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Biological Activity and Metabolism of Hercules AC-528 Components in Rats and Cockroaches1, 2

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Abstract:

Technical Hercules AC-528 (Delnav) was separated by partition chromatography into eight different fractions. The major Components were the cis and trans isomers of 2,3-p-dioxanedithiol S,S-bis(O,O-diethyl phosphorodithioate). The structure, toxicity to house flies and rats, ant cholinesterase activity and stability to alkaline hydrolysis were studied for these eight Hercules AC-528 components. Radioactive Hercules AC-528 was prepared and the metabolism in rats and cockroaches studied for the cis and trans isomers, 2-p-dioxenethiol S-(O,O-diethyl phosphorodithioate) and bis(diethoxyphosphinothioyl) disulfide. In a wide variety of in vivo and in vitro biological systems the cis and trans isomers were the most stable of the radioactive components; the single exception was a study on hydrolysis by human plasma where the dioxene derivative was the most stable. In a sub-acute feeding study with rats, Hercules AC-528 was found to accumulate to a small degree in fat. However, the residues disappeared rapidly when feeding of Hercules AC-528 was discontinued.

Other factors in investigating Hercules AC-528 included: cholinesterase depression and recovery in rats following administration of a sub-lethal dose; the effect of sub-acute feeding on rat plasma, red blood corpuscle and brain cholinesterase activity; metabolism of the components of Hercules AC-528 by Periplaneta americana (L.) and rat liver slices; the formation of more polar, non-hydrolyzed metabolites from the radioactive components by rats and cockroaches; and the nature of the hydrolysis products formed from the components in human plasma and following oral administration to rats.

Document Type: Research Article

Publication date: February 1, 1959

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  • Journal of Economic Entomology is published bimonthly in February, April, June, August, October, and December. The journal publishes articles on the economic significance of insects and is divided into the following sections: apiculture & social insects; arthropods in relation to plant disease; forum; insecticide resistance and resistance management; ecotoxicology; biological and microbial control; ecology and behavior; sampling and biostatistics; household and structural insects; medical entomology; molecular entomology; veterinary entomology; forest entomology; horticultural entomology; field and forage crops, and small grains; stored-product; commodity treatment and quarantine entomology; and plant resistance. In addition to research papers, Journal of Economic Entomology publishes Letters to the Editor, interpretive articles in a Forum section, Short Communications, Rapid Communications, and Book Reviews.
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