Methoprene, a juvenile hormone （JH） analog, is a widely used insecticide that also accelerates behavioral development in honey bees （Apis mellifera）. JH regulates the transition from nursing to foraging in adult w...Methoprene, a juvenile hormone （JH） analog, is a widely used insecticide that also accelerates behavioral development in honey bees （Apis mellifera）. JH regulates the transition from nursing to foraging in adult worker bees, and treatment with JH or methoprene have both been shown to induce precocious foraging. To determine how methoprene changes honey bee behavior, we compared JH titers ofmethoprene-treated and untreated bees. Behavioral observations confirmed that methoprene treatment significantly increased the number of precocious foragers in 3 out of 4 colonies. In only 1 out of 4 colonies, however, was there a significant difference in JH titers between the methoprene- treated and control bees. Further, in all 4 colonies, there was no significant differences in JH titers between precocious and normal-aged foragers. These results suggest that methoprene did not directly affect the endogenous JH secreted by corpora allata. Because methoprene caused early foraging without changing workers＇ JH titers, we conclude that methoprene most likely acts directly on the JH receptors as a substitute for JH.展开更多
Allatostatins （ASTs）, a family of insect neuropeptide, can inhibit juvenile hormone （JH） biosynthesis by the corpora allata （CA） in Diploptera punctata, and therefore be regarded as potential leads for the disco...Allatostatins （ASTs）, a family of insect neuropeptide, can inhibit juvenile hormone （JH） biosynthesis by the corpora allata （CA） in Diploptera punctata, and therefore be regarded as potential leads for the discovery of new insect growth regulators （1GRs）. But several shortcomings, such as their sensitivity to peptidases and high cost, impeded their practical application in pest management. In order to discover new IGRs, one AST analog B1 possessing non-peptide group was discovered with high ability to inhibit JH biosynthesis in vitro （IC50： 0.09 μmol/L） in our previous studies. In the present work, two series of B1 analogs with different substituents on the N-terminus region were designed and synthesized. The result suggested that benzene showed better activity than other heterocycles, and the para-substitution on the benzene was beneficial for activity. Moreover, analogs with logP value over 2.0 exhibited good activity, which indicated the hydrophobicity is important to the bioactivity. Three dimension quantitative structure-activity relationship （3D-QSAR） studies were performed to highlight the structural require- ments of ASTanalogs, which demonstrated introduction of bulkier substituents on the N-terminus would increase the activity. Analog Ⅱ12 （IC50： 0.08 μmol/L） exhibited similar inhibitory activity to the lead B1, but its synthetic route was simpler than B1. Therefore, Ⅱ12 could be used as a new lead compound for the discovery eco-friendly IGRs.展开更多
Insect growth regulators play an important role in integrated pest management strategies.The FGLa–allatostatins（ASTs）are a family of neuropeptides that can inhibit juvenile hormone（JH）biosynthesis by the corpora ...Insect growth regulators play an important role in integrated pest management strategies.The FGLa–allatostatins（ASTs）are a family of neuropeptides that can inhibit juvenile hormone（JH）biosynthesis by the corpora allata（CA）of Diploptera punctata in vitro,are regarded as insect growth regulator candidates.In the search for new potential mimics and to explore the effect of linker length on inhibiting JH biosynthesis,a series of AST analogs were synthesized by modifying the linker of K24,which was found to have a significant effect on JH biosynthesis in vitro in our previous study.Functional evaluation demonstrated that all the target compounds can activate the Dippu-Ast R,albeit with different potencies.Analog L6 with the longest linker（n=5）,exhibited not only a promising effect on inhibition of JH biosynthesis both in vitro and in vivo,but also good activity in inhibiting basal oocyte growth.Structure–activity relationships（SAR）studies showed that longer linkers provided greater contribution to activity.展开更多
文摘Methoprene, a juvenile hormone （JH） analog, is a widely used insecticide that also accelerates behavioral development in honey bees （Apis mellifera）. JH regulates the transition from nursing to foraging in adult worker bees, and treatment with JH or methoprene have both been shown to induce precocious foraging. To determine how methoprene changes honey bee behavior, we compared JH titers ofmethoprene-treated and untreated bees. Behavioral observations confirmed that methoprene treatment significantly increased the number of precocious foragers in 3 out of 4 colonies. In only 1 out of 4 colonies, however, was there a significant difference in JH titers between the methoprene- treated and control bees. Further, in all 4 colonies, there was no significant differences in JH titers between precocious and normal-aged foragers. These results suggest that methoprene did not directly affect the endogenous JH secreted by corpora allata. Because methoprene caused early foraging without changing workers＇ JH titers, we conclude that methoprene most likely acts directly on the JH receptors as a substitute for JH.
基金financially supported by the National Natural Science Foundation of China(No.21372257)the grants from the National Key Research and Development Plan(No.2017YFD0200504)
文摘Allatostatins （ASTs）, a family of insect neuropeptide, can inhibit juvenile hormone （JH） biosynthesis by the corpora allata （CA） in Diploptera punctata, and therefore be regarded as potential leads for the discovery of new insect growth regulators （1GRs）. But several shortcomings, such as their sensitivity to peptidases and high cost, impeded their practical application in pest management. In order to discover new IGRs, one AST analog B1 possessing non-peptide group was discovered with high ability to inhibit JH biosynthesis in vitro （IC50： 0.09 μmol/L） in our previous studies. In the present work, two series of B1 analogs with different substituents on the N-terminus region were designed and synthesized. The result suggested that benzene showed better activity than other heterocycles, and the para-substitution on the benzene was beneficial for activity. Moreover, analogs with logP value over 2.0 exhibited good activity, which indicated the hydrophobicity is important to the bioactivity. Three dimension quantitative structure-activity relationship （3D-QSAR） studies were performed to highlight the structural require- ments of ASTanalogs, which demonstrated introduction of bulkier substituents on the N-terminus would increase the activity. Analog Ⅱ12 （IC50： 0.08 μmol/L） exhibited similar inhibitory activity to the lead B1, but its synthetic route was simpler than B1. Therefore, Ⅱ12 could be used as a new lead compound for the discovery eco-friendly IGRs.
基金supported by the National Natural Science Foundation of China (No. 21372257)the National Basic Research Program of China (973 Program, No. 2010CB126104)+1 种基金the Natural Sciences and Engineering Research Council of Canadasupported by China Scholarship Council (CSC) to study in the laboratory of SST at University of Toronto,Canada
文摘Insect growth regulators play an important role in integrated pest management strategies.The FGLa–allatostatins（ASTs）are a family of neuropeptides that can inhibit juvenile hormone（JH）biosynthesis by the corpora allata（CA）of Diploptera punctata in vitro,are regarded as insect growth regulator candidates.In the search for new potential mimics and to explore the effect of linker length on inhibiting JH biosynthesis,a series of AST analogs were synthesized by modifying the linker of K24,which was found to have a significant effect on JH biosynthesis in vitro in our previous study.Functional evaluation demonstrated that all the target compounds can activate the Dippu-Ast R,albeit with different potencies.Analog L6 with the longest linker（n=5）,exhibited not only a promising effect on inhibition of JH biosynthesis both in vitro and in vivo,but also good activity in inhibiting basal oocyte growth.Structure–activity relationships（SAR）studies showed that longer linkers provided greater contribution to activity.
