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RISS 인기검색어
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- 저자 : 장일무 ( Hee Joo Lee (검색결과 2 건)
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이희주,차영애,안정욱,장일무,Lee, Hee-Joo,Cha, Young-Y.,Ahn, Jung-W.,Chang, Ill-M. 생화학분자생물학회 1984 한국생화학회지 Vol.17 No.3
9-$\beta$-D-Arabinofuranosyladenine-5'-methoxyacetate (ara-A-MA) 및 1-$\beta$-D-Arabinofuranosylcytosine-5'-methoxyacetate (ara-C-MA)를 합성하였다. 이들 물질의 항암작용을 검토한 바, sarcoma 180 암세포를 이식한 mice중 생리식염수만 공급 받은 negative 대조군은 생존일수가 $16.3{\pm}4.1$일이었고, positive 대조군인 ara-C(13.9 mg/kg/mouse)를 투여 받은 실험군은 생존일수가 $22.0{\pm}2.5$ 일이었다. ara-A-MA를 투여 받은 시험군은 $20.8{\pm}2.9$일(19.4 mg/kg/mouse) 이었고, ara-C-MA를 투여 받은 실험군은 $23.1{\pm}3.3$일(18.0 mg/kg/mouse) 및 $20.1{\pm}2.2$일(1.8 mg/kg/mouse)의 생존일수를 각각 나타내었다. 한편 이들 합성 화합물은 DNA 합성을 억제하는 작용을 나타내었는데, ara-A-MA는 Fischers media에 배양한 sarcoma 180 암세포의 DNA 생합성을 $10^{-3}\;M$ 농도에는 57% 그리고 $10^{-4}\;M$에서 50%를 억제하고, ara-C-MA는 94% 및 80%를 각각의 농도에서 억제시켰다. 이들 결과는 ara-A-MA 및 ara-C-MA가 ara-A 및 ara-C의 prodrug으로서 역할을 할 수 있는 가능성을 시사한다. 9-$\beta$-D-Arabinofuranosyladenine-5'-methoxyacetate (ara-A-MA) and 1-$\beta$-D-Arabinofuranosylcytosine-5'-methoxyacetate (ara-C-MA) were synthesized. Their antitumor activities were evaluated against sarcoma 180 tumor cells inoculated in mice. When administered intra peritoneally once daily for 6 days, average life-spans for those which received ara-A-MA, ara-C-MA, ara-C and saline (0.9%) were; $20.8{\pm}2.9$(19.4 mg/kg/mouse) and $19.1{\pm}2.5$(1.9 mg/kg/mouse) days; $23.1{\pm}3.3$(18.0 mg/kg/mouse) and $20.1{\pm}2.2$(1.8 mg/kg/mouse) days; $22.0{\pm}2.5$(13.9 mg/kg/mouse) days; and $16.3{\pm}4.1$ days, respectively. This survival study indicates that ara-A-MA and ara-C-MA exhibit antitumor activities as much potent as their parent compounds of ara-C. DNA biosynthesis in Sarcoma 180 cells in vitro were also inhibited by ara-A-MA. At the concentrations of $10^{-3}$ and $10^{-4}\;M$, ara-A-MA and ara-C-MA showed 57 and 50%, 94 and 80% inhibitions of DNA synthesis in comparison with that of negative control group, respectively.
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이희주,차영애,안정욱,장일무 ( Hee Joo Lee,Young Y . Cha,Jung W . Ahn,Ill M . Chang ) 생화학분자생물학회 1984 BMB Reports Vol.17 No.3
9-β-D-Arabinofuranosyladenine-5`-methoxyacetate (ara-A-MA) and 1-β-D-arabinofuranosylcytosine-5`-methoxyacetate (ara-C-MA) were synthesized. Their antitumor activities were evaluated against sarcoma 180 tumor cells inoculated in mice. When administered intraperitoneally once daily for 6 days, average life-spans for those which received ara-A-MA, ara-C-MA, ara-C and saline (0.9%) were; 20.8±2.9(19.4 ㎎/㎏/mouse) and 19.1±2.5 (1.8 ㎎/㎏/mouse) days; 23.1±3.3(18.0 ㎎/㎏/mouse) and 20.1±2.2(1.8 ㎎/㎏/mouse) days; 22.0±2.5(13.9 ㎎/㎏/mouse) days; and 16.3±4.1 days, respectively. This survival study indicates that ara-A-MA and ara-C-MA exhibit antitumor activities as much potent as their parent compounds of ara-C. DNA biosynthesis in Sarcoma 180 cells in vitro were also inhibited by ara-A-MA. At the concentrations of 10^(-3) and 10^(-4) M, ara-A-MA and ara-C-MA showed 57 and 50%, 94 and 80% inhibitions of DNA synthesis in comparison with that of negative control group, respectively.
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