Published January 1, 2022 | Version v1
Journal article Open

Strigolactone Analogs: Two New Potential Bioactiphores for Glioblastoma

  • 1. Canakkale Onsekiz Mart Univ, Sch Grad Studies, Grad Program Mol Biol & Genet, TR-17020 Canakkale, Turkey
  • 2. Friedrich Schiller Univ Jena, Univ Klinikum Jena, Grad Program Mol Med, D-07740 Jena, Germany
  • 3. Gebze Tech Univ, Inst Biotechnol, TR-41400 Kocaeli, Turkey
  • 4. Balikesir Univ, Fac Sci & Arts, Dept Mol Biol & Genet, TR-10145 Balikesir, Turkey
  • 5. Univ Turin, Dept Chem, I-10125 Turin, Italy
  • 6. Canakkale Onsekiz Mart Univ, Fac Arts & Sci, Dept Mol Biol & Genet, TR-17020 Canakkale, Turkey

Description

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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