Insect resistance to insecticides

The past 40 years have seen insect resistance to insecticides develop from a scientific curiosity to an immense practical problem that threatens man's ability to control not only the insect pests of agriculture but also the insect vectors that transmit major human and animal diseases. The spread of genes for cross and multiple resistance among insect pests has rendered most of our present insecticides obsolescent and very few novel insecticides are under development as substitutes. The most feasible strategy to maintain adequate control of insect pests is integrated pest management or I P M, in which insecticide management is a useful component. However, much of our present planning for the future of insect control is carried out in ignorance of past failures. We must learn from the past if we are to retain the use of chemical insecticides as a viable component of IPM.     

Effect of disposition on the relative delayed neurotoxicity potency among leptophos analogs

The oxons of leptophos, its desbromo analog, and its ethoxy analog all inhibit hen brain neurotoxic esterase (NTE) to a similar degree in vitro, but have large differences in minimum effective oral doses for organophosphorus-induced delayed neurotoxicity. The potencies of leptophos and ethoxyleptophos are increased 10-fold when administered to hens intravenously (iv), but the potency of desbromoleptophos is nearly the same whether administered iv or po. Leptophos distributes nearly five times more rapidly from the central compartment than does desbromoleptophos, and its attenuated oral potency may be due to slower net absorption and/or dilution by compartments other than nervous tissue. Intravenously administered phenylphosphonothionates are excreted rapidly into the gastrointestinal tract and a large proportion of the dose is eliminated in the first 48 hr. Indirect evidence indicates that ethoxyleptophos is more rapidly degraded and ethoxyleptophos-inhibited NTE recovers more rapidly than does NTE inhibited by leptophos or desbromomleptophos. It is proposed that differential aging of ethoxyleptophos chiral isomers as well as pharmacokinetic factors may contribute to the apparently anomalous behavior of these three analogs.     

Investigations into carbamate insecticide selectivity: I: Evaluation of potential selectophores

In an effort to improve the generally unfavorable mouse/housefly toxicity ratio of most carbamate insecticides, potential selectophores (nitrile, carbamoyl oxime, carboxylic ester, or amide) were incorporated into a series of phenyl N-methylcarbamates. In addition to the insect and mouse toxicity determinations, the anticholinesterase activity of these compounds was determined for purified housefly head acetylcholinesterase and bovine erythrocyte acetylcholinesterase. The presence of these functional groups, in general, did not give enhanced selectivity ratios and, in one case, (o-N-methylcarbamoyloxyiminomethylphenyl N-methylcarbamate), a very unfavorable selectivity ratio of <0.03 was obtained. A mechanism implicating a Beckmann rearrangement is advanced to rationalize the high rodenticidal activity of this molecule. In general, the carbamates showed poor insecticidal activity when applied alone to the housefly, but, when the flies were pretreated with piperonyl butoxide, the compounds were quite toxic. Finally, an explanation is derived which seeks to justify the inability of these potential selectophores to improve the mouse/housefly toxidity ratio.     

Conversion of mesophilic to psychrophilic bacteria

The minimum temperature of growth of the mesophilic bacterium Pseudomonas aeruginosa has been significantly lowered from approximately 11 degrees to 0 degrees C. This shift in the minimum temperature of growth was accompanied by a corresponding decrease in the maximum temperature of growth. Transfer of this genetic characteristic by a transducing phage grown on a psychrophile or by ultraviolet mutagenesis was used to accomplish these shifts in range of growth temperature.     

Production of delayed ataxia by carbamate acid esters

Thirty-eight carbamates and thiocarbamates were evaluated for the production of delayed neurotoxicity in the mature White Leghorn hen. Several thiocarbamates including phenyl-N-ethylthiocarbamate and s-2,3-dichloroallyl diisopropylthiocarbamate (diallate) produced symptoms of severe delayed neurotoxicity following repeated oral administration. The results of these experiments do not preclude the possibility that neurotoxic carbamates and organophosphorous compounds may share a common site of action.