Strigolactone Analogs: Two New Potential Bioactiphores for Glioblastoma | Zendy

Gizem Antika | Zendy; Zeynep Özlem Cinar | Zendy; Esma Seçen | Zendy; Mehmet Özbil | Zendy; Esra Tokay | Zendy; Feray Köçkar | Zendy; Cristina Prandi | Zendy; Tugba Boyunegmez Tumer | Zendy

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Strigolactone Analogs: Two New Potential Bioactiphores for Glioblastoma

Author(s) -

Gizem Antika,

Zeynep Özlem Cinar,

Esma Seçen,

Mehmet Özbil,

Esra Tokay,

Feray Köçkar,

Cristina Prandi,

Tugba Boyunegmez Tumer

Publication year - 2022

Publication title -

acs chemical neuroscience

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.158

H-Index - 69

ISSN - 1948-7193

DOI - 10.1021/acschemneuro.1c00702

Subject(s) - pharmacophore , cell cycle checkpoint , downregulation and upregulation , in silico , apoptosis , cell cycle , strigolactone , cell growth , cancer cell , cancer research , chemistry , biology , microbiology and biotechnology , cancer , gene , bioinformatics , biochemistry , genetics , arabidopsis , mutant

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.

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