The use of biopesticides and related alternative management products is increasing. New tools, including semiochemicals and plant-incorporated protectants (PIPs), as well as botanical and microbially derived chemicals, are playing an increasing role in pest management, along with plant and animal genetics, biological control, cultural methods, and newer synthetics. The goal of this Perspective is to highlight promising new biopesticide research and development (R&D), based upon recently published work and that presented in the American Chemical Society (ACS) symposium "Biopesticides: State of the Art and Future Opportunities," as well as the authors' own perspectives. Although the focus is on biopesticides, included in this Perspective is progress with products exhibiting similar characteristics, namely those naturally occurring or derived from natural products. These are target specific, of low toxicity to nontarget organisms, reduced in persistence in the environment, and potentially usable in organic agriculture. Progress is being made, illustrated by the number of biopesticides and related products in the registration pipeline, yet major commercial opportunities exist for new bioherbicides and bionematicides, in part occasioned by the emergence of weeds resistant to glyphosate and the phase-out of methyl bromide. The emergence of entrepreneurial start-up companies, the U.S. Environmental Protection Agency (EPA) fast track for biopesticides, and the availability of funding for registration-related R&D for biorational pesticides through the U.S. IR-4 program provide incentives for biopesticide development, but an expanded effort is warranted both in the United States and worldwide to support this relatively nascent industry. ABSTRACT: The use of biopesticides and related alternative management products is increasing. New tools, including semiochemicals and plant-incorporated protectants (PIPs), as well as botanical and microbially derived chemicals, are playing an increasing role in pest management, along with plant and animal genetics, biological control, cultural methods, and newer synthetics. The goal of this Perspective is to highlight promising new biopesticide research and development (R&D), based upon recently published work and that presented in the American Chemical Society (ACS) symposium "Biopesticides: State of the Art and Future Opportunities," as well as the authors' own perspectives. Although the focus is on biopesticides, included in this Perspective is progress with products exhibiting similar characteristics, namely those naturally occurring or derived from natural products. These are target specific, of low toxicity to nontarget organisms, reduced in persistence in the environment, and potentially usable in organic agriculture. Progress is being made, illustrated by the number of biopesticides and related products in the registration pipeline, yet major commercial opportunities exist for new bioherbicides and bionematicides, in part occasioned by the emergence of weeds resistant to ...
Insecticide resistance is a growing threat to mosquito control programs around the world, thus creating the need to discover novel target sites and target-specific compounds for insecticide development. Emerging evidence suggests that mosquito inward rectifier potassium (Kir) channels represent viable molecular targets for developing insecticides with new mechanisms of action. Here we describe the discovery and characterization of VU041, a submicromolar-affinity inhibitor of Anopheles (An.) gambiae and Aedes (Ae.) aegypti Kir1 channels that incapacitates adult female mosquitoes from representative insecticide-susceptible and -resistant strains of An. gambiae (G3 and Akron, respectively) and Ae. aegypti (Liverpool and Puerto Rico, respectively) following topical application. VU041 is selective for mosquito Kir channels over several mammalian orthologs, with the exception of Kir2.1, and is not lethal to honey bees. Medicinal chemistry was used to develop an analog, termed VU730, which retains activity toward mosquito Kir1 but is not active against Kir2.1 or other mammalian Kir channels. Thus, VU041 and VU730 are promising chemical scaffolds for developing new classes of insecticides to combat insecticide-resistant mosquitoes and the transmission of mosquito-borne diseases, such as Zika virus, without harmful effects on humans and beneficial insects.
Aedes aegypti and Anopheles gambiae are two mosquito species that represent significant threats to global public health as vectors of Dengue virus and malaria parasites, respectively. Although mosquito populations have been effectively controlled through the use of synthetic insecticides, the emergence of widespread insecticide-resistance in wild mosquito populations is a strong motivation to explore new insecticidal chemistries. For these studies, Ae. aegypti and An. gambiae were treated with commercially available plant essential oils via topical application. The relative toxicity of each essential oil was determined, as measured by the 24-h LD50 and percentage knockdown at 1 h, as compared with a variety of synthetic pyrethroids. For Ae. aegypti, the most toxic essential oil (patchouli oil) was ∼1,700-times less toxic than the least toxic synthetic pyrethroid, bifenthrin. For An. gambiae, the most toxic essential oil (patchouli oil) was ∼685-times less toxic than the least toxic synthetic pyrethroid. A wide variety of toxicities were observed among the essential oils screened. Also, plant essential oils were analyzed via gas chromatography/mass spectrometry (GC/MS) to identify the major components in each of the samples screened in this study. While the toxicities of these plant essential oils were demonstrated to be lower than those of the synthetic pyrethroids tested, the large amount of GC/MS data and bioactivity data for each essential oil presented in this study will serve as a valuable resource for future studies exploring the insecticidal quality of plant essential oils. KeywordsAedes aegypti, Anopheles gambiae, plant essential oil, synthetic pyrethroid, terpene RightsThis article is the copyright property of the Entomological Society of America and may not be used for any commercial or other private purpose without specific permission of the Entomological Society of America. ABSTRACT Aedes aegypti and Anopheles gambiae are two mosquito species that represent significant threats to global public health as vectors of Dengue virus and malaria parasites, respectively. Although mosquito populations have been effectively controlled through the use of synthetic insecticides, the emergence of widespread insecticide-resistance in wild mosquito populations is a strong motivation to explore new insecticidal chemistries. For these studies, Ae. aegypti and An. gambiae were treated with commercially available plant essential oils via topical application. The relative toxicity of each essential oil was determined, as measured by the 24-h LD 50 and percentage knockdown at 1 h, as compared with a variety of synthetic pyrethroids. For Ae. aegypti, the most toxic essential oil (patchouli oil) was $1,700-times less toxic than the least toxic synthetic pyrethroid, bifenthrin. For An. gambiae, the most toxic essential oil (patchouli oil) was $685-times less toxic than the least toxic synthetic pyrethroid. A wide variety of toxicities were observed among the essential oils screened. Also, plant essential oils were ...
BackgroundThe phenolic monoterpenoid carvacrol, which is found in many plant essential oils (thyme, oregano and Alaska yellow cedar), is highly active against pest arthropods, but its mechanisms of action are not fully understood. Here, carvacrol is shown to bind in a membrane preparation containing insect nicotinic acetylcholine receptors (nAChRs).
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