• Asian Pacific Journal of Cancer Prevention
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• 제16권6호
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• pp.2355-2359
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• 2015

Background: Combination chemotherapy of 5 fluorouracil (5-FU) and leucovorin (LV) with oxaliplatin, mainly FOLFOX regimens, has shown considerable antitumor activity and a tolerable toxicity profile in gastric cancer. The goal of this study was to retrospectively compare the efficacy and toxicity of modified FOLFOX-6 (mFOLFOX6) regimen in advanced gastric cancer (AGC) patients with good and poor performance status (PS). Materials and Methods: AGC patients receiving the mFOLFOX6 regimen including oxaliplatin $85mg/m^2$, bolus of 5-FU $400mg/m^2$ and LV $400mg/m^2$ on the first day, followed by $2400mg/m^2$ of 5- FU as a continious infusion over 46 hour for first-line treatment were eligible for the study. Results: A total 58 patients with a median age of 59.5 (32-81) were included. The median follow up of the study was 9.2 months. Thirty patients (51.7%) with an ECOG PS 0-1 were assigned to the good PS arm, while 28 patients (48.3%) with ECOG PS 2 were in the poor PS arm. Overall response rates were 36.6 and 28.8%, respectively (p=0.91). Median PFS was 6.7 and 6.3 months in good PS and poor PS arms (p=0.50) and median OS was 9.6 and 10.4 months (p=0.55). As compared with good PS arm, poor PS arm was associated with more grade 3-4 neutropenia and anemia. Dose reduction and dose delays were also significantly higher. Conclusions: In this study, mFOLFOX6 was similarly effective in both arms. Although hematologic toxicity was significantly higher in patients with poor PS, it remained manageable. Our results suggest that this regimen may be an effective treatment option for AGC patients with poor PS.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1993년도 제2회 신약개발 연구발표회 초록집
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• pp.177-177
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• 1993

뇌모세혈관내피세포로 구성된 혈액-뇌관문(BBB)은 tight junction으로 구성되어 있을뿐만 아니라 fenestra가 없는 등 BBB가 가진 특성으로 인해 물질 수송에 장벽역할을 하기 때문에 주로 중추신경계 질환시의 약물요법에 많은 제한이 따른다. 따라서 뇌로의 효율적인 약물 송달방법에 대해 많은 연구가 진행중에 있는데 본 연구에서는 BBB의 hyperosmotic opening법을 이용하여 뇌로 잘 수송되지 않는 약물의 뇌송달 방법에 대해 연구하고자 하였다. 먼저 수용성으로 인해 BBB 에 잘 통과하지 않는 물질로 신장 및 뇌영상 촬영시 사용되는 방사성 의약품이 Tc-DTPA를 이용하여, hyperosmotic opening법에 의한 뇌투과 증가정도를 검토하였으며, 실험방법이 확립됨에 따라 뇌암의 항암요법을 위해 뇌로의 투과가 적은 항암제(5-Fluorouracil, 5-FU)의 뇌송달에 대해 본 방법을 적용하여 검토하였다. 실험동물로는 S.D.계 웅성 랫트를 사용하였으며, 실험방법은 다음과 같이 하였다. 랫트의 좌측 외경동맥(left external carotid artery)에 혈류의 역방향으로 혈관 분지점에서 1-2mm 전까지 PE-50 catheter를 삽입하고, 1.6 molal L－(＋)－ arabinose 고장액(1580mOsm)을 0.12ml/sec의 일정한 속도로 30초간 infusion함으로 BBB를 opening 한 다음, 5분 후에 Tc-DTPA를 대퇴 정맥으로 주사하여 0, 10, 30초, 1, 1.5, 2, 3, 4, 5, 7 및 10분 간격으로 대퇴동맥에 설치한 카테타로부터 혈액을 채취하고 마지막 혈액을 취한 후 즉시 단두하여 뇌를 적출하였다. 채취한 뇌를 액체질소에 담근 후 tissue Tek으로 고정하고 autoradiography를 하기 위한 slice와 농도측정을 위해 필요한 부위를 취한 후 감마카운터로 Tc-DTPA의 brain각 부위별 및 혈장농도를 측정하였다. 뇌조직중 혈액부피의 측정은 Tc-albumin를 이용하여 구하였다. 같은 방법으로 5-FU에 대한 실험도 행하였고, 이때 각 혈장 및 조직중의 5-FU함량은 HPLC로 하였다.

