ORIGINAL RESEARCH article
Front. Pharmacol.
Sec. Ethnopharmacology
Volume 16 - 2025 | doi: 10.3389/fphar.2025.1601384
This article is part of the Research TopicNovel Technologies and Methods for Monitoring Exogenous Harmful Residues in Traditional and Local Medicinal Plants and FungiView all articles
Screening and Identification the H1R antagonists from natural products by the BODIPY FL histamine recognition and DPHDanchored bombardment coupled with target cell extraction
Provisionally accepted
- 1China Pharmaceutical University, Nanjing, China
- 2BYHEALTH Institute of Nutrition & Health, Guangzhou, China
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Introduction: Histamine, as an important mediator of allergy, inhibiting its binding to H1 receptors (H1R) is a key method to alleviate allergic diseases. Natural products with anti-allergic properties are an important source of natural H1R antagonists.: In this study, a rapid method for identifying the H1R antagonists from natural products via the BODIPY FL histamine recognition and diphenhydramine (DPHD)-anchored bombardment coupled with target cell extraction was developed. And the activity of the H1R antagonist was further validated both in vitro and in vivo through the BODIPY FL histamine recognition, intracellular fluorescence calcium ion (Ca 2+ ) kinetic recognition, molecular docking, and animal experiments. Results: The binding of fluorescent histamine to H1R was notably inhibited by Ephedra sinica Stapf (ESS) and Dictamnus dasycarpus Turcz (DdT). Ephedrine and pseudoephedrine in ESS, and dictamnine and limonin in DdT, were screened as potential H1R antagonists using the target cell extraction of the DPHD-anchored bombardment. With the BODIPY FL histamine recognition results revealed the significant blocking effects on H1R binding by pseudoephedrine (50 μM) and dictamnine (100 μM). Pseudoephedrine (200 μM) and dictamnine (100 μM) markedly decreased the histamine-induced increase in intracellular calcium ion (Ca 2+ ) concentration. Docking results indicated strong binding affinity for both components to H1R, with dictamnine exhibiting a higher affinity than pseudoephedrine. Ultimately, the ameliorative effect of dictamnine on allergic rhinitis mice was confirmed through nasal symptom score, serum pharmacodynamic indices (Immunoglobulin E (IgE), histamine, IL-2, IL-4, IL-6, and TNF-α), and histopathology.This study showed that dictamnine (validation in vitro and in vivo) and pseudoephedrine (validation in vitro) may serve as potential H1R antagonists. This study offered valuable insights for future developments in antihistamines.
Keywords: BODIPY FL histamine, H1R antagonists, Target cell extraction, HPLC-Q-TOF-MS, Natural Products, Dictamnine, Pseudoephedrine
Received: 27 Mar 2025; Accepted: 30 Apr 2025.
Copyright: © 2025 Li, Hu, Chen, Di and Qi. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
* Correspondence: Jin Qi, China Pharmaceutical University, Nanjing, China
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