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Epigenetic modulation and apoptotic induction by a novel imidazo-benzamide derivative in human lung adenocarcinoma

Amrutha Arjunan1, Sankar Pajaniradje2, Arul Prakash Francis1

  • 1Department of Biochemistry and Molecular Biology, School of Life Sciences, Pondicherry University, Puducherry, Puducherry, 605 014, India.

Daru : Journal of Faculty of Pharmacy, Tehran University of Medical Sciences
|October 13, 2021
PubMed
Abstract

Insights

A new imidazo-benzamide derivative, TBUEIB, shows significant anti-cancer potential against lung cancer cells. It works by targeting epigenetic factors like DNMT1, potentially reactivating tumor suppressor genes and inducing cancer cell death.

Area of Science:

  • Oncology
  • Molecular Biology
  • Epigenetics

Background:

  • Lung cancer is a leading global cause of cancer death.
  • Imidazo-benzamide derivatives show promise as anti-cancer agents.

Purpose of the Study:

  • To investigate the cytotoxicity of a novel imidazo-benzamide derivative, N-(2-(3-(tert-butyl)ureido)ethyl)-4-(1H-imidazol-1-yl)benzamide (TBUEIB), in the A549 lung cancer cell line.
  • To explore the anti-cancer mechanisms of TBUEIB, focusing on its effects on cell proliferation and apoptosis.

Main Methods:

  • Cytotoxicity was assessed using MTT, LDH, and trypan blue assays.
  • Apoptotic potential was evaluated through various staining techniques, DNA fragmentation assays, and western blotting.
  • In silico studies were performed to assess interactions with epigenetic proteins.

Main Results:

  • TBUEIB inhibited 50% of A549 cells at a concentration of 106 μM.
  • The compound modulated the apoptotic marker caspase-3 and the epigenetic regulator DNA Methyltransferase 1 (DNMT1).
  • In silico analyses indicated favorable interactions with DNMT1, Histone deacetylase (HDAC), and UHRF1.

Conclusions:

  • The novel compound TBUEIB exhibits potential anti-cancer activity against lung cancer cells.
  • TBUEIB primarily targets DNMT1, potentially reactivating tumor suppressor genes and inducing apoptosis.
  • The compound's interaction with multiple epigenetic targets suggests it may act as a multi-target anti-cancer agent.
Keywords:
Anti-cancerApoptosisBenzamide derivativesDNA methyltransferaseEpigenetic

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