Koumoto Y, Hisamoto Y, Shinoda S, Yamamoto S
Faculty of Pharmaceutical Sciences, Okayama University, Japan.
Chem Pharm Bull (Tokyo). 1990 Jun;38(6):1648-52. doi: 10.1248/cpb.38.1648.
The effects of various synthetic triamines having a general structure, H2N(CH2)xNH(CH2)yNH2, where x = 2-5 and y = 2-8 (abbreviated, x-y; with 3-4 being spermidine itself), on poly(U)-directed polypeptide synthesis of Escherichia coli and on growth of its polyamine-requiring mutants were examined in comparison with those of spermidine. Except for 2-2 and 2-3, all of the triamines stimulated more or less polypeptide synthesis at suboptimal Mg2+ concentrations, but the Mg2+ concentration required for the maximal stimulatory effect was different for each triamine. The degree of maximal stimulation caused by 3-3 (norspermidine), 4-4 (homospermidine), or 4-5 was nearly comparable with that by spermidine. The acetylspermidines were inactive, however, they inhibited the spermidine-stimulated polyphenylalanine synthesis. Many of the triamines examined reduced the ratio of leucine to phenylalanine incorporation into polypeptides during poly(U)-directed translation, and the degree of this effect did not necessarily correspond with that of the stimulatory effect. Moreover, 2-4, 2-5, 3-3 and 4-4 could stimulate the growth of a polyamine auxotroph of E. coli, MA 261, as effectively as did spermidine. However, 3-3 was the only triamine which could fully replaced spermidine in promoting growth of a mutant strain, KK 101, which is more dependent on polyamines than MA 261. Thus, these results demonstrated that some synthetic triamines were as active as spermidine in eliciting these effects, and also that there were some differences among these effects in the structural requirement for triamine.
研究了具有通式H2N(CH2)xNH(CH2)yNH2(其中x = 2 - 5且y = 2 - 8,简称为x - y;3 - 4为亚精胺本身)的各种合成三胺对大肠杆菌的聚(U)指导的多肽合成及其多胺需求型突变体生长的影响,并与亚精胺的影响进行了比较。除2 - 2和2 - 3外,所有三胺在亚最佳Mg2+浓度下或多或少都刺激了多肽合成,但每种三胺产生最大刺激作用所需的Mg2+浓度不同。由3 - 3( norspermidine)、4 - 4(高亚精胺)或4 - 5引起的最大刺激程度与亚精胺的几乎相当。然而,乙酰化亚精胺没有活性,它们抑制了亚精胺刺激的聚苯丙氨酸合成。在聚(U)指导的翻译过程中,许多所研究的三胺降低了亮氨酸与苯丙氨酸掺入多肽的比例,并且这种作用的程度不一定与刺激作用的程度相对应。此外,2 - 4、2 - 5、3 - 3和4 - 4可以像亚精胺一样有效地刺激大肠杆菌多胺营养缺陷型菌株MA 261的生长。然而,3 - 3是唯一一种在促进比MA 261更依赖多胺的突变菌株KK 101生长方面能完全替代亚精胺的三胺。因此,这些结果表明,一些合成三胺在引发这些效应方面与亚精胺一样具有活性,并且在这些效应中三胺的结构要求也存在一些差异。