• 한국미생물·생명공학회지
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• 제20권2호
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• pp.150-155
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• 1992

토양 분리 균주로부터 얻은 배양액을 20-80 황산암모늄으로 분획한 후 세포의 cytosine deaminase의 성질을 검토하였다. 이 효소는 cytosine과 5-fluorocytosine(5-FC)에 기질 특이성을 가짐으로서 각각 uracil과 5-fluorouracil(5-FU)로 전환을 촉매하였다. 효소안정성에 대한 온도와 보존기간은 tris-HC1 완충용액에서 검토한 결과 최적온도는 $50^{\circ}C$ 부근이하에서 90 이상의 잔존활성을, 보존시간은 4일정도에서 80 이상의 잔존활성을 유지하였다. 최대 pH 8.0과 $37^{\circ}C$의 온도에서 나타났다. 활성에 적당한 pH는 8.0~8.5였고, 온도는 37~$45^{\circ}C$의 범위였다.

• Journal of Microbiology and Biotechnology
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• 제15권3호
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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.

• 대한한방내과학회지
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• 제33권4호
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• pp.387-404
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• 2012

Objectives : This study was to observe anticancer and related immunomodulatory effects of Kwibi-tang extracts (KBTe) on non-small cell lung carcinoma (squamous epithelial carcinoma), NCI-H520, xenograft Balb/c nu-nu nude mice. Methods : Three different dosages of KBTe, 50, 100 and 200 mg/kg were orally administered once a day for 42 days from 11 days after tumor cell inoculation. Six groups, each of 8 mice per group were used in the present study. Changes in body weight, tumor volume and weight, lymphatic organs (spleen and popliteal lymph node), serum interferon (IFN)-${\gamma}$ levels, splenocytes NK cell activity and peritoneal macrophage activities, splenic tumor necrosis factor (TNF)-${\alpha}$, interleukin (IL)-$1{\beta}$ and IL-10 contents were observed with tumor mass and lymphatic organ histopathology to detect anticancer and immunomodulatory effects. The results were compared with a potent cytotoxic anticancer agent, 5-FU (5-Fluorouracil) 30 mg/kg, intraperitoneal treatment (3-day intervals for 42 days, the optimal effective treatment regimes already confirmed). Results & Conclusions : This study suggest that over 50 mg/kg of KBTe showed favorable anticancer effects on the NCI-H520 cell xenograft with immunomodulatory effects. Although relatively lower anticancer effects were observed in KBTe 200 mg/kg treated mice as compared with 5-FU 30 mg/kg treated mice, no meaningful favorable immunomodulatory effects were observed after 5-FU treatment in the present study.

• 대한한의학회지
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• 제16권2호
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• pp.414-432
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• 1995

In order to prove the antitumer effect of Bupleuri Radix(BR) and Artemisiae capillaris Herba(ACH) experimently, studies were done. The antitumer effect against hepatic cancer such as Hep G2, PLC & Hep 313, and also th synergastic action was evaulatcd in the combined treatment with anticancer drugs using chiefly for liver cancer, such as mitomycin(MMC), cisplatin(CPT) and 5-fluorouracil(5-FU). The results were obtained as follows: 1. IC50 against Hep G2, Hep 3B and PLC was 15.5ug/ml, 25.4ug/ml, 31.25ug/ml in Mitomycin (MMC), 92.5ug/ml, 50.2ug/ml, 62.5ug/ml in cisplatin(CPT) and 125ug/ml in 5-fluouracil(5- FU) respectively. 2. The antitumor effect was shown in the all concentrations of ACH, BR and below 55%-Cytotoxic effect against Hep G2 as compared with the date of control was shown in the concentration of $10^{-4}g/ml$ above of BR but not in ACH and also BR and ACHI revealed the synergistic effect with MMC. 3. The antitumor effect was shown in the concentration of $10^{-5}g/ml$ above of ACH, BR and below 55%-Cytotoxic effect against Hep 3B as compared with the data of control was shown in the concentration of $10^{-5}g/ml$ above of ACH but not in BH and also BR & ACH revealed the svnergistic effect with MMC. 4. The antitumor effect was shown in the all concentrations of ACH, BR and 55%-Cytotoxic effect against PLC as compared with the data of control was shown in the concentration of $10^{-5}g/ml$ above of ACH but not in BR and also ACH revealed the synergistic effect with MMC. From the above results it was concluded that Artemisiae capillaris had antitumor effect against PLC, Hep 3B, Bupleuri Radix against Hep G2 and also MMC showed the most synergistic effect in the anticancer drugs.

