Photoswitchable COX-2-Selective Inhibitors as Light-Regulated Anti-Inflammatory Agents

J Am Chem Soc. 2026 May 13;148(18):19226-19237. doi: 10.1021/jacs.6c03529. Epub 2026 Apr 28.

Abstract

Despite their extensive use, the therapeutic potential of nonsteroidal anti-inflammatory drugs (NSAIDs) remains significantly constrained by adverse side effects. This limitation primarily arises from insufficient selectivity, as current NSAIDs inhibit not only the inducible cyclooxygenase-2 (COX-2) isoform at sites of inflammation but also constitutive COX-2 in healthy tissues and, frequently, cyclooxygenase-1. To address this challenge, we developed photoswitchable NSAIDs that combine COX-2 selectivity with light-controlled activity to enable spatiotemporal confinement of the therapeutic effect at inflamed tissues. Following computational design and screening of a library of azoaromatic derivatives of celecoxib─the most widely used COX-2 selective NSAID─three photoswitchable analogues were synthesized, which exhibited reversible and efficient trans-cis photoconversion. Light-controlled and selective COX-2 inhibition was demonstrated for these compounds in vitro, reaching up to 5-fold potency enhancement in macrophage assays upon photoisomerization from the initial, dark-adapted trans isomer to the cis state. The best candidate displayed in vivo efficacy in a zebrafish model of acute inflammation, where administration of the photoinduced cis form reduced leukocyte recruitment at the wound site. These findings position photoswitchable NSAIDs as a promising alternative to conventional drugs for treating inflammation and related conditions, including cancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal* / chemical synthesis
  • Anti-Inflammatory Agents, Non-Steroidal* / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal* / pharmacology
  • Celecoxib* / chemistry
  • Celecoxib* / pharmacology
  • Cyclooxygenase 2 Inhibitors* / chemical synthesis
  • Cyclooxygenase 2 Inhibitors* / chemistry
  • Cyclooxygenase 2 Inhibitors* / pharmacology
  • Cyclooxygenase 2* / metabolism
  • Humans
  • Inflammation / drug therapy
  • Light*
  • Macrophages / drug effects
  • Molecular Structure
  • Photochemical Processes
  • Zebrafish

Substances

  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase 2
  • Anti-Inflammatory Agents, Non-Steroidal
  • Celecoxib