丙磺舒在阿维菌素作用棉铃虫细胞中的增效机制研究

丙磺舒是ABCC转运蛋白抑制剂,用系列浓度阿维菌素和200μmol/L丙磺舒的食物饲喂棉铃虫,检测中肠组织中阿维菌素的含量。结果表明:与单独使用阿维菌素相比,混合使用丙磺舒后阿维菌素在中肠中的平均驻留时间(MRT)增加了13%,消除半衰期(t1/2z)增加了27%,药物峰值提高了2.8倍。细胞活力测定发现,亚致死剂量阿维菌素与400μmol/L丙磺舒混用后,棉铃虫细胞的活力降低了67.1%。表明抑制ABCC转运蛋白可以提高阿维菌素在棉铃虫中肠的驻留能力,提高药物对棉铃虫细胞的毒力。

The Synergism Mechanism of Probenecid on Avermectins Treating Helicoverpa Armigera Cell

Probenecid is inhibitor of ABC transport. In this research, we use artificial feed contain 30 mg/L avermectins and 200 μmol/L probenecid to feed Helicoverpa armigera and detect the content of avermectins in Helicoverpa armigera midgut. The results showed that compared with the using avermectin alone, after mixed with probenecid, the average dwell time (MRT) of avermectins in midgut increased by 13%, the Half-life (t1/2 z) increased by 27%, and Peak concentration increased 2.8 times. It was found that after using combination of sublethal dose avermectins and 400 μmol/L probenecid, Ha cell viability reduced by 67.1% by cell vitality determination. These phenomenon indicated that inhibition of ABC transporters can improve intestinal resident ability of avermectins in the Ha midgut, improve drug toxicity to the cells of Ha.