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制备氚标23-羟基白桦酸(3H-23-HBA),并对其在正常鼠及荷瘤鼠的体内分布进行初步探索。23-HBA经23位氧化、硼氚化钠还原后制得3H-23-HBA,考察了标记物的纯度和稳定性,并在ICR小鼠、接种肝癌HepA肿瘤的小鼠体内研究其生物分布特征。结果显示:(1)所得标记物放射化学纯度>95%,放射性比活度为3.33×105Bq/μg(23-HBA);(2)标记化合物的四氢呋喃溶液在–20℃稳定;(3)小鼠尾静脉注射3H-23-HBA(10mg/kg,3.7×105Bq/只)后,在血中清除慢,血浆中原形药约占60%;(4)小鼠尾静脉注射3H-23-HBA(10mg/kg,3.7×105Bq/只)后,在胆、肝、肠浓聚,消除慢;肿瘤鼠肺、胆中摄取高于正常鼠,尤其是胆,至注射后8h仍高达106.89%±47.4%ID/g。实体瘤与对侧肌肉组织的摄取比约为2。3H-23-HBA纯度高,稳定性好,适用于23-HBA药代动力学研究。
Tritiated 23-hydroxy-betulinic acid (3H-23-HBA) was prepared and its distribution in vivo in normal and tumor-bearing mice was explored. H-23-HBA was prepared by 23-HBA oxidation with sodium trititanate. The purity and stability of the 23-HBA were investigated. The biodistribution of the 23-HBA was studied in ICR mice and mice inoculated with HepA tumor feature. The results showed that: (1) The radiochemical purity of the obtained marker was> 95% and the specific activity of radioactivity was 3.33 × 105Bq / μg (23-HBA); (2) The tetrahydrofuran solution of the labeled compound was stable at -20 ℃; 3H-23-HBA (10 mg / kg, 3.7 × 10 5 Bq / mouse) was injected into the tail vein of mice to clear the blood slowly and accounted for about 60% of the original drug in plasma. (4) 3H-23-HBA (10mg / kg, 3.7 × 105Bq / only), the concentration of gallbladder, liver and intestine was slow and the elimination was slow. The uptake of lung and gall in tumor mice was higher than that of normal mice, especially gall bladder, up to 106.89% ± 47.4% ID / g. Solid tumor and contralateral muscle tissue uptake ratio of about 2.3H-23-HBA high purity, good stability, suitable for 23-HBA pharmacokinetic studies.