Insect detoxifying enzymes: their importance in pesticide synergism and resistance.

Pyrethroid esterases of Trichoplusia ni, Spodoptera littoralis and Bemisia tabaci hydrolyze the trans-isomers of various pyrethroids more extensively than the cis-isomers. Profenofos fed to T. ni larvae at a level inhibiting the gut pyrethroid esterases by 65% with trans-permethrin and of 95% with cis-cypermethrin increased the toxicity of topically applied trans-permethrin by fourfold and cis-cypermethrin by 20-fold. Similar assays with S. littoralis resulted in an increase of about threefold in the toxicity of both compounds. Monocrotophos, profenofos, acephate, and methidathion inhibited pyrethroid esterase activity in B. tabaci and synergized considerably the toxicity of cypermethrin. The remarkable tolerance of the predator Chrysopa carnea to pyrethroids is attributed to the presence of a high level of pyrethroid esterase activity with a unique specificity for hydrolyzing the cis-isomer. Phenyl saligenin cyclic phosphonate, a potent inhibitor for larval pyrethroid esterases synergized the toxicity of trans-permethrin by 68-fold from an LD50 of 17,000 micrograms/g to 250 micrograms/g. In contrast, oxidase inhibitors such as piperonyl butoxide, SV-1, and MPP synergized considerably the toxicity of pyrethroids in Tribolium castaneum and Musca domestica. Hence the predominant pathway for pyrethroid detoxification in insects, whether hydrolytic or oxidative, depends largely on the insect species. The high toxicity of the recent developed acylureas results from their high retention in the insects. Assays using radiolabeled diflubenzuron and chlorfluazuron applied to fourth instar T. castaneum larvae revealed a rapid elimination of diflubenzuron (T1/2 approximately equal to 7 h) as compared with chlorfluazuron (T1/2 > 100 h). Addition of 100 ppm DEF to the diet increased both the retention time and the toxicity of diflubenzuron in both T. castaneum and S. littoralis, which was due probably to the inhibition of diflubenzuron hydrolase activity. Esterases, hydrolyzing pyrethroids, and acylureas may serve as tools for evaluating potential synergists and for monitoring resistance in various agricultural pests due to increased metabolism.