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BACKGROUND: The lesser grain borer, Rhyzopertha dominica is a serious pest of stored grains. Fumigation and contact insecticides play a major role in managing this pest globally. While insects are developing genetic resistance to chemicals, hormonal analogues such as s-methoprene play a key role in reducing general pest pressure as well as managing pest populations that are resistant to fumigants and neurotoxic contact insecticides. However, resistance to s-methoprene has been reported in R. dominica with some reports showing a remarkable high resistance, questioning the use of this compound and other related analogues in grain protection. The current study attempts to identify possible molecular mechanisms that contribute in resistance to s-methoprene in R. dominica. RESULTS: Transcriptome analysis of resistant and susceptible strains of this pest species identified a set of differentially expressed genes related to cytochrome P450s, indicating their potential role in resistance to s-methoprene. Laboratory bioassays were performed with s-methoprene treated wheat grains in presence and absence of piperonyl butoxide (PBO), a cytochrome P450 inhibitor. The results indicate that PBO, when applied alone, at least at the concentration tested here, had no effect on R. dominica adult emergence, but has a clear synergistic effect to s-methoprene. The number of produced progeny decreased in presence of the inhibitor, especially in the resistant strain. In addition, we also identified CYP complement (CYPome) of R. dominica, annotated and analysed phylogenetically, to understand the evolutionary relationships with other species. CONCLUSIONS: The information generated in current study suggest that PBO can effectively be used to break resistance to s-methoprene in R. dominica.

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Bed bugs have become a common urban pest with consequences on human health and economic costs to the hotel and tourism sectors. Insecticide resistance is considered an important factor in the current bed bug resurgence, and multiple resistance mechanisms could be working in the resistant bed bug populations. In the present study, we determined the resistance profile to four insecticides with a different mode of action in Cimex lectularius L. (Heteroptera: Cimicidae) field-collected colonies from Argentina. Furthermore, the synergism effect of piperonyl butoxide (PBO) with deltamethrin was investigated to explore the contribution of detoxification metabolism to resistance. Our results showed that most of the field-collected colonies are extremely resistant to deltamethrin and propoxur, much more than to azametiphos and imidacloprid. The differences in resistance ratios among field-collected colonies could be associated with different modes of action of insecticides used in control pest and the mechanisms involved in the resistance. PBO pretreatment led to a significantly decreased RR in pyrethroid-resistant colonies, suggesting an upturn of monooxygenase activity for deltamethrin detoxification. However, the high RR detected could involve other mechanisms as part of the whole resistant phenotype in colonies of C. lectularius resistant to pyrethroids.

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Objective. Due to the importance of controlling ectoparasites, associated with the necessity of technical knowledge on the safety of topical treatment with organophosphates, pyrethroids and piperonyl butoxide to the animal organism, this bioassay was carried out to evaluate the clinical safety of the association of dichlorvos (45%) + cypermethrin (5%) + piperonyl butoxide (25%) administered by spray on the skin of cattle, through the study of clinical parameters, biochemical, haematological and behavioral changes. Materials and methods. Sixteen crossbred animals with a mean age of 18 months, males and females grouped into two treatments with eight animals each: T1 (1:800 v/v) and T2 (1:200 v/v). Were collected blood samples at six different times: before treatment (BT), 24, 48, 72, 96 and 192 hours post treatment (HPT). Results. The antiparasitic association administered by spray on the skin did not result in changes in the enzymatic activity of ALT, AST, GGT and ALP, as well as in serum albumin, triglycerides, cholesterol, urea and creatinine, demonstrating the safety of this antiparasitic compound for maintaining hepatic and renal functionality. The erythrocyte, leukocyte and platelet studies showed no changes caused by treatments, and no clinical signs and behavioral changes were observed after treatment. Conclusions. These findings demonstrated good safety margin for spray treatment on the skin with this antiparasitic compound, even when administered at a dilution of 1:200 v/v, which is four times the dose recommended for ectoparasite control.

Objetivo. Debido a la importancia del control de ectoparásitos en bovinos, asociado a la necesidad de conocimientos técnicos sobre la seguridad del tratamiento tópico con organofosforados, piretroides y butóxido de piperonilo, se realizó este bioensayo para la evaluación de la seguridad clínica de la asociación de diclorvos (45%) + cipermetrina (5%) + butóxido de piperonilo (25%), administrado por aspersión en la piel del ganado bovino, a través del estudio de los parámetros clínicos, bioquímicos, hematológicos y comportamentales. Materiales y métodos. Dieciséis animales entre machos y hembras cruzados con edad media de 18 meses, agrupados en dos tratamientos de ocho animales cada uno: T1 (1:800 v/v) y T2 (1:200 v/v). Fueron colectadas muestras de sangre en seis momentos diferentes: antes del tratamiento (BT), 24, 48, 72, 96 y 192 horas post tratamiento (HPT). Resultados. La asociación antiparasitaria administrada por aspersión en la piel no alteró la actividad enzimática de ALT, AST, GGT y FA, así como la albúmina, triglicéridos, colesterol, urea y creatinina, que demuestra la seguridad de este compuesto antiparasitario en la función renal y hepática. El análisis de eritrocitos, leucocitos y plaquetas no mostraron cambios en los tratamientos, tampoco fueron observados signos clínicos y de comportamiento post tratamiento. Conclusiones. Estos resultados demostraron buen margen de seguridad en el tratamiento por aspersión en la piel con este compuesto antiparasitario, incluso cuando se administra en una dilución de 1:200 v/v, que es cuatro veces la dosis recomendada para el control de ectoparásitos.

