2. Academic Validation
  3. Perezone and its phenyl glycine derivative induce cytotoxicity via caspases on human glial cancer cells

Perezone and its phenyl glycine derivative induce cytotoxicity via caspases on human glial cancer cells

  • Nat Prod Res. 2024 Jun;38(11):1823-1833. doi: 10.1080/14786419.2023.2225121.
M Mirian Estévez-Carmona 1,  M Teresa Ramírez-Apan 2,  Montserrat Zaragoza-Ojeda 3,  Anita Vega-Miranda 4,  Francisco Arenas-Huertero 3,  William F Reynolds 5,  Marco A Obregón-Mendoza 2
Affiliations

Affiliations

  • 1 Departamento de Farmacia, Escuela Nacional de Ciencias Biológicas, Instituto Politécnico Nacional, Wilfrido Massieu SN, U. A. Zacatenco, Ciudad de México, México.
  • 2 Instituto de Química, Universidad Nacional Autónoma de México, Circuito Exterior, Ciudad Universitaria, Ciudad de México, México.
  • 3 Laboratorio de Investigación en Patología Experimental, Hospital Infantil de México Federico Gómez, Ciudad de México, México.
  • 4 Laboratorio de Transducción de Señales, Instituto Nacional de Enfermedades Respiratorias, Ismael Cosío Villegas, Ciudad de México, México.
  • 5 Department of Chemistry, University of Toronto, Toronto, Ontario, Canada.
PMID: 37341748 DOI: 10.1080/14786419.2023.2225121
Abstract

The new phenyl glycine derivative of perezone was obtained in a single reaction step in CA. 80% yield which showed remarkable cytotoxic activity against the astrocytoma U-251 cell line. After 24 h of exposure, both perezone (IC50 = 6.83 ± 1.64 µM) and its phenyl glycine derivative (2.60 ± 1.69 µM) showed cytotoxic effect on U-251 cells but were five times less cytotoxic on the non-tumoral SVGp12 cell line (IC50 = 28.54 ± 1.59 and 31.87 ± 1.54 µM respectively). Both compounds induced cellular morphological changes (pyknosis or cytoplasmic vacuolization) and increased the expression of caspases 3, 8, and 9 genes related to Apoptosis. In the acute toxicity study, phenyl glycine perezone (DL50 = 2000 mg/Kg) demonstrated to be less toxic than perezone (DL50 = 500 mg/Kg). Phenylglycine-perezone can envisage a beneficial therapeutic potential.

Keywords

Phenyl glycine-perezone; apoptosis; cancer cell line; caspases; cytotoxic activity; natural product.

Figures
Products