Skin irritation has been reported to be the main adverse effect of excessive use of N,N-diethyl-m-toluamide (DEET) and ethyl 3-acetyl(butyl)amino (IR3535) commercial repellents. Therefore, there is an interest in alternatives of natural origin such as essential oils (EOs) and major compounds, which have repellent effects but have no contraindications. The main purpose of the present study was to identify the repellent effect of selected terpenes on Aedes aegypti Linnaeus, 1762 (Diptera: Culicidae) by in silico analysis based on their affinity with the odorant protein AaegOBP1. The protein-metabolite interactions in 20 terpenes were analyzed using the SwissDock tool. Terpenes presenting the highest affinity compared with commercial repellents were selected to evaluate repellent activity at concentrations 0.1, 10, and 25% against Ae. aegypti. Different periods (0–2, 2–15, 15–60 min) were evaluated with DEET as a positive control. The toxicity of terpenes was verified through Osiris and Molinspiration Cheminformatics Software, and cytotoxicity assays in Vero and HepaRG cells were performed using the MTT method. Two formulations were prepared with polyethylene glycol to evaluate skin long-lasting in vivo assay. The results showed four terpenes: geranyl acetate, nerolidol, α-bisabolol, and nerol, with affinity to AaegOBP1 comparable with DEET and IR3535. Geranyl acetate, nerolidol, and their mixtures showed no cytotoxicity and protection percentages close to 100% during the test at concentrations 10 and 25%. Long-lasting assays with geranyl acetate and nerolidol formulate showed 3 h as maximum protection time with 100% protection percentage. These metabolites and their mixtures are candidates to repellent formulations with times and protection percentages similar to DEET.
Mosquito borne diseases are on the rise because of their fast spread worldwide and the lack of effective treatments. Here we are focusing on the development of a novel anti-malarial and virucidal agent with biocidal effects also on its vectors. We have synthesized a new quinoline (4,7-dichloroquinoline) derivative which showed significant larvicidal and pupicidal properties against a malarial and a dengue vector and a lethal toxicity ranging from 4.408 µM/mL (first instar larvae) to 7.958 µM/mL (pupal populations) for Anopheles stephensi and 5.016 µM/mL (larva 1) to 10.669 µM/mL (pupae) for Aedes aegypti. In-vitro antiplasmodial efficacy of 4,7-dichloroquinoline revealed a significant growth inhibition of both sensitive strains of Plasmodium falciparum with IC50 values of 6.7 nM (CQ-s) and 8.5 nM (CQ-r). Chloroquine IC50 values, as control, were 23 nM (CQ-s), and 27.5 nM (CQ-r). In vivo antiplasmodial studies with P. falciparum infected mice showed an effect of 4,7-dichloroquinoline compared to chloroquine. The quinoline compound showed significant activity against the viral pathogen serotype 2 (DENV-2). In vitro conditions and the purified quinoline exhibited insignificant toxicity on the host system up to 100 µM/mL. Overall, 4,7-dichloroquinoline could provide a good anti-vectorial and anti-malarial agent.
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