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Routing NSAIDs into the Golgi apparatus induces autophagy and apoptosis in cancer cells

Aditi1, Tripti Mishra1, Asima Sahu1

  • 1Department of Chemistry, Indian Institute of Technology (IIT) Gandhinagar Palaj Gandhinagar Gujarat 382355 India Sudipta.basu@iitgn.ac.in.

RSC Medicinal Chemistry
|August 4, 2025
PubMed

Insights

A novel ibuprofen conjugate targets the Golgi apparatus, inducing cancer cell death via autophagy and apoptosis. This compound shows promise for cancer therapy and studying Golgi apparatus function.

Area of Science:

  • Chemical Biology
  • Molecular Biology
  • Cancer Research

Background:

  • The Golgi apparatus (GA) is crucial for protein modification and secretion, and its dysfunction is linked to cancer.
  • Targeting the GA with drugs offers a potential strategy for enhanced anti-cancer effects.
  • Developing specific agents to deliver therapeutics to the GA remains a challenge.

Purpose of the Study:

  • To design and synthesize novel NSAID-based conjugates for Golgi apparatus targeting.
  • To evaluate the anti-cancer efficacy and mechanism of action of these conjugates.
  • To explore the potential of these compounds as tools for chemical biology and cancer therapy.

Main Methods:

  • Synthesis of NSAID-based conjugates incorporating a fluorophore and a Golgi-homing moiety.
  • Screening of conjugates for cytotoxicity in various cancer cell lines (HCT-116, A549, Caco-2, MCF7).
  • Investigation of cellular localization, self-assembly, and mechanism of action, including autophagy and apoptosis induction, and effects on 3D spheroids.

Main Results:

  • A specific ibuprofen-1,8-naphthalimide-phenylsulfonamide conjugate (7a) demonstrated significant cytotoxicity against multiple cancer cell lines.
  • Compound 7a self-assembled into nanoscale structures and efficiently localized to the GA and ER, inducing morphological damage.
  • 7a triggered autophagy and apoptosis, leading to cancer cell death, and reduced 3D spheroid growth, with no observed toxicity in non-cancerous cells.

Conclusions:

  • The synthesized ibuprofen derivative (7a) effectively targets the Golgi apparatus and exhibits potent anti-cancer activity.
  • Compound 7a induces cancer cell death through autophagy and apoptosis, highlighting its therapeutic potential.
  • This conjugate serves as a valuable chemical biology tool for investigating Golgi apparatus function in cancer.

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