Can Organophosphates and Carbamates Cause Synergisms by Inhibiting Esterases Responsible for Biotransformation of Pyrethroids?

Hydrolysis catalyzed by general esterases (GEs) is the most efficient route for hydrolyzation of pyrethroid insecticides. Organophosphate (OP) and carbamate (CB) insecticides are known to inhibit GEs in addition to acetylcholinesterase (AChE), which is their main target. We hypothesize that synergies can be induced by OPs and CBs when mixed with pyrethroids, due to their inhibition of GE-dependent detoxification of pyrethroids. To test this hypothesis, we conducted mixture toxicity experiments with Daphnia magna using alpha-cypermethrin (alpha-cyp) in combination with the noninsecticidal OP tetraisopropyl pyrophosphoramide (iso-OMPA) and five AChE inhibitors diazinon, chlorpyrifos, chlorfenviphos, parathion, and aldicarb. In addition, the in vivo GE activity inhibition was measured for all compounds. Up to 10-fold synergy was found between alpha-cyp and iso-OMPA, and the degree of synergy correlated linearly with the inhibition of the GE activity. No synergy, however, was found in any of the insecticide mixtures nor was the GE activity inhibited within the nonlethal concentration range tested. It was concluded that the effect of the insecticides on AChE occurred at lower concentrations than their effect on GEs, making the daphnids become immobilized before any synergistic effects on mortality could be observed. The implications of the findings are discussed from a risk assessment perspective.

Automated summary

The study discussed the importance of hydrolysis catalyzed by esterases for the breakdown of pyrethroid insecticides, as well as the inhibitory effects of organophosphate and carbamate insecticides on esterase activity. The results showed that no synergistic effects were observed within the nonlethal concentration range of the insecticide mixtures, and the inhibition of esterase activity occurred before daphnids showed signs of paralysis.