the conversion of $O_2$ ion and $H_2O$$_2$ respectively These findings taken together indicate that the death of L1210 cells by the water fraction of Auemisia atgyi, may be induced at least in part by the detrimental action of reactive oxygen species (ROS) including $O_2$- in spite of substantial extorts of SOD and GPx to overcome the attack of ROS.

Granulocyte-macrophage colony stimulating factor protects dendritic cells from anticancer drug-induced apoptosis (수지상세포에서 GM-CSF의 항암제유도 세포사멸 방지효과에 관한 연구)

  • Joo, Hong-Gu
    • Korean Journal of Veterinary Research
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    • v.43 no.4
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    • pp.607-613
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    • 2003
  • Dendritic cells (DCs) play an essential role in a variety of immune reactions involving $CD4^+$ T cells and have been used to enhance tumor-specific immune responses. Immunosuppression in patients with cancer includes the downregulation of function and number of DCs. Although DCs have been studied, the apoptosis of Des induced by anticancer drugs for chemotherapy remains largely uncharacterized. This study demonstrated that GM-CSF protects DCs from 5-fluorouracil (5-FU) or mitomycin C-induced apoptosis. After 6 - 10 days culture, DCs were characterized by specific surface marker, CD11c and MHC class II. MTT assay revealed that GM-CSF significantly enhanced the viability of DCs treated with 5-FU or mitomycin C. The percentage of dead cells of DCs was determined by cell size using FACScan and GM-CSF was clearly effective. However, GM-CSF did not increase the expression of MHC class II on viable DCs gated, suggesting that GM-CSF may differentially regulate critical factors involved in the function of DCs. For the quantitative analysis of apoptosis, annexin V-FITC staining was performed. 5-FU induced the apoptosis of DCs and GM-CSF significantly protects DCs from 5-FU-induced apoptosis. Taken together, the results in this study that GM-CSF has an anti-apoptosis effect on DCs may provide patients with cancer with clinical benefits to overcome the immunosuppression induced by the decrease of number and functional insufficiency of DCs.

A Case of Pellagra Induced by Isoniazid during Treatment of Pulmonary Tuberculosis (폐결핵 치료중 Isoniazid에 의해 발생한 Pellagra 1례)

  • Jeon, Ho Seok;Han, Min Soo;Ahn, Ju Eui;Lee, Yang Deok;Cho, Yongseon
    • Tuberculosis and Respiratory Diseases
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    • v.57 no.2
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    • pp.180-182
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    • 2004
  • A Case of Pellagra Induced by Isoniazid during Treatment of Pulmonary Tuberculosis Pellagra is a disease caused by a deficiency of nicotinic acid or niacin. It is mostly found among people eating corn-based diets in parts of China, Africa and India. It is also induced by drugs, such as isoniazid or 5-fluorouracil. Isoniazid inhibits the conversion of tryptophan to niacin and may induce pellagra, particularly in poorly nourished patients. Pellagra should be suspected whenever tuberculous patients under the treatment with isoniazid develop mental, neurological or gastrointestinal symptoms, even in the absence of typical skin changes. Herein, our experienced of a case of pellagra induced by isoniazid during treatment of pulmonary tuberculosis is reported. The patient was referred due to a skin rash and drowsy mental status. Her skin lesion developed during treatment for pulmonary tuberculosis. Her symptoms were improved after discontinuation of antituberculous agents and on the administration of nicotinamide.

Antitumor evaluation and antimicrobial activity of geranyl phenyl ethers

  • Oh Hyun-Ju;Shin Ji-Hee;Chung Woo-Young;Han Du-Seok;Baek Seung-Hwa
    • Advances in Traditional Medicine
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    • v.2 no.1
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    • pp.52-57
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    • 2002
  • Geranyl phenyl ethers 1, 2, 3, 4 and 5, 5-fluorouracil 6 and adriamycin 7 as references were tested for their growth inhibitory effects against tumor cell lines and NIH 3T3 fibroblasts using two different assays, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) and sulforhodamine B protein (SRB) assays. These results suggest that methyl-4-[{(2E)-3,7-dimethyl-2,6-octadienyl}oxy]-3-methoxy benzoate 1 showed growth inhibition activity against tumor cell lines. The maximum activity exhibited by methyl-4-[{(2E)-3,7-dimethyl-2,6-octadienyl}oxy]-3-hydroxybenzoate 3 against Staphylococcus epidermidis (MIC, $1,000{\mu}g/ml$).

