Strigolactone Analogs: Two New Potential Bioactiphores for Glioblastoma.


Journal

ACS chemical neuroscience
ISSN: 1948-7193
Titre abrégé: ACS Chem Neurosci
Pays: United States
ID NLM: 101525337

Informations de publication

Date de publication:
02 03 2022
Historique:
pubmed: 10 2 2022
medline: 5 3 2022
entrez: 9 2 2022
Statut: ppublish

Résumé

Strigolactones (SLs), carotenoid-derived phytohormones, control the plant response and signaling pathways for stressful conditions. In addition, they impact numerous cellular processes in mammalians and present new scaffolds for various biomedical applications. Recent studies demonstrated that SLs possess potent antitumor activity against several cancer cells. Herein, we sought to elucidate the inhibitory effects of SL analogs on the growth and survival of human brain tumor cell lines. Among four tested SLs, we showed for the first time that two lead bioactiphores, indanone-derived SL and EGO10, can inhibit cancer cell proliferation, induce apoptosis, and induce G1 cell cycle arrest at low concentrations. SL analogs were marked by increased expression of Bax/Caspase-3 genes and downregulation of Bcl-2. In silico studies were conducted to identify drug-likeness, blood-brain barrier penetrating properties, and molecular docking with Bcl-2 protein. Taken together, this study indicates that SLs may be promising antiglioma agents, presenting novel pharmacophores for further preclinical and clinical assessment.

Identifiants

pubmed: 35138812
doi: 10.1021/acschemneuro.1c00702
pmc: PMC8895406
doi:

Substances chimiques

GR24 strigolactone 0
Heterocyclic Compounds, 3-Ring 0
Lactones 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

572-580

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Auteurs

Gizem Antika (G)

Graduate Program of Molecular Biology and Genetics, School of Graduate Studies, Canakkale Onsekiz Mart University, Canakkale 17020, Turkey.

Zeynep Özlem Cinar (ZÖ)

Graduate Program of Molecular Biology and Genetics, School of Graduate Studies, Canakkale Onsekiz Mart University, Canakkale 17020, Turkey.

Esma Seçen (E)

Graduate Program of Molecular Medicine, Universitätsklinikum Jena, Friedrich-Schiller-Universität Jena, Jena 07740, Germany.

Mehmet Özbil (M)

Gebze Technical University, Institute of Biotechnology, 41400 Gebze, Kocaeli, Turkey.

Esra Tokay (E)

Department of Molecular Biology and Genetics, Faculty of Sciences and Arts, Balikesir University, Balikesir 10145, Turkey.

Feray Köçkar (F)

Department of Molecular Biology and Genetics, Faculty of Sciences and Arts, Balikesir University, Balikesir 10145, Turkey.

Cristina Prandi (C)

Department of Chemistry, University of Turin, 10125 Turin, Italy.

Tugba Boyunegmez Tumer (TB)

Department of Molecular Biology and Genetics, Faculty of Arts and Science, Canakkale Onsekiz Mart University, 17020 Canakkale, Turkey.

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Classifications MeSH