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目的研究蝶酸(pterinacid,PTA)对天然蓖麻毒素(ricin)及重组蓖麻毒素A链蛋白(rRTA)的拮抗作用。方法用无细胞体系中荧光素酶合成抑制实验和体外细胞毒性实验评价PTA对全分子ricin和rRTA的拮抗效果。结果PTA在两种体系中均显示出了对ricin和rRTA的拮抗作用,且呈剂量依赖性。结论利用PTA作为小分子探针,建立了针对ricin/RTA小分子抑制剂的体外生物学评价系统,为以后用于拮抗ricin/RTA的全新小分子化合物筛选奠定了基础。
Objective To investigate the antagonistic effect of pterinacid (PTA) on natural ricin and recombinant ricin A chain protein (rRTA). Methods The antitumor effects of PTA on ricin and rRTA were evaluated by luciferase inhibition assay and in vitro cytotoxicity assay in cell-free system. Results PTA showed antagonism of ricin and rRTA in both systems in a dose-dependent manner. Conclusion The in vitro biological evaluation system targeting ricin / RTA small molecule inhibitors was established using PTA as a small molecule probe, which laid the foundation for the screening of novel small molecule compounds for antagonizing ricin / RTA in the future.