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Synthesis, Characterization and Anticancer Efficacy Evaluation of Benzoxanthone Compounds toward Gastric Cancer
Yuan Fu1, Yunran Xu1, Yunjun Liu1
1School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China.
Abstract:
Three benzoxanthone derivatives were synthesized through a new photochemical strategy. The in vitro cytotoxic activity of these compounds was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, and their partition coefficients (logP) were measured by shake flask method. The pK values of the compounds were detected by potentionmetric titration. The interaction of the compounds with calf thymus DNA (CT-DNA) was investigated by electronic absorption, luminescence spectra and viscosity. A molecular docking analysis was performed. The antitumor efficacy of the compounds was evaluated by cell apoptosis, cell cycle arrest, intracellular Ca2+ concentrations and reactive oxygen species (ROS) levels. The mitochondrial membrane potential was assayed using JC-1 (5,5',6,6'-tetrachloro-1,1,3',3'-tetraethyl-imidacarbocyanine iodide) as the fluorescence probe. The expression of Bcl-2 family protein, caspase 3 and poly ADP-ribose polymerase (PARP) was explored by western blot. The results showed that the compounds induced apoptosis through a ROS-mediated mitochondrial dysfunction pathway. This work provides an efficient approach to synthesize benzoxanthone derivatives, and is helpful for understanding the apoptotic mechanism.
Insights
Three novel benzoxanthone derivatives were synthesized and show potent anticancer activity. These compounds induce programmed cell death (apoptosis) via a reactive oxygen species (ROS)-mediated mitochondrial pathway, offering a new therapeutic strategy.
Area of Science:
- Medicinal Chemistry
- Photochemistry
- Molecular Biology
Background:
- Benzoxanthone derivatives are explored for therapeutic potential.
- Developing efficient synthetic routes for novel compounds is crucial.
- Understanding mechanisms of action for anticancer agents is a key research area.
Purpose of the Study:
- To synthesize new benzoxanthone derivatives using a novel photochemical strategy.
- To evaluate the in vitro cytotoxic and antitumor activities of these compounds.
- To elucidate the mechanism of action, focusing on apoptosis induction and mitochondrial dysfunction.
Main Methods:
- Photochemical synthesis of benzoxanthone derivatives.
- In vitro assays: MTT, pKa, logP, DNA interaction (spectroscopy, viscosity).
- Antitumor efficacy assessment: apoptosis, cell cycle, Ca2+, ROS, mitochondrial membrane potential (JC-1), Western blot (Bcl-2, caspase 3, PARP).
Main Results:
- Successful synthesis of three benzoxanthone derivatives.
- Compounds demonstrated significant in vitro cytotoxic and antitumor activities.
- Mechanism elucidated: apoptosis induction via ROS-mediated mitochondrial dysfunction.
Conclusions:
- The study presents an efficient photochemical synthesis for benzoxanthone derivatives.
- The synthesized compounds exhibit promising anticancer properties.
- The findings contribute to understanding the apoptotic pathway, particularly mitochondrial dysfunction and ROS involvement.
