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用体外无细胞RNA合成系统对阿克拉霉素B(AcM—B)和阿霉素(ADM)抑制个同DNA模板的依赖DNA的RNA合成作了研究。两药抑制双链NDA模板显著强于单链DNA,作用依次为交序双链DNA(Poly[d(A—T)]和poly[d(G—C)])>同序双链DNA(polydG.polydC和polydA.polydT)》单链DNA(polydA,polydT和polydC)。抑制作用可被增加的DNA模板所逆转。这表明两药主要嵌入DNA双螺旋,特别抑制交序碱基排列的双链DNA.有立体效应。比较双链DNA模板的IC_50证明AcMB和ADM虽然更明显抑制含A—T顺序的DNA,但对A—T和G—C顺序DNA均有显著抑制制。另外AcM—B比ADM抑制DNA顺序的选择性高。
The in vitro RNAi-free RNA synthesis system was used to study the DNA-dependent RNA synthesis of amlymin B (AcM-B) and doxorubicin (ADM) inhibiting DNA templates. Two drugs inhibited the double-stranded NDA template was significantly stronger than single-stranded DNA, followed by sequential double-stranded DNA (Poly[d(A-T)] and poly[d(G-C)])> homologous double-stranded DNA ( polydG.polydC and polydA.polydT) single-stranded DNA (polydA, polydT and polydC). Inhibition can be reversed by increased DNA templates. This indicates that the two drugs mainly intercalate into DNA double helices, specifically inhibiting the double-stranded DNA of the aligned base sequences. There are steric effects. Comparing the IC_50 of the double-stranded DNA template demonstrated that AcMB and ADM significantly inhibited the DNA containing the A-T sequence, but significantly inhibited both A-T and G-C sequential DNA. In addition, AcM-B has a higher selectivity for inhibiting DNA sequence than ADM.