RESUMO
The bed bug (Cimex lectularius L.) is one of the most prolific and burdensome indoor pests, and suppression of bed bug populations is a global priority. Understanding bed bug behavior is important to the development of new tactics for their control. Major gaps exist in our understanding of how host cues, insecticide resistance, and exposure modality impact the repellency of formulated products to bed bugs. Here, we validate the use of a binary choice olfactometer for assessing bed bug repellency behaviors using N,N-diethyl-3-methylbenzamide (DEET) in a dose-dependent manner, while considering the role of host-associated stimuli (with vs. without CO2), exposure modality (olfactory vs. olfactory and contact), and resistance status (susceptible vs. resistant) on repellency. We observed that host-seeking insecticide-susceptible bed bugs were repelled only when olfactorily exposed to high concentrations of DEET. However, exposure to DEET by contact repelled insecticide-susceptible bed bugs at 100-fold lower dose of DEET. Further, we demonstrate for the first time that insecticide-resistant bed bugs were significantly more responsive to DEET than susceptible bed bugs. We conclude that the 2-choice olfactometer is an effective tool for assessing the behavioral responses of bed bugs to spatial and contact repellents.
Assuntos
Percevejos-de-Cama , DEET , Comportamento de Busca por Hospedeiro , Repelentes de Insetos , Animais , Percevejos-de-Cama/efeitos dos fármacos , DEET/farmacologia , Repelentes de Insetos/farmacologia , Comportamento de Busca por Hospedeiro/efeitos dos fármacos , Olfatometria , FemininoRESUMO
BACKGROUND: The Lone Star tick, Amblyomma americanum is important to human health because of a variety of pathogenic organisms transmitted to humans during feeding events, which underscores the need to identify novel approaches to prevent tick bites. Thus, the goal of this study was to test natural and synthetic molecules for repellent activity against ticks in spatial, contact and human fingertip bioassays. METHODS: The efficacy of essential oils and naturally derived compounds as repellents to Am. americanum nymphs was compared in three different bioassays: contact, spatial and fingertip repellent bioassays. RESULTS: Concentration response curves after contact exposure to 1R-trans-chrysanthemic acid (TCA) indicated a 5.6 µg/cm2 concentration required to repel 50% of ticks (RC50), which was five- and sevenfold more active than DEET and nootkatone, respectively. For contact repellency, the rank order of repellency at 50 µg/cm2 for natural oils was clove > geranium > oregano > cedarwood > thyme > amyris > patchouli > citronella > juniper berry > peppermint > cassia. For spatial bioassays, TCA was approximately twofold more active than DEET and nootkatone at 50 µg/cm2 but was not significantly different at 10 µg/cm2. In spatial assays, thyme and cassia were the most active compounds tested with 100% and 80% ticks repelled within 15 min of exposure respectively and was approximately twofold more effective than DEET at the same concentration. To translate these non-host assays to efficacy when used on the human host, we quantified repellency using a finger-climbing assay. TCA, nootkatone and DEET were equally effective in the fingertip assay, and patchouli oil was the only natural oil that significantly repelled ticks. CONCLUSIONS: The differences in repellent potency based on the assay type suggests that the ability to discover active tick repellents suitable for development may be more complicated than with other arthropod species; furthermore, the field delivery mechanism must be considered early in development to ensure translation to field efficacy. TCA, which is naturally derived, is a promising candidate for a tick repellent that has comparable repellency to commercialized tick repellents.
Assuntos
Amblyomma , Óleos Voláteis , Animais , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Amblyomma/efeitos dos fármacos , Repelentes de Insetos/farmacologia , Humanos , Óleos de Plantas/farmacologia , Óleos de Plantas/química , Ninfa/efeitos dos fármacos , Bioensaio , DEET/farmacologiaRESUMO
To explore novel terpenoid repellents, 22 candidate terpenoid derivatives were synthesized and tested for their electroantennogram (EAG) responses and repellent activities against Aedes albopictus. The results from the EAG experiments revealed that 5-(2-hydroxypropan-2-yl)-2-methylcyclohex-2-en-1-yl formate (compound 1) induced distinct EAG responses in female Aedes albopictus. At concentrations of 0.1, 1, 10, 100, and 1000 mg/L, the EAG response values for compound 1 were 179.59, 183.99, 190.38, 193.80, and 196.66 mV, demonstrating comparable or superior effectiveness to DEET. Repellent activity analysis indicated significant repellent activity for compound 1, closest to the positive control DEET. The in silico assessment of the ADMET profile of compound 1 indicates that it successfully passed the ADMET evaluation. Molecular docking studies exhibited favourable binding of compound 1 to the active site of the odorant binding protein (OBP) of Aedes albopictus, involving hydrophobic forces and hydrogen bond interactions with residues in the OBP pocket. The QSAR model highlighted the influential role of hydrogen-bonding receptors, positively charged surface area of weighted atoms, polarity parameters of molecules, and maximum nuclear-nuclear repulsion force of carbon-carbon bonds on the relative EAG response values of the tested compounds. This study holds substantial significance for the advancement of new terpenoid repellents.
