Abstract
In the era of green economy, trehalase inhibitors represent a valuable chance to develop non-toxic pesticides, being hydrophilic compounds that do not persist in the environment. The lesson on this topic that we learned from the past can be of great help in the research on new specific green pesticides. This review aims to describe the efforts made in the last 50 years in the evaluation of natural compounds and their analogues as trehalase inhibitors, in view of their potential use as insecticides and fungicides. Specifically, we analyzed trehalase inhibitors based on sugars and sugar mimics, focusing on those showing good inhibition properties towards insect trehalases. Despite their attractiveness as a target, up to now there are no trehalase inhibitors that have been developed as commercial insecticides. Although natural complex pseudo di- and trisaccharides were firstly studied to this aim, iminosugars look to be more promising, showing an excellent specificity profile towards insect trehalases. The results reported here represent an overview and a discussion of the best candidates which may lead to the development of an effective insecticide in the future.
Highlights
Insecticides and fungicides have played a fundamental role in raising the quality of our lives, for crop protection in agriculture, and to avoid the spreading of harmful pests causing lethal human diseases, such as malaria
The development of non-toxic environmentally friendly insecticides and fungicides for human health and for crop protection is of particular relevance, especially for less developed countries
Trehalase hydrolyses trehalose to two glucose units, a process which is essential to the life functions of several organisms, in particular fungi and insects, but does not affect vertebrates, who do not depend on the hydrolysis of this sugar
Summary
Insecticides and fungicides have played a fundamental role in raising the quality of our lives, for crop protection in agriculture, and to avoid the spreading of harmful pests causing lethal human diseases, such as malaria. Due to the biological relevance of trehalose and trehalose processing enzymes in pathological and physiological states, in particular for the important role of trehalose-derived glucose in larvae survival and development, trehalase inhibitors have been regarded in recent years as an interesting target for the identification of novel insecticides and fungicides. Several potent trehalase inhibitors were isolated from natural sources These compounds include pseudodisaccharide structures and their glycosyl derivatives containing a sugar or a polyhydroxylated carbocycle (such as validamycins, validoxylamines, salbostatin and trehazolin, see Section 2). This review aims to describe the efforts made in the last 50 years in the evaluation of natural compounds and their analogues as trehalase inhibitors, in view of their potential use as insecticides and fungicides. This review collects the efforts made by the researchers in the evaluation of carbohydrate-, carbocyclic-, and iminosugar-based compounds as trehalases inhibitors of different origins
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