De Clercq E, Huang G F, Torrence P F, Fukui T, Kakiuchi N, Ikehara M
Nucleic Acids Res. 1977 Oct;4(10):3643-53. doi: 10.1093/nar/4.10.3643.
Poly (2-azaadenylic acid) [(aza2A)n] and poly(2-azainosinic acid [(aza2I)n], two newly synthesized analogues of (A)n and (I)n, in which CH-2 of the purine ring is replaced by a nitrogen atom, have been evaluated in various biological assay systems. (Aza2A) n formed a complex with (U)n and (br5U)n, and (aza2I)n formed a complex with (C)n and (br5C)n, but these complexes were markedly destabilized relative to the corresponding (A)n or (I)n complexes. The (aza2A)n-and (aza2I)n-derived complexes failed to stimulate the production of interferon in primary rabbit kidney cells and human diploid fibroblasts, under conditions (A)n. (U)n, (I)n. (C)n and (I)n. (br5C)n induced high amounts of interferon. both (aza2A)n and (aza2I)n exerted a marked inhibitory effect on the endogenous RNA directed DNA polymerase (reverse transcriptase) activity associated with murine leukemia virus. They caused a relatively mild inhibition of complement activity in an hemolytic assay system.
聚(2-氮杂腺苷酸)[(aza2A)n]和聚(2-氮杂肌苷酸)[(aza2I)n]是(A)n和(I)n的两种新合成类似物,其中嘌呤环的CH-2被氮原子取代,已在各种生物学检测系统中进行了评估。(aza2A)n与(U)n和(br5U)n形成复合物,(aza2I)n与(C)n和(br5C)n形成复合物,但相对于相应的(A)n或(I)n复合物,这些复合物明显不稳定。在(A)n、(U)n、(I)n、(C)n和(I)n·(br5C)n诱导大量干扰素的条件下,(aza2A)n和(aza2I)n衍生的复合物未能刺激原代兔肾细胞和人二倍体成纤维细胞中干扰素的产生。(aza2A)n和(aza2I)n均对与鼠白血病病毒相关的内源性RNA指导的DNA聚合酶(逆转录酶)活性产生显著抑制作用。在溶血检测系统中,它们对补体活性产生相对较轻的抑制作用。