Functional characterization of OR51B5 and OR1G1 in human lung epithelial cells as potential drug targets for non-type 2 lung diseases

Cell Biol Toxicol. 2024 Nov 13;40(1):96. doi: 10.1007/s10565-024-09935-9.

Abstract

Background: Hypersensitivity to odorants like perfumes can induce or promote asthma with non-type 2 inflammation for which therapeutic options are limited. Cell death of primary bronchial epithelial cells (PBECs) and the release of the pro-inflammatory cytokines interleukin-6 (IL-6) and IL-8 are key in the pathogenesis. Extra-nasal olfactory receptors (ORs) can influence cellular processes involved in asthma. This study investigated the utility of ORs in epithelial cells as potential drug targets in this context.

Methods: We used the A549 cell line and primary bronchial epithelial cells using air-liquid interface culture system (ALI-PBECs). OR expression was investigated by RT-PCR, Western blot, and Immunofluorescence. Effects of OR activation by specific ligands on intracellular calcium concentration, cAMP, Phospholipase C (PLC), cell viability, and IL-6 and IL-8 secretion were analyzed by calcium imaging, enzyme immunoassays, Annexin V/ propidium iodide -based fluorescence-activated cell staining or by ELISA, respectively.

Results: By screening A549 cells, the OR51B5 agonists Farnesol and Isononyl Alcohol and the OR1G1 agonist Nonanal increased intracellular Ca2 + . OR51B5 and OR1G1 mRNAs and proteins were detected. Both receptors showed a preferential intracellular localization. OR51B5- but not OR1G1-induced Ca2 + dependent on both cAMP and PLC signaling. Farnesol, Isononyl Alcohol, and Nonanal, all reduced cell viability and induced IL-8 and IL-6 release. The data were verified in ALI-PBECs.

Conclusion: ORs in the lung epithelium might be involved in airway-sensitivity to odorants. Their antagonism could represent a promising strategy in treatment of odorant-induced asthma with non-type 2 inflammation.

Keywords: Inflammation; Lung epithelial cell; Odorant sensitivity; Olfactory receptor; Therapeutic targets.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • A549 Cells
  • Calcium* / metabolism
  • Cell Survival / drug effects
  • Cyclic AMP / metabolism
  • Epithelial Cells* / drug effects
  • Epithelial Cells* / metabolism
  • Humans
  • Interleukin-6* / genetics
  • Interleukin-6* / metabolism
  • Interleukin-8* / metabolism
  • Lung / drug effects
  • Lung / metabolism
  • Lung / pathology
  • Receptors, Odorant* / genetics
  • Receptors, Odorant* / metabolism
  • Type C Phospholipases / metabolism

Substances

  • Receptors, Odorant
  • Interleukin-6
  • Interleukin-8
  • Calcium
  • Cyclic AMP
  • Type C Phospholipases