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Volume 31, Issue 40
  • ISSN: 0929-8673
  • E-ISSN: 1875-533X

Abstract

Background/Aim

Glioblastoma is an extensively malignant neoplasm of the brain that predominantly impacts the human population. To address the challenge of glioblastoma, herein, we have searched for new drug-like candidates by extensive computational and biochemical investigations.

Methods

Approximately 950 compounds were virtually screened against the two most promising targets of glioblastoma, , epidermal growth factor receptor (EGFR) and phosphoinositide 3-kinase (PI3K). Based on highly negative docking scores, excellent binding capabilities and good pharmacokinetic properties, eight and seven compounds were selected for EGFR and PI3K, respectively.

Results

Among those hits, four natural products (, , , and ) exerted dual inhibitory effects on EGFR and PI3K in our analysis; therefore, their capacity to suppress the cell proliferation was assessed in U87 cell line (type of glioma cell line). The compounds , , and exhibited significant anti-proliferative capability with IC values of 11.97 ± 0.73 µM, 28.27 ± 1.52 µM, and 22.93 ± 1.63 µM respectively, while displayed weak inhibitory potency (IC = 74.97 ± 2.30 µM).

Conclusion

This study has identified novel natural products that inhibit the progression of glioblastoma; however, further examinations of these molecules are required in animal and tissue models to better understand their downstream targeting mechanisms.

© 2024 Bentham Science Publishers
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2024-11-02

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/content/journals/cmc/10.2174/0109298673293279240404080046
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Novel Natural Inhibitors for Glioblastoma by Targeting Epidermal Growth Factor Receptor and Phosphoinositide 3-kinase
Curr. Med. Chem. 31, 6596 (2024); https://doi.org/10.2174/0109298673293279240404080046
/content/journals/cmc/10.2174/0109298673293279240404080046
/content/journals/cmc/10.2174/0109298673293279240404080046
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  • Article Type: Research Article
Keyword(s): EGFR; Glioblastoma; molecular docking; MTT assay; PI3K; U87 cell line; virtual screening

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