Homospisulosine induced apoptosis in cervical carcinoma cells is associated with phosphorylation of Bcl-2 and up-regulation of p27/Kip1.

Apoptosis Cancer Ceramide Homospisulosine Marine Sphingoid bases Sphingosine-1-phosphate Spisulosine

Journal

Journal of applied biomedicine
ISSN: 1214-0287
Titre abrégé: J Appl Biomed
Pays: Poland
ID NLM: 101221755

Informations de publication

Date de publication:
Dec 2023
Historique:
received: 11 05 2023
accepted: 28 11 2023
medline: 19 12 2023
pubmed: 19 12 2023
entrez: 19 12 2023
Statut: ppublish

Résumé

Spisulosine (1-deoxysphinganine) is a sphingoid amino alcohol isolated from the sea clams that showed potent antiproliferative activity against a broad spectrum of solid tumors but failed in clinical trials due to neurotoxicity. However, its structural similarity to other bioactive sphingoids, interesting mode of action, and appreciable potency against cancer cells make it a suitable lead for future anticancer drug development. The present study was conducted to elucidate mechanisms of the antiproliferative/cytotoxic effects of newly synthesized spisulosine analog homospisulosine (KP7). The evaluation was performed on cervical carcinoma cells, representing an in vitro model of one of the most common cancer types and a significant worldwide cause of women's cancer mortality. Treatment with homospisulosine (2.0 μM) for 24, 48, and 72 h significantly inhibited the growth of HeLa cells in vitro and induced apoptosis detectable by DNA fragmentation, externalization of phosphatidylserine, dissipation of mitochondrial membrane potential, activation of caspase-3 and cleavage of PARP. In addition, treating HeLa cells with spisulosine increased p27 and Bcl-2 on protein levels and phosphorylation of Bcl-2 on Ser70 residue. These results support the potential for spisulosine analogs represented here by homospisulosine for future therapeutic development.

Identifiants

pubmed: 38112461
doi: 10.32725/jab.2023.019
doi:

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

218-227

Subventions

Organisme : Slovak Grant Agency for Science VEGA No
ID : 1/0278/23
Pays : Slovakia
Organisme : Slovak Grant Agency for Science VEGA No
ID : 1/0539/21
Pays : Slovakia
Organisme : Slovak Grant Agency for Science VEGA No
ID : 1/0653/19
Pays : Slovakia
Organisme : Operational Programme Integrated Infrastructure
ID : ITMS2014
Pays : Slovakia
Organisme : Operational Programme Integrated Infrastructure
ID : 313011V455
Pays : Slovakia

Déclaration de conflit d'intérêts

The authors report no conflicts of interest in this work.

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Auteurs

Martina Bago Pilatova (MB)

Pavol Jozef Safarik University, Faculty of Medicine, Department of Pharmacology, Kosice, Slovak Republic.

Natalia Nosalova (N)

Pavol Jozef Safarik University, Faculty of Medicine, Department of Pharmacology, Kosice, Slovak Republic.

Gabriela Ockajakova (G)

Pavol Jozef Safarik University, Faculty of Medicine, Department of Pharmacology, Kosice, Slovak Republic.

Martin Kello (M)

Pavol Jozef Safarik University, Faculty of Medicine, Department of Pharmacology, Kosice, Slovak Republic.

Klaudia Kotorova (K)

Pavol Jozef Safarik University, Faculty of Medicine, Department of Pharmacology, Kosice, Slovak Republic.

Peter Takac (P)

University of Veterinary Medicine and Pharmacy, Department of Pharmacology and Toxicology, Kosice, Slovak Republic.

Peter Petik (P)

Pavol Jozef Safarik University, Faculty of Medicine, Department of Pathology, Kosice, Slovak Republic.

Peter Bohus (P)

Pavol Jozef Safarik University, Faculty of Medicine, Department of Pathology, Kosice, Slovak Republic.

Kvetoslava Stankova (K)

Pavol Jozef Safarik University, Faculty of Science, Department of Organic Chemistry, Institute of Chemical Sciences, Kosice, Slovak Republic.

Miroslava Martinkova (M)

Pavol Jozef Safarik University, Faculty of Science, Department of Organic Chemistry, Institute of Chemical Sciences, Kosice, Slovak Republic.

Roman Mezencev (R)

Georgia Institute of Technology, School of Biological Sciences, Atlanta, GA, USA.

Classifications MeSH