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Strigolactone Analogs: Two New Potential Bioactiphores for Glioblastoma

[Image: see text] 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 demon...

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Autores principales: Antika, Gizem, Cinar, Zeynep Özlem, Seçen, Esma, Özbil, Mehmet, Tokay, Esra, Köçkar, Feray, Prandi, Cristina, Tumer, Tugba Boyunegmez
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8895406/
https://www.ncbi.nlm.nih.gov/pubmed/35138812
http://dx.doi.org/10.1021/acschemneuro.1c00702
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author Antika, Gizem
Cinar, Zeynep Özlem
Seçen, Esma
Özbil, Mehmet
Tokay, Esra
Köçkar, Feray
Prandi, Cristina
Tumer, Tugba Boyunegmez
author_facet Antika, Gizem
Cinar, Zeynep Özlem
Seçen, Esma
Özbil, Mehmet
Tokay, Esra
Köçkar, Feray
Prandi, Cristina
Tumer, Tugba Boyunegmez
author_sort Antika, Gizem
collection PubMed
description [Image: see text] 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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spelling pubmed-88954062022-03-07 Strigolactone Analogs: Two New Potential Bioactiphores for Glioblastoma Antika, Gizem Cinar, Zeynep Özlem Seçen, Esma Özbil, Mehmet Tokay, Esra Köçkar, Feray Prandi, Cristina Tumer, Tugba Boyunegmez ACS Chem Neurosci [Image: see text] 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. American Chemical Society 2022-02-09 /pmc/articles/PMC8895406/ /pubmed/35138812 http://dx.doi.org/10.1021/acschemneuro.1c00702 Text en © 2022 American Chemical Society https://creativecommons.org/licenses/by/4.0/Permits the broadest form of re-use including for commercial purposes, provided that author attribution and integrity are maintained (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Antika, Gizem
Cinar, Zeynep Özlem
Seçen, Esma
Özbil, Mehmet
Tokay, Esra
Köçkar, Feray
Prandi, Cristina
Tumer, Tugba Boyunegmez
Strigolactone Analogs: Two New Potential Bioactiphores for Glioblastoma
title Strigolactone Analogs: Two New Potential Bioactiphores for Glioblastoma
title_full Strigolactone Analogs: Two New Potential Bioactiphores for Glioblastoma
title_fullStr Strigolactone Analogs: Two New Potential Bioactiphores for Glioblastoma
title_full_unstemmed Strigolactone Analogs: Two New Potential Bioactiphores for Glioblastoma
title_short Strigolactone Analogs: Two New Potential Bioactiphores for Glioblastoma
title_sort strigolactone analogs: two new potential bioactiphores for glioblastoma
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8895406/
https://www.ncbi.nlm.nih.gov/pubmed/35138812
http://dx.doi.org/10.1021/acschemneuro.1c00702
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