Chemical insecticides targeting the digestive system of diamondback moth (DBM), Plutella xylostella, have not been developed.  The discovery of an insecticide with novel mode of action is a challenge for the control of DBM.  In this study, a class of selenium- and difluoromethyl-modified azoles (fluoroazole selenoureas, FASU) were designed and synthesized for the control of DBM.  Of these azoles, compound B4 showed the highest insecticidal activity against DBM.  The LC₅₀ of third- and second-instar larvae reached 32.3 and 4.6 μg mL^–1, respectively.  The midgut tissue of larvae was severely disrupted, and the larval intestinal tissue was dotted with unique red spots after treatment with compound B4.  Compound B4 led to disintegration of the peritrophic matrix, swelling of the midgut epithelium, fracture of the microvilli, and extensive leakage of cellular debris in the midgut lumen.  Surviving larvae grew very slowly, and the larval duration was significantly prolonged after exposure to compound B4 at sublethal doses (LC₁₀, LC₂₅ and LC₅₀).  Furthermore, the pupation rate, emergence rate and pupae weight were significantly decreased.  Compound B4 also induced abnormal pupae, causing adults to be trapped in the cocoon or failure to fly due to twisted wings.  These results demonstrated that FASU could reduce the population of DBM in sublethal doses.  FASU is the first synthetic insecticidal lead compound that has been shown to disrupt the midgut tissue of the larvae of DBM, and its mode of action totally differs from that of commercial chemical insecticides.

The acetylcholinesterase 2 (AChE2) cloned from Plutella xylostella was first successfully expressed in methylotrophic yeast Pichia pastoris GS115.  One transformant with high-level expression of the recombinant AChE (rAChE, 23.2 U mL^–1 in supernatant) was selected by plating on increasing concentrations of antibiotic G418 and by using a simple and specific chromogenic reaction with indoxyl acetate as a substrate.  The maximum production of rAChE reached about 11.8 mg of the enzyme protein per liter of culture.  The rAChE was ?rst precipitated with ammonium sulfate (50% saturation) and then puri?ed with procainamide af?nity column chromatography.  The enzyme was puri?ed 12.1-fold with a yield of 22.8% and a high speci?c activity of 448.3 U mg^–1.  It was sensitive to inhibition by methamidophos and pirimicarb, the calculated 50% inhibitory concentration (IC₅₀) values of the two pesticides were 0.357 and 0.888 mg L^–1, respectively, and the calculated 70% inhibitory concentration (IC₇₀) values were 0.521 and 0.839 mg L^–1, respectively.  The results suggested that it has a potential application in the detection of pesticide residues.

Insecticidal activities of the petroleum ether-, chloroform-, ethyl acetate-, and water-soluble fractions of the methanolicextract of Ficus sarmentosa var. henryi were assayed against Musca domestica adults. The chloroform- and ethyl acetatesolublefractions were the most active with 92.6 and 88.9% mortalities (24 h after treatment) respectively. Therefore, thetwo fractions were combined and four compounds, isolated from the fractions by activity-guided fractionation, wereelucidated as 7-hydroxycoumarin, apigenin, eriodictyol, and quercetin by spectroscopic method and displayed excellentinsecticidal activities against adults of M. domestica and 4th instar larva of Aedes albopictus. Among those, 7-hydroxycoumarin showed the strongest insecticidal activities with lethal concentrations (LC50) values of 72.13 μg g-1sugar and 4.87 μg mL-1 (48 h after treatment) against the test insects respectively. The cytoxicities of these compounds onBTI-Tn-5B1-4 cell were also investigated for the insecticidal mechanism and found that quercetin represented superiorinhibitory activity with MTT assay and reactive oxygen species (ROS) against BTI-Tn-5B1-4 cell, but slightly weaker thanthat of the positive control (azadirachtin) and significantly greater than the negative control (DMSO only). Meanwhile,eriodictyol demonstrated the strongest effect on the mitochondrial membrane potentials (MMP). In conclusion, based ontheir comparative toxicities to commercial insecticides and their cytotoxic effects, some of the compounds from theF. sarmentosa have potential as botanical insecticides.