Strigolactone Analogs: Two New Potential Bioactiphores for Glioblastoma.
G1-phase arrest
Glioblastoma
SL analogs
antiglioma effect
antiproliferative
apoptotic effect
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
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
572-580Références
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