Development of neuropeptide analogs capable of traversing the integument: A case study using diapause hormone analogs in Helicoverpa zea

Insect Biochemistry and Molecular Biology
Qi-Rui ZhangDavid L Denlinger

Abstract

Diapause hormone and its analogs terminate pupal diapause in Helicoverpa zea when injected, but if such agents are to be used as effective diapause disruptors it will be essential to develop simple techniques for administering active compounds that can exert their effect by penetrating the insect epidermis. In the current study, we used two molecules previously shown to have high diapause-terminating activity as lead molecules to rationally design and synthesize new amphiphilic compounds with modified hydrophobic components. An assay for diapause termination identified 13 active compounds with EC50's ranging from 0.9 to 46.0 pmol per pupa. Three compounds, Decyl-1963, Dodecyl-1967, and Heptyl-1965, selected from the 13 compounds most active in breaking diapause following injection, also successfully prevented newly-formed pupae from entering diapause when applied topically. These compounds feature straight-chain, aliphatic hydrocarbons from 7 to 12 carbons in length; DH analogs with either a short-chain length of 4 or an aromatic phenethyl group failed to act topically. Compared to a high diapause incidence of 80-90% in controls, diapause incidence in pupae receiving a 10 nmole topical application of Decyl-1963, Dodecyl-1967, o...Continue Reading

References

Jan 1, 1986·Comparative Biochemistry and Physiology. C, Comparative Pharmacology and Toxicology·G M HolmanR J Nachman
Jul 5, 1994·Proceedings of the National Academy of Sciences of the United States of America·P W MaW L Roelofs
Oct 29, 1996·Proceedings of the National Academy of Sciences of the United States of America·R L AbernathyR J Nachman
Sep 24, 2011·Proceedings of the National Academy of Sciences of the United States of America·Qirui ZhangDavid L Denlinger

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