有機リン剤抵抗性イエバエに対するサリゲニン環状リン酸エステル類の作用機構
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概要
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Salithion, one of saligenin cyclic phosphates (SCPs) was effective against organophosphorus (OP)-resistant houseflies. The synergism of some non-insecticidal SCPs, K-1 and K-2, with fenitrothion was found in the resistant strains. One of the OP-selection was the alteration of acetylcholinesterase (AChE) to be insensitive against the oxon-type of OPs, and the insensitive AChE had low affinity with OP-oxons, whereas salioxon had a high inhibitory activity for the enzyme of the resistant insects. On the other hand, the OP-selection also increases high activities of detoxifying enzymes, including glutathione transferase (GSH-t), which also catalyzed the demethylation of fenitrothion. Salithion was stable against the biodegradation. Moreover, SCPs inhibited the degradation of fenitrothion. Both the demethylation of fenitrothion and the glutathione (GSH) conjugation of 1-chloro-2, 4-dinitrobenzene were inhibited by the GSH conjugate of SCPs, i.e., S-(2-hydroxybenzyl)glutathione, in a manner of competition with GSH. SCPs inhibited the GSH-t directly and irreversibly in the absence of GSH. In conclusion, SCPs play significant role as effective inhibitors on the important points of OP-resistant mechanisms, AChE and GSH-t, in different mode, that is, a phosphorylation and an alkylation. These actions are considered to contribute to the biological activities of SCPs, i.e., the high insecticidal potency of salithion against OP-resistant insects and the synergistic effect of K-1 and K-2 with some OPs.
- 日本農薬学会の論文
- 1991-08-20
著者
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