• 대한방사선기술학회지:방사선기술과학
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• 제38권4호
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• pp.463-475
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• 2015

본 논문은 상당히 진행된 중위 식도암의 동시항암화학 방사선치료에 대한 분석의 것이다. 사용한 항암제는 전통적으로 사용되어온 시스플라틴, 5-플루오로우라실에, 도쎄탁실을 추가 시행하였다. 과거 식도암의 방사선치료에서는 총 선량 50.4 Gy/28회를 처방하였다. 하지만 현대의 방사선치료기술의 비약적인 발전으로, 호흡동조치료와 세기변조방사선치료를 적용하여, 정상조직의 손상을 최대한 감소시키면서 총 선량을 50.4 Gy이상으로 증가시키는 것이 가능하다. 이에 우리는, 도쎄탁실, 시스플라틴, 5-플루오로우라실 이라는 새로운 3제 병합요법(DCF-R)에 추가하여, 4DCT 모의시뮬레이션을 기반으로 한 호흡동조 세기변조방사선치료(gated-IGRT) 총 선량 70.2 Gy/39회를 동시에 시도하였으며, 치료기간 동안, 그리고 치료 종료 후 임상적으로 환자에게 위중한 합병증 및 부작용 발생은 관찰되지 않았다. 또한 생존율 향상을 이루어 냈다. 이를 바탕으로, 식도암의 새로운 치료방법을 제안한다.

• Natural Product Sciences
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• 제13권3호
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• pp.234-240
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• 2007

The present study investigated the anti-tumor activity of ethyl acetate extract of Acanthospermum hispidum DC against daltons ascites lymphoma in mice. The extract was prepared by cold maceration with ethyl acetate for 3 - 7 days and evaporated in vacuum to dry. (Yield : 14.2 g, 1.42% w/w). The extract was fractionated by column chromatography by using gradient elution technique and the diterpenes fraction isolated (0.649 g). Both extract and the fraction were administered as oral suspension with tween 20 in water to tumor bearing mice (DAL) and changes in dead cell count, histopathology of tumor cells, hematological parameters and median survival time (MST) were examined and compared with that of tumor control or 5-Fluorouracil (5-FU). The results indicate that both ethyl acetate extract and fraction possess anti-tumor activity. The study suggests that Acanthospermum hispidum DC seems promising as a source of diterpenes for potential anti-tumor activity.

• Bulletin of the Korean Chemical Society
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• 제26권11호
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• pp.1865-1868
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• 2005

• 생약학회지
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• 제27권1호
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• pp.42-46
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• 1996

The medicinal formula, Kilkyungtang (KKT) and two modified Kilkyungtangs (KKT-1 and KKT-2), which were supplemented by the additional crude drug, Houttuyniae herba (KKT-1), and Oldenlandiae diffusae herba (KKT-2) to KKT, had been applied widely as decoctions for the treatment of malignant tumors. Cytotoxic activities against two tumor cell lines, A549 and $B16-F_0$ were investigated. However, none of them were found to exhibit significant cytotoxicity upon tested tumor cells below the concentration of $1000{\mu}g/ml$. However, cytotoxic activities of three reputed antitumor agents, i.e., mitomycin C (MMC), cisplatin (CPT) and 5-fluorouracil (5-FU) was significantly potentiated by the combined treatment of them with KKT, KKT-1 and KKT-2 respectively, especially against A549 (human non small cell lung adenocarcinoma), in vitro.