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. 2020 Aug 1;30(15):127260.
doi: 10.1016/j.bmcl.2020.127260. Epub 2020 May 21.

Application of natural products as insecticide candidates: Semisynthesis and biological evaluation of some novel osthole-based esters

Yong Guo  1 , Zhiyan Liu  2 , Enhua Hou  2 , Nannan Ma  2 , Yinping Gen  2 , Pengchao Che  2 , Ruige Yang  3
Affiliations

Application of natural products as insecticide candidates: Semisynthesis and biological evaluation of some novel osthole-based esters

Yong Guo et al. Bioorg Med Chem Lett. .

Abstract

Natural products are very important sources for the development of new pesticides. Osthole, derived from many medical plants such as Cnidium, Angelica and Citrus plants, is a naturally occurring coumarin compound. To discover the new natural products-based insecticides, thirty-one osthole-based esters containing O-acyl-hydroxylamine groups were prepared, and their structures were identified by different spectral analysis methods. Derivatives A7, A17, A20 and A25 displayed more potent growth inhibitory (GI) activity than the botanical insecticide, toosendanin. Over half of target osthole derivatives had more effective larvicidal effect on P. xylostella than toosendanin. Among all title derivatives, compound A18 displayed more pronounced larvicidal activity (LC50 = 0.64 μmol mL-1) when compared with toosendanin (LC50 = 0.94 μmol mL-1). Some interesting results of structure-activity relationships (SARs) of these osthole derivatives were also discussed. In addition, the hemolysis and cytotoxicity assays indicated that these osthole derivatives showed very low toxicity toward normal mammalian cells.

Keywords: Cytotoxic activity; Hemolytic activity; Insecticidal activity; Natural product; Osthole derivative; Structure–activity relationship.

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Conflict of interest statement

Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

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