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Malachite Green Assay for the Discovery of Heat-Shock Protein 90 Inhibitors
Published on: January 20, 2023
Diterpenoids from Zhumeria majdae roots as potential heat shock protein 90 (HSP90) modulators
Reza Zadali1, Samad Nejad-Ebrahimi2, Abbas Hadjiakhoondi3
1Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084, Fisciano (SA), Italy; Department of Pharmacognosy, Faculty of Pharmacy, Tehran University of Medical Sciences (TUMS), Tehran, Iran; Department of Pharmacognosy, Faculty of Pharmacy, Islamic Azad University-Damghan Branch, Iran.
Abstract:
Four undescribed and 17 known diterpenoids were isolated from the roots of Zhumeria majdae Rech.f. & Wendelbo. Using 1D and 2D NMR spectroscopy, ECD spectroscopy, and HRESIMS data analysis, the structures of the undescribed compounds were elucidated. The anti-proliferative activity of isolated compounds was evaluated against HeLa and MCF7 cancer cell lines. The binding affinity of all compounds to HSP90, one of the targets for the modern anticancer therapy, was investigated using surface plasmon resonance. The results demonstrated that lanugon Q interacted with the chaperone. To explain its mechanism of action, experimental and computational tests were also conducted.
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