Assuntos
Aedes , Repelentes de Insetos , Animais , Feminino , DEET/farmacologia , Terpenos , Simulação de Acoplamento Molecular , Relação Quantitativa Estrutura-Atividade , Repelentes de Insetos/farmacologia , Repelentes de Insetos/química , Simulação por Computador , CarbonoRESUMO
BACKGROUND: The majority of vector-borne disease cases in the USA are caused by pathogens spread by ticks, most commonly the blacklegged tick, Ixodes scapularis. Personal protection against tick bites, including use of repellents, is the primary defense against tick-borne diseases. Tick repellents registered by the Environmental Protection Agency (EPA) are well documented to be safe as well as effective against ticks. Another group of tick repellent products, 25(b) exempt or minimum risk products, use alternative, mostly botanically derived, active ingredients. These are considered to pose minimal risk to human health and therefore are exempt from EPA registration; efficacy testing is not mandated for these products. METHODS: We used a finger bioassay to evaluate the repellency against I. scapularis nymphs for 11 formulated 25(b) exempt products together with two positive control DEET-based EPA registered products. Repellency was assessed hourly from 0.5 to 6.5 h after product application. RESULTS: The DEET-based products showed ≥ 97% repellency for all examined timepoints. By contrast, an average of 63% of ticks were repelled in the first 1.5 h after application across the 11 25(b) exempt products, and the average fell to 3% repelled between 2.5 and 6.5 h. Ten of the 11 25(b) exempt products showed statistically similar efficacy to DEET-based products at 30 min after application (repellency of 79-97%). However, only four 25(b) exempt products maintained a level of repellency similar to DEET-based products (> 72%) at the 1.5-h mark, and none of these products were effective in repelling ticks at the timepoints from 2.5 to 6.5 h after application. CONCLUSIONS: Neither the claims on the labels nor specific active ingredients and their concentrations appeared to predict the duration of efficacy we observed for the 25(b) exempt products. These products are not registered with the EPA, so the methods used to determine the application guidelines on their labels are unclear. Consumers should be aware that both the level of efficacy and the duration of repellency may differ among unregulated 25(b) exempt repellent products labeled for use against ticks. We encourage more research on these products and the 25(b) exempt active ingredients they contain to help determine and improve their efficacy as repellents under different conditions.
Assuntos
Repelentes de Insetos , Ixodes , Picadas de Carrapatos , Animais , Humanos , DEET/farmacologia , Repelentes de Insetos/farmacologia , Ninfa , Bioensaio/métodosRESUMO
Resumen: Objetivo: Determinar la eficacia de repelentes comerciales disponibles en Yucatán contra el mosquito Aedes aegypti, vector del dengue, Chikungunya y Zika. Material y métodos: Se determinó el tiempo de protección con base en el protocolo WHO/CTD/WHOPES/IC y la NOM-032-SSA2-2014. Resultados: Sólo el repelente con DEET (N, N-dietil-3-metilbenzamida) al 25% cumplió con la protección recomendada. La eficacia fue directamente proporcional a la concentración del DEET; aquéllos con componentes botánicos fueron poco o nada protectores. Conclusiones: Los resultados muestran que los repelentes con DEET proveen protección contra Ae. Aegypti; los repelentes botánicos, incluyendo las pulseras impregnadas, ofrecen nula protección.
Abstract: Objective: We assessed the efficacy of commercial repellents available in Yucatan against Aedes aegypti, vector of dengue, Chikungunya and Zika. Materials and methods: Protection time was determined based on WHO/CTD/ WHOPES/IC y la NOM-032-SSA2-20I4. Results: Products with DEET (N, N-diethyl-3-methylbenzamide) at 25% met the recommended protection. Efficacy was directly proportional to the concentration of DEET; botanicals repellents resulted no protective. Conclusions: Repellents with DEET provided more protection against Ae. aegypti and botanical repellents, including impregnated wristbands, provided no protection.
Assuntos
Humanos , Animais , Feminino , Aedes/efeitos dos fármacos , Preparações de Plantas/farmacologia , DEET/farmacologia , Comportamento Alimentar/efeitos dos fármacos , Mordeduras e Picadas de Insetos/prevenção & controle , Repelentes de Insetos/farmacologia , Pomadas , Fatores de Tempo , Aerossóis , Preparações de Plantas/administração & dosagem , DEET/administração & dosagem , Repelentes de Insetos/administração & dosagem , Repelentes de Insetos/química , MéxicoRESUMO
Casi todos necesitamos en alguna oportunidad un repelente contra insectos, ya sea en un asado al aire libre o en un paseo por bosques o playas. Sin embargo, existe preocupación por la seguridad del empleo de dietiltoluamida (DEET) que es usado en casi todos los productos porque se han comunicado reacciones adversas y la gente tiene miedo de aplicarlos en sus niños. ¿Cuáles son efectivo e inocuos?. Los autores revisan los principales estudios en relación a los repelentes de insectos y proponen recomendaciones para un uso óptimo