A Versatile Natural Neolignan as a Potential Pesticide Resource: Synthesis and Insecticidal Evaluation of Honokiol Derivatives Featuring a Bis(benzoxazole) Scaffold
Inspired by the insecticidal scaffold honokiol, bis(benzoxazole)-fused analogs were designed and synthesized. Compounds 5h, 7d, 8f, 8m, and 9a exhibited potent oral toxicity (LC 50 = 3.2–12.6 mg/L) and antifeedant activity (AFC 50 = 1.0–3.3 mg/L) against Plutella xylostella, outperforming honokiol, toosendanin, and rotenone. In greenhouse trials, compound 8f (100 mg/L, 48 h) achieved 51.1% corrected mortality and 75.8% leaf protection. Against Mythimna separata, compounds 5f, 6f, 6n, 7a, and 8g showed pronounced growth inhibition (LC 50 = 90–360 mg/L), exceeding honokiol and toosendanin. Acetylcholinesterase (AChE) was identified as a potential target in P. xylostella, and Chitinase inhibition disrupted M. separata development. Negligible cytotoxicity (IC 50 > 100 μM) against the human keratinocyte cell line (HaCaT) suggests a favorable safety profile for mammalian exposure. The novel architectures, potent efficacy, and good safety profile highlight the potential of these honokiol-inspired compounds as promising insecticidal candidates.
Authors
- Chun Yang (ORCID: https://orcid.org/0000-0001-5813-0914)
- Xiaoyan Zhi (ORCID: https://orcid.org/0009-0006-3337-1328)
- Fang Wang (ORCID: https://orcid.org/0000-0002-5971-2622)
- Hao Fu (ORCID: https://orcid.org/0000-0002-4267-3807)
- Xinyu Zhang (ORCID: https://orcid.org/0000-0003-2051-2655)
- Yan-Qiong Guo
- Jin-qiu Duan
- Ying Liu
Institutions
- Shanxi Agricultural University (CN)
Publication Details
- Journal
- Journal of Agricultural and Food Chemistry
- Published
- 2026-06-30
- DOI
- https://doi.org/10.1021/acs.jafc.5c14664
- Primary Topic
- Magnolia and Illicium research
- Type
- article
- Field-Weighted Citation Impact
- 0.00