Evaluation of the Insecticidal Activity of Powders of Ageratum conyzoide L. Leaves and Roots of Securidaca longepedunculata Fresen on the Germination Rate of Cowpea Infected with Callosobruchus maculatus

Cowpea is a vegetable that contributes to food security in Guinea. Despite its importance, more than 30% of its production is lost between harvesting, storage and consumption. The main cowpea pest is Callosobruchus maculatus. The commonly used control strategy is essentially based on chemicals whose use is toxic, expensive and restrictive. In the search for alternatives to chemical control, this work was undertaken to evaluate the insecticidal potential of Ageratum conyzoid leaf powders and Securidaca longepedunculata roots. Powder toxicity and insecticidal efficacy tests were performed separately on groups of 20 Callosobruchus maculatus using 3 doses of Ageratum conyzoid leaf powders and Securidaca longepedunculata roots in jars each containing 100 g cowpea. The mortality of Callosobruchus maculatus and the impact of powders were noted respectively for 96 h and 4 months after infestation. The germination capacity of the treated seeds was assessed at the start of the study. Doses of 1 and 8 g of Ageratum conyzoides leaf powders and Securidaca longepedunculata roots were applied respectively to every 100 g of cowpea and led to 100% mortality of Callosobruchus maculatus. At these same doses, more than half of the treated seeds were attacked during the 4 months of storage. Germination tests have shown that powders of Ageratum conyzoides leaves and roots of Securidaca longepedunculata have no negative effect on the germination power of cowpea seeds. Therefore, they could be considered as excellent bio-insecticides that socio-professional strata (farmers and warehouse workers) can use in the fight against cowpea insects intended for storage.

Synthesis and Insecticidal Activity of Derivants of 3,13-Ester Mesaconitine

[Objective] The experiment aimed to explore the relations between structure of aconitine, aconitine derivatives and insecticide. [Method] The aconitine derivatives such as 3-acetyl mesaconitine, 3-propionyl mesaconitine, 3-acetyl-13-Benzoyl-mesaconitine and 3-propionyl-13-Benzoyl-mesaconitine were synthesized by mesaconitine with acetic anhydride or propionic anhydride and their insecticidal activities were also determined. [Result] When the concentration was 500 mg/L, the insecticidal activities of mesaconitine against Nilaparvata legen and Aphis were 50% and 30% respectively while the insecticidal activities of 3-acetyl mesaconitine, 3-propionyl mesaconitine, 3-acetyl-13-Benzoyl-mesaconitine and 3-propionyl-13-Benzoyl-mesaconitine against Aphis medicagini were 40%, 30%, 30% and 20% respectively at 500 mg/L. [Conclusion] After hydroxyl esterification, the insecticidal activity of mesaconitine was declined and the existence of hydroxyl at 3rd position in mesaconitine played very important influences on insecticidal activity.

Expression, Purification and Insecticidal Activity Analysis of Cry1Ac without Helix α-1

[Objective] This study aimed to analyze the expression, purification and insecticidal activity of Cry1Ac without helix α-1 of domain I in E. coli. [Method] Plasmid of B. thuringiensis HD-1 was used as the template for amplification of Cry1Ac gene, which was linked with pET28a vector to construct the recombinant plasmid. After transformation and IPTG induction, expression of target protein was detected by using SDS-PAGE method. Target protein was extracted and coated on the surface of feed for H. armigera to determine the insecticidal activity. [Result] Cry1Acdela1 gene could normally express the target protein in E. coli. However, the target protein existed in the form of inclusion body. Results of bioassay analysis showed that under the same concentration, fatality rate of activated Cry1Ac toxin reached above 75%, while that of Cry1Acdelα1 was only about 10%. [Conclusion] E. coli-expressed Cry1Acdelα1 had no insecticidal activity against H. armigera.

Diamide derivatives containing a trifluoromethylpyridine skeleton:Design,synthesis,and insecticidal activity

Diamide derivatives are biologically active molecules that have been widely applied in recent years in research on pesticides,especially insecticides.Using a simple and environmentally friendly scheme,a series of new diamide derivatives containing a trifluoromethylpyridine skeleton was designed,synthesized,and confirmed by^(1)H,^(19)F and^(13)C NMR,and HR-MS.Their insecticidal activities against Plutella xylostella and Helicoverpa armigera were measured and the relationship between structure and activity was investigated.Eight of the title compounds(D2,D5,D10,D21,D28,D29,D30 and D33)showed 100%activity against P.xylostella at 500 mg L^(-1).One compound,D33,still showed 100%activity against P.xylostella at 100 mg L^(-1)and had the lowest LC_(50)(lethal concentration 50%,3.7 mg L^(-1))among the synthesized compounds.Molecular docking analysis revealed that D33 could be thoroughly embedded in the active pocket of the ryanodine receptor via hydrogen bonding in a manner similar to the commercial insecticide chlorantraniliprole.

