Abstract
The Aedes aegypti mosquito serves as a major vector for viral diseases, such as dengue, chikungunya, and Zika, which are spreading across the globe and threatening public health. In addition to increased vector transmission, the prevalence of insecticide-resistant mosquitoes is also on the rise, thus solidifying the need for new, safe and effective insecticides to control mosquito populations. We recently discovered that cinnamodial, a unique drimane sesquiterpene dialdehyde of the Malagasy medicinal plant Cinnamosma fragrans, exhibited significant larval and adult toxicity to Ae. aegypti and was more efficacious than DEET–the gold standard for insect repellents–at repelling adult female Ae. aegypti from blood feeding. In this study several semi-synthetic analogues of cinnamodial were prepared to probe the structure-activity relationship (SAR) for larvicidal, adulticidal and antifeedant activity against Ae. aegypti. Initial efforts were focused on modification of the dialdehyde functionality to produce more stable active analogues and to understand the importance of the 1,4-dialdehyde and the α,ß-unsaturated carbonyl in the observed bioactivity of cinnamodial against mosquitoes. This study represents the first investigation into the SAR of cinnamodial as an insecticide and antifeedant against the medically important Ae. aegypti mosquito.
Highlights
Mosquitoes are vectors of numerous human pathogens, such as the malaria parasite, dengue virus, chikungunya virus, and Zika virus, which affect over 300 million people annually [1,2,3]
Since the antifeedant and repellent activity of CDIAL are found to be mediated by modulation of a sensory receptor (TRPA1) in the mosquito, we developed a structural model to understand how CDIAL interacts with transient receptor potential A1 (TRPA1) and to explain the difference in activities of CDIAL and the prepared derivatives
Our previous results showed that 1 could effectively kill mosquito larvae in an aqueous environment, penetrate the cuticle of adult female mosquitoes, reduce the feeding of mosquitoes when added to a sucrose solution, and reduce the propensity of mosquitoes to blood feed when dried onto the surface of a membrane feeder
Summary
Mosquitoes are vectors of numerous human pathogens, such as the malaria parasite, dengue virus, chikungunya virus, and Zika virus, which affect over 300 million people annually [1,2,3]. Chikungunya and Zika viruses, both historically limited to parts of Africa and Asia, have recently emerged into global threats with increased transmission in the Americas [4,5]. The arboviruses that cause dengue, Zika, chikungunya and yellow fevers can all be transmitted to humans by the mosquito Aedes aegypti (L.). Vector control strategies remain the primary method to control and prevent the spread of mosquito-borne diseases [8]; control of mosquitoes with insecticides is often the only method proven to reduce vector populations during an emerging epidemic [9]
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