The anticancer, anti-oxidant, and antibacterial activities of chitosan-lecithin-coated parthenolide/tyrosol hybrid nanoparticles

J Biomater Sci Polym Ed. 2023 Aug;34(11):1603-1617. doi: 10.1080/09205063.2023.2177473. Epub 2023 Feb 20.

Abstract

Tyrosol (TYR) and parthenolide (PLT) have been used as synthetic antioxidant and natural anticancer compounds. In the current study, we aimed to synthesize an encapsulated complex of both PLT and TYR in a hybrid coating layer consisting of lecithin and chitosan molecules, a proper biocompatible drug delivery system to evaluate its antibacterial and anticancer potentials on human liver HepG2 and pancreatic Panc cancer cell lines. The chitosan-lecithin-coated PLT/TYR nanoparticles (clPT-NPs) were synthesized applying an auto-self-assembling method. The clPT-NPs were characterized utilizing DLS, FTIR, zeta potential, and TEM analysis. The clPT-NPs' antioxidant activity was measured by running ABTS and DPPH antioxidant assays. Moreover, the antibacterial potential of clPT-NPs was evaluated by applying disk diffusion, MIC, and MBC assays. Finally, the nanoparticles' cytotoxicity and apoptotic activity were studied by conducting MTT, Flow cytometry, AO/PI cell staining, and real-time PCR techniques. The clPT-NPs (38 nm) exhibited significant antioxidant activity by inhibiting ABTS and DPPH radicals at 187 and 290 μg/mL IC50 concentrations, respectively. Also, the nanoparticles induced a notable antibacterial activity against Staphylococcus aureus at 0.0625 mg/mL MIC and 0.125 mg/mL MBC concentrations. The clPT-NPs selectively decreased the cancer cells' survival and increased the apoptotic dead cells by up-regulating apoptotic gene expression (BAX and Cas-8) and down-regulating BCL-2 anti-apoptotic gene expression. The PLT toxicity has been merged with improved TYR antioxidant activity, which has been functionalized in a safe, biocompatible hybrid nano-delivery system.

Keywords: Parthenoloid; antibacterial; antioxidant; apoptotic; cancer-selective cytotoxicity; chitosan-lecithin-coated PLT/TYR nanoparticles (clPT-NPs).

MeSH terms

  • Anti-Bacterial Agents* / pharmacology
  • Antineoplastic Agents* / pharmacology
  • Antioxidants* / pharmacology
  • Apoptosis / drug effects
  • Apoptosis / genetics
  • Cell Line, Tumor
  • Chitosan*
  • Humans
  • Lecithins*
  • Nanoparticles* / chemistry
  • Staphylococcus aureus / drug effects

Substances

  • 4-hydroxyphenylethanol
  • Anti-Bacterial Agents
  • Antineoplastic Agents
  • Antioxidants
  • Chitosan
  • Lecithins
  • parthenolide