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Este estudo avaliou a eficácia antiparasitária da associação de cipermetrina (5%) + diclorvos (45%) + butóxido de piperonila (25%) contra H. irritans em bovinos naturalmente infestados. Para tal, foram utilizados 60 bovinos, fêmeas da raça nelore, com idade média de 50 meses, distribuídos em quatro grupos com 15 repetições cada. Após a randomização dos animais pelo número de moscas, os grupos foram sorteados e constituíram os seguintes tratamentos: T1 = Controle; T2 e T4= Tratados com a associação em estudo nas concentrações de 1:400 e 1:800, respectivamente; T3 = tratados com cipermetrina 15% +clorpirivos 25% + citronela 1% (Controle Positivo) na concentração de 1:800. As contagens de moscas foram efetuadas 3, 7, 14 e 21 dias após o tratamento (DPT). No terceiro DPT, os tratamentos T2, T3 e T4 apresentaram eficácia acima de 98%. No sétimo DPT, verificou-se nos animais tratados com a associação contendo butóxido de piperonila eficácia de 95,61 e 97,3% no controle de moscas nas doses de 1:800 e 1:400, respectivamente. Enquanto, bovinos do grupo T3 demonstraram eficácia de 93,82%. A eficácia antiparasitária permaneceu acima de 95% no 14° DPT em ambos os grupos T2 e T4. Neste mesmo dia experimental, bovinos do grupo T3 apresentaram eficácia de 88,24%. No 21° DPT, apenas o grupo T2 apresentou diminuição significativa (P<0,05) no número de moscas quando comparado aos demais tratamentos. Portanto, verificou-se neste estudo, o efeito sinergista do butóxido de piperonila sobre a atividade antiparasitária de piretróides e organofosforados, justificando o emprego terapêutico desta associação como uma alternativa eficaz em programas sanitários dos bovinos para controle da mosca dos chifres.

This study evaluated the effectiveness of cypermethrin (5%) associated to Dichlorvos (45%) and piperonyl butoxide (25%) against Haematobia irritans in naturally infested cattle. 60 Nelore females, aging about 50 months, were separated into four groups with 15animals each. After randomization by the number of flies, the groups were divided in the following treatments: T1 = control, T2 and T4 = treated with the association under study at concentrations of 1:400 and 1:800, respectively, T3 = treated with cypermethrin 15% + clorpirivos 25% + citronella 1% (positive control) at a concentration of 1:800. Counst of flies were taken 3, 7, 14 and 21 days post treatment (DPT). In the third DPT, treatments T2, T3 and T4 showed efficacy over 98%. At the seventh day, it was found in animals treated with the compound containing piperonyl butoxide efficacy of 95.61 and 97.3% in the control of flies at dose of 1:800 and 1:400, respectively. While cattle in the T3 group demonstrated efficacy of 93.82%. The effectiveness of antiparasitic remained above 95% at 14 ° DPT in both groups T2 and T4. In the same experimental day, animals of group T3 showed effectiveness of 88.24%. At 21 ° DPT, only the T2 group, was significantly decreased (P <0.05) in the number of flies when compared to other treatments. Therefore, it was found in this study, the synergistic effect of piperonyl butoxide on the antiparasitic activity of synthetic pyrethroids and organophosphates, representing an effective alternative in the chemotherapy control by the parasitism for horn flies in cattle.

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Foi avaliada, no presente estudo, a toxicidade de amidas análogas à piperina utilizando-se larvas de 3° instar de Ascia monuste orseis Godart e Spodoptera frugiperda (J.E. Smith). Os bioensaios consistiram na aplicação tópica de 0.5 æl das seguintes amidas: N-isopentil-(3,4-metilenodioxifenil)-amida, N-isopropil-(3,4-metilenodioxifenil)-amida, N-hexil-3-(3,4-metilenodioxifenil)-amida e butóxido de piperonila. Os valores de DL50 (mg i.a./ mg larva) das amidas N-isopropil e N-hexil para A. monuste foram 0.278 e 0.004, respectivamente; para S. frugiperda foram: 1.359 e 0.613, respectivamente. O maior valor das inclinações das curvas de dose-resposta dentre os compostos, para ambas as espécies de inseto foi obtido para N-isopropil, o que indica maior homogeneidade de resposta a esse produto. N-isopropil foi o composto que se mostrou mais promissor como inseticida pois foi mais tóxico a ambas espécies-praga investigadas.

The objective of this study was to evaluate the toxicity piperine amide analogs to 3rd-instar larvae of Ascia monuste orseis Godart and Spodoptera frugiperda (J.E. Smith). The bioassays were based on the topical application of 0.5 æl of the following amides: N-isopenthyl-(3,4-metilenodioxiphenyl)-amide, N-isopropyl-(3,4-metilenodioxiphenyl)-amide, N-hexyl-3-(3,4-etilenodioxiphenyl)-amide and piperonyl butoxide. The DL50 (mg a.i./ mg larva) values of the amides N-isopropyl e N-hexyl to A. monuste orseis were 0,278 and 0,004, respectively, and to S. frugiperda were 1.359 and 0.613, respectively. The steeper slopes of the dose-response curves for both species were obtained with N-isopropyl, indicating the higher homogeneity of response of the pest species studied to this compound. N-isopropyl was also the most promising piperine synthetic analog as insecticide agent among the compounds studied because it was the most toxic amide to both insect-pest species.