Purification, characterization and evaluation of insecticidal activity of trypsin inhibitor from Albizia lebbeck seeds

A Bowman-Birk inhibitor with activity against gut proteases of Helicoverpa armigera was extracted in 0.I M sodium phosphate buffer from defatted seed flour of Albizia lebbeck. It was purified to 29.62 folds with 51.43% recovery using ammonium sulfate precipitation, gel filtration chromatography on Sephadex G-100 column and ion ex- change chromatography on DEAE-Sephadex As0. The purified protein had a molecular weight of 12,303 daltons as determined by SDS-PAGE. It was found to be heat stable up to 60~C and had two pH optima of 7.5 and 9.0. The inhibitor exhibited non-competitive pattern of inhibition with a low Ki value of 0.2 ~tM. The inhibitoi- was found to be susceptible to varying concentrations of reducing agents like DTT and 2- mercaptoethanol, thereby indicating the role of disulphide bridges in maintaining its three dimensional structure and stability. The purified inhibitor caused mortality and suppressed larval growth ofPieris brassi- cae larvae. It was also found to be effective against gut trypsin extracted from Spodoptera littoralis. The sequence of the genes encoding for such inhibitors can be determined and the genes expressing protease inhibitors can be used in vegetable crops to confer resistance against insect pests and other plant pathogens.

Synthesis,Crystal Structure and Insecticidal Activity of N-(pyridin-2-ylmethyl)-1-phenyl-1,4,5,6,7,8-hexahydrocyclohepta[c]pyrazole-3-carboxamide

The title compound N-（pyridin-2-ylmethyl）- 1-phenyl- 1,4,5,6,7,8-hexahydrocy-clohepta[c]pyrazole-3-carboxamide 5 （C21I-I22N40, Mr = 346.42） has been synthesized andstructurally characterized by IR, 1H NMR, 13C NMR, H RMS and single-crystal X-raydiffraction. The crystal crystallizes in monoclinic system, space group P21/n with a = 8.668（2）,b = 22.236（4）, c = 9.539（2） A, β = 108.68（3）°, V = 1786.4（7）/k3, Z = 4, Dx= 1.288 g/cm3,F（000） = 736,μ（MoKa） = 0.649 mm^-1, the final R = 0.0354 and wR = 0.0933 with 3234observed reflections with I 〉 2σ（/）. The benzene and pyrazole rings are nearly coplanar with adihedral angle of 50.977（46）°. The dihedral angle between the central pyrazole and pyridinerings is 11.688（46）°. No classical hydrogen bonds were found in the molecules. Two adjacentmolecules in crystal packing of compound 5 were linked by two intramolecularhydrogen-bonding interactions C（15）-H（15）…O（1） to generate a stable structure. Compound 5had weak insecticidal activity against the diamondback moth （Plutella xylostella）, butexhibited good activity against cotton bollworm （Helicoverpa armigera）.

Study on Chemical Synthesis and Insecticidal Activity of Peptideκ-CTx-btg02

[Objectives]This study was conducted to investigate the chemical synthesis of peptideκ-CTx-btg02.[Methods]Linear peptideκ-CTx-btg02 was synthesized by solid phase peptide synthesis(SPPS).After oxidation and folding of the linear peptide,mass spectrometry identification and high performance liquid chromatography(HPLC)purification were performed.Then,the MTT method and insect injection method were applied to study its insecticidal activity.[Results]The peptideκ-CTx-btg02 was successfully synthesized by the SPPS method,and identified for the formation of disulfide bonds by mass spectrometry identification,and the purity after HPLC separation was greater than 95%.The MTT experiment showed that the peptideκ-CTx-btg02 could inhibit the growth of insect cells sf9,with a half effective dose of 0.13 nM.The insect injection experiment showed that the peptideκ-CTx-btg02 could effectively kill Tenebrio molitor,with a half lethal dose of 15.6 nM.The results of the electrophysiological experiment showed that 10μM peptideκ-CTx-btg02 had no blocking activity on murine acetylcholineα2β3 andα3β4.Therefore,the peptideκ-CTx-btg02 had a good inhibitory effect on the growth of insect cells,highly effective insecticidal activity and weak mammalian toxicity.[Conclusions]This study lays a foundation for the development of new,safe and efficient peptide biological insecticides.

