Pinostilbene as a Potential Cytotoxic Agent in Cancer Cell Lines: Improvement of Solubility and Stability by...

Area of Science:

• Pharmacology
• Materials Science

Background:

• Pinostilbene, a natural stilbene, possesses antioxidant, antimicrobial, and neuroprotective properties.
• It demonstrates anticancer activity but suffers from poor solubility and stability, hindering drug development.

Purpose of the Study:

• To investigate pinostilbene's cytotoxicity in colon cancer cells.
• To improve pinostilbene's physicochemical properties via cyclodextrin encapsulation.

Main Methods:

• Cytotoxicity assessed using the neutral red assay in Caco-2 cells.
• Cyclodextrin screening, fluorescence spectroscopy, and molecular docking identified optimal encapsulation.
• Complex formation confirmed by DSC and SEM; release monitored spectrophotometrically.

Main Results:

• Pinostilbene displayed in vitro cytotoxicity against Caco-2 cells.
• Hydroxypropyl-β-cyclodextrin showed the highest encapsulation constant (10,074.45 M⁻¹), with 1:1 stoichiometry.
• Encapsulation increased solubility tenfold, reduced degradation to <15% over 3 months, and modulated release based on pH.

Conclusions:

• Pinostilbene is a potent antiproliferative agent with potential as a drug candidate.
• Cyclodextrin complexation effectively addresses pinostilbene's solubility and stability issues.
• This approach facilitates its potential application in the pharmaceutical and food industries.