Cytotoxic and Antimicrobial Activities of Bioactive Monoterpenophenols

  • Oh In Kio;Lee Hyun Ok;Ahn Jong Woong;Kim Hyung Min;Shin Ji Hee;Lim Jin A;Chun Hyun Ja;Baek Seung Hwa
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.16 no.6
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    • pp.1270-1276
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    • 2002
  • Compounds 1 - 12 were tested for their growth inhibitory effects against tumor cell lines using two different 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) and sulforhodamine B protein (SRB) assays and antimicrobial activity. The cytotoxic activity of methyl-4-[{(2E)-3,7-dimethyl-2,6-octadienyl}oxy]-3-methoxy benzoate (1) exhibit more active than that of 5-fluorouracil (11) on human oral epithelioid carcinoma (KB, ATCC No. OCL 17) cell lines. But this compound (1) on human skin melanoma (SK-MEL-3, HBT 69) cell lines shows less active than that of adriamycin (12). However, compound 9 showed the antimicrobial activity against S. epidermidis (MIC, 15.625 ㎍/㎖), S. aureus, C. albicans (MIC, 31.25 ㎍/㎖), S. mutans, S. typhimurium, P. putida (MIC. 125 ㎍/㎖) and P. aeruginosa (MIC, 500 ㎍/㎖).

Cellular Prion Protein Enhances Drug Resistance of Colorectal Cancer Cells via Regulation of a Survival Signal Pathway

  • Lee, Jun Hee;Yun, Chul Won;Lee, Sang Hun
    • Biomolecules & Therapeutics
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    • v.26 no.3
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    • pp.313-321
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    • 2018
  • Anti-cancer drug resistance is a major problem in colorectal cancer (CRC) research. Although several studies have revealed the mechanism of cancer drug resistance, molecular targets for chemotherapeutic combinations remain elusive. To address this issue, we focused on the expression of cellular prion protein ($PrP^C$) in 5-FU-resistant CRC cells. In 5-FU-resistant CRC cells, $PrP^C$ expression is significantly increased, compared with that in normal CRC cells. In the presence of 5-FU, $PrP^C$ increased CRC cell survival and proliferation by maintaining the activation of the PI3K-Akt signaling pathway and the expression of cell cycle-associated proteins, including cyclin E, CDK2, cyclin D1, and CDK4. In addition, $PrP^C$ inhibited the activation of the stress-associated proteins p38, JNK, and p53. Moreover, after treatment of 5-FU-resistant CRC cells with 5-FU, silencing of $PrP^C$ triggered apoptosis via the activation of caspase-3. These results indicate that $PrP^C$ plays a key role in CRC drug resistance. The novel strategy of combining chemotherapy with $PrP^C$ targeting may yield efficacious treatments of colorectal cancer.

Safety and Management of Toxicity Related to Aflibercept in Combination with Fluorouracil, Leucovorin and Irinotecan in Malaysian Patients with Metastatic Colorectal Cancer

  • Yusof, Mastura Md;Abdullah, Nik MA;Sharial, MSN Mohd;Zaatar, Adel
    • Asian Pacific Journal of Cancer Prevention
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    • v.17 no.3
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    • pp.973-978
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    • 2016
  • Background: Between October 2012 and February 2015, 25 patients with metastatic colorectal cancer (mCRC) (mean age, $57.0{\pm}12.1years$) were granted access to aflibercept via the Aflibercept Named Patient Program at four centers. Materials and Methods: Here we reported the initial experience of aflibercept / FOLFIRI in combination. We evaluated treatment-related adverse events (AEs), progression-free survival (PFS) and overall survival (OS). Results: The majority of the patients experienced gastrointestinal toxicity (grade 1-2), with diarrhea (52%), mucositis (52%), and nausea/vomiting (20%) being largely observed. Neutropenia (16%) and febrile neutropenia (8%) were common grade 3-4 hematological events. Aflibercept-related toxicity was managed as per practice guidelines. No grade 5 event was reported. Median PFS was 6.12 months (95% CI, 4.80-7.20) and OS was 12 months (95% CI, 9.80-14.18). The partial response (PR), stable disease (SD), and progressive disease (PD) rates were 25% (95% CI: 23.4-27.0), 37.5% (95% CI: 31.6-43.3), and 37.5% (95% CI: 22.5-52.5), respectively. Conclusions: Aflibercept/FOLFIRI can be administered safely in a second line setting to Malaysian patients with mCRC, as the AEs experienced were generally reversible and manageable. The safety and efficacy outcomes were consistent with those observed in Western populations.

