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First insights into insecticidal activity against Aedes aegypti and partial biochemical characterization of a novel low molecular mass chymotrypsin‐trypsin inhibitor purified from Lonchocarpus sericeus seeds 下载免费PDF全文
Luiz CP Almeida Filho Pedro MS Tabosa Denise C Hissa Ilka M Vasconcelos Ana FU Carvalho 《Pest management science》2018,74(6):1362-1373
BACKGROUND
Arboviroses such as dengue, Zika and chikungunya represent a serious public health issue as a consequence of the absence of approved vaccines or specific antiviral drugs against the arboviruses that cause them. One way to prevent these diseases is by combating the vector mosquito, Aedes aegypti (Diptera), which has serine proteases in the midgut. Protease inhibitors are molecules that can block enzyme activity, impairing digestion and nutrition, which can lead to death. Thus, we purified and characterized a novel chymotrypsin‐trypsin inhibitor (LsCTI) from Lonchocarpus sericeus seeds and investigated its effect upon Ae. aegypti egg hatching, larval development and digestive proteases.RESULTS
LsCTI showed a single protein band in sodium dodecyl sulfate–polyacrylamide gel electrophoresis (SDS‐PAGE), and the molecular mass determined by matrix‐assisted laser desorption ionization time‐of‐flight mass spectrometry (MALDI‐TOF‐MS) was 8870.45 Da. Kinetics analyses revealed a noncompetitive type of inhibition and low inhibition constant (Ki) for chymotrypsin (8.24 x 10‐8 m ). The thermal resistance was remarkable, even at 100 °C for 180 min. The inhibitor concentration required for 50‐percent enzyme inhibition (IC50) of LsCTI was 4.7 x 10‐7 m for Ae. aegypti midgut larval enzymes. LsCTI did not affect egg hatchability at 0.3 mg mL‐1, but caused a high larval mortality rate (77%) and delayed development (37%).CONCLUSIONS
LsCTI is a novel protease inhibitor with remarkable biochemical characteristics and is a potential tool to control Ae. aegypti development. © 2017 Society of Chemical Industry2.
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Synthesis and structure–activity relationships of carbohydrazides and 1,3,4‐oxadiazole derivatives bearing an imidazolidine moiety against the yellow fever and dengue vector,Aedes aegypti 下载免费PDF全文
Fatih Tok Bedia Kocyigit‐Kaymakcioglu Alden S Estep Aaron D Gross Werner J Geldenhuys James J Becnel Jeffrey R Bloomquist 《Pest management science》2018,74(2):413-421
BACKGROUND
1,3,4‐Oxadiazole and imidazolidine rings are important heterocyclic compounds exhibiting a variety of biological activities. In this study, novel compounds with oxadiazole and imidazolidine rings were synthesized from 3‐(methylsulfonyl)‐2‐oxoimidazolidine‐1‐carbonyl chloride and screened for insecticidal activities. The proposed structures of the 17 synthesized compounds were confirmed using elemental analysis, infrared (IR), proton nuclear magnetic resonance (1H‐NMR), and mass spectroscopy.RESULTS
None of the compounds showed larvicidal activity at the tested concentrations against first‐instar Aedes aegypti larvae. However, nine compounds exhibited promising adulticidal activity, with mortality rates of ≥80% at 5 µg per mosquito. Further dose–response bioassays were undertaken to determine median lethal dose (LD50) values. Compounds 1 , 2b , 2c , 2d , 2 g , 3b , 3c , 3 g, and 3 h were effective, with typical LD50 values of about 5 ? 10 µg per mosquito against female Ae. aegypti. Compounds 2c (bearing a nitro group on the aromatic ring; LD50 = 2.80 ± 0.54 µg per mosquito) and 3 h ( double halogen groups at 2,4 position on the phenyl ring; LD50 = 2.80 ± 0.54 µg per mosquito) were the most promising compounds.CONCLUSION
Preliminary mode of action studies failed to show consistent evidence of either neurotoxic or mitochondria‐directed effects. Further chemical synthesis within this series may lead to the development of new effective insecticides. © 2017 Society of Chemical Industry5.
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Ranil Waliwitiya Christopher J Kennedy Carl A Lowenberger 《Pest management science》2009,65(3):241-248
BACKGROUND: Aedes aegypti L. is the major vector of dengue fever and dengue hemorrhagic fever. In an effort to find effective tools for control programs to reduce mosquito populations, the authors assessed the acute toxicities of 14 monoterpenoids, trans‐anithole and the essential oil of rosemary against different larval stages of Ae. aegypti. The potential for piperonyl butoxide (PBO) to act as a synergist for these compounds to increase larvicidal activity was also examined, and the oviposition response of gravid Ae. aegypti females to substrates containing these compounds was evaluated in behavioral bioassays. RESULTS: Pulegone, thymol, eugenol, trans‐anithole, rosemary oil and citronellal showed high larvicidal activity against all larval stages of Ae. aegypti (LC50 values 10.3–40.8 mg L?1). The addition of PBO significantly increased the larvicidal activity of all test compounds (3–250‐fold). Eugenol, citronellal, thymol, pulegone, rosemary oil and cymene showed oviposition deterrent and/or repellent activities, while the presence of borneol, camphor and β‐pinene increased the number of eggs laid in test containers. CONCLUSIONS: This study quantified the lethal and sublethal effects of several phytochemical compounds against all larval stages of Aedes aegypti, providing information that ultimately may have potential in mosquito control programs through acute toxicity and/or the ability to alter reproductive behaviors. Copyright © 2008 Society of Chemical Industry 相似文献
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A glycoprotein α‐amylase inhibitor from Withania somnifera differentially inhibits various α‐amylases and affects the growth and development of Tribolium castaneum 下载免费PDF全文
Sainath S Kasar Kiran R Marathe Amey J Bhide Abhijeet P Herwade Ashok P Giri Vijay L Maheshwari Pankaj K Pawar 《Pest management science》2017,73(7):1382-1390
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Electrophysiological and behavioural responses of the tea geometrid Ectropis obliqua (Lepidoptera: Geometridae) to volatiles from a non‐host plant,rosemary, Rosmarinus officinalis (Lamiaceae) 下载免费PDF全文
Zhengqun Zhang Lei Bian Xiaoling Sun Zongxiu Luo Zhaojun Xin Fengjian Luo Zongmao Chen 《Pest management science》2015,71(1):96-104