Screening and Identification of TRPV1-Targeting Peptides from Apis mellifera Venom with Inflammatory Modulatory Potential

peer-reviewed · Journal of Natural Products · 2026

peer-reviewed · Journal of Natural Products · 2026. Kai Wang et al. Bee venom from Apis mellifera has been traditionally used to treat inflammatory disorders, largely due to its…
Date 2026-04-24
Type peer-reviewed
Venue Journal of Natural Products
Publisher American Chemical Society (ACS)
Contribution downstream-application
DOI 10.1021/acs.jnatprod.5c01554
Citations (OpenAlex) 0

Abstract

Bee venom from Apis mellifera has been traditionally used to treat inflammatory disorders, largely due to its bioactive peptide components. However, comprehensive characterization of these peptides and their interaction with transient receptor potential vanilloid 1 (TRPV1), a key receptor in nociception and inflammation, remains limited. In this study, we systematically profiled the A. mellifera venom peptidome and identified TRPV1-targeting peptides with inflammatory modulatory potential. De novo sequencing-based peptidomics generated an in-house database of 472 peptides (average local confidence, ALC ≥ 50%), including 103 high-confidence peptides (ALC ≥ 80%). Ten novel peptides were identified as candidate TRPV1-targeting peptides through pull-down screening. Among them, three peptides (P1: GNGGGGLGSGGSLGLGHE, P2: MLLAVARSVP, and P3: NQEVEEERLKY) were synthesized and tested for anti-inflammatory activity in LPS-stimulated RAW 264.7 macrophages. All three peptides significantly suppressed TNF-α secretion, with P1 achieving 62.5% inhibition at 10 μM, and modulated IL-6 and IL-1β in a dose-dependent manner. Proteomic profiling and pathway enrichment analyses indicated that these peptides exert anti-inflammatory effects through NF-κB suppression and the modulation of redox and metabolic pathways. This study provides the first evidence that A. mellifera venom contains peptides identified through TRPV1-based affinity screening, including three novel TRPV1-targeting peptides with inflammatory modulatory potential.

Authors

  1. Kai Wang · Chinese Academy of Agricultural Sciences, Gembloux Agro-Bio Tech, Institute of Apiculture Research, University of Liège
  2. Jiangtao Qiao · Hebei University of Engineering
  3. Chao Ji
  4. Eric Haubruge · Gembloux Agro-Bio Tech, University of Liège
  5. Gauthier Eppe · University of Liège
  6. Xianbin Meng · Shenzhen Medical Academy of Research and Translation
  7. Christopher Kune · University of Liège
  8. Loïc Quinton · Centre National de la Recherche Scientifique, Commissariat à l’Énergie Atomique et aux Énergies Alternatives, Universidad Autónoma del Estado de Morelos, University of Liège, École Polytechnique
  9. Hongcheng Zhang · Chinese Academy of Agricultural Sciences, Institute of Apiculture Research

Methods and tools

  • Honeybee venom TRPV1-targeting peptides: PEAKS de novo sequencing of Apis mellifera venom produced a 472-peptide database, from which pull-down screening found ten novel TRPV1-binding peptides; three were synthesized and shown to be anti-inflammatory.

Methods it uses

  • PEAKS: Commercial DP-based de novo

Data deposited

  • Peptidomics-guided identification of TRPV1-targeting peptides from Apis mellifera venom and macrophage proteomics — as deposited · PXD075103

Cites (2)

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