CDS-1548 induces apoptosis in HeLa cells by activating caspase 3

Oncol Lett. 2019 Aug;18(2):1881-1887. doi: 10.3892/ol.2019.10511. Epub 2019 Jun 21.

Abstract

Cervical cancer continues to be a threat to female health globally. In the present study, the potential anticancer activity of 2-[2-hydroxyl-1-(4-methoxy phenyl) ethyl]-3-(4-benzyloxy phenyl) isoindolin-1-one (CDS-1548), was evaluated in HeLa cells. CDS-1548 is an organic small-molecule compound characterized by two chiral centers, with the nuclear parent 1H-isoindolin-1-one. CDS-1548 administration significantly elevated the transcriptional activity of p53 and its downstream target genes in a dose-dependent manner. Additionally, CDS-1548 treatment increased the expression levels of p53 and mouse double minute 2 homolog, as well as inducing apoptosis in HeLa cells. Furthermore, CDS-1548 treatment downregulated the expression of B-cell lymphoma 2, upregulated Bcl-2 homologous antagonist killer, promoted the release of cytochrome c from mitochondria to cytoplasm, and activated the production of caspase 3 and 9. Collectively, these results suggested that CDS-1548 inhibited HeLa cell proliferation by promoting G2/M cell cycle phase arrest and inducting of mitochondria-mediated apoptosis.

Keywords: G2/M arrest; HeLa; apoptosis; p53; small-molecule inhibitor.