Abstract

Haedoxan A (HA) is a major active ingredient in the herbaceous perennial plant lopseed (Phryma leptostachya L.), which is used as a natural insecticide against insect pests in East Asia. Here, we report that HA delayed the decay rate of evoked excitatory junctional potentials (EJPs) and increased the frequency of miniature EJPs (mEJPs) on the Drosophila neuromuscular junction. HA also caused a significant hyperpolarizing shift of the voltage dependence of fast inactivation of insect sodium channels expressed in Xenopus oocytes. Our results suggest that HA acts on both axonal conduction and synaptic transmission, which can serve as a basis for elucidating the mode of action of HA for further designing and developing new effective insecticides.

Highlights

  • The herbaceous perennial plant lopseed Phryma leptostachya L., the sole species of the familyPhrymaceae, is widely distributed in the Himalayas, temperate Asia, and northern East America and is traditionally used as a natural insecticide in East Asia [1,2]

  • These findings revealed potential targets of action of Drosophila neuromuscular junction (NMJ) and on voltage‐gated insect sodium channels expressed in Haedoxan A (HA) andXenopus laid aoocytes

  • We investigated the effects of HA on excitatory transmission at the Drosophila NMJ

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Summary

Introduction

The herbaceous perennial plant lopseed Phryma leptostachya L., the sole species of the familyPhrymaceae, is widely distributed in the Himalayas, temperate Asia, and northern East America and is traditionally used as a natural insecticide in East Asia [1,2]. The herbaceous perennial plant lopseed Phryma leptostachya L., the sole species of the family. Since the 1960s, Taniguchi et al [3,4,5] have isolated a series of Phryma lignans with 3,7-dioxabicyclo [3.3.0] octane skeleton, such as phrymarolin I, phrymarolin II, and haedoxan A (HA). HA is the sole ingredient with higher insecticidal activity against the housefly compared with commercial synthetic pyrethroids [5]. Phrymarolin I and II belong to a class of dilignans deprived of the 3-phenyl-2-hydroxymethyl-1, 4-benzodioxane framework of haedoxans and are totally inactive [8,9,10,11,12]. Leptostachyol acetate, whose chemical structure is very similar to those of phrymarolin-I and II, is active against larvae of three different mosquito species [13] and housefly [14]

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