Wang Liya, Schmidl Sebastian R, Stülke Jörg
a Department of Anatomy, Physiology and Biochemistry , Swedish University of Agricultural Sciences, The Biomedical Center , Uppsala , Sweden.
Nucleosides Nucleotides Nucleic Acids. 2014;33(4-6):296-304. doi: 10.1080/15257770.2013.853783.
Mycoplasma pneumoniae (Mpn) is a human pathogen causing acute respiratory diseases and accounts for approximately 30% cases of community-acquired pneumonia. Co-infection with Mycoplasmas compromises the efficacy of anticancer and antiviral nucleoside analog-based drugs due to the presence of Mycoplasma thymidine phosphorylase (TP). In this study, a TP-deficient strain of Mpn was generated in order to study the effect of Mpn TP in the metabolism of nucleoside analogs. Deficiency in TP activity led to increased uptake and incorporation of radiolabeled deoxyuridine and uracil but thymidine uptake was not affected. The activities of enzymes in the salvage of thymidine and deoxyuridine, e.g., thymidine kinase and uracil phosphoribosyltransferase were upregulated in the TP-deficient mutant, which may explain the increased uptake of deoxyuridine and uracil. Thirty FDA-approved anticancer and antiviral nucleoside and nucleobase analogs were used to screen their inhibitory activity toward the TP mutant and the wild type strain. Seven analogs were found to inhibit strongly the growth of both wild type and TP mutant. Differences in the inhibitory effect of several purine analogs between the two strains were observed. Further study is needed in order to understand the mechanism of inhibition caused by these analogs. Our results indicated that TP is not an essential gene for Mpn survival and TP deficiency affects other enzymes in Mpn nucleotide metabolism, and suggested that Mycoplasma nucleotide biosynthesis pathway enzymes are potential targets for future development of antibiotics.
肺炎支原体(Mpn)是一种引起急性呼吸道疾病的人类病原体,约占社区获得性肺炎病例的30%。由于支原体胸苷磷酸化酶(TP)的存在,支原体共感染会降低基于抗癌和抗病毒核苷类似物的药物疗效。在本研究中,为了研究Mpn TP在核苷类似物代谢中的作用,构建了一株TP缺陷型Mpn菌株。TP活性的缺乏导致放射性标记的脱氧尿苷和尿嘧啶的摄取和掺入增加,但胸苷摄取不受影响。在TP缺陷型突变体中,胸苷和脱氧尿苷补救途径中的酶活性,如胸苷激酶和尿嘧啶磷酸核糖基转移酶上调,这可能解释了脱氧尿苷和尿嘧啶摄取的增加。使用30种美国食品药品监督管理局(FDA)批准的抗癌和抗病毒核苷及核苷碱基类似物筛选它们对TP突变体和野生型菌株的抑制活性。发现7种类似物强烈抑制野生型和TP突变体的生长。观察到两种菌株之间几种嘌呤类似物的抑制作用存在差异。为了了解这些类似物引起抑制的机制,还需要进一步研究。我们的结果表明,TP不是Mpn生存所必需的基因,TP缺陷会影响Mpn核苷酸代谢中的其他酶,并表明支原体核苷酸生物合成途径酶是未来抗生素开发的潜在靶点。