Enhanced anticancer activity and endocytic mechanisms by polymeric nanocarriers of n-butylidenephthalide in leukemia cells

Clin Transl Oncol. 2021 Jun;23(6):1142-1151. doi: 10.1007/s12094-020-02500-w. Epub 2020 Sep 28.

Abstract

Purpose: The purpose of this study was to investigate the antitumor mechanisms of n-butylidenephthalide (BP) and to further examine the delivery efficacy of polycationic liposome containing PEI and polyethylene glycol complex (LPPC)-encapsulated BP in leukemia cells.

Methods: MTS, flow cytometric and TUNEL assays were performed to assess cell viability and apoptosis. BP and BP/LPPC complex delivery efficiency was analyzed by full-wavelength fluorescent scanner and fluorescence microscope. The expressions of cell cycle- and apoptosis-related proteins were conducted by Western blotting.

Results: The results showed that BP inhibited leukemia cell growth by inducing cell cycle arrest and cell apoptosis. LPPC-encapsulated BP rapidly induced endocytic pathway activation, resulting in the internalization of BP into leukemia cells, causing cell apoptosis within 1 h.

Conclusions: LPPC encapsulation enhanced the cytotoxic activity of BP and did not influence the effects of BP induction that suggested LPPC-encapsulated BP might be developed as anti-leukemia drugs in future.

Keywords: Cell apoptosis; Cell cycle; Leukemia; Polycationic liposome containing PEI and polyethylene glycol complex (LPPC); n-Butylidenephthalide (BP).

MeSH terms

  • Apoptosis
  • Cell Survival
  • Drug Carriers*
  • Endocytosis
  • Humans
  • Leukemia / drug therapy*
  • Liposomes
  • Nanotechnology
  • Phthalic Anhydrides / administration & dosage*
  • Polyelectrolytes
  • Tumor Cells, Cultured

Substances

  • Drug Carriers
  • Liposomes
  • Phthalic Anhydrides
  • Polyelectrolytes
  • polycations
  • butylidenephthalide