Strigolactone Analogs: Two New Potential Bioactiphores for Glioblastoma.
Gizem AntikaZeynep Özlem CinarEsma SeçenMehmet ÖzbilEsra TokayFeray KöçkarCristina PrandiTugba Boyunegmez TumerPublished in: ACS chemical neuroscience (2022)
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.
Keyphrases
- molecular docking
- cell cycle arrest
- pi k akt
- blood brain barrier
- cell death
- cell proliferation
- signaling pathway
- induced apoptosis
- molecular dynamics simulations
- endothelial cells
- case control
- poor prognosis
- papillary thyroid
- cerebral ischemia
- genome wide
- binding protein
- oxidative stress
- squamous cell
- cell cycle
- induced pluripotent stem cells
- long non coding rna
- case report
- squamous cell carcinoma
- tissue engineering
- risk assessment
- young adults
- cell therapy
- protein protein
- free survival
- adverse drug
- human health
- brain injury