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8-Nitrotryptanthrin inhibits colorectal cancer progression via TGF-β/SMAD and PI3K/AKT/mTOR pathways

Cheng-Yu Sun1, Kai-Ping Cong2,3, Dan-Dan Zhao4

  • 1Department of Colorectal Surgery, The Affiliated Xuzhou Clinical College of Xuzhou Medical University, Xuzhou, Jiangsu, China.

Frontiers in Pharmacology
|September 8, 2025
PubMed
Abstract

Insights

8-Nitrotryptanthrin (8-Nitrotryp) shows significant anticancer effects against colorectal cancer (CRC) by inhibiting cell proliferation and inducing apoptosis. This novel compound effectively targets key signaling pathways involved in CRC progression.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Colorectal cancer (CRC) presents a significant global health challenge, with limited therapeutic options for advanced stages.
  • Tryptanthrin (Tryp) derivatives are being explored for their potential anticancer properties.

Purpose of the Study:

  • To investigate the anticancer effects of 8-nitrotryptanthrin (8-Nitrotryp) on colorectal cancer (CRC) cell lines.
  • To elucidate the underlying molecular mechanisms of 8-Nitrotryp's action, focusing on key signaling pathways.

Main Methods:

  • Evaluation of 8-Nitrotryp's effects on CRC cell proliferation, colony formation, and migration.
  • Assessment of mitochondrial membrane potential (MMP) and induction of apoptosis.
  • Proteomic analysis and Western blotting to examine the PI3K/AKT/mTOR and TGF-β/SMAD pathways and epithelial-mesenchymal transition (EMT).

Main Results:

  • 8-Nitrotryp significantly inhibited proliferation, colony formation, and migration in HCT116 and SW480 CRC cells, showing greater potency than Tryp.
  • 8-Nitrotryp suppressed MMP and induced early apoptosis, while downregulating PI3K, inhibiting AKT/mTOR phosphorylation, and reducing TGF-β1-induced SMAD2 phosphorylation.
  • The compound effectively suppressed the EMT process in CRC cells.

Conclusions:

  • 8-Nitrotryp demonstrates potent anticancer activity against CRC by modulating the TGF-β/SMAD and PI3K/AKT/mTOR signaling pathways.
  • The observed suppression of EMT is mechanistically linked to the inhibition of the TGF-β/SMAD pathway.
  • 8-Nitrotryp shows promise as a multi-target therapeutic agent for CRC, warranting further investigation.
Keywords:
8-nitrotryptanthrincolorectal neoplasmsphosphatidylinositol 3-kinasessignal transductiontransforming growth factor beta

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