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

Autor: Estévez-Carmona MM; Departamento de Farmacia, Escuela Nacional de Ciencias Biológicas, Instituto Politécnico Nacional, Wilfrido Massieu SN, U. A. Zacatenco, Ciudad de México, México., Ramírez-Apan MT; Instituto de Química, Universidad Nacional Autónoma de México, Circuito Exterior, Ciudad Universitaria, Ciudad de México, México., Zaragoza-Ojeda M; Laboratorio de Investigación en Patología Experimental, Hospital Infantil de México Federico Gómez, Ciudad de México, México., Vega-Miranda A; Laboratorio de Transducción de Señales, Instituto Nacional de Enfermedades Respiratorias, Ismael Cosío Villegas, Ciudad de México, México., Arenas-Huertero F; Laboratorio de Investigación en Patología Experimental, Hospital Infantil de México Federico Gómez, Ciudad de México, México., Reynolds WF; Department of Chemistry, University of Toronto, Toronto, Ontario, Canada., Obregón-Mendoza MA; Instituto de Química, Universidad Nacional Autónoma de México, Circuito Exterior, Ciudad Universitaria, Ciudad de México, México.
Jazyk: angličtina
Zdroj: Natural product research [Nat Prod Res] 2024 Jun; Vol. 38 (11), pp. 1823-1833. Date of Electronic Publication: 2023 Jun 21.
DOI: 10.1080/14786419.2023.2225121
Abstrakt: 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 (IC 50 = 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 (IC 50 = 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 (DL 50 = 2000 mg/Kg) demonstrated to be less toxic than perezone (DL 50 = 500 mg/Kg). Phenylglycine-perezone can envisage a beneficial therapeutic potential.
Databáze: MEDLINE
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