el Kouni M H, Naguib F N
Division of Biology and Medicine, Brown University, Providence, RI 02912.
Int J Parasitol. 1990 Feb;20(1):37-44. doi: 10.1016/0020-7519(90)90170-r.
Adult Schistosoma mansoni can utilize radiolabelled cytidine, uridine, uracil, orotate, deoxycytidine and thymidine for the synthesis of its nucleic acids. In this respect, cytidine is the most efficiently utilized pyrimidine precursor. Cytosine, thymine and orotidine are transported into the parasites but not metabolized. High performance liquid chromatography analysis of the nucleobase, nucleoside and nucleotide pools from in vivo metabolic studies and assays of enzyme activities in cell-free extracts indicate the presence of nucleoside and nucleotide kinases which phosphorylate the various nucleosides to their respective nucleoside mono-, di- and triphosphates. Uridine, thymidine and deoxyuridine can also be cleaved to their respective nucleobases by uridine phosphorylase. Uracil can be converted directly to UMP by orotate phosphoribosyltransferase or by the sequential actions of uridine phosphorylase and uridine kinase. Nucleoside 5'-monophosphates were dephosphorylated by active phosphohydrolases. All enzymes tested were found in the cytosol fraction with the exception of the phosphohydrolases which were associated mainly with the particulate fraction. No deamination of cytosine, cytidine, deoxycytidine, CMP or dCMP was detected either in vivo or in vitro. The active metabolism of cytidine and absence of deamination and phosphorolysis of cytidine derivatives in schistosomes raise the possibility of using cytidine analogues for the selective treatment of schistosomiasis.
成年曼氏血吸虫能够利用放射性标记的胞苷、尿苷、尿嘧啶、乳清酸、脱氧胞苷和胸苷来合成其核酸。在这方面,胞苷是利用效率最高的嘧啶前体。胞嘧啶、胸腺嘧啶和乳清苷被转运到寄生虫体内但不参与代谢。对体内代谢研究中的核碱基、核苷和核苷酸库进行高效液相色谱分析,以及对无细胞提取物中的酶活性进行测定,结果表明存在核苷和核苷酸激酶,它们可将各种核苷磷酸化为各自的核苷一磷酸、二磷酸和三磷酸。尿苷、胸苷和脱氧尿苷也可被尿苷磷酸化酶裂解为各自的核碱基。尿嘧啶可通过乳清酸磷酸核糖基转移酶直接转化为UMP,或通过尿苷磷酸化酶和尿苷激酶的顺序作用转化为UMP。核苷5'-单磷酸被活性磷酸水解酶去磷酸化。除主要与颗粒部分相关的磷酸水解酶外,所有测试的酶均存在于胞质溶胶部分。在体内或体外均未检测到胞嘧啶、胞苷、脱氧胞苷、CMP或dCMP的脱氨基作用。血吸虫中胞苷的活跃代谢以及胞苷衍生物不存在脱氨基和磷酸解作用,这增加了使用胞苷类似物选择性治疗血吸虫病的可能性。