Related Experiment Video

Updated: Jan 27, 2026

Measuring Nitrite and Nitrate, Metabolites in the Nitric Oxide Pathway, in Biological Materials using the Chemiluminescence Method
08:25

Measuring Nitrite and Nitrate, Metabolites in the Nitric Oxide Pathway, in Biological Materials using the Chemiluminescence Method

Published on: December 25, 2016

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Novel anticancer paeonol derivatives possessing a nitric oxide donor moiety as TrxR inhibitors: design, synthesis,

Ce Shi1, Weisen Zhong2, Guowei Qiang2

  • 1Department of Orthopedics, The Affiliated Suqian Hospital of Xuzhou Medical University, Suqian, 223800, China.

Bioorganic & Medicinal Chemistry Letters
|January 25, 2026
PubMed

Insights

Novel paeonol chalcone derivatives were synthesized to release nitric oxide (NO) and target thioredoxin reductase (TrxR). Compound 11f demonstrated significant anticancer activity by inducing apoptosis and cell cycle arrest.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Biochemistry

Background:

  • The tumor microenvironment (TME) influences cancer progression and treatment outcomes.
  • Redox processes involving reactive oxygen species (ROS) and nitric oxide (NO) regulate cell signaling within the TME.

Purpose of the Study:

  • To synthesize novel paeonol chalcone derivatives with enhanced anticancer activity.
  • To investigate the potential of these compounds to release NO and target thioredoxin reductase (TrxR).

Main Methods:

  • Synthesis of mono- and di-substituted nitrate derivatives of paeonol chalcones.
  • Antiproliferative activity evaluation using the CCK-8 assay across multiple cancer cell lines (BGC823, HCT116, Hep G2, MCF-7).
  • Assessment of TrxR inhibitory activity, induction of S-phase arrest, and apoptosis in cancer cells.

Main Results:

  • Compound 11f exhibited significant antiproliferative effects across tested cancer cell lines.
  • Compound 11f demonstrated potent in vitro and in vivo thioredoxin reductase inhibition.
  • Compound 11f induced S-phase arrest and promoted apoptosis in MCF-7 cells.

Conclusions:

  • Paeonol chalcone derivatives show enhanced anticancer potential.
  • The synergistic effects of NO release and TrxR inhibition contribute to the observed anticancer activity.
Keywords:
Antitumor activityNitric oxide donorPaeonol derivativeTrxR inhibitor

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