Insecticidal Activity and Field Efficacy of Novel Insecticide Cyhalodiamide against Different Lepidoptera Pests

[ Objective] The paper was to study the insecticidal activity and field efficacy of cyhalediamide, a novel insecticide developed by Zhejiang Research Institute of Chemical Industry, Ltd. [ Method] Toxicity of cyhalodiamide against Plutella xylostella, Spodoptera exigua, Prodenia litura and Chilo suppressalis were tasted in the laboratory by leaf-dipping method, and the field efficacy of cyhalodiamide against P. xylostella, S. exigua, P. litura, Pieris rapae, C. suppressalis and Cnaphalocrocis medinalis was evaluated. [ Result] The LCs0 values of cyhalodiamide against P. xylostella, S. exigua, P. litura and C. suppressalis were 0. 046, 0.072, 0.071 and 1.95 mg/L, respectively, almost equivalent to that of flubendiamide and ehlorantraniliprole. The control efficacy of 20% Z4042 SC （30 g/hm2） against P. xylostella, S. exigua, P. litura and P. rapae was 90.1% - 96.3 % after spraying for 7 d, and its control efficacy against C. suppressalis and C. medinalis was 82.9% -90.5% after spraying for 15 d. No crop injury was observed at the test dosage. [Conclusion] The study provided reference for field control against Lepidoptera pests.

Insecticidal Activity of Crystals and Spores of Purified Bacillus thuringiensis 00-50-5 Strain against Trichoplusia ni Hubner

[ Objective] The paper was to study pathogenic mechanism and action mode of Bacillus thuringiensis （Bt） 00-50-5 strain against Trichoplusia ni Hub- ner. [Method] The crystals and spores of B. thuringiensis 00-50-5 strain were first isolated and purified, and their insecticidal activities against T. ni were com- pared. [ Result] Either the mixture of pure crystals and pure spores of 00-50-5 strain, or only pure crystals could kill T. n/larvae under the concentration of 100 p.g/mL after 48 h, and the mortality rate reached 100% ; pure spores could not kill the larvae. Determination results of median lethal concentration showed that in- secticidal activity of pure crystal of Bt 00-50-5 strain （LGs0 =0.32 p~/mL） was higher than the mixture of crystals and spores （LCs0 =0.48）, but the insecticidal acti^ty of pure spores was very low （LC50 〉 500.00）. Therefore, the crystals were primarily responsible for causing death of larvae. [ Conclusion] The paper provides theoretical basis for application of Bt 00-50-5 strain.

Insecticidal Activity of Piperine Isolated from Piper sarmentosum

In order to clarify the insecticidal active ingredients of Piper sarmentosum,one active ingredient was isolated from ethanol extract of P. sarmentosum by bioassay-guided fractionation method. Its chemical structures were identified to be piperine by MS,1H NMR,13C NMR. The insecticidal activity of piperine and ethanol extract of P. sarmentosum against Aleurodicus dispels Russell were tested by leaf dip method. The results showed that piperine and ethanol extract of P. sarmentosum exhibited strong insecticidal activity against adults and nymphs of A. dispels; LC50values against adults were 28. 59 and 224. 31 mg/L,and LC50values against nymphs were 65. 91 and 336. 68 mg/L,respectively. There was no significant difference between piperine and azadirachtin against adults and nymphs of A.dispels. Therefore,piperine might be one of the main insecticidal ingredients of P. sarmentosum. In addition,piperine and ethanol extract showed ovicidal activity with different mode of action,piperine reduced the survival rate of newly hatched nymphs while ethanol extract impacted hatch of eggs.

Preparation and Insecticidal Activity of Sea Anemone Peptide AP-GI from Aiptasia pallida

[Objectives] This study was conducted to synthesize sea anemone peptide Ap-GI and investigate its insecticidal activity. [Methods] The linear peptide Ap-GI was synthesized by solid phase peptide synthesis(SPPS), and the linear peptide was subjected to the two-step oxidative folding, mass spectrometry identification and high performance liquid chromatography(HPLC) purification. Then, the MTT method and insect injection method were used to study its insecticidal activity. [Results] The synthesized sea anemone peptide had a purity of 95%. The test results of the MTT method showed that the peptide Ap-GI had the activity of inhibiting the growth of insect cells sf9 with the median effective dose of 0.7 nM;and the test results of the injection method on yellow mealworms showed that the peptide Ap-GI had high insecticidal activity, and the median lethal dose was 16.9 nM. [Conclusions] The sea anemone peptide Ap-GI from Aiptasia pallida has a good inhibitory effect on the growth of insect cells and high-efficiency insecticidal activity, which can lay a foundation for the development of new, safe and efficient peptide biological insecticides.

