硫代寡核苷酸在小鼠体内脏器生物分布研究

To investigate the organic biodistribution of phosphorothioated oligodeoxynucleotides (PSODN) in mice.PSODN: (5'-CATGCCCCAAAGCCAC-3') targeted to HBVpre-C/C region was synthesized.The PSODN was radiolabeled with 32P at the 5' terminus with T4-polynucleotide Kinase and was injected via the lateral tail vein of mice.Samples of blood were collected and various organs were removed respectively at various time points.Total radioactivity in each sample was measured in a liquid scintillation counter.Plasmal levels of PSODN were rapidly depleted, with a half-life of approximately 1～2 minutes.The liver retained the highest amount of PSODN;At the time point of 30 minute, the degree of redioactivity in organs was as following:Liver>kidney>lung>heart>spleen>brain.PSODN in liver decreased gradually, which was about 2.93% of injected dose at 24 hour.Liver was the satisfied organ for antisense therapy.And the recommended drug injection interval was 24hours.