Eco-Friendly Insecticide Discovery via Peptidomimetics: Design, Synthesis, and Aphicidal Activity of Novel Insect Kinin Analogues
| العنوان: | Eco-Friendly Insecticide Discovery via Peptidomimetics: Design, Synthesis, and Aphicidal Activity of Novel Insect Kinin Analogues |
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| المؤلفون: | Chuanliang Zhang, Xiaoqing Wu, Dunlun Song, Xinling Yang, Yun Ling, Qu Yanyan |
| المصدر: | Journal of Agricultural and Food Chemistry. 63:4527-4532 |
| بيانات النشر: | American Chemical Society (ACS), 2015. |
| سنة النشر: | 2015 |
| مصطلحات موضوعية: | Hindgut contraction, Insecticides, animal structures, Stereochemistry, Peptidomimetic, media_common.quotation_subject, Molecular Sequence Data, Kinins, General Chemistry, Insect, Biology, Kinin, Pentapeptide repeat, Structure-Activity Relationship, chemistry.chemical_compound, Design synthesis, chemistry, Biochemistry, Aphids, Drug Design, Animals, Amino Acid Sequence, General Agricultural and Biological Sciences, Lead compound, media_common |
| الوصف: | Insect kinin neuropeptides are pleiotropic peptides that are involved in the regulation of hindgut contraction, diuresis, and digestive enzyme release. They share a common C-terminal pentapeptide sequence of Phe(1)-Xaa(2)-Yaa(3)-Trp(4)-Gly(5)-NH2 (where Xaa(2) = His, Asn, Phe, Ser, or Tyr; Yaa(3) = Pro, Ser, or Ala). Recently, the aphicidal activity of insect kinin analogues has attracted the attention of researchers. Our previous work demonstrated that the sequence-simplified insect kinin pentapeptide analogue Phe-Phe-[Aib]-Trp-Gly-NH2 could retain good aphicidal activity and be the lead compound for the further discovery of eco-friendly insecticides which encompassed a broad array of biochemicals derived from micro-organisms and other natural sources. Using the peptidomimetics strategy, we chose Phe-Phe-[Aib]-Trp-Gly-NH2 as the lead compound, and we designed and synthesized three series, including 31 novel insect kinin analogues. The aphicidal activity of the new analogues against soybean aphid was determined. The results showed that all of the analogues exhibited aphicidal activity. Of particular interest was the analogue II-1, which exhibited improved aphicidal activity with an LC50 of 0.019 mmol/L compared with the lead compound (LC50 = 0.045 mmol/L) or the commercial insecticide pymetrozine (LC50 = 0.034 mmol/L). This suggests that the analogue II-1 could be used as a new lead for the discovery of potential eco-friendly insecticides. |
| تدمد: | 1520-5118 0021-8561 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8d5741ce4569780852282efc821f61b1 https://doi.org/10.1021/acs.jafc.5b01225 |
| رقم الأكسشن: | edsair.doi.dedup.....8d5741ce4569780852282efc821f61b1 |
| قاعدة البيانات: | OpenAIRE |
Find this issue from the American Chemical Society | تدمد: | 15205118 00218561 |
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