Preparation of Sea Anemone Peptide Toxin Ap-TxI and Its Insecticidal Activity

[Objectives]This study was conducted to synthesize sea anemone peptide toxin Ap-TxI and investigate its insecticidal activity. [Methods] The sea anemone linear peptide toxin Ap-TxI was synthesized by the solid-phase peptide synthesis(SPPS), and six cysteines were oxidized to form three disulfide bonds by a three-step directional oxidation method. Then, purification by high performance liquid chromatography(HPLC) and mass spectrometry identification were performed. Finally, the insect cytotoxicity and insecticidal activity of Ap-TxI were studied by the MTT method and insect injection method. [Results] The oxidized peptide Ap-TxI with three disulfide bonds in natural configuration was successfully synthesized by the SPPS method, and its purity was >90% by HPLC analysis. The results of the MTT method showed that Ap-TxI was active on the growth of insect cells sf9, with a half effective dose of 0.2 nM;and the results of the mealworm injection test showed that the polypeptide Ap-TxI had high insecticidal activity with a median lethal dose of 11.7 nM. [Conclusions] The sea anemone peptide toxin Ap-TxI with high insecticidal effect was obtained, laying a foundation for the development of new, efficient and safe biological insecticides.

Evaluation of the Insecticidal Activity of the Aerial Part of Pseudocytisus integrifofius （Salisb） Rehder on Grain Borer, Rhyzopertha dominica Fab, （Bostrychidae） and Wheat Weevil, Sitophilus granarius Linn, （Curculionidae）

This study aims to evaluate the potentialities of Pseudocytisus integrifolius （Salisb） Rehder （Brassicaceae） as a botanical insecticide for the protection of stored wheat against two pests of stored grain. The essential oil of Pseudoeytisus integrifolius was tested at different doses on adults of Rhyzopertha dominica Fab. （Bostrychidae） and Sitophilus granarius Linn. （Curculionidae）, at a temperature of 28 ~C and a relative humidity of 75%. This oil has insecticidal activity and gives, for the studied adults, a very significant reduction. The essential oil extracted from Pseudocytisus integrifolius is toxic on Rhyzopertha dominica with LDs0 = 2.61 ~tL/30g grain and LDs0 = 3.99 ~L/30g grain for Sitophilus granarius, the chemical composition analysis shows the richness of the essential oil compounds known for their insecticidal properties as dimethyl disulfide （DMDS） and dimethyl trisulfide explains the results.

Bioactive Compounds and Insecticidal Activity of Hysterionica pinifolia, a Native South American Plant

Phytochemical investigation of the purified fractions of the active dichloromethane extract of Hysterionica pinifolia (Poir.) Baker led to the identification of five compounds. New acetylenic alcohol (E)-undec-3-en-5,7-diyne-1-ol (1) and three other compounds (3), (4), and (5) were reported for the first time in this species. Furthermore, forty-six components from the volatile fraction of H. pinifolia were identified. These compounds were elucidated using 1D and 2D NMR spectroscopy as well as MS-ESI and GC-FID-MS experiments. The dichloromethane extract, its fractions, and the methanolic extract were tested for insecticidal activity against Tribolium castaneum under laboratory conditions. The dichloromethane extract and the fraction F2 were found to be active, showing high larval mortality. The dichloromethane extract was also active against T. castaneum adults. The results have shown that H. pinifolia could be considered, in a near future, as a potential source for the development of a botanical insecticide for pest control.

Insecticidal Activity of the Powders Obtained from the Bauxite Red Mud, Zyzygium aromaticum and Citrus sinensis Peel Extracts on the Conservation of Corn against Sitophilus zeamais: Physicochemical Properties

The remarkable push of technologies increasingly recommends materials for their constructions.Hence the extraction of alumina is for different uses.The exploitation of bauxite pollutes the surrounding areas in this case the discharge of mud wheel.Furthermore,the excessive use of dangerous conventional synthetic insecticides continues to be in circulation in Cameroon despite the known adverse effects.These problems lead us to formulate bio insecticides from rejection of the extraction of alumina and extracts of S.aromaticum and Citrus sinensis which respectively offer us essential oils eugenol and limonene having insecticidal properties against the main insects,pests of corn stocks,Sitophilus zeamais.From the kinetic point of view of the adsorption of the extracts of eugenol,limonene and their association by the red mud,the adsorption curve shows that the Eu/Li mixture(30/70)is better by 0.36 mg/g during the 24 h.The results showed a high toxicity of the Eu-Li binary mixture of ratio 30/70 with respective mortality rates of 95.88%after 8 days of exposure to the concentration of 5 mL/L on the adults of Sitophilus zeamais.The other composites induce an average rate of 80%.The results from the physicochemical analysis of corn before and after treatment with formulated insecticides showed a slight loss in nutritional quality of 14.90%in ash,12.5%in protein,16.14%in lipids and 13.63%in total sugars for 180 days.The powdery formulation from red mud and Eu-Li(30/70)mixture can therefore ensure the protection of corn stocks against Sitophilus zeamais in a farming environment.

