ABSTRACT

The focus of the staged work was radiolabelled 5,7,3ʹ, 4ʹ tetra-hydroxy flavone (Luteolin), isolated from Plantago lanceolata L., (F. Plantaginaceae), with ^99mtechnetium (^99mTc) to produce a natural tracer ^99mTc-Luteolin (^99mTc-Lut), and to evaluate the biological distribution in silico and in vivo. Labeling was carried out by reduction reaction using SnCl₂ as reducing agent giving a maximum radiochemical yield (RCY) up to 97% at 40°C, pH4, for 30 min., with concentration of ^99mTc and Luteolin of 150 μL. The tracer (^99mTc-Lut) showed 12 h., in vitro stability. In silico ADMET screening of ^99mTc-Lut indicated its high bioavailability in all body organs. The bio-distribution profile indicating the highly uptake of the tracer ^99mTc-Lut, in tumor mice target/non-target ratio (T/NT) up to two-fold compared to normal mice, whereas the clearance from mice was observed via both renal and feces pathway. ^99mTc-Lut, could be valued as a probable natural radiopharmaceutical tracer for tumor appearance.

摘要

分阶段研究的重点是放射性标记的5,7,3ʹ，4ʹ四羟基黄酮（木犀草素），该植物从车前草（F. Plantaginaceae）中分离出来，并带有^99m tech（^99m Tc）以产生天然示踪剂^99m Tc -木犀草素（^99m Tc-Lut），并评估在计算机和体内的生物分布。通过使用SnCl ₂作为还原剂的还原反应进行标记，在40°C，pH4的条件下，在^99m Tc的浓度和150μL的木犀草素的作用下，最大放射化学产率（RCY）高达97％。示踪剂（^99m Tc-Lut）在体外显示12小时稳定。在计算机上对^99m Tc-Lut进行ADMET筛查表明其在所有身体器官中的生物利用度较高。生物分布图表明示踪剂^99m Tc-Lut在肿瘤小鼠中的靶标/非靶标比率（T / NT）的摄取高达正常小鼠的两倍，而从小鼠中清除则通过两种肾脏和粪便途径。^99m Tc-Lut，可能被视为可能用于肿瘤外观的天然放射性药物示踪剂。