• Microbiology and Biotechnology Letters
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• v.31 no.3
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• pp.292-296
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• 2003

The antibacterial effect against cariogenic bacteria was evaluated in combination of 5-FC and intracellular cytosine deaminase from Chromobacterium violaceum YK 391. While S. mutans, L. parabuchneri and A. naeslundii showed antibacterial effect against 10 mM of 5-FU, S. intermedius, S. mitis, S. agalactiae, L. lactis, A. israelii, A. viscosus don't caused antibacterial effect. The addition of the cytosine deaminase and 10 mM of 5-FC to S. mutans, S. sanguis, L. brevis, L. parabuchneri, L. oris and A. naeslundii caused weakly antibacterial effect. S. sanguis caused weakly antibacterial effect against 10 mM of 5-FC. These results suggested that combination of the cytosine deaminase and 5-FC was showed the possibility to precautionary measures of dental caries.

• Journal of Digestive Cancer Research
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• v.6 no.2
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• pp.73-77
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• 2018

A 70-year-old female diagnosed with pancreatic ductal adenocarcinoma was treated by pylorus-preserving pancreaticoduodenectomy (PPPD) and adjuvant concurrent chemoradiotherapy with 5-fluorouracil. Pancreatic ductal adenocarcinoma pT3N0 (stage IIA) was pathologically confirmed. Abdominal computed tomography (CT) findings 14 months after PPPD showed 10 mm sized solitary liver metastasis in segment 3. After 12 cycles of gemcitabine and 9 cycles of capecitabine plus oxaliplatin, the metastatic nodule increased in size to 27 mm. Tumorectomy at segment 3 of liver was done. 25 months after tumorectomy, chest CT showed 23 mm sized cavitary nodule in right upper lobe of lung. The result of percutaneous biopsy favored metastatic adenocarcinoma. Two sets of stereotactic body radiation therapy were done and the patient has survived without further disease progression for 6 years after initial diagnosis. This case suggests that selected population of recurrent pancreatic cancer patients with solitary liver or pulmonary metastasis can be treated by resection of metastatic site and ablative therapies.

• YAKHAK HOEJI
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• v.50 no.2
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• pp.65-69
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• 2006

Novel 4'-hydroxymethyl branched thioapiosyl nucleosides were synthesized in this study. The introduction of hydroxymethyl group in the 4'-position was accomplished by a [3,3]-sigmatropic rearrangement. Thioapiosyl sugar moiety was constructed by sequential ozonolysis, reduction and cyclization. The pyrimidine nucleosidic bases (uracil, 5-fluorouracil, 5-iodouracil, 5-chlorouracil, 5-bromouracil) were efficiently coupled by Vorbruggen glycosyl condensation procedure (per-silyated base and TMSOTf). The antiviral activities of the synthesised compounds were evaluated against the HIV-1, HSV-1, HSV-2 and EMCV 5-Iodouracil 18 showed weak antiviral activity against HSV-1 $(EC_{50}=30.7{\mu}M)$.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1993.04a
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• pp.114-114
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• 1993

항암성 또는 항 virus성 약물개발 목적으로 천연의 pyrimidine nucleoside의 구조유사체로 pyrimidine acyclonucleoside들을 합성하였다. Pyrimidine acyclonucleoside를 염기 uracil, thymine 및 5-fluorouracil을 원료로 하여 합성하고 구조를 NMR, IR data를 써서 확인하였다. 이들 합성 화합물들은 L$_{1210}$ 암세포를 이용하여 in vitro 항암성 작용을 검색하였다. 합성된 화합물들 중 5-fluorouraoil-acyclonucleoside들은 약간이나마 모 5FU보다 높은 항암성 작용을 보였다. 유도체들은 5-FU의 N$^1$에 glycosidic 결합이 아닌 alkyl 결합을 하고있어, 모 5FU를 그리 쉽게 유리시키리라 보아지지 않으므로 이들의 작용성은 acyclonucleoside형태일 것 같아 이들의 작용기전 연구가 필요하다고 보아진다. 한편 얻은 유도체들은 HSV-1 및 HSV-2를 이용하여 항 virus성 작용을 검색한 결과 2500$\mu\textrm{g}$/ml 농도에서 유의성 있는 억제 작용성을 보이지 않았다.

• Macromolecular Research
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• v.14 no.4
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• pp.461-465
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• 2006

Two types of injectable system using thermosensitive chitosan (chitosan-g-NIPAAm), hydrogel and microparticles (MPs)-embedded hydrogel were developed as drug carriers for controlled release and their pharmaceutical potentials were investigated. 5-Fluorouracil (5-FU)-loaded, biodegradable PLGA MPs were prepared by a double emulsion method and then simply mixed with an aqueous solution of thermosensitive chitosan at room temperature. All 5-FU release rates from the hydrogel matrix were faster than bovine serum albumin (BSA), possibly due to the difference in the molecular weight of the drugs. The 5-FU release profile from MPs-embedded hydrogel was shown to reduce the burst effect and exhibit nearly zero-order release behavior from the beginning of each initial stage. Thus, these MPs-embedded hydrogels, as well as thermosensitive chitosan hydrogel, have promising potential as an injectable drug carrier for pharmaceutical applications.