Ethnobotanical Investigation of Insecticidal Plants and Evaluation of the Insecticidal Activity of Capsicum chinense on Sitophilus zeamaïs of Maize and Aphis craccivora of Groundnuts: Case of Boffa, BokéRegion (Republic of Guinea)

The present study, which aims to contribute to the valorization of Capsicum chinense, focuses on ethnobotanical investigations and evaluation of insecticidal activity on Sitophilus zeamaïs and Aphis craccivora, as well as the germination power of infected maize and peanut grains treated and not treated with Capsicum chinense leaf powder. To do this, the moisture content of corn and peanuts was determined by the techniques: drying in the sun and in the oven. The insecticidal effect of the powder was tested on maize and peanut kernels infected by the AGRAR (2013) method, followed by a test of the germination potency of these treated grains. The average moisture values of corn and groundnut kernels are 14.51% and 12.25% respectively. The results show, a higher insecticidal efficacy of Capsicum chinense leaf powder on Sitophilus zeamaïs and Aphis craccivora with doses (2, 4 and 8 g). The average germination rates of maize and peanut kernels infected and treated with this powder are: (16.5%;63%;99.5%) and (21.25%;96.5%;99.75%), respectively. This study could be a bio-insecticide alternative for the peasant community in the conservation of cereal and legume products.

Synthesis,insecticidal activity and stability study of novel nitromethylene neonicotinoids with five-membered aromatic heterocycles

Twenty-four novel neonicotinoid analogues with nitromethylene and five-membered aromatic heterocycles were designed and synthesized.All target molecular structures have been confirmed by analytical and spectral data.Some compounds exhibited notable insecticidal activities against aphid(Aphis medicaginis)and brown planthopper(Nilaparvata lugens).The aqueous stability test confirmed that the stabilities of those compounds were superior to the leading compound,and the photostability was even better than that of imidacloprid.

Design, Synthesis and Insecticidal Activity of Novel Anthranilic Diamides Containing Oxime Ester and Diacylhydrazine Moieties

Two series of novel anthranilic diamides containing oxime ester and diacylhydrazine moieties were designed and synthesized.Their structures were characterized by melting points,1H NMR,13C NMR and high resolution mass spectrometry（HRMS）.The single crystal structure of compound 7e was determined by X-ray diffraction and their evaluated insecticidal activity against oriental armyworm（Mythimna separata） indicates that some of the compounds exhibited moderate insecticidal activities.Among the 20 compounds,6a and 6b show 100％ larvicidal activity against Mythimna separate Walker at the test concentration of 100 mg/L.

Synthesis and Insecticidal Activity of Novel N-Pyridylpyrazole Carbonyl Thioureas

A series of novel N-pyridylpyrazole carbonyl thioureas were designed and synthesized. Their structures were characterized by melting points, 1H NMR, IR and elemental analysis or HRMS. The bioassay tests indicated that some of these compounds exhibited moderate insecticidal activity against Mythirnna separata Walker and Culex pipiens pallens. Among 17 compounds, 5n and 5p showed 100% larvicidal activity against Mythimna separata Walker at the test concentration of 100 mg/L.

Syntheses and Insecticidal Activity of Spirocyclic Tetronic Acid Derivatives Containing Oxime Ether Moiety

In order to develop novel spirocyclic tetronic acid lead compounds,a series of new spirocyclic tetronic acid derivatives containing oxime ether moiety was synthesized and bioassayed.The stmctures of 16 target compounds were characterized by lH NMR spectra,13C NMR spectra and high-resolution mass spectrometer(HRMS).Preliminary bioassays indicated that most of the title compounds displayed excellent insecticidal activity against Aphis fabae and Nilapmyata lugens at 100 mg/L.In particular,compound 6k showed the similar activity(LC50=6.87 mg/L)against A.fabae as the spirotetramat(LC50=4.56 mg/L)and had better efIects(LC50=l.64 mg/L)against N.lugens in comparison with spirotetramat(LC5o=7.90 mg/L).The study showed that compound 6k exhibited more promising and broad-spectrum insecticide activity and may serve as a new insecticidal agent for sucking pests.