在黑腹果蝇抗毒扁豆碱品系中，对氨基甲酸酯抑制剂硫酸毒扁豆碱的体外乙酰胆碱酯酶抑制作用的研究。

An investigation of the in vitro inhibition of acetylcholinesterase by the carbamate inhibitor eserine sulphate in eserine resistant strains of Drosophila melanogaster.

Burnell A M, Wilkins N P

Biology Department, St Patrick's College, Maynooth, Co. Kildare, Ireland.

Comp Biochem Physiol C Comp Pharmacol Toxicol. 1988;90(1):215-20. doi: 10.1016/0742-8413(88)90122-3.

Abstract

The kinetics of inhibition of AChE by the carbamate inhibitor eserine sulphate were investigated in five resistant strains of Drosophila melanogaster. 2. The dissociation constant (Kd) was higher and the carbamylation constant was lower relative to the control in four of these. 3. No change was observed in the decarbamylation constants (k3) of the five strains. 4. The Vmax of AChE was higher in the five resistant stocks than in the Canton-S/TM2 controls but no change in the Km of AChE for acetylthiocholine was observed. No electrophoretic variants of AChE were detected. 5. No increase in the activity of nonspecific esterases was detected in the resistant lines. 6. These results indicate that resistance to eserine sulphate may occur in D. melanogaster by a reduction in affinity of AChE for the inhibitor.

摘要

在五个黑腹果蝇抗性品系中研究了氨基甲酸酯抑制剂硫酸毒扁豆碱对乙酰胆碱酯酶（AChE）的抑制动力学。2. 其中四个品系相对于对照，解离常数（Kd）更高，氨甲酰化常数更低。3. 五个品系的脱氨甲酰化常数（k3）未观察到变化。4. 五个抗性品系中AChE的Vmax高于Canton-S/TM2对照，但未观察到AChE对乙酰硫代胆碱的Km有变化。未检测到AChE的电泳变体。5. 在抗性品系中未检测到非特异性酯酶活性增加。6. 这些结果表明，黑腹果蝇对硫酸毒扁豆碱的抗性可能是由于AChE对抑制剂的亲和力降低所致。