• Journal of Microbiology and Biotechnology
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• v.15 no.3
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• pp.477-483
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• 2005

Corynebacterium ammoniagenes ATCC 6872, which does not accumulate pyrimidine nucleoside or nucleotide, was metabolically engineered to secrete a large amount of thymidine. Characteristics of 5-fluorouracil resistance ($FU^r$), hydroxyurea resistance ($HU^r$), trimethoprim resistance ($TM^r$), thymidylate phosphorylase deficiency ($deoA^-$), inosine auxotrophy ($ino^-$), 5-fluorocytosine resistance ($FC^r$), thymidine kinase deficiency, and thymidine resistance ($thym^r$) were successively introduced into mutant strains KR3 and DY5T9-5, and shake-flask cultures were able to accumulate 408.1 mg/l and 428.2 mg/l of thymidine, respectively, as a major product. The mutant strains did not accumulate thymine at all and accumulated less than 10 mg/l of other pyrimidine nucleosides, such as cytosine, cytidine, and deoxycytidine, as byproducts.

• Journal of Veterinary Clinics
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• v.35 no.6
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• pp.311-314
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• 2018

Squamous cell carcinoma (SCC) is a form of neoplasm that origins from the epithelial surface of many organs. Ocular occurrence in small animals is rare, especially in the central cornea without the involvement of limbus or conjunctiva. In the current case, a 10-year-old, spayed female Shih-Tzu was presented with a central corneal mass. Through an ophthalmic examination the sign of corneal scarring around the mass was found. Pink fleshy lesion that protruded outward was removed through superficial keratectomy. The mass with the size of $8.5{\times}6.5$ millimeter was histopathologically diagnosed as corneal SCC infiltrating not only the epithelium, but also the superficial corneal stroma with surrounding superficial lymphoplasmacytic and neutrophilic chronic keratitis. Also, the adjacent, non-affected corneal epithelium was markedly hyperplastic and keratinized; the adjacent stroma was moderately vascularized and fibrotic. The pulse-dose therapy using 1% topical 5-flourouracil were applied for five cycles. The tumor has not recurred through nine months of follow-up time.

• Korean Journal of Veterinary Research
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• v.64 no.1
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• pp.8.1-8.5
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• 2024

An 18-year-old miniature Appaloosa stallion presented with 6 months of history of sanguineous crusts on medial hind limbs and discomfort of micturition. Cauliflower-like and small masses were treated with cryotherapy for 6 months, but the regrowth of masses occurred. Subsequently, local excision via laser and topical treatment with 5% 5-fluorouracil for 5 months were followed. However, the horse was euthanized 4 months later due to regrowth of the masses. The mass was diagnosed as penile papilloma with cellular atypia and Equus caballus papillomavirus type 2 (EcPV-2) DNA was detected. This is the first report of equine penile neoplasm with EcPV-2 infection in Asia.

• KSBB Journal
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• v.23 no.5
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• pp.452-459
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• 2008

To obtain maximal efficacy with minimal systemic side-effects, many studies have been carried out to achieve the controlled release of 5-fluorouracil (5-FU). In this study, biodegradable poly(L-lactide) (L-PLA) microparticles containing 5-FU were prepared by a process, called aerosol solvent extraction system (ASES), utilizing supercritical carbon dioxide. The effects of various organic solvents, drug/polymer feeding ratio, polymer molecular weight, and blending with the same polymers with different molecular weights on the formation of 5-FU loaded microparticles were investigated under a predetermined operating condition from our previous study. The drug recovery, entrapment efficiency, and in vitro drug release kinetics were determined by HPLC assays. The drug recovery obtained from the ASES process was found to be very high, whereas the drug entrapment efficiency was considerably low in all the experiments due to the poor affinity between L-PLA and 5-FU. These results indicated that the precipitation rate of L-PLA might be quite different from that of 5-FU so that there was little chance to form 5-FU loaded L-PLA microparticles.

• Journal of Yeungnam Medical Science
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• v.9 no.1
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• pp.75-89
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• 1992

The development of multi drug-resistant tumor cell population is a major problem in the chemotherapy of human cancer. These cells are often cross resistant to unrelated drugs and the precise mechanisms of multidrug resistant phenotype of tumor cells has not been fully elucidated. Cisplatin resistant tumor cell(SNU-1/$Cis_5$) was induced from human stomach cancer cell line(SNU-1) in vitro. Growth profiles of survival cells were observed during 5 days by thiazolyl blue (MTT) assay. To investigate the cross resistance of various anticancer drugs in SNU-1 and SNU-1/$Cis_5$, We compared the value of $IC_{50}$ - drug concentration at 50% survival of control and gained relative resistances (RR). The RR for SNU-1/$Cis_5$ were as follows; vinblastine, > 43.0 ; epirubicin, 22.9 ; dactinomycin, 16.0 ; etoposide, 15.0 ; vincristine, 9.2 ; adriamycin, 5.7 ; aclarubicin, 5.3. But 5-fluorouracil, methotrexate, daunorubicin have not cross resistance with cisplatin. Resistant inhibition values of $10{\mu}M$ verapamil for SNU-1/$Cis_5$ were as follows; vincristine, 13.1 ; epirubicin, 10.0 ; etoposide, 6.3 ; vinblastine, 4.4 ; dactinomycin, 3.6 ; daunorubicin, 2.4. Membrane proteins of 51,400 and 81,300 daltons were identified by radioiodination with SDS-PAGE, which might represented the drug resistance.