Survival Outcomes of Advanced and Recurrent Cervical Cancer Patients Treated with Chemotherapy: Experience of Northern Tertiary Care Hospital in Thailand

  • Boupaijit, Kuanoon;Suprasert, Prapaporn
    • Asian Pacific Journal of Cancer Prevention
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    • v.17 no.3
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    • pp.1123-1127
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    • 2016
  • Chemotherapy is the primary treatment for advanced and recurrent cervical cancer. To evaluate the survival outcomes of chemotherapy and the prognostic factors in this setting, we conducted a retrospective study by reviewing the medical records of advanced and recurrent cervical cancer patients treated with systemic chemotherapy at our institute between January, 2008 and December, 2014. One hundred and seventy-three patients met the criteria with a mean age of 50.9 years. 4.1% of them were HIV positive. The most common initial stage was stage IVB (30.1%) and the most common histology was squamous cell carcinoma (68.6%). Ninety-two (53.2%) patients were previously treated with concurrent chemoradiation with 53% developing combined sites of recurrence. The median recurrence free interval was 16.7 months. Cisplatin + 5 fluorouracil (5FU) (53.2%) was the most frequent first line chemotherapy followed by carboplatin + paclitaxel (20.2%) with an objective response of 39.3%. Seventy-two patients received subsequent chemotherapy. The median overall survival of all studied patients was 13.2 months. Only a recurrence free interval of less than 12 months was an independent prognostic factor for survival outcome. In conclusion, chemotherapy treatment for advanced and recurrent cervical cancer patients showed modest efficacy with a shorter recurrence free survival less than 12 months as a significant poor prognosis factor.

Apoptosis of Colorectal Cancer UTC116 Cells Induced by Cantharidinate

  • Liu, Bin;Gao, Hai-Cheng;Xu, Jing-Wei;Cao, Hong;Fang, Xue-Dong;Gao, Hai-Mei;Qiao, Shi-Xing
    • Asian Pacific Journal of Cancer Prevention
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    • v.13 no.8
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    • pp.3705-3708
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    • 2012
  • Effects of Cantharidinate on apoptosis of human colorectal cancer UTC-116 cells were investigated by means of 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay, H and E staining, flow cytometry, and Raman Spectra analysis. The results showed Cantharidinate to exert inhibitory action on proliferation of human colorectal cancer UTC-116 cells, inducing apoptosis, arresting cells in G1 phase, with decline of S and G2 phases. In addition, the results of Raman spectrum showed significant changes in the UTC-116 cells chemical structure with stretching after the application of Cantharidinate. Taken together, these results suggest that the treatment of human colorectal cancer with Cantharidinate may be associated with multiple molecular mechanisms for apoptosis. Furthermore, similar to fluorouracil, Cantharidinate should be considered as novel assistant drug for controlling the growth of human colorectal cancer UTC-116 cells.

Preparation and Drug-releasing Properties of Chitosan-based Thermosensitive Composite Hydrogel

  • Li, Heping;Yu, Tao;Li, Shan;Qin, Long;Ning, Jingheng
    • Journal of the Korean Chemical Society
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    • v.56 no.4
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    • pp.473-477
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    • 2012
  • The novel chitosan-based thermosensitive hydrogels were prepared as control-releasing drug carriers. N-carboxyethyl chitosan (ACS) was synthesized by microwave heating for 1 h through Michael addition of CS to acrylic acid in a grafting yield of 52.97%, which was proved to be a faster and more efficient way than ordinary methods. 5-Fu was modified with formaldehyde to synthesize N,N'-Bis(hydroxymethyl)-5-fluorouracil (5-Fu-OH). Then an esterification was performed using ACS and 5-Fu-OH to give 5-Fu-ACS. The new thermosensitive hydrogels were prepared by adding sodium glycerophosphate to the solution of compounds under a certain constant temperature. Simultaneously, the hydrogels' swelling rate, in vitro drug release rate and thermosensitive were studied, and found that the 5-Fu-ACS composite hydrogel had more excellent releasing effect, higher drug loading and better thermosensitive.