Evaluation of (–)-borneol derivatives against the Zika vector, Aedes aegypti and a non-target species, Artemia sp.

Abstract

Zika, dengue, and chikungunya are vector-borne diseases of pronounced concern transmitted by the mosquito Aedes aegypti Linn. (Diptera: Culicidae). The most important method to avoid outbreaks is to control mosquito spreading by the employment of insecticides and larvicides. Failure to control mosquito dispersal is mostly accounted to Ae. aegypti resistance to currently available larvicides and insecticides, encouraging the development of novel pesticides. In addition, the excessive use of larvicides poses serious threats to human health and the environment. Evaluation of natural products as larvicides in an attempt to overcome this situation is often found in the literature because products originated from nature are considered less toxic to non-target species and more eco-friendly. (–)-Borneol is a bicyclic monoterpene present in essential oils with moderate larvicidal activity. On account of these facts, it was of our interest to synthesize (–)-borneol ester derivatives aiming to study its structure-activity relationships against Ae. aegypti larvae. With the goal to estimate toxicity to a non-target species, evaluation of the lethal concentration 50% (LC₅₀) on Artemia sp. (Artemiidae) and calculation of selectivity towards Ae. aegypti were carried out. The most potent derivative, (–)-Bornyl chloroacetate, exhibited the highest suitability index, demonstrating lower environmental toxicity than other borneol ester derivatives. A parabolic relationship between (–)-borneol esters larvicidal activity and partition coefficient (Log P) was achieved and a correlation equation obtained, validating the importance of lipophilicity to the larvicidal activity of these compounds.

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